| Name | 5 HT1A |
|---|---|
| Synonyms | 5 HT 1A; serotonin receptor; 5 HT1A; 5 hydroxytryptamine (serotonin) receptor 1A; 5 hydroxytryptamine 1A receptor; 5HT1A; ADRB2RL1; ADRBRL 1… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 19605522 | Cussac D, Palmier C, Finana F, De Vries L, Tardif S, Leger C, Bernois S, Heusler P: Mutant 5-hydroxytryptamine 1A receptor D116A is a receptor activated solely by synthetic ligands with a rich pharmacology. J Pharmacol Exp Ther. 2009 Oct;331(1):222-33. Epub 2009 Jul 15. In contrast, affinities of the 5-HT (1A) ligands WAY100,635, spiperone, (-)-4-(dipropylamino)-1,3,4,5-tetrahydrobenz {c,d}indole-6-carboxamide (LY228,729), and 1-[2-(4-fluorobenzoylamino) ethyl]-4-(7-methoxynaphtyl) piperazine (S14506) and the prototypical 5-HT (1A) agonist (+)-8-OH-DPAT are only slightly affected by the mutation, suggesting a moderate contribution of Asp116 to the binding pocket for these latter. |
37(0,1,1,7) | Details |
| 11807610 | Sanabria-Bohorquez SM, Biver F, Damhaut P, Wikler D, Veraart C, Goldman S: Quantification of 5-HT (1A) receptors in human brain using p-MPPF kinetic modelling and PET. Eur J Nucl Med Mol Imaging. 2002 Jan;29(1):76-81. Epub 2001 Nov 22. Animal studies have suggested that 4-(2'-methoxyphenyl)-1-[2'-[ N-(2"-pyridinyl)- p-[(18) F] fluorobenzamido] ethyl] piperazine ( p-MPPF) may be a suitable positron emission tomography (PET) tracer of 5-HT (1A) receptors. |
36(0,1,1,6) | Details |
| 11104831 | Assie MB, Koek W: Estimation of apparent pA2 values for WAY 100635 at 5-HT1A receptors regulating release in anaesthetised rats. Eur J Pharmacol. 2000 Dec 8;409(2):173-7. |
6(0,0,0,6) | Details |
| 18556076 | de Souza Villa P, Menani JV, de Arruda Camargo GM, de Arruda Camargo LA, Saad WA: Activation of the serotonergic 5-HT1A receptor in the paraventricular nucleus of the hypothalamus inhibits water intake and increases urinary excretion in water-deprived rats. Regul Pept. 2008 Oct 9;150(1-3):14-20. Epub 2008 May 14. |
6(0,0,0,6) | Details |
| 15888508 | Odagaki Y, Toyoshima R, Yamauchi T: Trazodone and its active metabolite m-chlorophenylpiperazine as partial agonists at 5-HT1A receptors assessed by [35S] GTPgammaS binding. J Psychopharmacol. 2005 May;19(3):235-41. |
6(0,0,0,6) | Details |
| 12764106 | Teng YD, Bingaman M, Taveira-DaSilva AM, Pace PP, Gillis RA, Wrathall JR: Serotonin 1A receptor agonists reverse respiratory abnormalities in spinal cord-injured rats. J Neurosci. 2003 May 15;23(10):4182-9. |
6(0,0,0,6) | Details |
| 11564470 | van der Vegt BJ, de Boer SF, Buwalda B, de Ruiter AJ, de Jong JG, Koolhaas JM: Enhanced sensitivity of postsynaptic serotonin-1A receptors in rats and mice with high trait aggression. Physiol Behav. 2001 Sep 1-15;74(1-2):205-11. |
6(0,0,0,6) | Details |
| 19799970 | Smith VM, Hagel K, Antle MC: Serotonergic potentiation of photic phase shifts: examination of receptor contributions and early biochemical/molecular events. Neuroscience. 2010 Jan 13;165(1):16-27. Epub 2009 Sep 30. The mixed agonist/antagonist 1-(2-methoxyphenyl) 4-[4-(phthalimido) butyl]-piperazine hydrobromide (NAN-190) has been shown to greatly potentiate photic phase shifts in hamsters. NAN-190 is believed to act primarily through the 5-HT (1A) receptor, but also binds to several other receptors, making it uncertain as to which receptor underlies its potentiation of photic phase shifts. |
3(0,0,0,3) | Details |
| 12211089 | Udo de Haes JI, Bosker FJ, Van Waarde A, Pruim J, Willemsen AT, Vaalburg W, Den Boer JA: 5-HT (1A) receptor imaging in the human brain: effect of depletion and infusion on [(18) F] MPPF binding. Synapse. 2002 Nov;46(2):108-15. |
3(0,0,0,3) | Details |
| 16728720 | Lau DH, Thompson CS, Bellringer JF, Thomas PJ, Mumtaz FH, Morgan RJ, Mikhailidis DP: Doxazosin and receptor (1A, 2A, and 4) antagonists inhibit -mediated human cavernosal contraction. J Androl. 2006 Sep-Oct;27(5):679-85. Epub 2006 May 25. The effect of on human cavernosal tissues, as well as those of doxazosin (shown previously to have inhibitory action), ketanserin (5-HT (2A) receptor antagonist), NAN-190 (5-HT (1A) receptor antagonist), and SB 203186 (5-HT (4) receptor antagonist) on -mediated effects, were assessed using the organ bath technique, including electrical field stimulation study (EFS). |
3(0,0,0,3) | Details |
| 19122313 | Asagarasu A, Matsui T, Hayashi H, Tamaoki S, Yamauchi Y, Sato M: Design and synthesis of piperazinylpyridine derivatives as novel 5-HT1A agonists/5-HT3 antagonists for the treatment of irritable bowel syndrome (IBS). Chem Pharm Bull. 2009 Jan;57(1):34-42. These compounds, which were designed by pharmacophore analysis, bind to both subtype 1A (5-HT1A) and subtype 3 (5-HT3) receptors. The atom of the isoquinoline, a methoxy group and piperazine were essential to the pharmacophore for binding to these receptors. |
2(0,0,0,2) | Details |
| 12453592 | Papagiannopoulou D, Pirmettis I, Tsoukalas Ch, Nikoladou L, Drossopoulou G, Dalla C, Pelecanou M, Papadopoulou-Daifotis Z, Papadopoulos M, Chiotellis E: Oxotechnetium 99mTcO [SN (R) S][S] complexes as potential 5-HT1A receptor imaging agents. Nucl Med Biol. 2002 Nov;29(8):825-32. A series of 99mTcO [SN (R) S][S] complexes carrying the 1-(2-methoxyphenyl) piperazine moiety on the tridentate ligand [SN (R) S] was synthesized. |
2(0,0,0,2) | Details |
| 11338664 | Laszlovszky I, Acs T, Kiss B, Domany G: Substituted phenoxyalkylpiperazines as D3 receptor ligands. . Pharmazie. 2001 Apr;56(4):287-9. A novel series of potential antipsychotic agents were prepared by combination of condensed heterocycles containing bridgehead with (2-methoxyphenyl) piperazine using phenoxyalkyl spacer of variable length. The affinity of the compounds was determined at rat cloned D3 and rat D2, 5-HT1A receptors by an vitro receptor binding assay. |
1(0,0,0,1) | Details |
| 16392798 | Kumar JS, Majo VJ, Hsiung SC, Millak MS, Liu KP, Tamir H, Prabhakaran J, Simpson NR, Van Heertum RL, Mann JJ, Parsey RV: Synthesis and in vivo validation of [O-methyl-11C] 2-{4-[4-(7-methoxynaphthalen-1-yl) piperazin- 1-yl] butyl}-4-methyl-2H-[1,2,4] triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand. J Med Chem. 2006 Jan 12;49(1):125-34. Piperazine 10 is a 5-HT (1A) agonist with an EC (50) comparable to based on cAMP formation and GTP (gamma) S binding assays. |
36(0,1,1,6) | Details |
| 11202614 | Galeotti N, Ghelardini C, Bartolini A: Role of 5-HT1A receptors in a mouse passive avoidance paradigm. Jpn J Pharmacol. 2000 Dec;84(4):418-24. The administration of 5-HT1A-receptor antagonists NAN-190 (1-(2-methoxyphenyl)-4-[4-2-phthalimmido) butyl] piperazine) and WAY-100635 (N-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-N-2-pyridinyl-cyclohexanec arboxamide) produced a dose-dependent amnesic effect comparable to that obtained with the well-known amnesic agents and dicyclomine. |
36(0,1,1,6) | Details |
| 18598015 | Siracusa MA, Salerno L, Modica MN, Pittala V, Romeo G, Amato ME, Nowak M, Bojarski AJ, Mereghetti I, Cagnotto A, Mennini T: Synthesis of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands. J Med Chem. 2008 Aug 14;51(15):4529-38. Epub 2008 Jul 4. |
6(0,0,0,6) | Details |
| 12398907 | Prinssen EP, Colpaert FC, Koek W: 5-HT1A receptor activation and anti-cataleptic effects: high-efficacy agonists maximally inhibit haloperidol-induced catalepsy. Eur J Pharmacol. 2002 Oct 25;453(2-3):217-21. The anti-cataleptic effects of 5-HT (1A) receptor ligands with positive intrinsic activity [from high to low: 3-chloro-4-fluorophenyl-(4--4-[[(5-methyl-6-methylamino-pyridin-2-yl methyl)-amino]-methyl]-piperidin-1-yl-methanone salt (F 13714), eptapirone, 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), 2-[4-[4-(7-methoxy-1-naphtyl) piperazino] butyl]-4-methyl-2H,4H-1,2,4-triazin-3,5-dione salt (F 11461), 2-[4-[4-(7-benzofuranyl) piperazino] butyl]-4-methyl-2H,4H-1,2,4-triazin-3,5 -dione (F 12826), ipsapirone, and (s)-N-tert-butyl-3-(4-(2-methoxyphenyl) piperazine-1-yl)-2-phenylpropanamid e hydrochloride (WAY 100135)] and negative intrinsic activity [N-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-N-(2-pyridinyl) cyclohexane carboxamide dihydrochloride (WAY 100635)] were examined. |
6(0,0,0,6) | Details |
| 16941730 | Paluchowska MH, Bugno R, Charakchieva-Minol S, Bojarski AJ, Tatarczynska E, Chojnacka-Wojcik E: Conformational restriction in novel NAN-190 and MP3022 analogs and their 5-HT (1A) receptor activity. Arch Pharm. 2006 Sep;339(9):498-506. |
6(0,0,0,6) | Details |
| 19559623 | Zhang J, Zhang H, Cai W, Yu L, Zhen X, Zhang A: 'Click' D (1) receptor agonists with a 5-HT (1A) receptor pharmacophore producing D (2) receptor activity. Bioorg Med Chem. 2009 Jul 15;17(14):4873-80. Epub 2009 Jun 16. |
6(0,0,0,6) | Details |
| 16497294 | Bruins Slot LA, De Vries L, Newman-Tancredi A, Cussac D: Differential profile of antipsychotics at 5-HT1A and D2S receptors coupled to extracellular signal-regulated kinase. Eur J Pharmacol. 2006 Mar 18;534(1-3):63-70. Epub 2006 Feb 21. |
6(0,0,0,6) | Details |
| 15686885 | Evrard DA, Zhou P, Yi SY, Zhou D, Smith DL, Sullivan KM, Hornby GA, Schechter LE, Andree TH, Mewshaw RE: Studies towards the next generation of antidepressants. Bioorg Med Chem Lett. 2005 Feb 15;15(4):911-4. Part 4: derivatives of 4-(5--1H-indol-3-yl) cyclohexylamine with affinity for the serotonin transporter and the 5-HT1A receptor.. Compounds containing 1-(4-indolyl) piperazine and 2-(1H-indol-4-yloxy) ethylamine are promising leads for further SAR studies. |
3(0,0,0,3) | Details |
| 18339980 | Dennis RL, Chen ZQ, Cheng HW: Serotonergic mediation of aggression in high and low aggressive chicken strains. Poult Sci. 2008 Apr;87(4):612-20. (5-HT) regulates aggressive behavior via binding to its receptors, such as 5-HT1A and 1B, in humans and rodents. |
3(0,0,0,3) | Details |
| 12067006 | Nadeson R, Goodchild CS: Antinociceptive role of 5-HT1A receptors in rat spinal cord. . Br J Anaesth. 2002 May;88(5):679-84. RESULTS: The 5-HT1 agonist 1-(3-chlorophenyl)-piperazine dihydrochloride caused a dose-dependent antinociceptive effect, measured by both nociceptive tests. |
3(0,0,0,3) | Details |
| 11159702 | Newman-Tancredi A, Verriele L, Millan MJ: Differential modulation by GTPgammaS of agonist and inverse agonist binding to h5-HT (1A) receptors revealed by [3H]-WAY100,635. Br J Pharmacol. 2001 Jan;132(2):518-24. The interaction of serotonergic ligands at human (h) 5-HT (1A) receptors expressed in Chinese hamster ovary cells was examined with the selective 'neutral' 5-HT (1A) antagonist [(3) H]-WAY100,635. |
2(0,0,0,2) | Details |
| 19190523 | Foong JP, Bornstein JC: antagonists NAN-190 and SB 269970 block alpha2-adrenoceptors in the guinea pig. Neuroreport. 2009 Feb 18;20(3):325-30. The initial aim of this study was to use intracellular recording and specific antagonists to identify roles of 5-HT1A and 5-HT7 receptors of submucosal noncholinergic secretomotor neurons of guinea pig ileum, in vitro. |
2(0,0,0,2) | Details |
| 15829916 | Richter F, Mikulik O, Ebersberger A, Schaible HG: Noradrenergic agonists and antagonists influence migration of cortical spreading depression in rat-a possible mechanism of migraine prophylaxis and prevention of postischemic neuronal damage. J Cereb Blood Flow Metab. 2005 Sep;25(9):1225-35. The CSD blockade by the alpha (2)-antagonist yohimbine (1.75 mmol/L) was because of its action on inhibitory 5-HT (1A) receptors. |
1(0,0,0,1) | Details |
| 17892926 | Duffy-Whritenour JE, Zelikoff JT: Relationship between and the immune system in a teleost model. Brain Behav Immun. 2008 Feb;22(2):257-64. Epub 2007 Sep 24. Lymphocyte proliferation and extracellular (O2.-) production were examined in cells from bluegill sunfish injected with either 5-HTP (the immediate precursor to or pCPA (an inhibitor of the rate-limiting enzyme in synthesis), or, in vitro following exposure of immune cells to either the 5-HT (1A) receptor agonist, 8-OH-DPAT, or the receptor antagonist, NAN-190. |
1(0,0,0,1) | Details |
| 16710314 | McCreary AC, Glennon JC, Ashby CR Jr, Meltzer HY, Li Z, Reinders JH, Hesselink MB, Long SK, Herremans AH, van Stuivenberg H, Feenstra RW, Kruse CG: SLV313 (1-(2,3-dihydro-benzo [1,4] dioxin-5-yl)-4- [5-(4--phenyl)-pyridin-3-ylmethyl]-piperazine monohydrochloride): a novel dopamine D2 receptor antagonist and 5-HT1A receptor agonist potential antipsychotic drug. Neuropsychopharmacology. 2007 Jan;32(1):78-94. Epub 2006 May 17. |
165(2,2,2,5) | Details |
| 15341483 | Heinrich T, Bottcher H, Bartoszyk GD, Greiner HE, Seyfried CA, Van Amsterdam C: Indolebutylamines as selective 5-HT (1A) agonists. . J Med Chem. 2004 Sep 9;47(19):4677-83. The combination of structural elements -alkyl-amine and aryl-piperazine) known to introduce 5-HT (1A) receptor affinity and the proper selection of substituents (R on the moiety and R' on the aryl moiety) led to compounds with high receptor specificity and affinity. |
36(0,1,1,6) | Details |
| 15033384 | Hedlund PB, Kelly L, Mazur C, Lovenberg T, Sutcliffe JG, Bonaventure P: 8-OH-DPAT acts on both 5-HT1A and 5-HT7 receptors to induce hypothermia in rodents. Eur J Pharmacol. 2004 Mar 8;487(1-3):125-32. The 5-HT (1A) receptor antagonist (S)-N-tert-butyl-3-(4-(2-methoxyphenyl) piperazine-1-yl)-2-phenylpropanamid e (WAY-100135) (10 mg/kg, i.p.) inhibited the effect of 8-OH-DPAT at all doses in rats and mice. |
35(0,1,1,5) | Details |
| 11041316 | Dekeyne A, Brocco M, Adhumeau A, Gobert A, Millan MJ: The selective (5-HT) 1A receptor ligand, S15535, displays anxiolytic-like effects in the social interaction and Vogel models and suppresses dialysate levels of in the dorsal hippocampus of freely-moving rats. Psychopharmacology. 2000 Sep;152(1):55-66. |
5(0,0,0,5) | Details |
| 20164327 | Zhang J, Huang XY, Ye ML, Luo CX, Wu HY, Hu Y, Zhou QG, Wu DL, Zhu LJ, Zhu DY: Neuronal nitric oxide synthase alteration accounts for the role of 5-HT1A receptor in modulating anxiety-related behaviors. J Neurosci. 2010 Feb 17;30(7):2433-41. |
5(0,0,0,5) | Details |
| 15996562 | Kleven MS, Barret-Grevoz C, Bruins Slot L, Newman-Tancredi A: Novel antipsychotic agents with 5-HT (1A) agonist properties: role of 5-HT (1A) receptor activation in attenuation of catalepsy induction in rats. Neuropharmacology. 2005 Aug;49(2):135-43. Epub 2005 Apr 1. |
5(0,0,0,5) | Details |
| 11299323 | Parsons LH, Kerr TM, Tecott LH: 5-HT (1A) receptor mutant mice exhibit enhanced tonic, stress-induced and fluoxetine-induced serotonergic neurotransmission. J Neurochem. 2001 Apr;77(2):607-17. |
5(0,0,0,5) | Details |
| 16843842 | Defraiteur C, Lemaire C, Luxen A, Plenevaux A: Radiochemical synthesis and tissue distribution of p-[18F] DMPPF, a new 5-HT1A ligand for PET, in rats. Nucl Med Biol. 2006 Jul;33(5):667-75. Epub 2006 Jun 12. |
3(0,0,0,3) | Details |
| 12892833 | Zanoveli JM, Nogueira RL, Zangrossi H Jr: in the dorsal periaqueductal gray modulates inhibitory avoidance and one-way escape behaviors in the elevated T-maze. Eur J Pharmacol. 2003 Jul 25;473(2-3):153-61. The 5-HT1A receptor agonist 8--2-(di-n-propylamino) tetralin (8-OH-DPAT) impaired this response, suggesting an anxiolytic effect, and the preferential 5-HT2A receptor agonist 2,5-dimethoxy-4-iodoamphetamine (DOI) was ineffective. |
3(0,0,0,3) | Details |
| 11888572 | Fone KC, Topham IA: Alteration in agonist-induced behaviour following a implant in adult rats. Pharmacol Biochem Behav. 2002 Apr;71(4):815-23. The flat body posture, reciprocal forepaw treading, elevated hyperglycaemia, hypothermia and reduced hippocampal induced by the 5-HT (1A) agonist 8-OHDPAT (0.3 mg/kg ip) were all significantly attenuated by the implant. |
2(0,0,0,2) | Details |
| 18790822 | Didelot A, Ryvlin P, Lothe A, Merlet I, Hammers A, Mauguiere F: PET imaging of brain 5-HT1A receptors in the preoperative evaluation of temporal lobe epilepsy. Brain. 2008 Oct;131(Pt 10):2751-64. Epub 2008 Sep 12. |
1(0,0,0,1) | Details |
