| Name | 5 HT 2A |
|---|---|
| Synonyms | 5 HT 2; 5 HT 2A; 5 HT2; 5 HT2A; 5 hydroxytryptamine (serotonin) receptor 2A; 5 hydroxytryptamine 2A receptor; 5 hydroxytryptamine receptor 2A; HTR 2… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 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 |
| 15619109 | Terry AV Jr, Buccafusco JJ, Bartoszyk GD: Selective 5-HT2A receptor antagonist EMD 281014 improves delayed matching performance in young and aged rhesus monkeys. Psychopharmacology. 2005 Jun;179(4):725-32. Epub 2004 Dec 24. OBJECTIVES: The purpose of this study was to evaluate the selective 5-HT (2A) antagonist, 7-{4-[2-(4--phenyl)-ethyl]-piperazine-1-carbonyl}-1H--3-carbon itrile HCl (EMD 281014) in young and aged monkeys in a test designed to assess working memory function. |
32(0,1,1,2) | Details |
| 12062579 | Castro L, Maldonado I, Campos I, Varjao B, Angelo AL, Athanazio RA, Barbetta MC, Ramos AC, Fregoneze JB, De Castro e Silva E: Central administration of mCPP, a 5-HT (2B/2C) agonist, decreases water intake in rats. Pharmacol Biochem Behav. 2002 Jul;72(4):891-8. In the present study, we investigated in rats the effect of third ventricle injections of 1-(3-chlorophenyl) piperazine (mCPP), a 5-HT (2) receptor agonist, on water intake induced by three different physiological stimuli: fluid deprivation, acute salt load and hypovolemia. |
31(0,1,1,1) | Details |
| 19420729 | Yonezawa A, Yoshizumi M, Ise SN, Watanabe C, Mizoguchi H, Furukawa K, Tsuru H, Kimura Y, Kawatani M, Sakurada S: Synergistic actions of apomorphine and m-chlorophenylpiperazine on ejaculation, but not penile erection in rats. Biomed Res. 2009 Apr;30(2):71-8. The purpose of this study was to investigate whether the combination of a receptor agonist apomorphine and a 5-HT (2) receptor agonist m-CPP would potentiate penile erection and ejaculation in male rats. |
1(0,0,0,1) | Details |
| 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 tested antagonists of 5-HT2, 5-HT3, 5-HT4, and 5-HT6 serotoninergic subtypes were poorly active or inactive in the model. |
1(0,0,0,1) | Details |
| 17850172 | Warrington L, Lombardo I, Loebel A, Ice K: Ziprasidone for the treatment of acute manic or mixed episodes associated with bipolar disorder. CNS Drugs. 2007;21(10):835-49. Ziprasidone, a benzisothiazolyl piperazine-type atypical antipsychotic agent, has a unique receptor-binding profile. A potent antagonist of 5-HT (2A) and D (2) receptors, ziprasidone has an affinity for 5-HT (2A) receptors > 10-fold higher than its affinity for D (2) receptors. |
1(0,0,0,1) | Details |
| 12603368 | Johnson KW, Nelson DL, Dieckman DK, Wainscott DB, Lucaites VL, Audia JE, Owton WM, Phebus LA: Neurogenic dural protein extravasation induced by meta-chlorophenylpiperazine (mCPP) involves and 5-HT2B receptor activation. Cephalalgia. 2003 Mar;23(2):117-23. This effect was inhibited by non-selective 5-HT2 receptor antagonists (methysergide, LY53857, LY215840), by a peripherally restricted 5-HT2 receptor antagonist (xylamidine) and by a 5-HT2B selective receptor antagonist (LY202146). |
1(0,0,0,1) | Details |
| 19269287 | Rajkumar R, Pandey DK, Mahesh R, Radha R: 1-(m-Chlorophenyl) piperazine induces depressogenic-like behaviour in rodents by stimulating the neuronal 5-HT (2A) receptors: proposal of a modified rodent antidepressant assay. Eur J Pharmacol. 2009 Apr 17;608(1-3):32-41. Epub 2009 Mar 6. |
32(0,1,1,2) | Details |
| 11978164 | Caley CF, Cooper CK: Ziprasidone: the fifth atypical antipsychotic. Ann Pharmacother. 2002 May;36(5):839-51. 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. |
31(0,1,1,1) | Details |
| 11106874 | Maes M, van West D, De Vos N, Westenberg H, Van Hunsel F, Hendriks D, Cosyns P, Scharpe S: Lower baseline plasma and prolactin together with increased body temperature and higher mCPP-induced responses in men with pedophilia. Neuropsychopharmacology. 2001 Jan;24(1):37-46. It is hypothesized that the results are compatible with a decreased activity of the serotonergic presynaptic neuron and a 5-HT2 postsynaptic receptor hyperresponsivity. |
1(0,0,0,1) | 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. In this study we showed that MP349 bound with moderate affinity (K (i) = 234 nM) for alpha (1)-adrenoceptors, and with very low affinity (K (i) > 2600 nM) for 5-HT (2A), D (1), D (2) and benzodiazepine receptors. |
1(0,0,0,1) | 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. This effect of 8-OH-DPAT was minimally attenuated by the selective 5-HT1A receptor antagonist WAY 100635 but was reversibly and significantly reduced in the presence of ritanserin, a mixed 5-HT (2/7) receptor antagonist. 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. |
1(0,0,0,1) | Details |
| 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. The inhibitory effect of 8-OH-DPAT was effectively blocked by clozapine, a high affinity 5-HT (7) receptor antagonists with a very low affinity for 5-HT (2). |
1(0,0,0,1) | 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. MC1 seems to possess moderate agonist activity at 5-HT1A and 5-HT2A receptors, while acting on release in the rat prefrontal cortex. |
1(0,0,0,1) | Details |
| 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. Our data reveal that m-CPP induces the (1 ) and/or non-specific vasodilator effect and 5-HT (2) vasoconstrictor effects in the hindquarter vascular bed of the rat. |
1(0,0,0,1) | Details |
| 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 |
| 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). |
1(0,0,0,1) | Details |
| 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. |
1(0,0,0,1) | 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 |
| 11906967 | Centurion D, Ortiz MI, Saxena PR, Villalon CM: The atypical 5-HT2 receptor mediating tachycardia in pithed rats: pharmacological correlation with the 5-HT2A receptor subtype. Br J Pharmacol. 2002 Mar;135(6):1531-9. In pithed rats, intraperitoneally (i.p.) pre-treated with reserpine (5 mg kg (-1)), intravenous (i.v.) administration of 5-HT, 5- (5-MeO-T), 1-(3-chlorophenyl) piperazine (mCPP) and 5-carboxamidotryptamine (5-CT) (10, 30, 100 and 300 microg kg (-1) each), produced dose-dependent tachycardic responses. |
6(0,0,0,6) | Details |
| 12644293 | Nic Dhonnchadha BA, Bourin M, Hascoet M: Anxiolytic-like effects of 5-HT2 ligands on three mouse models of anxiety. Behav Brain Res. 2003 Mar 18;140(1-2):203-14. |
6(0,0,0,6) | Details |
| 11767117 | Sugimoto Y, Yoshikawa T, Noma T, Yamada J: The 5-HT2C/2B receptor agonist m-chlorophenylpiperazine (mCPP) inhibits 2-deoxy- (2-DG)-induced hyperphagia in rats. Biol Pharm Bull. 2001 Dec;24(12):1431-3. Suppressive effects of mCPP on hyperphagia induced by 2-DG were inhibited by the 5-HT2A/2B/2C receptor antagonist, ritanserin, although the 5-HT2, receptor antagonist ketanserin was without effect. |
1(0,0,0,1) | 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. Altogether the findings presented here confirm that evokes excitatory effects on the autonomous contractile auricle of S. officinalis and acts obviously over different receptors, whereby a (1)- and a 5-HT (2)-like seem to be involved. |
1(0,0,0,1) | 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). |
31(0,1,1,1) | Details |
| 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. |
6(0,0,0,6) | 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 |
| 17240844 | Yamauchi M, Hiraoka S, Imanishi T: [Role of the serotonergic nervous system in anxiety disorders and the anxiolytic mechanism of selective reuptake inhibitors]. Nihon Shinkei Seishin Yakurigaku Zasshi. 2006 Nov;26(5-6):193-8. In addition, some studies have suggested that 5-HT2A receptors and 5-HTIA receptors participate in anxiety disorders and the therapeutic mechanism. |
1(0,0,0,1) | 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. |
6(0,0,0,6) | Details |
| 12408724 | Liegeois JF, Eyrolles L, Ellenbroek BA, Lejeune C, Carato P, Bruhwyler J, Geczy J, Damas J, Delarge J: New pyridobenzodiazepine derivatives: modifications of the basic side chain differentially modulate binding to (D (4.2), D (2L)) and serotonin (5-HT (2A)) receptors. J Med Chem. 2002 Nov 7;45(23):5136-49. In the piperazine series, replacing the N-methyl group by a N-phenyl moiety (15-17, 30-32) provided a dramatic decrease of affinity for all receptors (K (i) > 1000 nM). |
5(0,0,0,5) | 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. |
1(0,0,0,1) | Details |