| 12570387 | Perrone R, Berardi F, Colabufo NA, Lacivita E, Leopoldo M, Tortorella V: Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl) alkyl]-1-aryl ketones as 5-HT (7) receptor ligands. J Med Chem. 2003 Feb 13;46(4):646-9. Structural requirements for 5-HT (7) receptor affinity and selectivity over that for the 5-HT (1A) receptor were studied on a series of 1-[omega-(4-aryl-1-piperazinyl) alkyl]-1-aryl ketones. The presence of a or methoxy substituent on aryl ketone moiety, alkyl chain length, and the nature of N-1-piperazine substituent were explored. 6-[4-(3-Benzisoxazolyl)-1-piperazinyl]-1-(2-hydroxyphenyl)-1- (40) and its methoxy analogue 43 exhibited high 5-HT (7) receptor affinities (Ki = 2.93 nM and 0.90 nM, respectively) and agonist properties when tested for 5-HT (7) receptor-mediated relaxation of substance P-induced guinea-pig ileum contraction. |
1(0,0,0,1) | Details |
| 16937076 | Parkel S, Rinken A: Characteristics of binding of [3H] WAY100635 to rat hippocampal membranes. . Neurochem Res. 2006 Sep;31(9):1135-40. Epub 2006 Aug 26. Kinetic analysis of binding of [(3) H][N-[2-[4-(2-[O-methyl-(3) H] methoxyphenyl)-1-piperazinyl] ethyl]-N-(2- pyridinyl) cyclohexane carboxamide ([(3) H] WAY100635) to 5-HT (1A) receptors in rat hippocampal membranes has revealed complex regulation mechanism for this radioligand. |
1(0,0,0,1) | Details |
| 15374751 | Dias Elpo Zomkowski A, Oscar Rosa A, Lin J, Santos AR, Calixto JB, Lucia Severo Rodrigues A: Evidence for serotonin receptor subtypes involvement in antidepressant like-effect in the mouse forced swimming test. Brain Res. 2004 Oct 15;1023(2):253-63. Pretreatment with p-chlorophenylalanine methyl ester (PCPA; 100 mg/kg, intraperitoneally (i.p.), an inhibitor of synthesis, for 4 consecutive days), methysergide (5 mg/kg, i.p., a antagonist), pindolol (32 mg/kg, i.p., a 5-HT (1A/1B) receptor/beta-adrenoceptor antagonist), N-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-N-(2-pyridynyl) cyclohexanec arboxamide (WAY 100635; 0.3 mg/kg, subcutaneously (s.c.), a selective 5-HT (1A) receptor antagonist), 1-(2-methoxyphenyl)-4 [-(2-phthalimido) butyl] piperazine) -190; 0.5 mg/kg, i.p., a 5-HT (1A) receptor antagonist), 1-(2-(1-pyrrolyl)-phenoxy)-3-isopropylamino- (isamoltane; 2.5 mg/kg, i.p., a 5-HT (1B) receptor antagonist), cyproheptadine (3 mg/kg, i.p., a 5-HT (2) antagonist) or ketanserin (5 mg/kg, i.p., a 5-HT (2A/2C) receptor antagonist), but not with (2 mg/kg, i.p., a beta-adrenoceptor antagonist), prevented the effect of (10 mg/kg, i.p.) in the FST. Taken together, the results firstly demonstrate that antidepressant-like effects in the FST seem to be mediated, at least in part, by an interaction with 5-HT (1A/1B) and 5-HT (2) receptors. |
1(0,0,0,1) | Details |
| 16914121 | Kao T, Shumsky JS, Jacob-Vadakot S, Himes BT, Murray M, Moxon KA: Role of the 5-HT2C receptor in improving weight-supported stepping in adult rats spinalized as neonates. Brain Res. 2006 Sep 27;1112(1):159-68. Epub 2006 Aug 17. We therefore extended our previous work with the 5-HT2C receptor agonist 1-(m-chlorophenyl)-piperazine hydrochloride (mCPP), which enhances weight-supported stepping when administered to adult rats spinalized as neonates, to identify the optimal dose for improved weight-supported stepping with minimal side effects. |
0(0,0,0,0) | Details |
| 15254141 | Chiou LC, Chuang KC, Wichmann J, Adam G: Ro 64-6198 [(1S,3aS)-8-(2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl)-1-phenyl-1,3,8-triaz a-spiro [4.5] decan-4-one] acts differently from nociceptin/orphanin FQ in rat periaqueductal gray slices. J Pharmacol Exp Ther. 2004 Nov;311(2):645-51. Epub 2004 Jul 13. The effect of Ro 64-6198 was not affected by naloxone (1 microM), sulpiride (10 microM), and [1-(2-methoxyphenyl)-4-[4-2-phthalimido) butyl] piperazine (NAN-190) (1 microM), respectively, the antagonist of opioid, D (2), and 5-HT (1A) receptors. |
0(0,0,0,0) | Details |
| 17517509 | Leopoldo M, Lacivita E, Colabufo NA, Niso M, Berardi F, Perrone R: Bivalent ligand approach on 4-[2-(3-methoxyphenyl) ethyl]-1-(2-methoxyphenyl) piperazine: synthesis and binding affinities for 5-HT (7) and 5-HT (1A) receptors. Bioorg Med Chem. 2007 Aug 1;15(15):5316-21. Epub 2007 May 6. |
164(2,2,2,4) | Details |
| 17194034 | Sharma BK, Singh P, Sharma S: Quantitative structure-activity relationship study of new potent and selective antagonists at the 5-HT (1A) and adrenergic alpha (1d) receptors: Derivatives of spiroethyl phenyl (substituted) piperazine. J Enzyme Inhib Med Chem. 2006 Oct;21(5):601-7. |
163(2,2,2,3) | Details |
| 19223188 | Khatri M, Rai SK, Alam S, Vij A, Tiwari M: Synthesis and pharmacological evaluation of new arylpiperazines N-[4-[4-(aryl) piperazine-1-yl]-phenyl]-amine derivatives: putative role of 5-HT1A receptors. Bioorg Med Chem. 2009 Mar 1;17(5):1890-7. Epub 2009 Jan 24. |
114(1,2,2,4) | Details |
| 15987834 | Assie MB, Ravailhe V, Faucillon V, Newman-Tancredi A: Contrasting contribution of 5-hydroxytryptamine 1A receptor activation to neurochemical profile of novel antipsychotics: frontocortical and hippocampal release in rat brain. J Pharmacol Exp Ther. 2005 Oct;315(1):265-72. Epub 2005 Jun 29. Several novel antipsychotics, such as bifeprunox, SSR181507 [(3-exo)-8-benzoyl-N-(((2S) 7-chloro-2,3-dihydro-1,4-benzodioxin-1-yl) methy l)-8-azabicyclo (3.2.1) -3- and SLV313 [1-(2,3-dihydro-benzo [1,4] dioxin-5-yl)-4-[5-(4-fluorophenyl)-pyridin-3-ylm ethyl]-piperazine], activate (5-HT) 1A receptors. |
88(1,1,1,8) | Details |
| 17763374 | Penjisevic J, Sukalovic V, Andric D, Kostic-Rajacic S, Soskic V, Roglic G: 1-cinnamyl-4-(2-methoxyphenyl) piperazines: synthesis, binding properties, and docking to (D (2)) and (5-HT (1A)) receptors. Arch Pharm. 2007 Sep;340(9):456-65. Docking analysis indicated that the binding to D (2) and 5-HT (1A) receptors is based on (i) interaction between protonated N1 of the piperazine ring and various residues, (ii) bonds between various moieties of the ligand and the residues of serine, or and (iii) edge-to-face interactions of the aromatic ring of the arylpiperazine moiety with or residues. |
87(1,1,1,7) | Details |
| 11315561 | Papagiannopoulou D, Pirmettis I, Maina T, Pelecanou M, Nikolopoulou A, Chiotellis E, Raptopoulou CP, Vlahos AT, Terzis A, Papadopoulos M, Chiotellis E: Development of novel mixed-ligand oxotechnetium [SNS/S] complexes as potential 5-HT1A receptor imaging agents. J Biol Inorg Chem. 2001 Mar;6(3):256-65. The complexes are carrying the 1-(2-methoxyphenyl) piperazine moiety, a fragment of the true 5-HT1A antagonist WAY 100635, either on the monodentate ligand [S] or on the tridentate ligand [SN (R) S]. |
35(0,1,1,5) | Details |
| 14718609 | Zuideveld KP, Van der Graaf PH, Newgreen D, Thurlow R, Petty N, Jordan P, Peletier LA, Danhof M: Mechanism-based pharmacokinetic-pharmacodynamic modeling of 5-HT1A receptor agonists: estimation of in vivo affinity and intrinsic efficacy on body temperature in rats. J Pharmacol Exp Ther. 2004 Mar;308(3):1012-20. Epub 2004 Jan 8. Between 5-HT (1A) agonists wide differences in in vivo affinity and efficacy were observed, with values of the pK (A) ranging from 5.67 for flesinoxan to 8.63 for WAY-100,635 [N-(2-(4-(2-methoxyphenyl)-1-piperazinyl) ethyl)-N-2-pyridinyl-cyclohexanec arboxamide] and of the log tau ranging from -1.27 for WAY-100,135 [N-(1,1-dimethylethyl)-4-(2-methoxyphenyl)-alpha-phenyl-1-piperazine-propa namide] to 0.62 for R-(+)-8--2-[di-n-propylamino) tetralin. |
35(0,1,1,5) | Details |
| 16421514 | Auclair AL, Kleven MS, Besnard J, Depoortere R, Newman-Tancredi A: Actions of novel antipsychotic agents on apomorphine-induced PPI disruption: influence of combined 5-HT1A receptor activation and dopamine D2 receptor blockade. Neuropsychopharmacology. 2006 Sep;31(9):1900-9. Epub 2006 Jan 18. |
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| 20007849 | Foong JP, Parry LJ, Gwynne RM, Bornstein JC: 5-HT (1A), SST (1), and SST (2) receptors mediate inhibitory postsynaptic potentials in the submucous plexus of the guinea pig ileum. Am J Physiol Gastrointest Liver Physiol. 2010 Mar;298(3):G384-94. Epub 2009 Dec 10. |
5(0,0,0,5) | Details |
| 11100975 | Harikumar KG, John PT, Chattopadhyay A: Role of disulfides and sulfhydryl groups in agonist and antagonist binding in serotonin1A receptors from bovine hippocampus. Cell Mol Neurobiol. 2000 Dec;20(6):665-81. The serotonin1A (5-HT1A) receptors are members of a superfamily of seven-transmembrane-domain receptors that couple to G-proteins. |
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| 15296084 | Silanes SP, Orus L, Oficialdegui AM, Martinez Esparza J, Lasheras B, Del Rio J, Monge A: New 3-[4-(2,3-dihydro-14-benzodioxin-5-yl) piperazin-1-yl]-1-(5-substituted benzo [b] thiophen-3-yl) derivatives with dual action at 5-HT (1A) serotonin receptors and serotonin transporter as a new class of antidepressants. Pharmazie. 2004 Jul;59(7):499-501. Compounds derived from 2,3-dihydro-(1,4-benzodioxin-5-yl) piperazine and benzo [b] thiophene with different substituents in 5 position (H, F, NO2, NH2, CH3 and OH) have been synthesized in order to obtain new dual antidepressant drugs. |
3(0,0,0,3) | Details |
| 16946546 | Feenstra RW, van den Hoogenband A, Stroomer CN, van Stuivenberg HH, Tulp MT, Long SK, van der Heyden JA, Kruse CG: SAR study of 1-aryl-4-(phenylarylmethyl) piperazines as ligands for both D2 and 5-HT1A receptors showing varying degrees of (Ant) agonism. Chem Pharm Bull. 2006 Sep;54(9):1326-30. |
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| 17284006 | O'Connor NA, Paisner DA, Huryn D, Shea KJ: Screening of 5-HT1A receptor antagonists using molecularly imprinted polymers. J Am Chem Soc. 2007 Feb 14;129(6):1680-9. |
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| 17490739 | Schneider AM, Simson PE: NAN-190 potentiates the impairment of retention produced by swim stress. Pharmacol Biochem Behav. 2007 May;87(1):73-80. Epub 2007 Apr 11. Systemic administration of the 5-HT1A receptor antagonist NAN-190 (1 mg/kg) immediately after forced swim markedly potentiated the stress-induced impairment of retention. |
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| 12692389 | Saifullah AS, Tomioka K: 5-HT (7)-like receptors mediate serotonergic modulation of photo-responsiveness of the medulla bilateral neurons in the cricket, Gryllus bimaculatus. Zoolog Sci. 2003 Mar;20(3):303-9. Application of 8-OH-DPAT that has affinity for both 5-HT (1A) and 5-HT (7) receptors suppressed the photo-responsiveness, like forskolin. |
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| 12441172 | Siniscalchi A, Rodi D, Cavallini S, Marino S, Ferraro L, Beani L, Bianchi C: Effects of cholecystokinin tetrapeptide (CCK (4)) and of anxiolytic drugs on outflow from the cerebral cortex of freely moving rats. Neurochem Int. 2003 Jan;42(1):87-92. Similarly the (A) receptors modulator, diazepam (2mg/kg, i.p.) and the 5-HT (1A) agonist (3mg/kg, i.p.) reduced outflow and caused the expected behavioral effects (reduced muscle tone, mild syndrome) which were prevented by the respective, selective antagonists, flumazenil (1mg/kg, i.p.) and NAN-190 (3mg/kg, i.p.). |
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| 11311404 | Yonehara N: Influence of serotonin receptor antagonists on substance P and release evoked by tooth pulp stimulation with electro-acupuncture in the trigeminal nucleus cudalis of the rabbit. Neurosci Res. 2001 May;40(1):45-51. We studied the effect of NAN-190 (5-HT (1A) antagonist), ketanserin (5-HT (2) antagonist) and ICS 205-930 (5-HT (3) antagonist) on tooth pulp stimulation (TPS)-induced release and substance P (SP) release in the superficial layers of the trigeminal nucleus caudalis (SpVc-I,II) in the presence or absence of electro-acupuncture (EAP). |
1(0,0,0,1) | Details |
| 14517765 | Sugimoto Y, Inoue K, Yamada J: Involvement of 5-HT (2) receptor in -induced hyperglycemia in mice. Horm Metab Res. 2003 Sep;35(9):511-6. i. p.-induced hyperglycemia was antagonized by the 5-HT (2C/2B) receptor agonist 1-(3-chlorophenyl) piperazine (mCPP), while the 5-HT (2B) receptor agonist BW 723C86 had no effect. |
0(0,0,0,0) | Details |
| 11093763 | Morikawa H, Manzoni OJ, Crabbe JC, Williams JT: Regulation of central synaptic transmission by 5-HT (1B) auto- and heteroreceptors. Mol Pharmacol. 2000 Dec;58(6):1271-8. N-(3-Trifluoromethylphenyl) piperazine, a 5-HT (1B) receptor agonist, potently inhibited 5-HT (1A) receptor-mediated slow inhibitory postsynaptic potentials (IPSPs) in the dorsal raphe of wild-type but not knockout mice. |
0(0,0,0,0) | Details |
| 11990069 | Boksa J, Mokrosz MJ, Charakchieva-Minol S, Tatarczynska E, Klodzinska A, Wesolowska A, Misztal S: 2-H- and 2-acyl-9- [omega-[4-(2-methoxyphenyl) piperazinyl]-alkyl]-1,2,3,4-tetrahydro-beta-car bolines as ligands of 5-HT1A and 5-HT2A receptors. Pol J Pharmacol. 2001 Sep-Oct;53(5):501-8. Three series of new unsubstituted or 2-acyl 1,2,3,4-tetrahydro-beta-carbolines (THBC), connected to 1-(o-methoxyphenyl) piperazine by 2-, 3- or 4-membered alkylene spacer (3, 4 or 5, respectively) in position 9, were synthesized and their 5-HT1A/5-HT2A receptor affinities and functional in vivo activities were investigated. |
86(1,1,1,6) | Details |
| 11989808 | Chilmonczyk Z, Cybulski M, Iskra-Jopa J, Chojnacka-Wojcik E, Tatarczynska E, Klodzinska A, Les A, Bronowska A, Sylte I: Interaction of 1,2,4-substituted piperazines, new serotonin receptor ligands, with 5-HT1A and 5-HT2A receptors. Farmaco. 2002 Apr;57(4):285-301. In the present paper, we describe affinities to 5-HT1A and 5-HT2A receptors of several new 1,2,4-trisubstituted piperazine derivatives. |
86(1,1,1,6) | Details |
| 14730096 | Boksa J, Charakchieva-Minol S, Duszynska B, Bugno R, Klodzinska A, Tatarczynska E, Chojnacka-Wojcik E, Bojarski AJ: Synthesis, in vitro and in vivo 5-HT1A/5-HT2A serotonin receptor activity of new hybrid 1,2,3,4-tetrahydro-gamma-carbolines with 1-(2-methoxyphenyl) piperazine moiety. Pol J Pharmacol. 2003 Nov-Dec;55(6):1013-9. |
34(0,1,1,4) | Details |
| 15336263 | Heinrich T, Bottcher H, Schiemann K, Holzemann G, Schwarz M, Bartoszyk GD, van Amsterdam C, Greiner HE, Seyfried CA: Dual 5-HT1A agonists and re-uptake inhibitors by combination of -butyl-amine and chromenonyl-piperazine structural elements in a single molecular entity. Bioorg Med Chem. 2004 Sep 15;12(18):4843-52. |
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| 11892924 | Leslie RA: Gepirone. Curr Opin Investig Drugs. 2001 Aug;2(8):1120-7. Gepirone, a pyridinyl piperazine 5-HT1A receptor agonist, has been developed by Fabre-Kramer as an antidepressant. |
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| 12885442 | Hassanain M, Bhatt S, Siegel A: Differential modulation of feline defensive rage behavior in the medial hypothalamus by 5-HT1A and 5-HT2 receptors. Brain Res. 2003 Aug 15;981(1-2):201-9. |
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| 15985260 | Jordan S, Chen R, Koprivica V, Hamilton R, Whitehead RE, Tottori K, Kikuchi T: In vitro profile of the antidepressant candidate OPC-14523 at rat and human 5-HT1A receptors. Eur J Pharmacol. 2005 Jul 11;517(3):165-73. |
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| 12031872 | Heimbold I, Drews A, Kretzschmar M, Varnas K, Hall H, Halldin C, Syhre R, Kraus W, Pietzsch HJ, Seifert S, Brust P, Johannsen B: Synthesis, biological and autoradiographic evaluation of a novel Tc-99m radioligand derived from WAY 100635 with high affinity for the 5-HT (1A) receptor and the alpha1-adrenergic receptor. Nucl Med Biol. 2002 May;29(4):375-87. The neutral "3+1" mixed-ligand complex combines 4-(6-mercaptohexyl)-1-(2-methoxyphenyl) piperazine as monodentate and 3-(N-methyl) azapentane-1,5-dithiol as tridentate unit with oxotechnetium (V). |
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| 15628665 | Kalipatnapu S, Pucadyil TJ, Harikumar KG, Chattopadhyay A: Ligand binding characteristics of the human serotonin1A receptor heterologously expressed in CHO cells. Biosci Rep. 2004 Apr;24(2):101-15. The serotonin1A (5-HT1A) receptors are important members of the superfamily of seven transmembrane domain G-protein coupled receptors. |