| 14767940 | Kumar K, Michalik D, Garcia Castro I, Tillack A, Zapf A, Arlt M, Heinrich T, Bottcher H, Beller M: Biologically active compounds through catalysis: efficient synthesis of N-(heteroarylcarbonyl)-N'-(arylalkyl) piperazines. Chemistry. 2004 Feb 6;10(3):746-57. A practical route for the synthesis of new biologically active 5-HT (2 A) receptor antagonists has been developed. Here, base-catalyzed hydroamination reactions of styrenes with benzylated piperazine proceeded in high yield even at room temperature. |
1(0,0,0,1) | Details |
| 19800913 | Pandey DK, Mahesh R, Kumar AA, Rao VS, Arjun M, Rajkumar R: A novel 5-HT (2A) receptor antagonist exhibits antidepressant-like effects in a battery of rodent behavioural assays: approaching early-onset antidepressants. Pharmacol Biochem Behav. 2010 Jan;94(3):363-73. Epub 2009 Oct 2. BIP-1 reversed the depressogenic-like effects of meta-chlorophenyl piperazine and augmented the antidepressant-like effects of amitryptiline and harmane. |
5(0,0,0,5) | Details |
| 12585687 | Meneses A: Involvement of 5-HT (2A/2B/2C) receptors on memory formation: simple agonism, antagonism, or inverse agonism?. Cell Mol Neurobiol. 2002 Dec;22(5-6):675-88. However, both drugs significantly and differentially antagonized the memory impairments induced by 1-(3-chlorophenyl) piperazine (mCPP), 1-naphtyl-piperazine (1-NP), mesulergine, or N-(3-trifluoromethylphenyl) piperazine (TFMPP). 3. |
5(0,0,0,5) | Details |
| 11448452 | Porter RH, Malcolm CS, Allen NH, Lamb H, Revell DF, Sheardown MJ: Agonist-induced functional desensitization of recombinant human 5-HT2 receptors expressed in CHO-K1 cells. Biochem Pharmacol. 2001 Aug 15;62(4):431-8. |
4(0,0,0,4) | 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. |
1(0,0,0,1) | Details |
| 12716945 | Zhang ZW: induces tonic firing in layer V pyramidal neurons of rat prefrontal cortex during postnatal development. J Neurosci. 2003 Apr 15;23(8):3373-84. The excitatory effects of at younger ages were attributed to 5-HT2A receptors because the effects were mimicked by the 5-HT2 agonist alpha-methyl- but not by the 5-HT3 agonist 1-(m-chlorophenyl)-biguanide, nor by the 5-HT2B/2C agonist 1-(3-chlorophenyl) piperazine, and were blocked by the 5-HT2A antagonists ketanserin and alpha-phenyl-1-(2-phenylethyl)-4-piperidinemethanol. The developmental decline of -induced excitatory effects was associated with a downregulation of 5-HT2A receptor function and a decrease in the input resistance during early life. |
1(0,0,0,1) | Details |
| 11754579 | Brea J, Rodrigo J, Carrieri A, Sanz F, Cadavid MI, Enguix MJ, Villazon M, Mengod G, Caro Y, Masaguer CF, Ravina E, Centeno NB, Carotti A, Loza MI: New 5-HT (2A), 5-HT (2B), and 5-HT (2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl) benzo and heterocycloalkanones. J Med Chem. 2002 Jan 3;45(1):54-71. Although piperidine fragments also confer higher affinity at 5-HT (2C) receptors, only piperazine-containing ligands were selective over 5-HT (2A). |
88(1,1,1,8) | 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). |
86(1,1,1,6) | Details |
| 11259531 | McKune CM, Watts SW: Characterization of the serotonin receptor mediating contraction in the mouse thoracic aorta and signal pathway coupling. J Pharmacol Exp Ther. 2001 Apr;297(1):88-95. Our hypothesis was further supported by the finding that antagonists with affinity for the 5-HT2A receptor, ketanserin, 1-(1-naphthyl) piperazine, spiperone, and LY53857, reduced -induced contraction. |
86(1,1,1,6) | Details |
| 15107597 | Kovacs A, Gacsalyi I, Wellmann J, Schmidt E, Szucs Z, Dubreuil V, Nicolas JP, Boutin J, Bozsing D, Egyed A, Tihanyi K, Spedding M, Szenasi G: Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. Cardiovasc Drugs Ther. 2003 Sep-Nov;17(5-6):427-34. Our aim was to specify the 5-HT (2) subtype selectivity of EGIS-7625 (1-benzyl-4-[(2-nitro-4-methyl-5-amino)-phenyl]-piperazine), a new 5-HT (2B) ligand, in receptor binding studies and characterize its pharmacology at 5-HT (2A), 5-HT (2B) and 5-HT (2C) receptors in in vivo experiments and in isolated organs, in vitro. |
84(1,1,1,4) | Details |
| 18816514 | Cai MY, Li Z, Huang Q, Song G: {[1-(Arylmethyl) piperidin-4-yl] oxy}-(trifluoromethyl)-pyridines: ketanserin analogues with insect growth regulating activity. Chem Biodivers. 2008 Sep;5(9):1844-55. It was also found that the substituted position of the CF (3) group at the ring played a key role, and that the introduction of 1-[bis (4-fluorophenyl) methyl] piperazine, an equivalent of the benzoylpiperidine moiety of ketanserin, resulted in bioactivities similar to those of the title compounds, which were in agreement with the model of ketanserin analogues binding to mammalian 5-HT (2) receptors. |
83(1,1,1,3) | Details |
| 12107618 | Abi-Saab W, Seibyl JP, D'Souza DC, Karper LP, Gueorgueva R, Abi-Dargham A, Wong ML, Rajhans S, Erdos JP, Heninger GR, Charney DS, Krystal JH: Ritanserin antagonism of m-chlorophenylpiperazine effects in neuroleptic-free schizophrenics patients: support for -2 receptor modulation of schizophrenia symptoms. Psychopharmacology. 2002 Jun;162(1):55-62. Epub 2002 Apr 5. RATIONALE: -2 (5-HT (2)) receptor antagonism has been hypothesized to have antipsychotic activity. |
4(0,0,0,4) | Details |
| 15963493 | Matsumoto K, Morishige R, Murakami Y, Tohda M, Takayama H, Sakakibara I, Watanabe H: Suppressive effects of isorhynchophylline on 5-HT2A receptor function in the brain: behavioural and electrophysiological studies. Eur J Pharmacol. 2005 Jul 11;517(3):191-9. |
4(0,0,0,4) | Details |
| 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. |
4(0,0,0,4) | Details |
| 11472789 | Maes M, De Vos N, Van Hunsel F, Van West D, Westenberg H, Cosyns P, Neels H: Pedophilia is accompanied by increased plasma concentrations of catecholamines, in particular Psychiatry Res. 2001 Aug 5;103(1):43-9. Plasma and concentrations were measured in pedophiles and normal men both in placebo conditions and after administration of meta-chlorophenylpiperazine (mCPP), a post-synaptic 5-HT2 receptor agonist. |
1(0,0,0,1) | Details |
| 15380867 | Landry ES, Guertin PA: Differential effects of 5-HT1 and 5-HT2 receptor agonists on hindlimb movements in paraplegic mice. Prog Neuropsychopharmacol Biol Psychiatry. 2004 Sep;28(6):1053-60. |
4(0,0,0,4) | Details |
| 17935799 | Nunes-de-Souza V, Nunes-de-Souza RL, Rodgers RJ, Canto-de-Souza A: 5-HT2 receptor activation in the midbrain periaqueductal grey (PAG) reduces anxiety-like behaviour in mice. Behav Brain Res. 2008 Feb 11;187(1):72-9. Epub 2007 Aug 30. |
3(0,0,0,3) | 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. |
3(0,0,0,3) | Details |
| 18533183 | de Leeuw AS, Westenberg HG: Hypersensitivity of 5-HT2 receptors in OCD patients. J Psychiatr Res. 2008 Sep;42(11):894-901. Epub 2008 Jun 3. |
3(0,0,0,3) | Details |
| 15118345 | Calama E, Moran A, Ortiz de Urbina AV, Martin ML, San Roman L: Vasoconstrictor responses to in the autoperfused hindquarters of spontaneously hypertensive rats. Pharmacology. 2004 Jun;71(2):66-72. Our data suggest that the vasoconstrictor response induced by in the autoperfused hindquarters of SHR is mainly mediated by the activation of 5-HT2A and 5-HT2C receptors. |
1(0,0,0,1) | 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. |
83(1,1,1,3) | Details |
| 12892843 | Bartoszyk GD, van Amsterdam C, Bottcher H, Seyfried CA: EMD 281014, a new selective 5-HT2A receptor antagonist. . Eur J Pharmacol. 2003 Jul 25;473(2-3):229-30. The 5-HT2A receptor ligand 7-[4-[2-(4--phenyl)-ethyl]-piperazine-1-carbonyl]-1H-indole-3-carbon itrile HCl (EMD 281014) selectively binds to human (h) and rat 5-HT2A receptors (IC50 values 0.35 and 1 nM, respectively; vs. 1334 nM for h5-HT2C) and inhibited -stimulated [35S] 5'-O-3-thiotriphosphate (GTPgammaS)-accumulation in h5-HT2A transfected Chinese hamster ovary cells (IC50 9.3 nM). |
82(1,1,1,2) | Details |
| 11597601 | Cooper RL, Chase RJ, Tabor J: Altered responsiveness to at the crayfish neuromuscular junction due to chronic p-CPA and m-CPP treatment. Brain Res. 2001 Oct 19;916(1-2):143-51. Injections of the 5-HT1 and 5-HT2 vertebrate receptor agonist, 1-(3-Chlorophenyl) piperazine dihydrochloride (m-CPP), for 1 week resulted in a decreased responsiveness to application of |
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| 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. |
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| 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. |