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| 11399905 | Jorgensen H, Kjaer A, Warberg J, Knigge U: Differential effect of 5-HT (1A) receptor antagonists on the secretion of corticotropin and prolactin. Neuroendocrinology. 2001 May;73(5):322-33. |
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| 11006953 | Heidenreich BA, Napier TC: Effects of serotonergic 5-HT1A and 5-HT1B ligands on ventral pallidal neuronal activity. Neuroreport. 2000 Sep 11;11(13):2849-53. |
3(0,0,0,3) | Details |
| 12045674 | Costes N, Merlet I, Zimmer L, Lavenne F, Cinotti L, Delforge J, Luxen A, Pujol JF, Le Bars D: Modeling [18 F] MPPF positron emission tomography kinetics for the determination of 5-hydroxytryptamine (1A) receptor concentration with multiinjection. J Cereb Blood Flow Metab. 2002 Jun;22(6):753-65. |
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| 18800769 | Leopoldo M, Lacivita E, De Giorgio P, Fracasso C, Guzzetti S, Caccia S, Contino M, Colabufo NA, Berardi F, Perrone R: Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. J Med Chem. 2008 Sep 25;51(18):5813-22. Starting from the previously reported 5-HT 7 receptor agents 4-7 with N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamide structure, the 1-(2-methylthiophenyl)-, 1-(2-diphenyl)-, 1-(2-isopropylphenyl)-, and 1-(2-methoxyphenyl) piperazine derivatives 8-31 were designed with the primary aim to obtain new compounds endowed with suitable physicochemical properties for rapid and extensive penetration into the brain. The affinities for 5-HT 7, 5-HT 1A, and D 2 receptors of compounds 8-31 were assessed, and several compounds displayed 5-HT 7 receptor affinities in the nanomolar range. |
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| 17369909 | Sapronov NS, Fedotova YO, Losev NA: Combined administration of -190 and 17beta- abolishes the amnesic effect of in middle-aged ovariectomized rats. Bull Exp Biol Med. 2006 Jul;142(1):80-2. Chronic combined administration of 5-HT1A receptor antagonist -190 and 17beta- improved conditioned passive avoidance performance in middle-aged ovariectomized rats with -induced amnesia. |
1(0,0,0,1) | Details |
| 19845681 | Queree P, Peters S, Sharp T: Further pharmacological characterization of 5-HT (2C) receptor agonist-induced inhibition of neuronal activity in the dorsal raphe nucleus in vivo. Br J Pharmacol. 2009 Nov;158(6):1477-85. Epub 2009 Oct 20. The present study extended this pharmacological characterization by comparing the actions of WAY 161503 with the 5-HT (2C) receptor agonists, Ro 60-0275 and 1-(3-chlorophenyl) piperazine (mCPP), as well as the non-selective agonist lysergic acid diethylamide (LSD) and the releasing agent 3,4-methylenedioxymethamphetamine (MDMA). |
0(0,0,0,0) | Details |
| 12850497 | Gatch MB: Discriminative stimulus effects of m-chlorophenylpiperazine as a model of the role of serotonin receptors in anxiety. Life Sci. 2003 Aug 1;73(11):1347-67. The roles of reuptake and 5-HT1A receptors have been well characterized, but the contribution of other serotonin receptor subtypes is not as clear. 1-(3-Chlorophenyl)-piperazine (mCPP), which binds non-selectively to a wide range of serotonin receptors, has often been used to produce anxiety in humans and in animal models. |
0(0,0,0,0) | Details |
| 15680266 | Alfredo BA, Ofir P: Effect of the postsynaptic 5-HT1A receptor antagonist MM-77 on stressed mice treated with 5-HT1A receptor agents. Eur J Pharmacol. 2005 Jan 31;508(1-3):155-8. Epub 2005 Jan 11. Only the 8-OH-DPAT-induced decrease of such an effect could be blocked by the postsynaptic antagonist of the 5-HT1A receptor 1-(2-methoxyphenyl)-4-[(4-succinimido) butyl]-piperazine (MM-77). |
85(1,1,1,5) | Details |
| 12218511 | Miranda F, Orozco G, Velazquez-Martinez DN: Full substitution of the discriminative cue of a 5-HT (1A/1B/2C) agonist with the combined administration of a 5-HT (1B/2C) and a 5-HT (1A) agonist. Behav Pharmacol. 2002 Jul;13(4):303-11. In generalization tests, INDO, 8--2-(di-n-propylamino) tetralin (8-OH-DPAT, a 5-HT (1A) agonist), 1-(3-trifluoromethylphenyl) piperazine (TFMPP, a 5-HT (1B) agonist), alpha-methyl- (a 5-HT (2C) agonist) or 2-methyl- (a 5-HT (3) agonist), were administered alone or in combination. |
84(1,1,1,4) | Details |
| 11220775 | Smith BN, Sollars PJ, Dudek FE, Pickard GE: Serotonergic modulation of retinal input to the mouse suprachiasmatic nucleus mediated by 5-HT1B and 5-HT7 receptors. J Biol Rhythms. 2001 Feb;16(1):25-38. As previously described in the hamster, a mixed 5-HT (1A/1B) receptor agonist, 1-[3-(trifluoromethyl) phenyl]-piperazine hydrochloride (TFMPP), reduced the amplitude of glutamatergic excitatory postsynaptic currents (EPSCs) evoked by selectively stimulating the optic nerve of wild-type mice. |
84(1,1,1,4) | Details |
| 12466248 | Wang SJ, Coutinho V, Sihra TS: Presynaptic cross-talk of beta-adrenoreceptor and 5-hydroxytryptamine receptor signalling in the modulation of release from cerebrocortical nerve terminals. Br J Pharmacol. 2002 Dec;137(8):1371-9. The inhibitory effect of could be mimicked by the selective 5-HT (1A) receptor agonist, 8--dipropylaminotetralin (8-OH-DPAT) and antagonized by 1-(2-methoxyphenyl)-4-(4-phthalimidobutyl) piperazine (NAN-190). 5. |
33(0,1,1,3) | Details |
| 11989622 | Bronowska A, Chilmonczyk Z, Les A, Edvardsen O, Ostensen R, Sylte I: Molecular dynamics of 5-HT1A and 5-HT2A serotonin receptors with methylated analogues. J Comput Aided Mol Des. 2001 Nov;15(11):1005-23. It was found that due to the presence of the methyl group in the piperazine ring the ligand position alters and the structure of the ligand-receptor complex is modified. |
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| 16438111 | Fedotova JO, Hartmann G, Lenard L, Sapronov NS: Effects of 5-HT1A receptor agonist and antagonist on anxiety in intact and ovariectomized female rats. Acta Physiol Hung. 2004;91(3-4):175-84. |
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| 15448978 | Veenema AH, Cremers TI, Jongsma ME, Steenbergen PJ, de Boer SF, Koolhaas JM: Differences in the effects of 5-HT (1A) receptor agonists on forced swimming behavior and brain metabolism between low and high aggressive mice. Psychopharmacology. 2005 Mar;178(2-3):151-60. Epub 2004 Sep 21. |
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| 19705871 | Lacivita E, Leopoldo M, Masotti AC, Inglese C, Berardi F, Perrone R, Ganguly S, Jafurulla M, Chattopadhyay A: Synthesis and characterization of environment-sensitive fluorescent ligands for human 5-HT1A receptors with 1-arylpiperazine structure. J Med Chem. 2009 Dec 10;52(23):7892-6. A series of "long-chain" 1-(2-methoxyphenyl) piperazine derivatives containing an environment-sensitive fluorescent moiety (4-amino-1,8-naphthalimide, 4-dimethylaminophthalimide, dansyl) was synthesized. |
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| 15146031 | Millan MJ, Gobert A, Roux S, Porsolt R, Meneses A, Carli M, Di Cara B, Jaffard R, Rivet JM, Lestage P, Mocaer E, Peglion JL, Dekeyne A: The serotonin1A receptor partial agonist S15535 [4-(benzodioxan-5-yl) 1-(indan-2-yl) piperazine] enhances cholinergic transmission and cognitive function in rodents: a combined neurochemical and behavioral analysis. J Pharmacol Exp Ther. 2004 Oct;311(1):190-203. Epub 2004 May 14. In the cortex, the selective 5-HT (1A) receptor antagonist WAY100,635 [(N-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-N-(2-pyridinyl) cyclo-hexanecarboxamide) dose-dependently (0.0025-0.63) blocked this action of S15535. |
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| 12467943 | Klaassen T, Riedel WJ, van Praag HM, Menheere PP, Griez E: Neuroendocrine response to meta-chlorophenylpiperazine and ipsapirone in relation to anxiety and aggression. Psychiatry Res. 2002 Dec 15;113(1-2):29-40. Fifteen patients and 16 normal controls received single oral doses of 0.5 mg/kg meta-chlorophenylpiperazine (MCPP), a 5-HT (2C) agonist, and 10 mg of ipsapirone, a 5-HT (1A) agonist, according to a double-blind, placebo-controlled, cross-over design. |
1(0,0,0,1) | Details |
| 11853106 | Haleem DJ, Saify ZS, Siddiqui S, Batool F, Haleem MA: Pre- and postsynaptic responses to 1-(1-naphthylpiperazine) following adaptation to stress in rats. Prog Neuropsychopharmacol Biol Psychiatry. 2002 Jan;26(1):149-56. The results are discussed in the context of an increase in the effectiveness of postsynaptic 5-HT-1A and 5-HT-1B receptors and a decrease in the effectiveness of presynaptic 5-HT-1A (somatodendritic) and 5-HT-1B (terminal) receptors following adaptation to stress. |
1(0,0,0,1) | Details |
| 15178373 | Janssen P, Tack J, Sifrim D, Meulemans AL, Lefebvre RA: Influence of 5-HT1 receptor agonists on feline stomach relaxation. Eur J Pharmacol. 2004 May 25;492(2-3):259-67. Pre-treatment with -synthase inhibitors and different (1) receptor antagonists N-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-N-2-pyridinyl-cyclohexaneca rboxamide (WAY-100635), 2-methyl-4-(5-methyl-[1,2,4] oxadiazol-3-yl)-biphenyl-4-carboxylic-acid [4-m ethoxy-3-(4-methyl-piperazin-1-yl)-phenyl] amide (GR-127935), N-acetyl-5-hydroxytryptophyl--amide (5-HTP-DP) and 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine-HCl (NAN-190) did not affect the -induced effect. |
0(0,0,0,0) | Details |
| 20347301 | Fiorino F, Severino B, De Angelis F, Perissutti E, Magli E, Frecentese F, Esposito A, Massarelli P, Nencini C, Santagada V, Caliendo G: New 5-HT (1A) receptor ligands containing a N'-cyanoisonicotinamidine nucleus: Synthesis and in vitro pharmacological evaluation. Bioorg Med Chem Lett. 2010 Mar 3. The combination of structural elements (heterocyclic nucleus, alkyl chain and 4-substituted piperazine) known to be critical in order to have affinity on 5-HT (1A) receptor and the proper selection of substituents led to compounds with high specificity and affinity towards serotoninergic receptors. |
84(1,1,1,4) | Details |
| 17526557 | Szereda-Przestaszewska M, Kaczynska K: Peripheral 5-HT1A receptors are not essential for increased ventilation evoked by systemic 8-OH-DPAT challenge in anaesthetized rats. Exp Physiol. 2007 Sep;92(5):953-61. Epub 2007 May 25. Blockade of 5-HT (1A) receptors with intravenous doses of 1-(2-metoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine (NAN 190; 20 microg kg (-1)) abolished all respiratory effects of 8-OH-DPAT challenge. |
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| 15098719 | Tada K, Kasamo K, Suzuki T, Matsuzaki Y, Kojima T: Endogenous inhibits firing activity of hippocampal CA1 pyramidal neurons during conditioned fear stress-induced freezing behavior through stimulating 5-HT1A receptors. Hippocampus. 2004;14(2):143-7. The selective (5-HT) 1A antagonists, N-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-N-(2-pyridinyl) cyclohexanec arboxamide (WAY-100635), and N-tert-butyl-3-[4-(2-methoxyphenyl) piperazine-1-yl]-2-phenylpropamide (WAY-100135) and depletion with parachlorophenylalanine (PCPA) completely abolished the decrease in firing frequency during CFS-induced freezing behavior. |
33(0,1,1,3) | Details |
| 12576284 | Tsoukalas C, Pirmettis I, Patsis G, Pelecanou M, Bodo K, Raptopoulou CP, Terzis A, Papadopoulos M, Chiotellis E: Novel oxorhenium and oxotechnetium MO (NS)(S) 2 complexes in the development of 5-HT1A receptor imaging agents. J Inorg Biochem. 2003 Jan 15;93(3-4):213-20. The bidentate [NS] ligand includes the 1-(2-methoxyphenyl) piperazine moiety which is a fragment of the true 5-HT (1A) antagonist WAY 100635. |
33(0,1,1,3) | Details |
| 12809949 | Wesolowska A, Paluchowska M, Chojnacka-Wojcik E: Involvement of presynaptic 5-HT (1A) and benzodiazepine receptors in the anticonflict activity of 5-HT (1A) receptor antagonists. Eur J Pharmacol. 2003 Jun 13;471(1):27-34. In the present paper, we examined the effect of lesions of neurons, produced by p-chloroamphetamine (p-CA; 2 x 10 mg/kg), and the influence of flumazenil (Ro 15-1788, 10 mg/kg), a benzodiazepine receptor antagonist, on the anticonflict activity of N-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-N-(2-pyridinyl) cyclohexanec arboxamide (WAY 100635) and trans-1-(2-methoxy-phenyl)-4-[4-succinimidocyclohexyl] piperazine (MP 349), pre- and postsynaptic 5-HT (1A) receptor antagonists, and 1-(2-methoxyphenyl)-4-(4-succinimidobutyl) piperazine (MM 77), a postsynaptic 5-HT (1A) receptor antagonist, in the Vogel conflict drinking test in rats. |
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| 18295406 | Qu CL, Huo FQ, Huang FS, Li YQ, Tang JS, Jia H: The role of receptor subtypes in the ventrolateral orbital cortex of -induced antinociception in the rat. Neuroscience. 2008 Mar 18;152(2):487-94. Epub 2007 Sep 21. Pretreatment with receptor antagonists (1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine hydrobromide (NAN-190), cyproheptadine hydrochloride (CPT) and 1-methyl-N-(8-methyl-8-azabicyclo [3.2.3]-oct-3-yl)-1H-indazole-3-carboxami de salt (LY-278,584)), specific for 5-HT (1A), 5-HT (2) and 5-HT (3) receptors, respectively, partially reversed the -evoked inhibition. |
32(0,1,1,2) | Details |
| 12505530 | Astier B, Lambas Senas L, Souliere F, Schmitt P, Urbain N, Rentero N, Bert L, Denoroy L, Renaud B, Lesourd M, Munoz C, Chouvet G: In vivo comparison of two 5-HT1A receptors agonists alnespirone (S-20499) and on locus coeruleus neuronal activity. Eur J Pharmacol. 2003 Jan 10;459(1):17-26. The aim of the present study was to compare, in chloral-hydrate anaesthetized rats, the alpha (2)-adrenergic properties of the selective 5-HT (1A) receptor agonist, alnespirone (S-20499), with those of a 5-HT (1A) receptor agonist exhibiting potent alpha (2)-adrenoceptor antagonist properties via its principal metabolite, 1-(2-pyrimidinyl)-piperazine. |
32(0,1,1,2) | Details |
| 12163345 | Rodriguez-Manzo G, Lopez-Rubalcava C, Hen R, Fernandez-Guasti A: Participation of 5-HT (1B) receptors in the inhibitory actions of on masculine sexual behaviour of mice: pharmacological analysis in 5-HT (1B) receptor knockout mice. Br J Pharmacol. 2002 Aug;136(8):1127-34. 1 The role of the (1B) (5-HT (1B)) receptor subtype in masculine sexual behaviour in mice was analysed in both 5-HT (1B) receptor knockout (KO (1B)) and wild-type (WT) animals. 2 Comparison of male copulatory behaviour of WT and KO (1B) strains revealed that KO (1B) mice become interested earlier in sexual behaviour, but require more stimulation to achieve ejaculation than its corresponding WT strain. 3 The pharmacological manipulation of male sexual activity in the WT strain showed that the precursor the 5-HT (1B) agonist (1-(m-trifluoromethylphenyl) piperazine (TFMPP) and the (1A) (5-HT (1A)) receptor agonist 8--2-di-n-propylamino-tetralin (8-OH-DPAT) all inhibited male copulatory behaviour in mice. 4 In KO (1B) mice, TFMPP lacked an effect, exerted a mild inhibitory effect while 8-OH-DPAT provoked only a tendency towards a reduction in the percentage of animals that achieved ejaculation. |
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| 12354565 | Chen J, Shen C, Meller E: 5-HT1A receptor-mediated regulation of mitogen-activated protein kinase phosphorylation in rat brain. Eur J Pharmacol. 2002 Oct 4;452(2):155-62. The effect of 8-OH-DPAT was blocked by pretreatment with the selective 5-HT (1A) receptor antagonists N-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-N-2-pyridinylcyclohexanecar boxamide (WAY 100635), 1-(2-methoxyphenyl)-4-(4-[2-phthalimido] butyl) piperazine (NAN-190) and 4--N-(2-[4-(2-methoxyphenyl) 1-piperazinyl] ethyl)-N-(2-pyridinyl) benz amide dihydrochloride (p-MPPF), but not by the weak partial agonist/antagonist 8-(2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl)-8-azaspiro (4.5) decane-7,9-d ione dihydrochloride (BMY 7378). |