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| 17059817 | Monti JM, Jantos H: Effects of the 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat. Eur J Pharmacol. 2006 Dec 28;553(1-3):163-70. Epub 2006 Sep 23. The effects of the 5-HT (2A/2C) receptor agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and of the selective 5-HT (2A) or 5-HT (2C) receptor antagonists 7-{4-[2-(4--phenyl)-ethyl]-piperazine-1-carbonyl}-1H--3-carbon itrile HCl (EMD 281014) and 5-methyl-1-[[-2-[(2-methyl-3-pyridyl) oxy]-5-pyridyl] carbamoyl]-6-trifluoro methylindoline HCl (SB-243213), respectively, on spontaneous sleep were studied in adult rats implanted for chronic sleep recordings. |
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| 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. Thus, besides an electron-withdrawing field effect and ortho substitution, which both influence binding to receptor subtypes, though to a different extent as revealed by regression coefficients in the multiparametric regression equations, the affinity of congeners 1a-r to 5-HT (1A) receptors proved to be linearly correlated with volume/polarizability descriptors, whereas their affinity to 5-HT (2A) receptors correlated with lipophilicity constants through a parabolic relationship. 1-[(1,2-Diphenyl-1H-4-imidazolyl) methyl]-4-(2-methoxyphenyl) piperazine (1b), with a D (2)/5-HT (1A) IC (50) ratio of approximately 1, was selected for a further pharmacological study. |
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| 11101359 | Ravina E, Casariego I, Masaguer CF, Fontenla JA, Montenegro GY, Rivas ME, Loza MI, Enguix MJ, Villazon M, Cadavid MI, Demontis GC: Conformationally constrained butyrophenones with affinity for (D (1), D (2), D (4)) and (5-HT (2A), 5-HT (2B), 5-HT (2C)) receptors: synthesis of aminomethylbenzo [b] furanones and their evaluation as antipsychotics. J Med Chem. 2000 Nov 30;43(24):4678-93. A series of novel conformationally restricted butyrophenones (6-aminomethyl-4,5,6,7-tetrahydrobenzo [b] furan-4-ones bearing 4-(6-fluorobenzisoxazolyl) piperidine, 4-(p-fluorobenzoyl) piperidine, 4-(o-methoxyphenyl) piperazine, 4-(2-pyridyl) piperazine, 4-(2-pyrimidinyl) piperazine, or linear butyro (or valero) phenone fragments) were prepared and evaluated as antipsychotic agents by in vitro assays for affinity for receptors (D (1), D (2), D (4)) and serotonin receptors (5-HT (2A), 5-HT (2B), 5-HT (2C)), by neurochemical studies, and by in vivo assays for antipsychotic potential and the risk of inducing extrapyramidal side effects. |
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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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| 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 effects of 5-HT)(1/2) receptor agonists for (1) and 5-HT (2) receptors on dark-phase ingestive behavior were evaluated in 12-h food-deprived, female Wistar rats. |
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| 16553644 | Kitazawa T, Ukai H, Komori S, Taneike T: Pharmacological characterization of -induced contraction in the chicken gastrointestinal tract. Auton Autacoid Pharmacol. 2006 Apr;26(2):157-68. The proventriculus (area of stomach adjacent to the oesophagus) and ileum are examined. applied cumulatively caused sustained contraction of the proventriculus that was not decreased by tetrodotoxin, atropine or l-nitro- methylester (l-NAME). alpha-Methyl- showed the same potency as that of indicating the involvement of the 5-HT (2) receptor. (+/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-amino-propane (DOI), and 1-(3-chlorophenyl) piperazine hydrochloride (mCPP) were potent, and 2-methyl-5-HT, 5-carboxamidotryptamine, BW723C86 and 6-chloro-2-(1-piperazinyl) pyrazine hydrochloride (MK212) were moderate, but (+/-)-8--2-dipropylaminotetralin hydrobromide (8-OH-DPAT), [endo-N-8-methyl-8-azabicyclo-(3,2,1) oct-3-yl]-2,3-dihydro-(1-methyl) ethyl -2-oxo-1H-benzimidazol-1-carboxamide (BIMU-8) and cisapride were weak agonists. Correlation of pEC (50) values of these agonists with documented pEC (50) values for 5-HT (2C) receptor was higher than 5-HT (2A) and 5-HT (2B). |
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| 18642697 | Kirillova VV, Dzhordzhikiya RK, Nigmatullina RR: Adrenergic and serotoninergic regulation of myocardial contractility in patients with various morphofunctional changes in the heart resulting from chronic heart failure. Bull Exp Biol Med. 2007 Oct;144(4):501-3. During left ventricular hypertrophy, the strength of myocardial contraction in response to exceeded that induced by and was realized via 5-HT2 receptors. |
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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. |
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| 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. |
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| 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. Clinical properties of atypical antipsychotics are based on their interaction with D (2) receptor and 5-HT (1A) and 5-HT (2A) receptors. 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. |
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| 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). |
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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. |
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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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| 19875674 | Rasbach KA, Funk JA, Jayavelu T, Green PT, Schnellmann RG: 5-hydroxytryptamine receptor stimulation of mitochondrial biogenesis. J Pharmacol Exp Ther. 2010 Feb;332(2):632-9. Epub 2009 Oct 29. Reverse transcription-polymerase chain reaction analysis confirmed the presence of 5-HT2A, 5-HT2B, and 5-HT2C receptor mRNA in RPTC. |
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| 19699736 | Moran A, de Urbina AV, Martin ML, Rodriguez-Barbero A, Roman LS: Characterization of the contractile 5-hydroxytryptamine receptor in the autoperfused kidney of L-NAME hypertensive rats. Eur J Pharmacol. 2009 Oct 12;620(1-3):90-6. Epub 2009 Aug 21. The selective 5-HT (2) receptor agonist alpha-methyl- (alpha-methyl- caused a local vasoconstrictor effect in the autoperfused rat kidney. The selective 5-HT (2B) receptor agonist BW723C86, the non-selective 5-HT (2C) receptor agonist (1-(3-chlorophenyl) piperazine), m-CPP, the (1) receptor agonist 5-carboxamidotryptamine (5-CT) and the selective 5-HT (3) receptor agonist (1-(m-chlorophenyl)-biguanide), m-CPBG, did not modify renal perfusion pressure. |
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| 11509227 | Vickers SP, Easton N, Malcolm CS, Allen NH, Porter RH, Bickerdike MJ, Kennett GA: Modulation of 5-HT (2A) receptor-mediated head-twitch behaviour in the rat by 5-HT (2C) receptor agonists. Pharmacol Biochem Behav. 2001 Jul-Aug;69(3-4):643-52. The preferential 5-HT (2C) receptor agonists Ro 60-0175, 6-chloro-2-[1-piperazinyl]-pyrazine HCl (MK-212), 1-(3-chlorophenyl) piperazine hydrochloride (mCPP), 1-(3-trifluoromethylphenyl) piperazine hydrochloride (TFMPP), and (S)-3-[(2,3-dihydro-5-methoxy-1H-inden-4-yl) oxy]-pyrollidine HCl (ORG-37684), the 5-HT (2A/2C) receptor agonist 2,5-dimethoxy-4-iodoamphetamine (DOI), the 5-HT (2B) receptor agonist 1-[5-thienylmethoxy-1-1H-3-indoyl] propan-2-amine hydrochloride (BW-723C86), and nor-D-fenfluramine were administered to rats subsequent to an acute challenge of SB-242084. |
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| 11070185 | Shaw AM, Bunton DC, Brown T, Irvine J, MacDonald A: Regulation of sensitivity to in pulmonary supernumerary but not conventional arteries by a 5-HT (1D)-like receptor. Eur J Pharmacol. 2000 Nov 10;408(1):69-82. The 5-HT (2) receptor agonist, 2,5 dimethoxy-4-iodoamphetamine hydrobromide (DOI) constricts both arteries. Neither the selective 5-HT (1D) receptor antagonist (1-(3-chlorophenyl)-4-[3, 3-diphenyl (2-(S,R) hydroxypropanyl) piperazine] hydrochloride (BRL15572) nor the 5-HT (1B) receptor antagonist (2,3,6, 7-tetrahydro-1'-methyl-5-[2'methyl-4'5-(methyl-1,2,4-oxadiazol-3-y l) biphenyl-4-carbonyl] furo [2,3-f] -3-spiro-4'-piperidine hydrochloride (SB224289) antagonised concentration-response curves induced by or (1)-receptor-selective agonists. |