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| 11282365 | Sorensen E, Gronli J, Bjorvatn B, Bjorkum A, Ursin R: Sleep and waking following microdialysis perfusion of the selective 5-HT1A receptor antagonist p-MPPI into the dorsal raphe nucleus in the freely moving rat. Brain Res. 2001 Apr 6;897(1-2):122-30. |
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| 15476688 | Praschak-Rieder N, Hussey D, Wilson AA, Carella A, Lee M, Dunn E, Willeit M, Bagby RM, Houle S, Meyer JH: depletion and loss in selective reuptake inhibitor-treated depression: an [(18) F] MPPF positron emission tomography study. Biol Psychiatry. 2004 Oct 15;56(8):587-91. With [(18) F] MPPF positron emission tomography (PET), (5-hydroxytryptamine, 5-HT) 1A receptor binding potential (5-HT (1A) BP) was measured after TD in various brain regions in -treated depression. |
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| 11350497 | Fernandez MM, Calama E, Moran A, Martin ML, San Roman L: Characterization of mechanisms involved in presynaptic inhibition of sympathetic pressor effects induced by some 5-HT1 receptor antagonists. J Auton Pharmacol. 2000 Oct-Dec;20(5-6):313-23. In a previous study, we showed that the presynaptic inhibitory action of 5-hydroxytryptamine receptor agonists on sympathetic pressor effects obtained in the pithed rats were mainly mediated by activation of 5-HT1A and 5-HT1D receptor subtypes. |
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| 12177685 | Hoerr R, Noeldner M: Ensaculin (KA-672 HCl): a multitransmitter approach to dementia treatment. CNS Drug Rev. 2002 Summer;8(2):143-58. Ensaculin, a novel benzopyranone substituted with a piperazine moiety, showed memory-enhancing effects in paradigms of passive and conditioned avoidance in both normal and artificially amnesic rodents. In receptor-binding studies, ensaculin was found to have high affinities to serotonergic 5-HT (1A) and 5-HT (7) receptors, adrenergic alpha (1), and dopaminergic D (2) and D (3) receptors. |
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| 15896731 | Mosher T, Hayes D, Greenshaw A: Differential effects of 5-HT2C receptor ligands on place conditioning and locomotor activity in rats. Eur J Pharmacol. 2005 May 16;515(1-3):107-16. Effects of the (5-HT)(1A/1B/2C) receptor agonist N-[3-(trifluoromethyl) phenyl] piperazine (TFMPP, 0-3.0 mg/kg s.c.) and the 5-HT2C receptor agonist 8,9-dichloro-2,3,4,4a-tetrahydro-1H-pyrazino [1,2-a] quinoxalin-5 (6H)-one (WAY 161503, 0-3.0 mg/kg s.c.) in place conditioning were measured in male Sprague-Dawley rats. Effects of TFMPP, alone and with the 5-HT (1A) receptor antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-N-2-pyridinyl-cyclohexanecarboxamine (WAY 100635), the 5-HT (1B) receptor antagonist N-[4-methoxy-3-(4-methyl-1-piperazinyl) phenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-1,1'-biphenyl-4-carbo xamide (GR 127935) or the 5-HT2C receptor antagonist 6-chloro-5-methyl-1-[[2-(2-methylpyrid-3-yloxy) pyrid-5-yl] carbamoyl] indoli ne (SB 242084) and of WAY 161503 alone and with SB 242084 on locomotor activity were also assessed. |
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| 17494642 | Wong H, Dockens RC, Pajor L, Yeola S, Grace JE Jr, Stark AD, Taub RA, Yocca FD, Zaczek RC, Li YW: 6-Hydroxybuspirone is a major active metabolite of assessment of pharmacokinetics and 5-hydroxytryptamine1A receptor occupancy in rats. Drug Metab Dispos. 2007 Aug;35(8):1387-92. Epub 2007 May 9. Both compounds appeared to be approximately 4-fold more potent in occupying presynaptic 5-HT (1A) receptors in the dorsal raphe than the postsynaptic receptors in the hippocampus. Oral dosing of in rats resulted in exposures (area under the concentration-time profile) of 6-OH- and 1-(2-pyrimidinyl)-piperazine (1-PP), another major metabolite of that were approximately 12 (6-OH-- and 49 (1-PP)-fold higher than the exposure of the parent compound. |
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| 11978164 | Caley CF, Cooper CK: Ziprasidone: the fifth atypical antipsychotic. Ann Pharmacother. 2002 May;36(5):839-51. Ziprasidone has demonstrated in vitro activity as a 5-HT (1A) receptor agonist and as a very weak inhibitor of and reuptake. DATA SYNTHESIS: Ziprasidone is a benzisothiazolyl piperazine-type atypical antipsychotic that shares the (2A)/ (2) (5-HT (2A)/D (2)) profile of the available atypical antipsychotics. |
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| 11124393 | Schreiber R, Selbach K, Asmussen M, Hesse D, de Vry J: Effects of (1/2) receptor agonists on dark-phase food and water intake in rats. Pharmacol Biochem Behav. 2000 Oct;67(2):291-305. The following agonists were tested: ipsapirone [preferred receptor (s) and dose range in mg/kg, IP: 5-HT (1A) and 3-30, respectively], CP-94,253 (5-HT (1B); 0.3-3), TFMPP (5-HT (1B/2C); 0. 3-10), m-CPP (5-HT (2C/1B); 0.3-10), ORG 37684 (5-HT (2C); 0.3-10), BW 723C86 (5-HT (2B); 3-30) and DOI (5-HT (2A/2C); 0.3-3). |
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| 17523441 | Barabanova SV, Fedotova IuO, Sapronov NS: [Effects of antagonists of 1A and 2A/2C subtypes of serotonin receptors on the depressive behavior and expression of c-Fos protein in hypothalamus of ovariectomized rats]. Eksp Klin Farmakol. 2007 Mar-Apr;70(2):3-7. We have studied the influence of a chronic administration of the 5-HT (2A/2C) receptor antagonist ketanserin (0.1 mg/kg, i.p.) and the 5-HT (1A) receptor antagonist NAN-190 (0.1 mg/kg, i.p.) alone or in combinations with 17beta- (0.5 mg per animal, i.m.) for 14 days on the depressive behavior and expression of c-Fos protein in the paraventricular nucleus of hypothalamus in adult ovariectomized (OVX) female rats. |
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| 16878490 | Sapronov NS, Fedotova IuO, Losev NA: [Optimizing effect of the combined administration of 8-OH-DPAT and galantamine on depression--anxiety behavior in old rats with dementia of Alzheimer's type]. Eksp Klin Farmakol. 2006 May-Jun;69(3):10-3. The effect of chronic (14 days) administration of the 5-HT (1A) receptors agonist 8-OH-DPAT (0.05 mg/kg, s.c.) and the 5-HT (1A) receptors antagonist -190 (0.1 mg/kg, i.p.) alone or in combination with the acetylcholinesterase inhibitor galantamine (1.0 mg/kg, i.p.) on depression and anxiety was studied in old (24 months) male rats with dementia of Alzheimer's type. |
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| 20022748 | Dilly S, Graulich A, Liegeois JF: Molecular modeling study of 4-phenylpiperazine and 4-phenyl-1,2,3,6-tetrahydropyridine derivatives: a new step towards the design of high-affinity 5-HT1A ligands. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1118-23. Epub 2009 Dec 6. However, the replacement of the piperazine moiety by a 1,2,3,6-tetrahydropyridine ring in 4-arylpiperazine-ethyl carboxamide derivatives was recently shown to be highly favourable for 5-HT (1A) affinity. |
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| 15733547 | Kommalage M, Hoglund AU: Involvement of spinal serotonin receptors in the regulation of intraspinal release. Eur J Pharmacol. 2005 Feb 21;509(2-3):127-34. The 5-HT1A receptor selective antagonist (S)-N-tert-butyl-3-(4-(2-methoxyphenyl) piperazine-1-yl)-2-phenylpropanamid e hydrochloride and the 5-HT2A receptor selective antagonist ketanserin inhibited the 8-OH-DPAT and the m5-HT induced release. |
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| 18190908 | Heusler P, Newman-Tancredi A, Loock T, Cussac D: Antipsychotics differ in their ability to internalise human D2S and human 5-HT1A receptors in HEK293 cells. Eur J Pharmacol. 2008 Feb 26;581(1-2):37-46. Epub 2007 Nov 28. Among antipsychotics with combined D (2)/5-HT (1A) properties, bifeprunox and (3-exo)-8-benzoyl-N-[[(2S) 7-chloro-2,3-dihydro-1,4-benzodioxin-1-yl] methyl ]-8-azabicyclo-[3.2.1] -3- (SSR181507) partially internalised HA-hD (2S) receptors, piperazine, 1-(2,3-dihydro-1,4-benzodioxin-5-yl)-4-[[5-(4-fluorophenyl)-3-pyridinyl] me thyl (SLV313) and N-[(2,2-dimethyl-2,3-dihydro-benzofuran-7-yloxy) ethyl]-3-(cyclopent-1-enyl )-benzylamine (F15063) were inactive. |
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| 11710750 | Mello e Souza T, Rodrigues C, Souza MM, Vinade E, Coitinho A, Choi H, Izquierdo I: Involvement of the serotonergic type 1A (5-HT1A) receptor in the agranular insular cortex in the consolidation of memory for inhibitory avoidance in rats. Behav Pharmacol. 2001 Sep;12(5):349-53. After recovery, animals were trained in a step-down inhibitory avoidance task (3.0-s, 0.4-mA footshock) and received, immediately after training, a 0.5-microl infusion of the serotonergic type 1A (5-HT1A) receptor agonist dipropylamino-8-hydroxy-1,2,3,4-tetrahydronaphthalene hydrobromide (8-OH-DPAT) or of the 5- HT1A receptor antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine hydrobromide (NAN-190), or of vehicle alone (20% DMSO). |
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| 15595840 | Pucadyil TJ, Kalipatnapu S, Harikumar KG, Rangaraj N, Karnik SS, Chattopadhyay A: G-protein-dependent cell surface dynamics of the human serotonin1A receptor tagged to yellow fluorescent protein. Biochemistry. 2004 Dec 21;43(50):15852-62. The serotonin (1A) receptor is an important member of the superfamily of seven transmembrane domain G-protein-coupled receptors and is the most extensively studied among the serotonin receptors. |
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| 16805803 | Khawaja XZ, Smith DL, Nawoschik SP, Zhang J, Dunlop J, Dilks DW, Olsen M, Schechter LE: WAY-100635 antagonist-induced plasticity of receptors: regulatory differences between a stable cell line and an in vivo native system. J Neurochem. 2006 Jul;98(1):134-45. We present evidence that the (1A) (5-HT (1A)) receptor antagonist, N-{2-[4-(2-methoxyphenyl)-1-piperazinyl]-ethyl}-N-(2-pyridinyl) cyclohexane carboxamide (WAY-100635), can induce receptor internalization in a human (h) 5-HT (1A) receptor Chinese hamster ovary (CHO-K1) cell system. Similar results were obtained for 8-OH-DPAT-mediated Ca (2+) mobilization after WAY-100635 treatment. h5-HT (1A) receptors labeled with [(3) H] WAY-100635, as well as [(3) H] 4-(2'-Methoxy)-phenyl-1-[2'-(N-2''-pyridinyl)-p-fluorobenzamido] ethy l-piperazine (MPPF), exhibited a time-dependent rate of cellular internalization that was blocked by endocytotic suppressors and was pertussis-toxin insensitive. |
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| 15801844 | Lopez-Rodriguez ML, Morcillo MJ, Fernandez E, Benhamu B, Tejada I, Ayala D, Viso A, Campillo M, Pardo L, Delgado M, Manzanares J, Fuentes JA: Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. J Med Chem. 2005 Apr 7;48(7):2548-58. Computational simulation of ligand-receptor interaction of 5-HT (1A) R agonists with selectivity over alpha1-adrenoceptors.. The aryl substituent of the piperazine moiety (Ar) consists of different benzofused rings mimicking the favorable voluminous substituents at ortho and meta positions predicted by 3D-QSAR analysis in the previously reported series I. |
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| 11167653 | Testa R, Guarneri L, Angelico P, Velasco C, Poggesi E, Cilia A, Leonardi A: Effect of different 5-hydroxytryptamine receptor subtype antagonists on the micturition reflex in rats. BJU Int. 2001 Feb;87(3):256-64. The affinity for the human recombinant serotoninergic 5-HT1A subtype (inhibition of specific binding of [3H] 8-hydroxy-2-(di-n-propylamino) tetralin) and the effects on the [35S] 5'-(gamma-thio) (GTPgammaS) binding in HeLa cells was also evaluated. |
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| 18995929 | Herold F, Chodkowski A, Izbicki L, Krol M, Kleps J, Turlo J, Nowak G, Stachowicz K, Dybala M, Siwek A: Novel 4-aryl-pyrido [1,2-c] pyrimidines with dual SSRI and 5-HT1A activity, part 1. Eur J Med Chem. 2009 Apr;44(4):1710-7. Epub 2008 Sep 30. |
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| 12480170 | Kojima T, Matsumoto M, Togashi H, Tachibana K, Kemmotsu O, Yoshioka M: Fluvoxamine suppresses the long-term potentiation in the hippocampal CA1 field of anesthetized rats: an effect mediated via 5-HT1A receptors. Brain Res. 2003 Jan 3;959(1):165-8. |
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| 18765418 | Lothe A, Didelot A, Hammers A, Costes N, Saoud M, Gilliam F, Ryvlin P: Comorbidity between temporal lobe epilepsy and depression: a [18F] MPPF PET study. Brain. 2008 Oct;131(Pt 10):2765-82. Epub 2008 Sep 2. We used a distinct 5-HT (1A) antagonist, [(18) F] MPPF, whose binding potential depends on both receptor density and extracellular concentration, in 24 patients with drug-resistant TLE and MRI evidence of hippocampal sclerosis but without prior antidepressant exposure. |
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| 16579052 | Fedotova IuO: [Effect of 8-OH-DPAT on the depressive behavior and monoamine metabolism in the hippocampus of ovariectomized rats]. Eksp Klin Farmakol. 2006 Jan-Feb;69(1):12-7. The influence of the chronic administration of the 5-HT1A receptor agonist 8-OH-DPAT (0.05 mg/kg, s.c.) and the 5-HT1A receptor antagonist NAN-190 (0.1 mg/kg, i.p.) alone or in combination with 17beta- (0.5 microg per animal, i.m.) for 14 days on the depression behavior and the monoamine level in hippocampus has been studied in adult ovariectomized (OVX) female rats. |
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| 17825569 | Paluchowska MH, Bugno R, Duszynska B, Tatarczynska E, Nikiforuk A, Lenda T, Chojnacka-Wojcik E: The influence of modifications in imide fragment structure on 5-HT (1A) and 5-HT (7) receptor affinity and in vivo pharmacological properties of some new 1-(m-trifluoromethylphenyl) piperazines. Bioorg Med Chem. 2007 Nov 15;15(22):7116-25. Epub 2007 Aug 22. New, flexible (7, 9, 11 and 13) and rigid (8, 10, 12 and 14) imides with a 1-(m-trifluorophenyl) piperazine fragment and a tetramethylene or a 1e,4e-cyclohexylene spacer, respectively, showed very high affinity (K (i)=0.3-34 nM) and agonistic in vivo activity for 5-HT (1A) receptors. |
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| 11068023 | Passchier J, van Waarde A, Doze P, Elsinga PH, Vaalburg W: Influence of P-glycoprotein on brain uptake of [18F] MPPF in rats. Eur J Pharmacol. 2000 Nov 3;407(3):273-80. Anesthetized male Wistar rats were injected i.v. with the 5-HT1A receptor antagonist [18F] MPPF (2 MBq, S.A.> 110 TBq/mmol) after treatment with saline (controls) or with the 5-HT1A receptor antagonist 1-(2'-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine (NAN-190) (2.5 mg/kg i.v.). |
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| 11068021 | Kishimoto K, Koyama S, Akaike N: Presynaptic modulation of synaptic transmission by tandospirone in rat basolateral amygdala. Eur J Pharmacol. 2000 Nov 3;407(3):257-65. The similar inhibition of miniature IPSC frequency was mimicked by a specific 5-HT1A receptor agonist 8--2-(di-n-propylamino) tetralin (8-OH-DPAT, 1 microM), and the effects of tandospirone were prevented in the presence of a specific 5-HT1A receptor antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine hydrobromide (NAN-190, 1 microM). |
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| 16032412 | Troelsen KB, Nielsen EO, Mirza NR: Chronic treatment with duloxetine is necessary for an anxiolytic-like response in the mouse zero maze: the role of the serotonin transporter. Psychopharmacology. 2005 Oct;181(4):741-50. Epub 2005 Sep 29. In mice treated chronically, (a) the hypothermic response to (5-HT) 1A and 5-HT1B receptor ligands, 8--2-(di-n-propylamino) tetralin (8-OHDPAT) and m-chlorophenyl piperazine (mCPP), respectively, was assessed and (b) serotonin transporter (SERT) and transporter (NET) densities in the cortex and hippocampus, respectively, were determined. |