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| 15999344 | Bruce KR, Steiger H, Joober R, Ng Ying Kin NM, Israel M, Young SN: Association of the promoter polymorphism -1438G/A of the 5-HT2A receptor gene with behavioral impulsiveness and function in women with bulimia nervosa. Am J Med Genet B Neuropsychiatr Genet. 2005 Aug 5;137B(1):40-4. |
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| 17138863 | Hackler EA, Turner GH, Gresch PJ, Sengupta S, Deutch AY, Avison MJ, Gore JC, Sanders-Bush E: 5-Hydroxytryptamine2C receptor contribution to m-chlorophenylpiperazine and N-methyl-beta-carboline-3-carboxamide-induced anxiety-like behavior and limbic brain activation. J Pharmacol Exp Ther. 2007 Mar;320(3):1023-9. Epub 2006 Nov 30. Activation of 5-hydroxytryptamine2C (5-HT (2C)) receptors by the 5-HT (2) receptor agonist m-chlorophenylpiperazine (m-CPP) elicits anxiety in humans and anxiety-like behavior in animals. |
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| 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. They were tested in radioligand binding experiments to evaluate their affinity for 5-HT 1A and 5-HT 2A serotonergic, alpha 1 adrenergic, D1, and D2 dopaminergic receptors. |
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| 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. 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. FR260010 showed high affinity for human 5-HT (2C) receptor (K (i): 1.10 nM) and high selectivity over (2A) (5-HT (2A)) receptor (K (i): 386 nM) and many other transmitter receptors. |
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| 14656323 | Paolucci E, Berretta N, Tozzi A, Bernardi G, Mercuri NB: Depression of mGluR-mediated IPSCs by in neurons of the rat substantia nigra pars compacta. Eur J Neurosci. 2003 Nov;18(10):2743-50. Similar results were obtained with alpha-methyl- and but not with 5-carboxamidotryptamine or 1-(3-chlorophenyl) piperazine. Our results demonstrate a powerful inhibition of the mGluR-IPSC by in midbrain neurons, most probably through stimulation of 5-HT2A and 5-HT4 receptors. |
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| 16935825 | Perveen T, Rafiq R, Haider S, Haleem DJ: Increased serotonergic functions following adminstration of 1-(1-naphthyl) piperazine in injected rats. Pak J Pharm Sci. 2006 Jul;19(3):194. a beta adrenergic antagonist, binds with 5-HT1 receptor. 1-(1-naphthyl) piperazine (1-NP) a derivative of quipazine has antagonist activity at 5-HT2 and agonist activity at 5-HT1 site. |
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| 11919705 | Wright TJ, Huddart H: The nature of the and 5-hydroxytryptamine receptors in buccal smooth muscle of the pest slug Deroceras reticulatum. J Comp Physiol B. 2002 Apr;172(3):237-49. Epub 2002 Jan 24. Serotonergic agonist and antagonist experiments using 1-(3-chlorophenyl) piperazine, 1-(m-chlorophenyl) biguanide, methiothepin, methysergide and metoclopramide strongly suggested that the receptor showed closest pharmacological affinity with the (1) receptor class of mammals but with some 5-HT (2) activity. |
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| 17350760 | Bercovici E, Cortez MA, Snead OC 3rd: 5-HT2 modulation of AY-9944 induced atypical absence seizures. . Neurosci Lett. 2007 May 11;418(1):13-7. Epub 2007 Mar 2. |
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| 11518476 | Franklin M, Cowen PJ: Effect of a low diet on the prolactin responses to the 5-HT2A agonist DOI in the rat. Pharmacopsychiatry. 2001 Jul;34(4):147-9. |
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| 16140281 | D'Souza DC, Gil RB, Zuzarte E, MacDougall LM, Donahue L, Ebersole JS, Boutros NN, Cooper T, Seibyl J, Krystal JH: - interactions in healthy men: implications for network models of psychosis and dissociation. Biol Psychiatry. 2006 Jan 15;59(2):128-37. Epub 2005 Sep 2. BACKGROUND: This study tested the hypothesis that deficits in type A (A)) receptor function might create a vulnerability to the psychotogenic and perceptual altering effects of serotonergic (5-HT (2A/2C)) receptor stimulation. |
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| 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. This study investigated the involvement of (1) and 5-HT (2) receptors in the antidepressant-like effect of in the mouse forced swimming test (FST). 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. |