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| 16216322 | Park WK, Jeong D, Cho H, Lee SJ, Cha MY, Pae AN, Choi KI, Koh HY, Kong JY: KKHA-761, a potent D3 receptor antagonist with high 5-HT1A receptor affinity, exhibits antipsychotic properties in animal models of schizophrenia. Pharmacol Biochem Behav. 2005 Oct;82(2):361-72. Epub 2005 Oct 10. KKHA-761, 1-{4-[3-(3,4-dimethoxy-phenyl)-isoxazol-5-yl]-butyl}-4-(2-methoxy-phenyl)- piperazine, has a high affinity (Ki=3.85 nM) for human D3 receptor with about 70-fold selectivity over the human D (2L) receptor (Ki=270 nM). |
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| 15680262 | Andrews CM, Kung HF, Lucki I: The 5-HT1A receptor modulates the effects of cocaine on extracellular and levels in the nucleus accumbens. Eur J Pharmacol. 2005 Jan 31;508(1-3):123-30. Epub 2005 Jan 12. |
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| 15653354 | Marchais-Oberwinkler S, Nowicki B, Pike VW, Halldin C, Sandell J, Chou YH, Gulyas B, Brennum LT, Farde L, Wikstrom HV: N-oxide analogs of WAY-100635: new high affinity 5-HT (1A) receptor antagonists. Bioorg Med Chem. 2005 Feb 1;13(3):883-93. |
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| 18469535 | Farrell MS, Gilmore K, Raffa RB, Walker EA: Behavioral characterization of serotonergic activation in the flatworm Planaria. Behav Pharmacol. 2008 May;19(3):177-82. This study characterized the behavioral and locomotor effects of a 5-HT1A agonist, a 5-HT1B/2C agonist, and a 5-HT1A antagonist to examine the role of receptor activation in this species. |
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| 11965359 | Popova NK, Amstislavskaya TG: Involvement of the 5-HT (1A) and 5-HT (1B) serotonergic receptor subtypes in sexual arousal in male mice. Psychoneuroendocrinology. 2002 Jul;27(5):609-18. |
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| 11804612 | Hemrick-Luecke SK, Evans DC: Comparison of the potency of MDL 100,907 and SB 242084 in blocking the (5-HT)(2) receptor agonist-induced increases in rat serum concentrations: evidence for 5-HT (2A) receptor mediation of the HPA axis. Neuropharmacology. 2002 Feb;42(2):162-9. Direct-acting receptor agonists increase serum in rats by activating receptors of the 5-HT (1A) or the 5-HT (2A/2C) subtypes. |
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| 14640559 | Orjales A, Mosquera R, Toledo A, Pumar MC, Garcia N, Cortizo L, Labeaga L, Innerarity A: Syntheses and binding studies of new [(aryl)(aryloxy) methyl] piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for and (NE) transporters. J Med Chem. 2003 Dec 4;46(25):5512-32. In a wide search program toward new, efficient, and fast-acting antidepressant drugs, we have prepared series of new compounds having an (aryl)(aryloxy) methyl moiety linked directly or through a methylene chain to different substituted and unsubstituted cycles (isoquinoline, piperazine, piperidine, tetrahydropyran, or cyclopentane). These compounds have been evaluated for their affinities for (5-HT) transporter (SERT) and 5-HT (1A) and 5-HT (2A) receptors. |
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| 12046990 | Iwahori Y, Ikegaya Y, Matsuki N: Hyperpolarization-activated current I (h) in nucleus of solitary tract neurons: regional difference in serotonergic modulation. Jpn J Pharmacol. 2002 Apr;88(4):459-62. The effect of was blocked by NAN-190, a 5-HT1A receptor antagonist. |
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| 17258195 | Sato M, Ago Y, Koda K, Nakamura S, Kawasaki T, Baba A, Matsuda T: Role of postsynaptic serotonin1A receptors in -induced increase in release in rat prefrontal cortex. Eur J Pharmacol. 2007 Mar 22;559(2-3):155-60. Epub 2006 Dec 29. The present study examined the role of (5-HT) 1A receptors in -induced increases in release in rat prefrontal cortex. On the other hand, local application of (3 and 10 microM), the 5-HT1A receptor agonist 8--2-(di-n-propylamino) tetralin (1 and 10 microM), and the dopamine D4 receptor antagonist 3-(4-(4-iodophenyl) piperazine-1-yl) methyl-1H-pyrrolo [2,3-b] (1 and 10 microM) into the cortex did not affect release in the prefrontal cortex. |
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| 11239924 | Vis P, Della Pasqua O, Kruk M, Martin D, Mocaer E, Danhof M, Jochemsen R: Population pharmacokinetic-pharmacodynamic modelling of S 15535, a 5-HT (1A) receptor agonist, using a behavioural model in rats. Eur J Pharmacol. 2001 Mar 2;414(2-3):233-43. The pharmacokinetic-pharmacodynamic relationship of S 15535 (1-(benzodioxan-5-yl) 4-(indan-2-yl) piperazine) and its active 5- metabolite S 32784 (1-(benzodioxan-5-yl) 4-(5-hydroxyindan-2-yl) piperazine), and as a reference, were studied in male Wistar rats using a behavioural model of anxiety by determining the reduction in the number of fear-induced ultrasonic vocalisations. |
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| 18238859 | Minato K, Suzuki R, Asagarasu A, Matsui T, Sato M: Biotransformation of 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl) piperazin-1-yl] butyl}qui nazolin-4 (3H)-one (TZB-30878), a novel (5-HT) 1A agonist/5-HT3 antagonist, in human hepatic cytochrome P450 enzymes. Drug Metab Dispos. 2008 May;36(5):831-40. Epub 2008 Jan 31. This compound has quinazoline, piperazine, and quinoline rings. |
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| 12523493 | Wesolowska A, Borycz J, Paluchowska MH, Chojnacka-Wojcik E: Pharmacological analysis of the hypothermic effects of NAN-190 and its analogs, postsynaptic 5-HT1A receptor antagonists, in mice. Pol J Pharmacol. 2002 Jul-Aug;54(4):391-9. In this study, we examined the role of (5-HT) 1A and alpha1-adrenergic receptors in the hypothermia induced by 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl]-piperazine (NAN-190) and its analogs, 1-(2-methoxyphenyl)-4-[(4-succinimido) butyl] piperazine (MM77) and trans-1 (2-methoxyphenyl)-4-[4-(2-phthalimido) cyclohexyl] piperazine (MP245), which--like NAN-190--showed a high affinity for 5-HT1A and alpha1-adrenoceptors. |
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| 17263189 | de Paulis T: Drug evaluation: PRX-00023, a selective 5-HT1A receptor agonist for depression. Curr Opin Investig Drugs. 2007 Jan;8(1):78-86. EPIX Pharmaceuticals Inc (formerly Predix Pharmaceuticals Inc) is developing PRX-00023, an oral aryl piperazine 5-HT1A agonist, for the potential treatment of depression. |
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| 12433595 | Villalobos-Molina R, Gallardo-Ortiz IA, Lopez-Guerrero JJ, Ibarra M: Evidence that NAN-190-induced hypotension involves vascular alpha1-adrenoceptor antagonism in the rat. Eur J Pharmacol. 2002 Nov 22;455(1):59-64. The effect of NAN-190 (1-(2-methoxyphenyl)-4-[4-(2-phthalimido]-butyl] piperazine), described as a mixed 5-HT (1A) receptor agonist/antagonist, on cardiovascular function was studied. |
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| 18007421 | Bojarski AJ, Mokrosz MJ, Duszynska B, Koziol A, Bugno R: New imide 5-HT1A receptor ligands - modification of terminal fragment geometry. Molecules. 2004 Feb 28;9(3):170-7. |
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| 11294742 | Miyawaki T, Goodchild AK, Pilowsky PM: Rostral ventral medulla 5-HT1A receptors selectively inhibit the somatosympathetic reflex. Am J Physiol Regul Integr Comp Physiol. 2001 May;280(5):R1261-8. |
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| 18673144 | Weber KC, Honorio KM, Andricopulo AD, Da Silva AB: Two-dimensional QSAR studies on arylpiperazines as high-affinity 5-HT (1A) receptor ligands. Med Chem. 2008 Jul;4(4):328-35. |
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| 19735696 | Naumenko VS, Kondaurova EM, Popova NK: Central 5-HT3 receptor-induced hypothermia in mice: interstrain differences and comparison with hypothermia mediated via 5-HT1A receptor. Neurosci Lett. 2009 Nov 6;465(1):50-4. Epub 2009 Sep 6. |
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| 11259559 | Harrison AA, Markou A: Serotonergic manipulations both potentiate and reduce brain stimulation reward in rats: involvement of serotonin-1A receptors. J Pharmacol Exp Ther. 2001 Apr;297(1):316-25. |
4(0,0,0,4) | Details |
| 12204476 | Santana L, Uriarte E, Fall Y, Teijeira M, Teran C, Garcia-Martinez E, Tolf BR: Synthesis and structure-activity relationships of new arylpiperazines: para substitution with electron-withdrawing groups decrease binding to 5-HT (1A) and D (2A) receptors. Eur J Med Chem. 2002 Jun;37(6):503-10. Electron-withdrawing phenyl ring substituents para to the piperazine strongly reduced activity at both receptors. |
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| 18187421 | Lopez JJ, Lorch M: Location and orientation of serotonin receptor 1a agonists in model and complex lipid membranes. J Biol Chem. 2008 Mar 21;283(12):7813-22. Epub 2008 Jan 9. Most of the agonists orient approximately parallel to the membrane plane, with the exception of quipazine, whose piperazine ring is found in the region, whereas its ring is located within the lipid hydrophobic chain. |
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| 15972834 | Hsiao CF, Wu N, Chandler SH: Voltage-dependent currents in trigeminal motoneurons of early postnatal rats: modulation by receptors. J Neurophysiol. 2005 Sep;94(3):2063-72. Epub 2005 Jun 22. HVA current inhibition was mimicked by 5-CT, a 5-HT1 receptor agonist, and by R (+)-8-hydroxydipropylaminotetralin hydrobromide (8-OH-DPAT), a specific 5-HT1A agonist. The effects of were blocked by the 5-HT1A antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine hydrobromide (NAN-190) but not by ketanserin, a 5-HT (2/1C) antagonist. |
2(0,0,0,2) | Details |
| 12477356 | Leopoldo M, Berardi F, Colabufo NA, De Giorgio P, Lacivita E, Perrone R, Tortorella V: Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl) butyl] arylcarboxamides as potent and selective D (3) receptor ligands. J Med Chem. 2002 Dec 19;45(26):5727-35. Changes in the aromatic ring linked to N-1 piperazine ring led to the identification of 2-methoxyphenyl and 2,3-dichlorophenyl derivatives (compounds 6 and 13) displaying moderate D (3) affinity (K (i) = 145 and 31 nM, respectively). In this way, we identified several high-affinity D (3) ligands (0.13 nM < K (i)'s < 4.97 nM) endowed with high selectivity over D (2), D (4), 5-HT (1A), and alpha (1) receptors. |
1(0,0,0,1) | Details |
| 14557612 | Schneider AM, Wilkins E, Firestone A, Everbach EC, Naylor JC, Simson PE: Enhanced retention in the passive-avoidance task by 5-HT (1A) receptor blockade is not associated with increased activity of the central nucleus of the amygdala. Learn Mem. 2003 Sep-Oct;10(5):394-400. The effect of blockade of 5-HT1A receptors was investigated on (1). retention in a mildly aversive passive-avoidance task, and (2). spontaneous single-unit activity of central nucleus of the amygdala (CeA) neurons, a brain site implicated in modulation of retention. |
1(0,0,0,1) | Details |
| 17074317 | Harada K, Aota M, Inoue T, Matsuda R, Mihara T, Yamaji T, Ishibashi K, Matsuoka N: Anxiolytic activity of a novel potent 5-HT2C receptor antagonist FR260010: a comparison with diazepam and Eur J Pharmacol. 2006 Dec 28;553(1-3):171-84. Epub 2006 Sep 28. These results suggest that FR260010 is a novel, potent, orally active and brain penetrable antagonist of 5-HT (2C) receptor, and may have therapeutic potential for treatment of anxiety, with more desirable profiles than benzodiazepines or (1A) (5-HT (1A)) receptor agonists. Hyperfunction of brain (2C) (5-HT (2C)) receptor is suggested to be involved in anxiety as evidenced by the fact that a putative 5-HT (2C) receptor agonist 1-(m-chlorophenyl)-piperazine (m-CPP) causes anxiety in humans. |
1(0,0,0,1) | Details |
| 15005884 | Leopoldo M, Berardi F, Colabufo NA, Contino M, Lacivita E, Perrone R, Tortorella V: Studies on 1-arylpiperazine derivatives with affinity for rat 5-HT7 and 5-HT1A receptors. J Pharm Pharmacol. 2004 Feb;56(2):247-55. Several 1-aryl-4-(2-arylethyl) piperazine derivatives were synthesized and tested in-vitro for their binding affinity for 5-HT (7) and 5-HT (1A) receptors. |
83(1,1,1,3) | Details |
| 15802819 | Sugimoto Y, Takashima N, Noma T, Yamada J: Inhibitory effects of the 5-HT (1A) receptor agonist on stress-induced hyperglycemia in mice: involvement of insulin and a metabolite, 1-(2-pyrimidinyl) piperazine (1-PP). Biol Pharm Bull. 2005 Apr;28(4):733-5. |
31(0,1,1,1) | Details |
| 15145080 | Johnson PJ, Bornstein JC: Neurokinin-1 and -3 receptor blockade inhibits slow excitatory synaptic transmission in myenteric neurons and reveals slow inhibitory input. Neuroscience. 2004;126(1):137-47. They were abolished by the 5-hydroxytryptamine (1A) receptor antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl]-piperazine (NAN-190), but unaffected by phentolamine, an alpha-adrenoceptor antagonist. |
31(0,1,1,1) | Details |
| 11860184 | Harikumar KG, Chattopadhyay A: Modulation of antagonist binding to serotonin1A receptors from bovine hippocampus by metal ions. Cell Mol Neurobiol. 2001 Oct;21(5):453-64. The serotonin1A (5-HT1A) receptors are members of a superfamily of seven transmembrane domain receptors that couple to G-proteins. |
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| 16438112 | Fedotova JO, Hartmann G, Lenard L, Sapronov NS: Involvement of 5-HT1A receptors in passive avoidance learning in intact and ovariectomized female rats. Acta Physiol Hung. 2004;91(3-4):185-96. |
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| 19464324 | Auclair AL, Kleven MS, Barret-Grevoz C, Barreto M, Newman-Tancredi A, Depoortere R: Differences among conventional, atypical and novel putative D (2)/5-HT (1A) antipsychotics on catalepsy-associated behaviour in cynomolgus monkeys. Behav Brain Res. 2009 Nov 5;203(2):288-95. Epub 2009 May 21. |
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| 16386718 | Egashira N, Yano A, Ishigami N, Mishima K, Iwasaki K, Fujioka M, Matsushita M, Nishimura R, Fujiwara M: Investigation of mechanisms mediating 8-OH-DPAT-induced impairment of spatial memory: involvement of 5-HT1A receptors in the dorsal hippocampus in rats. Brain Res. 2006 Jan 19;1069(1):54-62. Epub 2006 Jan 4. |
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| 14996544 | Dalton GL, Lee MD, Kennett GA, Dourish CT, Clifton PG: mCPP-induced hyperactivity in 5-HT2C receptor mutant mice is mediated by activation of multiple receptor subtypes. Neuropharmacology. 2004 Apr;46(5):663-71. In the present group of experiments, we evaluate the role of 5-HT1A, 5-HT1B and 5-HT2A receptors in mCPP-induced hyperactivity in 5-HT2C KO mice. |
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| 17657585 | Yi PL, Lin CP, Tsai CH, Lin JG, Chang FC: The involvement of serotonin receptors in suanzaorentang-induced sleep alteration. J Biomed Sci. 2007 Nov;14(6):829-40. Epub 2007 Jul 27. One ingredient of suanzaorentang, zizyphi spinosi semen, exhibits binding affinity for receptors, 5-HT (1A) and 5-HT (2), and for GABA receptors. |
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| 12166933 | Betti L, Botta M, Corelli F, Floridi M, Giannaccini G, Maccari L, Manetti F, Strappaghetti G, Tafi A, Corsano S: Alpha (1)-adrenoceptor antagonists. 4. J Med Chem. 2002 Aug 15;45(17):3603-11. Our aim was also to study the influence of the position of both the chloro and the methoxy groups on the piperazine phenyl ring, as well as the effect of the lengthening or shortening of the polymethylene spacer linking the phenylpiperazine moiety to the terminal heterocyclic portion. Biological evaluation by radioligand receptor binding assays toward alpha (1)-AR, alpha (2)-AR, and 5-HT (1A) serotoninergic receptors indicated compounds characterized by very good alpha (1)-AR affinity and selectivity. |
1(0,0,0,1) | Details |
| 11494406 | Lin CH, Huang YC, Tsai JJ, Gean PW: Modulation of voltage-dependent currents by in acutely isolated rat amygdala neurons. Synapse. 2001 Sep 15;41(4):351-9. The inhibition was mimicked by the selective 5-HT1A agonist 8--dipropylaminotetralin (8-OH-DPAT) and was reduced by the 5-HT1A antagonist NAN-190, indicating its mediation by 5-HT1A receptors. |
1(0,0,0,1) | Details |
| 17392733 | Lee JJ, Hahm ET, Lee CH, Cho YW: Serotonergic modulation of GABAergic and glutamatergic synaptic transmission in mechanically isolated rat medial preoptic area neurons. Neuropsychopharmacology. 2008 Jan;33(2):340-52. Epub 2007 Mar 28. Serotonergic inhibition of mIPSC frequency was mimicked by (+/-)-8--2-dipropylaminotetralin hydrobromide, a specific 5-HT (1A) receptor agonist, and blocked by 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine hydrobromide, a specific 5-HT (1A) receptor antagonist. 6--7-nitroquinoxaline-2,3-dione completely blocked spontaneous glutamatergic miniature excitatory postsynaptic currents (mEPSCs) in the MPOA. |
83(1,1,1,3) | Details |
| 19854053 | Gray DL, Xu W, Campbell BM, Dounay AB, Barta N, Boroski S, Denny L, Evans L, Stratman N, Probert A: Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting reuptake inhibitors and 5-HT1A partial agonists. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7. Epub 2009 Oct 12. |
83(1,1,1,3) | Details |
| 16153839 | Wyman PA, Marshall HR, Flynn ST, King RJ, Thompson M, Smith PW, Hadley MS, Price GW, Scott CM, Dawson LA: Identification of a potent and selective 5-HT1B receptor antagonist. . Bioorg Med Chem Lett. 2005 Nov 1;15(21):4708-12. An SAR study around the mixed 5-HT1ABD receptor antagonist SB-272183 found that introduction of cis-2,6-dimethyl substitution onto the piperazine ring was a key structural change, which imparted a combination of both excellent selectivity over the 5-HT1A and 5-HT1D receptors and low intrinsic activity. |
31(0,1,1,1) | Details |
| 12166089 | Tsuji K: [Effect of (+/-)-pindolol on the central 5-HT1A receptor by the use of in vivo microdialysis and hippocampal slice preparations]. Nihon Shinkei Seishin Yakurigaku Zasshi. 2002 Jun;22(3):85-95. |
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| 11754589 | Peglion JL, Goument B, Despaux N, Charlot V, Giraud H, Nisole C, Newman-Tancredi A, Dekeyne A, Bertrand M, Genissel P, Millan MJ: Improvement in the selectivity and metabolic stability of the 5-HT (1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols. J Med Chem. 2002 Jan 3;45(1):165-76. While S 15535 itself presents reasonable selectivity (158-fold) in this respect, trans piperazine derivatives 4-trans,35, 39, 41, 47, 64, 68, 69, 70, 71 displayed even more pronounced selectivity vs alpha1-adrenoceptors, with the nitro derivative 70 being highly selective (1259-fold). |
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| 11275295 | Sorensen E, Gronli J, Bjorvatn B, Ursin R: The selective 5-HT (1A) receptor antagonist p-MPPI antagonizes sleep--waking and behavioural effects of 8-OH-DPAT in rats. Behav Brain Res. 2001 Jun;121(1-2):181-7. |
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| 16767512 | Pucadyil TJ, Jafurulla M, Chattopadhyay A: Prolonged treatment with ligands affects ligand binding to the human serotonin (1A) receptor in Chinese hamster ovary cells. Cell Mol Neurobiol. 2006 May;26(3):247-57. Epub 2006 Apr 21. |
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| 19640898 | Miyazato M, Kaiho Y, Kamo I, Kitta T, Chancellor MB, Sugaya K, Arai Y, de Groat WC, Yoshimura N: Role of spinal serotonergic pathways in sneeze-induced urethral continence reflex in rats. Am J Physiol Renal Physiol. 2009 Oct;297(4):F1024-31. Epub 2009 Jul 29. To clarify the role of spinal serotonergic mechanisms in preventing stress urinary incontinence (SUI) during sneezing, we investigated the effect of intrathecal (it) application of 8-OH-DPAT (a 5-HT (1A) agonist), mCPP (a 5-HT (2B/2C) agonist), and fluoxetine (a reuptake inhibitor) using a rat model that can examine the neurally evoked continence reflex during sneezing. |
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| 18081887 | Fiske E, Portas CM, Gronli J, Sorensen E, Bjorvatn B, Bjorkum AA, Ursin R: Increased extracellular but no change in sleep after perfusion of a 5-HT1A antagonist into the dorsal raphe nucleus of rats. Acta Physiol. 2008 May;193(1):89-97. Epub 2007 Dec 14. AIM: The 5-HT (1A) receptor antagonist 4-Iodo-N-[2-[4-(methoxyphenyl)-1-piperazinyl] ethyl]-N-2-pyridinyl-benzamid e hydrochloride (p-MPPI) (10 microM) was perfused into the dorsal raphe nucleus (DRN) to study simultaneously the effects of the drug on the DRN and frontal cortex extracellular levels and concurring behavioural states. |
2(0,0,0,2) | Details |
| 11377919 | Harrison AA, Liem YT, Markou A: Fluoxetine combined with a serotonin-1A receptor antagonist reversed reward deficits observed during and amphetamine withdrawal in rats. Neuropsychopharmacology. 2001 Jul;25(1):55-71. |
2(0,0,0,2) | Details |
| 15018926 | Betti L, Floridi M, Giannaccini G, Manetti F, Paparelli C, Strappaghetti G, Botta M: Design, synthesis, and alpha (1)-adrenoceptor binding properties of new arylpiperazine derivatives bearing a nucleus as the terminal heterocyclic molecular portion. Bioorg Med Chem. 2004 Mar 15;12(6):1527-35. Following our research project aimed at obtaining new compounds with high affinity and selectivity toward alpha (1)-adrenoceptors (AR), a new class of piperazine derivatives was designed, synthesized and biologically tested. Biological data showed an interesting profile for the phenylpiperazine subclass found to have a nanomolar affinity toward alpha (1)-AR, and less pronounced affinity for alpha (2)-AR and the 5-HT (1A) serotoninergic receptor. |
1(0,0,0,1) | Details |
| 16682960 | Kim HW, Kwon YB, Roh DH, Yoon SY, Han HJ, Kim KW, Beitz AJ, Lee JH: Intrathecal treatment with sigma1 receptor antagonists reduces formalin-induced phosphorylation of NMDA receptor subunit 1 and the second phase of formalin test in mice. Br J Pharmacol. 2006 Jun;148(4):490-8. Epub 2006 May 8. BMY-14802 ((alpha-(4-fluorophenyl)-4-(5--2-pyrimidinyl)-1-piperazinebutanol hydrochloride) (10-100 nmol, sigma (1) receptor antagonist and 5-HT (1A) receptor agonist) dose dependently reduced formalin-induced pain behaviors in both phases. |
1(0,0,0,1) | Details |
| 19560916 | Zajdel P, Subra G, Verdie P, Gabzdyl E, Bojarski AJ, Duszynska B, Martinez J, Pawlowski M: Sulfonamides with the N-alkyl-N'-dialkylguanidine moiety as 5-HT7 receptor ligands. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4827-31. Epub 2009 Jun 13. A series of arylsulfonamides containing incorporated in the structure of secondary amines (piperidine, piperazine) was synthesized on SynPhase Lanterns and evaluated for 5-HT (1A), 5-HT (2A), and 5-HT (7) receptors. |
82(1,1,1,2) | Details |
| 11448518 | Hasuo H, Akasu T: facilitates spatiotemporal propagation of optical signals in the hippocampal-septal pathway. Neurosci Res. 2001 Jul;40(3):265-72. Bicuculline blocked the -induced facilitation of the optical signal. 8--di-n-propylamino tetralin (8-OH-DPAT), a selective 5-HT (1A) agonist, mimicked the facilitation of 1-(2-Methoxyphenyl)-4-(4-phthalimidobutyl) piperazine (NAN-190), a 5-HT (1A) antagonist, blocked the facilitation induced by 5-HT. 5-HT enhanced the amplitude of the field potential in septal slices, where the optical signals had been enhanced. |
82(1,1,1,2) | Details |
| 19827295 | Fiorino F, Severino B, De Angelis F, Perissutti E, Magli E, Frecentese F, Esposito A, Massarelli P, Nencini C, Viti B, Santagada V, Caliendo G: Synthesis and in vitro pharmacological evaluation of a new series of 5-HT1A 5-HT2A and 5-HT2C receptor ligands containing a norbornene nucleus. Pharmazie. 2009 Sep;64(9):555-64. A series of 4-substituted piperazine derivatives bearing a norbornene nucleus have been prepared and their affinity for 5-HT1A, 5-HT2A and 5-HT2C receptors has been evaluated. |
82(1,1,1,2) | Details |
| 11438622 | Passchier J, van Waarde A, Vaalburg W, Willemsen AT: On the quantification of [18F] MPPF binding to 5-HT1A receptors in the human brain. J Nucl Med. 2001 Jul;42(7):1025-31. Previous studies have shown that 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pyridinyl)-p-[(18) F] fluorobenzamido] ethyl piperazine ([(18) F] MPPF) binds with high selectivity to (5-HT (1A)) receptors in man. |
82(1,1,1,2) | Details |
| 12087877 | Pruus K, Rudisaar R, Vaarmann A, Matto V, Allikmets L: 1-(1-naphthyl)-piperazine, a mixed 5-HT1A and 5-HT2A/2C receptor ligand, elicits an anxiolytic-like effect in the open-field test without changes in metabolism. Methods Find Exp Clin Pharmacol. 2002 Apr;24(3):151-7. |
31(0,1,1,1) | Details |
| 12202639 | Mori A, Kogo M, Ishihama K, Tanaka S, Enomoto A, Koizumi H, Matsuya T: Effect of on trigeminal rhythmic activities generated in in vitro brainstem block preparations. J Dent Res. 2002 Sep;81(9):598-602. In the present study, both the 5-HT (1A) phthalimido-butyl-piperazine, and the 5-HT (2C) agonist, 1-2,5-dimethoxy-4-iodophenyl-2-aminopropane, combined with N-methyl-D,L- and bicuculline, elicited trigeminal rhythmic activities in a whole brainstem block preparation. |
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| 12191650 | Caldwell HK, Albers HE: The effects of agonists on the hypothalamic regulation of sexual receptivity in Syrian hamsters. Horm Behav. 2002 Aug;42(1):78-84. In the present experiments, we investigated the role of 5-HT (1a/7) and 5-HT (2) receptor subtypes in the MPOA-AH in the control of lordosis. |
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| 19283364 | Paquette MA, Foley K, Brudney EG, Meshul CK, Johnson SW, Berger SP: The sigma-1 antagonist BMY-14802 inhibits -induced abnormal involuntary movements by a WAY-100635-sensitive mechanism. Psychopharmacology. 2009 Jul;204(4):743-54. Epub 2009 Mar 13. OBJECTIVES: Although BMY-14802 is widely used as a sigma-1 antagonist, it is also an agonist at (5-HT) 1A and adrenergic alpha-1 receptors. |
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| 18006194 | Andric D, Roglic G, Sukalovic V, Soskic V, Kostic-Rajacic S: Synthesis, binding properties and receptor docking of 4-halo-6-[2-(4-arylpiperazin-1-yl) ethyl]-1H-benzimidazoles, mixed ligands of D2 and 5-HT1A receptors. Eur J Med Chem. 2008 Aug;43(8):1696-705. Epub 2007 Oct 7. |
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| 16026684 | Djavadian RL, Wielkopolska E, Turlejski K: Postnatal treatment with NAN-190 but not with 5-HT1A receptor agonists retards growth of the rat brain. Int J Dev Neurosci. 2005 Aug;23(5):485-93. We investigated the influence of prolonged administration of the 5-HT1A receptor agonists (8-OH-DPAT or or its antagonist, NAN-190 to rat pups on development of their cortical barrel field. |
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| 18996171 | Ita ML, Cortes Mdel C, Valencia J, Eguibar JR: Activation of 5-HT1-receptors decreased gripping-induced immobility episodes in taiep rats. Neurosci Lett. 2009 Jan 9;449(2):147-50. Epub 2008 Oct 30. In male 8-month-old taiep rats we have studied the effect of systemic administration of serotonergic autoreceptor agonists and antagonists on gripping-induced IEs. 8--2-(di-n-propylamino) tetraline hydrobromide (8-OH-DPAT), a 5-HT (1A) agonist, and 3-trifluoromethylphenylpiperazine hydrochloride (TFMPP), a 5-HT (1B) agonist, produce a significant decrease in the frequency and mean duration of IEs. Systemic administration of spiperone and 1-(2-methoxyphenyl)-4 [4-(2-phthalimido) butyl] piperazine hydrobromide (NAN-190), (1) antagonists, increase IEs and their mean duration. |
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| 15892984 | Kubera M, Maes M, Kenis G, Kim YK, Lason W: Effects of and serotonergic agonists and antagonists on the production of tumor necrosis factor alpha and interleukin-6. Psychiatry Res. 2005 Apr 30;134(3):251-8. In the present article we examine the role of in modulating the production of two pro-inflammatory cytokines, i.e. interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNFalpha), as well as the role of 5-HT (1A) and 5-HT (2) receptors in this process. |
2(0,0,0,2) | Details |
| 17942093 | Wang R, Xu Y, Wu HL, Li YB, Li YH, Guo JB, Li XJ: The antidepressant effects of in the forced swimming test involve 5-HT1 and 5-HT2 receptors. Eur J Pharmacol. 2008 Jan 6;578(1):43-50. Epub 2007 Sep 19. Moreover, pre-treatment of pindolol (10 mg/kg, i.p., a beta-adrenoceptors blocker/5-HT (1A/1B) receptor antagonist), 4-(2'-methoxy-phenyl)-1-[2'-(n-2''-pyridinyl)-p-iodobenzamino-] ethyl-piper azine (p-MPPI, 1 mg/kg, s.c., a selective 5-HT (1A) receptor antagonist), or 1-(2-(1-pyrrolyl)-phenoxy)-3-isopropylamino- (isamoltane, 2.5 mg/kg, i.p., a 5-HT (1B) receptor antagonist) was found to prevent the effect of (10 mg/kg) in forced swimming test. |
2(0,0,0,2) | Details |
| 17649988 | Leopoldo M, Lacivita E, Contino M, Colabufo NA, Berardi F, Perrone R: Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. J Med Chem. 2007 Aug 23;50(17):4214-21. Epub 2007 Jul 25. Here we report the synthesis of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides 16-29 that were designed to elucidate both structure-affinity and -activity relationships for the 5-HT7 receptor, by targeting the substituent in 2-position of the aryl linked to the piperazine ring. The affinities of 16-29 for 5-HT7, 5-HT1A, 5-HT2A, and D2 receptors were assessed by radioligand binding assays. |
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| 11902118 | Zimmer L, Mauger G, Le Bars D, Bonmarchand G, Luxen A, Pujol JF: Effect of endogenous on the binding of the 5-hT1A PET ligand 18F-MPPF in the rat hippocampus: kinetic beta measurements combined with microdialysis. J Neurochem. 2002 Jan;80(2):278-86. |
2(0,0,0,2) | Details |
| 11489454 | Jeong HJ, Han SH, Min BI, Cho YW: 5-HT1A receptor-mediated activation of G-protein-gated inwardly rectifying K+ current in rat periaqueductal gray neurons. Neuropharmacology. 2001 Aug;41(2):175-85. I5-HT was mimicked by a 5-HT1A receptor selective agonist, 8-OH-DPAT, and was reversibly blocked by a 5-HT1A receptor antagonist, piperazine but not by a 5-HT2 receptor antagonist, ketanserin. |
2(0,0,0,2) | Details |
| 15165573 | Lehr T, Schipp R: Serotonergic regulation of the central heart auricles of Sepia officinalis L. (Mollusca, Cephalopoda). Comp Biochem Physiol A Mol Integr Physiol. 2004 May;138(1):69-77. The chronotropic effects of were blocked mainly by the (1,2) antagonist methiothepin (pA (2)=8.01), the 5-HT (1a) antagonist NAN-190 (pA (2)-) and in lesser extent by the (1,2) antagonist mianserin (pA (2)=6.81). |
1(0,0,0,1) | Details |
| 18456500 | Yoon J, Yoo EA, Kim JY, Pae AN, Rhim H, Park WK, Kong JY, Park Choo HY: Preparation of piperazine derivatives as 5-HT7 receptor antagonists. . Bioorg Med Chem. 2008 May 15;16(10):5405-12. Epub 2008 Apr 15. Among the synthesized compounds, 3c showed a good activity on 5-HT (7) receptors and a good selectivity on 5-HT (1a), 5-HT (2a), 5-HT (2c), and 5-HT (6) receptors. |
1(0,0,0,1) | Details |
| 11327592 | Sabb AL, Vogel RL, Kelly MG, Palmer Y, Smith DL, Andree TH, Schechter LE: 1,2,5-Thiadiazole derivatives are potent and selective ligands at human 5-HT1A receptors. Bioorg Med Chem Lett. 2001 Apr 23;11(8):1069-71. Amino acid derivatives of 1,2,5-thiadiazol-3-yl-piperazine related to (+)-WAY-100135 and WAY-100635 are potent 5-HT1A receptor agonists and antagonists, which have selective affinity for 5-HT1A receptors versus alpha1 and (D2, D3, and D4) receptors. |
82(1,1,1,2) | Details |
| 20000410 | Cai M, Li Z, Fan F, Huang Q, Shao X, Song G: Design and synthesis of novel insecticides based on the serotonergic ligand 1-[(4-aminophenyl) ethyl]-4-[3-(trifluoromethyl) phenyl] piperazine (PAPP). J Agric Food Chem. 2010 Mar 10;58(5):2624-9. 1-[(4-Aminophenyl) ethyl]-4-[3-(trifluoromethyl) phenyl] piperazine (PAPP) is a 5-HT (1A) agonist and was reported to display high affinity for receptor from the parasitic nematode Haemonchus contortus . |
31(0,1,1,1) | Details |
| 16813429 | Chiotellis A, Tsoukalas C, Pelecanou M, Papadopoulos A, Raptopoulou C, Terzis A, Pirmettis I, Papadopoulos M, Chiotellis E: Synthesis and characterization of novel "3 + 2" oxorhenium complexes, ReO [SNO][NN]. Inorg Chem. 2006 Jul 10;45(14):5635-40. The [SNO][NN] mixed-ligand system was applied in the synthesis of the oxorhenium complex 5 in which the 1-(2-methoxyphenyl) piperazine moiety, a fragment of the true 5-HT1A antagonist WAY 100635, has been incorporated in the NN bidentate ligand (NN is N-{3-[4-(2-methoxyphenyl) piperazin-1-yl] propyl}pyridine-2-aldimine). |
31(0,1,1,1) | Details |
| 12726821 | Tordera R, Pei Q, Newson M, Gray K, Sprakes M, Sharp T: Effect of different 5-HT1A receptor antagonists in combination with paroxetine on expression of the immediate-early gene Arc in rat brain. Neuropharmacology. 2003 Jun;44(7):893-902. |
3(0,0,0,3) | Details |
| 15341484 | Heinrich T, Bottcher H, Gericke R, Bartoszyk GD, Anzali S, Seyfried CA, Greiner HE, Van Amsterdam C: Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT (1A) receptor agonists and reuptake inhibitors. J Med Chem. 2004 Sep 9;47(19):4684-92. |
3(0,0,0,3) | Details |
| 11323141 | Zhang Y, Yang Z, Gao X, Wu G: The role of 5-hydroxytryptamine1A and 5-hydroxytryptamine1B receptors in modulating spinal nociceptive transmission in normal and carrageenan-injected rats. Pain. 2001 May;92(1-2):201-11. Intrathecal injection of the (1A) (5-HT1A) receptor agonist 8--DPAT hydroxybromide (8-OH-DPAT) (0.305, 1.525, 3.05, and 15.25 mM) dose-dependently increased Adelta- and C-responses and post-discharge in most of the WDR neurons. |
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| 15698535 | Ginawi OT, Al-Majed AA, Al-Suwailem AK: NAN-190, a possible specific antagonist for methamphetamine. . Regul Toxicol Pharmacol. 2005 Mar;41(2):122-7. Epub 2004 Dec 19. Effect of NAN-190, a selective 5-HT (1A) receptor antagonist, on methamphetamine-induced locomotor activity, anorexia, analgesia, and hyperthermia was investigated in male mice. |
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| 11198126 | Winsauer PJ, Moerschbaecher JM: Differential effects of agonists and antagonists on the repeated acquisition and performance of response sequences in monkeys. Behav Pharmacol. 2000 Nov;11(7-8):535-53. As a means of characterizing the role of 5-HT1A and 5-HT2A receptors in learning, agonists and antagonists with selective affinities for each receptor subtype (i.e. 8-hydroxy-dipropylaminotetralin (8-OH-DPAT), (-)-4-(dipropylamino)-1,3,4,5-tetrahydrobenz-(c,d,) -6-carboxamide (LY228729), (+/-)-1-(4-iodo-2,5-dimeth-oxyphenyl)-2-aminopropane hydrochloride (DOI), 4-iodo-N-[2- [4-(methoxyphenyl)-1-piperazinyl] ethyl]-N-2-pyridinyl-benzamide hydrochloride (p-MPPI), N-[2- [4- (2-methoxyphenyl)-1-piperazinyl] ethyl] -N-2-pyridinyl-cyclohexanecarboxamide (WAY-100635), 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyllpiperazine hydrobromide (NAN-190) and ritanserin) were administered to monkeys responding under a multiple schedule of repeated acquisition and performance. |
2(0,0,0,2) | Details |
| 15634021 | Costantino L, Gandolfi F, Sorbi C, Franchini S, Prezzavento O, Vittorio F, Ronsisvalle G, Leonardi A, Poggesi E, Brasili L: Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent sigma ligands. J Med Chem. 2005 Jan 13;48(1):266-73. Thus, to confirm the ability of the piperazine derivative to bind to sigma (1) receptors in a different way than piperidines, we synthesized and tested a series of piperazine compounds; the comparison of their affinity with that of the corresponding piperidines strongly supports the possibility of a different binding mode. While the compounds here described are on the whole selective for sigma vs 5-HT (1A) and D (2) receptors, 9aa, 9ba and 9ab possess a remarkable affinity for both sigma and 5-HT (1A) receptors, with K (i) in the nanomolar range, and are selective with respect to D (2) receptors. |
2(0,0,0,2) | Details |
| 18367171 | Lee JJ, Hahm ET, Lee CH, Cho YW: 5-HT1A receptor-mediated activation of a G-protein-coupled inwardly rectifying K+ current in rat medial preoptic area neurons. Eur J Pharmacol. 2008 May 31;586(1-3):114-22. Epub 2008 Mar 4. The -activated K+ current was mimicked by a 5-HT1A receptor agonist, (+/-)-8--2-dipropylaminotetralin hydrobromide, and was reversibly blocked by a 5-HT1A receptor antagonist, 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine hydrobromide, but not by a 5-HT2 receptor antagonist, ketanserin. |
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| 15493297 | Herold F, Krol M, Kleps J: Synthesis of new hexahydro- and octahydropyrido [1,2-c] pyrimidine derivatives with an arylpiperazine moiety as ligands for 5-HT1A and 5-HT2A receptors. Acta Pol Pharm. 2004 Mar-Apr;61(2):139-50. The final products III-XXVI were obtained by condensation of aryl- or heteroaryl- piperazine with the bromobutyl derivatives IIa-f. |
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| 15582454 | Chu W, Tu Z, McElveen E, Xu J, Taylor M, Luedtke RR, Mach RH: Synthesis and in vitro binding of N-phenyl piperazine analogs as potential D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87. Binding studies were also conducted to determine if the compounds bound to sigma (sigma (1) and sigma (2)) and (5-HT (1A), 5-HT (2A), 5-HT (2B), 5-HT (2C), 5-HT (3), 5-HT (4), 5-HT (5), 5-HT (6), and 5-HT (7)) receptors. |
2(0,0,0,2) | Details |
| 15450869 | Lehr T, Schipp R: An antagonistic receptor system in the auricles of the systemic heart complex of Sepia officinalis L. (Cephalopoda) shows 5-HT1 and 5-HT4 subtype properties. Comp Biochem Physiol C Toxicol Pharmacol. 2004 Jun;138(2):213-9. In pharmacological bioassays on isolated ring-shaped auricle preparations of Sepia officinalis, the action of the specific agonists 8-OH-DPAT (5-HT1a), CP-93129 (5-HT1b), TFMPP (5-HT1b) and RS-67333 (5-HT4) on these autonomously contractile compartments was studied. 8-OH-DPAT and CP-93129 induced mainly positive effects on frequency and tone on the isotonically suspended auricles. |
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| 15452682 | Markou A, Harrison AA, Chevrette J, Hoyer D: Paroxetine combined with a 5-HT (1A) receptor antagonist reversed reward deficits observed during amphetamine withdrawal in rats. Psychopharmacology. 2005 Mar;178(2-3):133-42. Epub 2004 Sep 25. |
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| 11167306 | Dwyer D, Browning J: Endurance training in Wistar rats decreases receptor sensitivity to a agonist. Acta Physiol Scand. 2000 Nov;170(3):211-6. Improved resistance to the fatiguing effects of the agonist suggests desensitization of central serotonin receptors, probably the 5-HT1A receptors. |
1(0,0,0,1) | Details |
| 16376083 | Betti L, Zanelli M, Giannaccini G, Manetti F, Schenone S, Strappaghetti G: Synthesis of new piperazine-pyridazinone derivatives and their binding affinity toward alpha1-, alpha2-adrenergic and 5-HT1A serotoninergic receptors. Bioorg Med Chem. 2006 Apr 15;14(8):2828-36. Epub 2005 Dec 20. |
82(1,1,1,2) | Details |
| 12486804 | Tsai CL, Wang LH, Tsai CC: Role of and in the behavioral thermoregulation of female tilapia during the prespawning phase. J Exp Zool. 2002 Oct 1;293(5):443-9. This effect was mimicked by the agonist of 5-HT1A, 1B, and 2C receptors, N-3-trifluoromethylphenyl piperazine. |
81(1,1,1,1) | Details |
| 15727878 | Bojarski AJ, Paluchowska MH, Duszynska B, Klodzinska A, Tatarczynska E, Chojnacka-Wojcik E: 1-Aryl-4-(4-succinimidobutyl) piperazines and their conformationally constrained analogues: synthesis, binding to (5-HT1A, 5-HT2A, 5-HT7), alpha1-adrenergic, and dopaminergic D2 receptors, and in vivo 5-HT1A functional characteristics. Bioorg Med Chem. 2005 Mar 15;13(6):2293-303. Starting with the structure of potent 5-HT (1A) ligands, that is, MM77 [1-(2-methoxyphenyl)-4-(4-succinimidobutyl) piperazine, 4] and its constrained version 5 (MP349), previously obtained in our laboratory, a series of their direct analogues with differently substituted aromatic ring (R=H, m-Cl, m-CF (3), m-OCH (3), p-OCH (3)) were synthesized. |
66(0,2,2,6) | Details |
| 19607850 | Youn J, Misane I, Eriksson TM, Millan MJ, Ogren SO, Verhage M, Stiedl O: Bidirectional modulation of classical fear conditioning in mice by 5-HT (1A) receptor ligands with contrasting intrinsic activities. Neuropharmacology. 2009 Oct-Nov;57(5-6):567-76. Epub 2009 Jul 15. |
9(0,0,0,9) | Details |
| 11728188 | Perrone R, Berardi F, Colabufo NA, Leopoldo M, Lacivita E, Tortorella V, Leonardi A, Poggesi E, Testa R: trans-4-[4-(Methoxyphenyl) cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT (1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl) propyl]-1-arylpiperazine s. J Med Chem. 2001 Dec 6;44(25):4431-42. Among the new derivatives emerged trans-4-[4-(3-methoxyphenyl) cyclohexyl]-1-(2-pyridinyl) piperazine (trans-8a) and trans-N-[4-(3-methoxyphenyl) cyclohexyl]-2-(2-pyridyloxy) ethylamine (trans-8b). |
8(0,0,0,8) | Details |
| 11166326 | Milligan G, Kellett E, Dacquet C, Dubreuil V, Jacoby E, Millan MJ, Lavielle G, Spedding M: S 14506: novel receptor coupling at 5-HT (1A) receptors. . Neuropharmacology. 2001 Mar;40(3):334-44. |
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| 18778728 | Khorana N, Young R, Glennon RA: Effect of 8--2-(N,N-di-n-propylamino) tetralin and MDMA on the discriminative stimulus effects of the classical hallucinogen DOM in rats. Pharmacol Biochem Behav. 2009 Jan;91(3):385-92. Epub 2008 Aug 17. Co-administration of the 5-HT1A serotonin receptor agonist (+/-) 8--2-(N,N-di-n-propylamino) tetralin [(+/-) 8-OH DPAT] enhances the discriminative stimulus effects of the classical hallucinogen 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) in rats. |
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| 12192569 | Zimmer L, Pain F, Mauger G, Plenevaux A, Le Bars D, Mastrippolito R, Pujol JF, Renaud B, Laniece P: The potential of the beta-Microprobe, an intracerebral radiosensitive probe, to monitor the [(18) F] MPPF binding in the rat dorsal raphe nucleus. Eur J Nucl Med Mol Imaging. 2002 Sep;29(9):1237-47. Epub 2002 Jul 25. The aim of this study was to demonstrate the ability of a recently developed beta (+)-range sensitive intracerebral probe (beta-Microprobe) to measure the binding kinetics of [(18) F] MPPF, a well-documented 5-HT (1A) serotoninergic receptor ligand, in the dorsal raphe nucleus (DRN) of the anaesthetised rat. |
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| 18639866 | Galusca B, Costes N, Zito NG, Peyron R, Bossu C, Lang F, Le Bars D, Estour B: Organic background of restrictive-type anorexia nervosa suggested by increased serotonin 1A receptor binding in right frontotemporal cortex of both lean and recovered patients: [18F] MPPF PET scan study. Biol Psychiatry. 2008 Dec 1;64(11):1009-13. Epub 2008 Jul 18. |
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| 12237254 | Welsby PJ, Carr IC, Wilkinson G, Milligan G: Regulation of the avidity of ternary complexes containing the human 5-HT (1A) receptor by mutation of a receptor contact site on the interacting G protein alpha subunit. Br J Pharmacol. 2002 Oct;137(3):345-52. |
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| 19647047 | Bhatt S, Bhatt RS, Zalcman SS, Siegel A: Peripheral and central mediators of lipopolysaccharide induced suppression of defensive rage behavior in the cat. Neuroscience. 2009 Nov 10;163(4):1002-11. Epub 2009 Jul 30. A determination of the central mechanisms governing LPS suppression revealed that pretreatment of the medial hypothalamus with PGE (2) or 5-HT (1A) receptor antagonists each completely blocked the suppressive effects of LPS, while microinjections of a TNF-alpha antibody into the medial hypothalamus were ineffective. |
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| 19434397 | Verheij MM, Veenvliet JV, Groot Kormelink T, Steenhof M, Cools AR: Individual differences in the sensitivity to serotonergic drugs: a pharmacobehavioural approach using rats selected on the basis of their response to novelty. Psychopharmacology. 2009 Aug;205(3):441-55. Epub 2009 May 12. The 5-HT1A agonist 8-OH-DPAT and the 5-HT2 agonists mCPP and DOI decreased the duration of avoidance behaviour in LR rats, but increased it in HR rats. |
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| 15588097 | Leopoldo M, Berardi F, Colabufo NA, Contino M, Lacivita E, Niso M, Perrone R, Tortorella V: Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents. J Med Chem. 2004 Dec 16;47(26):6616-24. A series of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides was prepared and their affinity for 5-HT) 5-HT7, 5-HT (1A), and 5-HT (2A) receptors was measured by in vitro binding assays. In relation to 5-HT7 receptor affinity, receptor binding studies indicated that (i) the optimal alkyl chain length was five methylenes, (ii) an unsubstituted 1,2,3,4-tetrahydronaphthalenyl nucleus was preferred, and (iii) the substitution pattern of the aryl ring linked to the piperazine ring played a crucial role. |
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| 11198050 | Wilson AW, Costall B, Neill JC: Manipulation of operant responding for an -paired conditioned stimulus in the rat by pharmacological alteration of the serotonergic system. J Psychopharmacol. 2000;14(4):340-6. Results are consistent with involvement of the dopaminergic and systems, in particular activation of 5-HT1A and 5-HT1B receptor subtypes, in mediation of the conditioned or secondary reinforcing properties of Results showed that the releaser d-fenfluramine, the selective reuptake inhibitor fluoxetine, the 5-HT1A receptor agonist 8--2 [di-n-propylamino] tetralin, the partial 5-HT1A receptor agonist and the 5-HT1B/5-HT2C receptor agonist 1-(3-trifluoromethylphenyl) piperazine, but not the 5-HT2A/5-HT2C receptor agonist 1-(2,5-dimethoxy-4-iodophenylaminopropane)-2, selectively reduced responding on a lever leading to presentation of an paired conditioned stimulus. |
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| 15893022 | Sukalovic V, Andric D, Roglic G, Kostic-Rajacic S, Schrattenholz A, Soskic V: Synthesis, dopamine D2 receptor binding studies and docking analysis of 5-[3-(4-arylpiperazin-1-yl) propyl]-1H-benzimidazole, 5-[2-(4-arylpiperazin-1-yl) ethoxy]-1H-benzimidazole and their analogs. Eur J Med Chem. 2005 May;40(5):481-93. Epub 2005 Apr 1. 5-[3-(4-Arylpiperazin-1-yl) propyl]-1H-benzimidazoles and 5-[2-(4-arylpiperazin-1-yl) ethoxy]-1H-benzimidazoles were synthesized and their affinity for the D1, D2 and 5-HT1A receptors examined. The main features of ligand-D2 receptor interactions revealed by docking analyses were: salt bridge between piperazine ring protonated N1 and Asp 86, bonds of ligand bezimidazole part with Ser 141, Ser 122 and His 189, edge-to-face interactions of arylpiperazine aromatic ring with 178, Tyr 216 and Trp 182 and bond between ethereal in ethylenoxy ligands and of 185 or Trp 115. |
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| 12181435 | Newman-Tancredi A, Cussac D, Marini L, Millan MJ: Antibody capture assay reveals bell-shaped concentration-response isotherms for h5-HT (1A) receptor-mediated Galpha (i3) activation: conformational selection by high-efficacy agonists, and relationship to trafficking of receptor signaling. Mol Pharmacol. 2002 Sep;62(3):590-601. In contrast, the partial agonists (-)-pindolol and 4-(benzodioxan-5-yl) 1-(indan-2-yl) piperazine (S15535) displayed sigmoidal stimulation isotherms, whereas spiperone and other inverse agonists sigmoidally inhibited [(35) S] GTPgammaS binding. Agonist-induced stimulation and inverse agonist-induced inhibition of Galpha (i3) activation were i) abolished by pretreatment of CHO-h5-HT (1A) cells with pertussis toxin; ii) reversed by the selective 5-HT (1A) antagonist (N-[2-[4-(2-methoxy-phenyl)-1-piperazinyl] ethyl]-N-(2-pyridinyl)-cyclohexa ne-carboxamide) (WAY100,635), and iii) absent in nontransfected CHO cell membranes. isotherms could be modified by altering concentration; only stimulatory actions were observed at 300mM NaCl, whereas only inhibitory actions were seen at 10 mM NaCl. |
1(0,0,0,1) | Details |
| 18799312 | Bromidge SM, Bertani B, Borriello M, Faedo S, Gordon LJ, Granci E, Hill M, Marshall HR, Stasi LP, Zucchelli V, Merlo G, Vesentini A, Watson JM, Zonzini L: 6-[2-(4-Aryl-1-piperazinyl) ethyl]-2H-1,4-benzoxazin-3 (4H)-ones: dual-acting 5-HT1 receptor antagonists and reuptake inhibitors. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5653-6. Epub 2008 Aug 28. Investigation of a series 6-[2-(4-aryl-1-piperazinyl) ethyl]-2H-1,4-benzoxazin-3 (4H)-ones has led to the discovery of potent 5-HT (1A/1B/1D) receptor antagonists with and without additional SerT affinity. |
1(0,0,0,1) | Details |
| 12361392 | Asproni B, Pau A, Bitti M, Melosu M, Cerri R, Dazzi L, Seu E, Maciocco E, Sanna E, Busonero F, Talani G, Pusceddu L, Altomare C, Trapani G, Biggio G: Synthesis and pharmacological evaluation of 1-[(1,2-diphenyl-1H-4-imidazolyl) methyl]-4-phenylpiperazines with clozapine-like mixed activities at D (2), and (A) receptors. J Med Chem. 2002 Oct 10;45(21):4655-68. As for the modification of the piperazine N (4)-phenyl ring, the affinities for both D (2) like and 5-HT (1A) receptors were progressively increased by introduction of ortho-methoxy and ethoxy groups (1b,o, respectively). |
66(0,2,2,6) | Details |
| 12803776 | Wesolowska A, Paluchowska MH, Golembiowska K, Chojnacka-Wojcik E: Pharmacological characterization of MP349, a novel 5-HT1A-receptor antagonist with anxiolytic-like activity, in mice and rats. J Pharm Pharmacol. 2003 Apr;55(4):533-43. The purpose of this study was to further characterize the pharmacological effects of MP349 (trans-1-(2-methoxyphenyl)-4-(4-succinimidocyclohexyl) piperazine), a new 5-HT (1A) postsynaptic receptor antagonist, using several biochemical and behavioural assays. |
37(0,1,1,7) | Details |
| 16258751 | de Bortoli VC, Nogueira RL, Zangrossi H Jr: Effects of fluoxetine and on the panicolytic-like response induced by the activation of 5-HT1A and 5-HT2A receptors in the rat dorsal periaqueductal gray. Psychopharmacology. 2006 Jan;183(4):422-8. Epub 2005 Oct 29. METHODS: Male Wistar rats, subchronically (3-6 days) or chronically (21-24 days) treated with fluoxetine (10 mg/kg i.p.) or chronically treated with (0.3 mg/kg i.p.), were intra-DPAG injected with (20 nmol), the 5-HT1A receptor agonist (+/-)-8--2-(di-n-propylamino) tetralin hydrobromide (8-OH-DPAT; 8 nmol) or the preferential 5-HT2A receptor agonist (+/-)-1-(2,5-dimethoxy-4-iodophenyl) piperazine dihydrochloride (DOI; 16 nmol). |
36(0,1,1,6) | Details |
| 18446327 | de Bortoli VC, Nogueira RL, Zangrossi H Jr: Alprazolam potentiates the antiaversive effect induced by the activation of 5-HT (1A) and 5-HT (2A) receptors in the rat dorsal periaqueductal gray. Psychopharmacology. 2008 Jun;198(3):341-9. Epub 2008 Apr 30. MATERIALS AND METHODS: Male Wistar rats, subchronically (3-6 days) or chronically (14-17 days) treated with alprazolam (2 and 4 mg/kg, i.p.) were intra-DPAG injected with (+/-)-8--2-(di-n-propylamino) tetralin hydrobromide (8-OH-DPAT), (+/-)-1-(2,5-dimethoxy-4-iodophenyl) piperazine dihydrochloride (DOI), and midazolam, respectively, 5-HT (1A), 5-HT (2A/2C), and benzodiazepine receptor agonists. |
35(0,1,1,5) | Details |
| 11277605 | Sanchez H, Velazquez-Martinez DN: Discriminative stimulus properties of indorenate, a 5-HT1A, 5-HT1B and 5-HT2C agonist: a study in rats. J Psychopharmacol. 2001 Mar;15(1):29-36. Generalization to the discriminative stimulus properties of INDO was observed with the 5-HT1A receptor agonist 8-OH-DPAT (1.0 mg/kg produced 90% generalization) and the 5-HT (1B/2C) receptor agonist 1-(3-trifluoromethylphenyl) piperazine (TFMPP) (3.0 mg/kg produced up to 75% generalization). |
34(0,1,1,4) | Details |
| 14769389 | Jakus R, Graf M, Juhasz G, Gerber K, Levay G, Halasz P, Bagdy G: 5-HT2C receptors inhibit and 5-HT1A receptors activate the generation of spike-wave discharges in a genetic rat model of absence epilepsy. Exp Neurol. 2003 Dec;184(2):964-72. We have determined the effects of the 5-HT (2C) receptor preferring agonist m-chlorophenyl-piperazine (m-CPP), the selective 5-HT (2C) receptor antagonist SB-242084, the selective 5-HT (1A) receptor antagonist WAY-100635, two selective re-uptake inhibitors (SSRI, fluoxetine and and their combinations in this model. |
34(0,1,1,4) | Details |
| 14556235 | Oz M, Zhang L, Rotondo A, Sun H, Morales M: Direct activation by of recombinant human 5-HT1A receptors: comparison with human 5-HT2C and 5-HT3 receptors. Synapse. 2003 Dec 15;50(4):303-13. Magnitudes of maximal DA induced currents were 42 +/- 3% of maximal responses and blocked by the 5-HT2 antagonist, piperazine (1 microM). |
7(0,0,0,7) | Details |
| 17704821 | Defraiteur C, Plenevaux A, Scuvee-Moreau J, Rouchet N, Goblet D, Luxen A, Seutin V: Characterization of 4-(2-hydroxyphenyl)-1-[2'-[N-(2''-pyridinyl)-p-fluorobenzamido] ethyl] piper azine (p-DMPPF) as a new potent 5-HT1A antagonist. Br J Pharmacol. 2007 Nov;152(6):952-8. Epub 2007 Aug 20. |
7(0,0,0,7) | Details |
| 14985263 | Merlet I, Ostrowsky K, Costes N, Ryvlin P, Isnard J, Faillenot I, Lavenne F, Dufournel D, Le Bars D, Mauguiere F: 5-HT1A receptor binding and intracerebral activity in temporal lobe epilepsy: an [18F] MPPF-PET study. Brain. 2004 Apr;127(Pt 4):900-13. Epub 2004 Feb 25. |
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| 18406538 | Sterniczuk R, Stepkowski A, Jones M, Antle MC: Enhancement of photic shifts with the 5-HT1A mixed agonist/antagonist NAN-190: intra-suprachiasmatic nucleus pathway. Neuroscience. 2008 May 15;153(3):571-80. Epub 2008 Mar 6. |
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| 11806866 | Bagdy G, Graf M, Anheuer ZE, Modos EA, Kantor S: Anxiety-like effects induced by acute fluoxetine, or m-CPP treatment are reversed by pretreatment with the 5-HT2C receptor antagonist SB-242084 but not the 5-HT1A receptor antagonist WAY-100635. Int J Neuropsychopharmacol. 2001 Dec;4(4):399-408. The possible role of 5-HT1A and 5-HT2C receptors in the anxiety induced by fear, acute treatment with SSRI antidepressants or the receptor agonist m-CPP were tested in the social interaction anxiety test in male Sprague-Dawley rats. |
3(0,0,0,3) | Details |
| 15720784 | Iskra-Jopa J, Golembiowska K, Dziubina A, Cybulski M, Duszynska B, Chilmonczyk Z: In-vivo effects of the 1,2,4-piperazine derivatives MM5 and MC1, putative agonists, on and release in rat prefrontal cortex. J Pharm Pharmacol. 2005 Feb;57(2):205-11. Both compounds, 1-[4-(4-chinolin-2-yl-piperazin-1yl)-butyl] piperidin-2-on (MM5) and 1-[4-(2-methyl-4-chinolin-2-yl-piperazin-1-yl)-butyl]-8-azaspiro [4.5] decano-7,9-dion (MC1), produced hypothermia in mice and showed affinity for 5-HT1A receptors in-vitro. |
3(0,0,0,3) | Details |
| 15661577 | Lee HJ, Ban JY, Cho SO, Seong YH: Stimulation of 5-HT1A receptor with 8-OH-DPAT inhibits peroxide-induced neurotoxicity in cultured rat cortical cells. Pharmacol Res. 2005 Mar;51(3):261-8. The protective effect of 8-OH-DPAT (100 microM) was completely blocked by the simultaneous treatment of 1-(2-methoxyphenyl)-4-[4-(2-phthalimideo) butyl] piperazine (NAN-190, 10muM), a selective 5-HT (1A) receptor antagonist, but not in the presence of the receptor blocker spiperone (10 microM), indicating that the protective effect of 8-OH-DPAT was mediated via 5-HT (1A) receptors. |
3(0,0,0,3) | Details |
| 16049570 | El Mansari M, Blier P: Responsiveness of 5-HT (1A) and 5-HT2 receptors in the rat orbitofrontal cortex after long-term reuptake inhibition. J Psychiatry Neurosci. 2005 Jul;30(4):268-74. RESULTS: After administration of paroxetine for either 3 weeks or 8 weeks, there was no modification in the inhibitory effect of the preferential 5-HT (2A) receptor agonist (+)-1-(4-iodo-2,5-dimethoxyphenyl)-2-aminopropane hydrochloride (DOI) or the preferential 5-HT (2C) receptor agonist 3-chlorophenyl piperazine dihydrochloride (mCPP). |
3(0,0,0,3) | Details |
| 18603331 | Zajdel P, Subra G, Verdie P, Bojarski AJ, Duszynska B, Basista K, Obniska J, Martinez J, Pawlowski M: The influence of an ethylene spacer on the 5-HT (1A) and 5-HT (2A) receptor affinity of arylpiperazine derivatives of amides with N-acylated amino acids and 3-differently substituted pyrrolidine-2,5-diones. Eur J Med Chem. 2009 Feb;44(2):800-8. Epub 2008 Jul 7. |
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| 11673027 | Van Bogaert P, De Tiege X, Vanderwinden JM, Damhaut P, Schiffmann SN, Goldman S: Comparative study of hippocampal neuronal loss and in vivo binding of 5-HT1a receptors in the KA model of limbic epilepsy in the rat. Epilepsy Res. 2001 Nov;47(1-2):127-39. |
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| 11958829 | Popova NK, Ivanova EA: 5-HT (1A) receptor antagonist p-MPPI attenuates acute effects in mice and rats. Neurosci Lett. 2002 Mar 29;322(1):1-4. |
3(0,0,0,3) | Details |
| 11755134 | Cosi C, Koek W: Agonist, antagonist, and inverse agonist properties of antipsychotics at human recombinant 5-HT (1A) receptors expressed in HeLa cells. Eur J Pharmacol. 2001 Dec 14;433(1):55-62. Haloperidol, chlorpromazine, thioridazine, pimozide, and sertindole showed Na (+)-dependent inverse agonist activity at h5-HT (1A) receptor that could be antagonized by (s)-N-tert-butyl-3-(4-(2-methoxyphenyl) piperazine-1-yl)-2-phenylpropanamid e [(s)-WAY 100135]. |
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| 11113483 | Hascoet M, Bourin M, Nic Dhonnchadha BA: The influence of and its metabolite 1-PP, on the activity of paroxetine in the mouse light/dark paradigm and four plates test. Pharmacol Biochem Behav. 2000 Sep;67(1):45-53. The results suggested that a balance between pre- and postsynaptic 5-HT (1A) receptor was implicated in the anxiolytic-like effect of paroxetine. |
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| 11441431 | Mechan AO, O'Shea E, Elliott JM, Colado MI, Green AR: A dose of 3,4-methylenedioxymethamphetamine (MDMA; ecstasy) to rats results in a long-term defect in thermoregulation. Psychopharmacology. 2001 Jun;155(4):413-8. CONCLUSIONS: A dose of MDMA resulted in impaired thermoregulation when rats were exposed to high ambient temperature. 5-HT1A receptor mechanisms were unaltered. |
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| 15619112 | Bert B, Felicio LF, Fink H, Nasello AG: The use of sudden darkness in mice: a behavioural and pharmacological approach. Psychopharmacology. 2005 Jun;179(4):846-53. Epub 2004 Dec 24. In the second part, responses to the 5-HT (1A) receptor agonist 8-OH-DPAT (0.5 and 1.0 mg/kg) and 5-HT (2C) receptor agonist mCPP (1.0 and 2.0 mg/kg) were investigated in male Swiss mice. |
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| 11432685 | Broocks A, Meyer T, Gleiter CH, Hillmer-Vogel U, George A, Bartmann U, Bandelow B: Effect of aerobic exercise on behavioral and neuroendocrine responses to meta-chlorophenylpiperazine and to ipsapirone in untrained healthy subjects. Psychopharmacology. 2001 May;155(3):234-41. In contrast, the increases of observed after administration of the 5-HT1A agonist ipsapirone were of the same magnitude during the pre- and post-training challenge sessions. |
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| 16750888 | Lall GS, Harrington ME: Potentiation of the resetting effects of light on circadian rhythms of hamsters using and neuropeptide Y receptor antagonists. Neuroscience. 2006 Sep 1;141(3):1545-52. Epub 2006 Jun 5. Both BMY 7378 and NAN-190 are thought to block release via acting as agonists at the 1A (5-HT1A) autoreceptors on cells in the raphe, and also block response of target cells by acting as antagonists at post-synaptic 5-HT1A receptors, for example, in the suprachiasmatic nuclei or the intergeniculate leaflet. |
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| 17584957 | Papageorgiou A, Denef C: Stimulation of growth hormone release by in cultured rat anterior pituitary cell aggregates: evidence for mediation by 5-HT2B, 5-HT7, 5-HT1B, and ketanserin-sensitive receptors. Endocrinology. 2007 Sep;148(9):4509-22. Epub 2007 Jun 21. Basal GH release was stimulated by the 5-HTR2 agonists 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane, m-chlorophenyl piperazine, and alpha-methyl 5-carboxytryptamine (agonist at 5-HTR1, -5, and -7); (preferential 5-HTR7 agonist); and the selective 5-HTR1B agonist CP93129 but not the 5-HTR1A agonists 7-(dipropylamino) tetralin-1-ol-8--2-(di-n-propylamino) tetralin and the 5-HTR1B/D agonist |
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| 15542624 | Lane EL, Cheetham S, Jenner P: uptake inhibitor-induced rotation in -lesioned rats involves both D1 and D2 receptors but is modulated through and receptors. J Pharmacol Exp Ther. 2005 Mar;312(3):1124-31. Epub 2004 Nov 12. To determine the involvement of the individual monoamine transporters in the production of motor activity, the effect of the nonselective monoamine uptake inhibitor BTS 74 398 1-([1-(3,4-dichlorophenyl) cyclobutyl]-2-(3-diaminethylaminopropylthio) ethanone monocitrate) and the selective GBR 12909 [1-(2-(bis-(4-fluorphenyl)-methyl) ethyl)-4-(3-phenylpropyl) piperazine) dihydrochloride], (nisoxetine), and (fluvoxamine) reuptake inhibitors on circling in the unilateral -lesioned rat was investigated. |
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| 15452415 | Calama E, Moran A, Ortiz de Urbina AV, Martin ML, San Roman L: m-CPP, a 5-HT2C receptor agonist that modifies the perfusion pressure of the hindquarter vascular bed of anesthetized rat. Pharmacology. 2005 Feb;73(2):70-5. Epub 2004 Sep 27. Both vasodilatation and vasoconstriction were inhibited by the (1,2 ) receptor antagonist methiothepin, whereas the 5-HT (2 ) receptor antagonist ritanserin blocked only the vasoconstrictor responses. 1-[4-(1-Adamantanecarboxamido) butyl]-4-(2-methoxyphenyl) piperazine (a 5-HT (1A) receptor antagonist) and ICI 118,551 (a beta (2)-receptor antagonist) failed to modify the vasodilator responses of m-CPP. |
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| 16173953 | Calama E, Ortiz de Urbina AV, Moran A, Martin ML, San Roman L: Effect of on neurogenic vasoconstriction in the isolated, autoperfused hindquarters of the rat. Clin Exp Pharmacol Physiol. 2005 Oct;32(10):894-900. The effects of were mimicked by 5-carboxamidotryptamine (a 5-HT1 receptor agonist) and L-694 247 (a selective 5-HT1D receptor agonist), but not by 8--2-dipropylaminotetralin (a 5-HT1A receptor agonist), CGS-12066B (a 5-HT1B receptor agonist), alpha-methyl- (a 5-HT2 receptor agonist), 1-(3-chlorophenyl) piperazine (a 5-HT2C receptor agonist) or 1-phenylbiguanide (a 5-HT3 receptor agonist). |
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| 12522075 | Mlinar B, Falsini C, Corradetti R: Pharmacological characterization of 5-HT (1B) receptor-mediated inhibition of local excitatory synaptic transmission in the CA1 region of rat hippocampus. Br J Pharmacol. 2003 Jan;138(1):71-80. The aim of the present work was the pharmacological characterization of the receptor involved in this action. 2 Poly-epscs, evoked by electrical stimulation of the stratum radiatum and recorded in whole-cell voltage-clamp from CA1 pyramidal neurones, were studied in mini-slices of the CA1 region under pharmacological block of (A), (B), and 5-HT (1A) receptors. 3 The 5-HT (1B) receptor selective agonist 1,4-dihydro-3-(1,2,3,6-tetrahydro-4-pyridinyl)-5H-pyrrolo [3,2-b] pyridin-5- one dihydrochloride (CP 93129) inhibited poly-epscs (EC (50)=55 nM), an effect mimicked by the 5-HT (1B) ligands 5-carboxamidotryptamine (5-CT; EC (50)=14 nM) and methylergometrine (EC (50)=78 nM), but not by 1-(3-chlorophenyl) piperazine dihydrochloride (mCPP; 10 micro M) or 7-trifluoromethyl-4 (4-methyl-1-piperazinyl)-pyrrolo [1,2-a] quinoxaline dimaleate (CGS 12066B; 10 micro M). 4 The effects of CP 93129 and 5-CT were blocked by the selective 5-HT (1B) receptor antagonist 3-[3-(dimethylamino) propyl]-4-hydroxy-N-[4-(4-pyridinyl) phenyl] benzamide dihydrochloride (GR 55562; K (B) approximately 100 nM) and by cyanopindolol (K (B)=6 nM); methiothepin (10 micro M) and dihydroergotamine (1 micro M). |
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