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| 17207863 | Cornelio AM, Nunes-de-Souza RL: Anxiogenic-like effects of mCPP microinfusions into the amygdala (but not dorsal or ventral hippocampus) in mice exposed to elevated plus-maze. Behav Brain Res. 2007 Mar 12;178(1):82-9. Epub 2007 Jan 17. Although systemic studies with 5-HT (2) receptor agonists and antagonists suggest a facilitatory role for this receptor subtype in anxiety, somewhat inconsistent results have been obtained when such compounds have been directly applied to limbic targets such as the hippocampus and amygdala. |
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| 16841562 | Graf M: 5-HT2c receptor activation induces grooming behaviour in rats: possible correlations with obsessive-compulsive disorder. Neuropsychopharmacol Hung. 2006 Mar;8(1):23-8. Certain 5-HT2 receptor agonists were reported to exacerbate symptoms in OCD patients. |
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| 12152119 | Hayes ES, Adaikan PG: Metachlorophenylpiperazine (m-CPP) induced intracavernous pressure responses in anaesthetized rats. Int J Impot Res. 2002 Aug;14(4):287-94. Here we have recorded the effects of metachlorophenylpiperazine (m-CPP) on intracavernous pressure (ICP) in anesthetized rats pretreated with various pharmacological agents in an attempt to determine the mechanism and relevance of the m-CPP induced ICP response to other models of erection. m-CPP elicited consistent and significantly greater increases in ICP (71.5+/-6.6 mmHg) compared with the mixed 5-HT (2a/2c) agonists trifluoromethylphenylpiperazine (3.4+/-1.3 mmHg) and quipazine (10.9+/-1.8 mmHg). |
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| 15916857 | Abrams JK, Johnson PL, Hay-Schmidt A, Mikkelsen JD, Shekhar A, Lowry CA: Serotonergic systems associated with arousal and vigilance behaviors following administration of anxiogenic drugs. Neuroscience. 2005;133(4):983-97. Anxiogenic drugs with diverse pharmacological properties including the receptor antagonist the 5-HT2A/2C receptor agonist m-chlorophenyl piperazine (mCPP), the alpha2-adrenoreceptor antagonist yohimbine, and the benzodiazepine receptor partial inverse agonist N-methyl-beta-carboline-3-carboxamide (FG-7142) induced increases in behavioral arousal and vigilance behaviors consistent with an increase in anxiety state. |
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| 17888556 | Korff S, Stein DJ, Harvey BH: Stereotypic behaviour in the deer mouse: pharmacological validation and relevance for obsessive compulsive disorder. Prog Neuropsychopharmacol Biol Psychiatry. 2008 Feb 15;32(2):348-55. Epub 2007 Aug 29. We also studied behavioural responses to the 5-HT (2A/C) agonist, meta-chlorophenylpiperazine (mCPP) and the D2 agonist, quinpirole (2 mg/kg and 5 mg/kg respectively x 4 days). |
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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. Two sets of new o-methoxyphenylpiperazine (MPP; series a) and 1,2,3,4-tetrahydroisoquinoline (THIQ; series b) derivatives, containing various imide moieties derived from NAN190, were synthesized and evaluated in vitro for their ability to bind to the 5-HT (1A) and 5-HT (2A) receptors. |
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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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| 11104830 | Ochi T, Goto T: The antinociceptive effect induced by FR140423 is mediated through spinal 5-HT2A and 5-HT3 receptors. Eur J Pharmacol. 2000 Dec 8;409(2):167-72. |
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| 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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| 14755634 | Patel JG, Bartoszyk GD, Edwards E, Ashby CR Jr: The highly selective (5-HT) 2A receptor antagonist, EMD 281014, significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test. Synapse. 2004 Apr;52(1):73-5. We examined the effect of the highly selective (5-HT)(2A) receptor antagonist 7-[4-[2-(4--phenyl)-ethyl]-piperazine-1-carbonyl]-1H-indole-3-carbon itrile HCl (EMD 281014) in congenital learned helpless male rats in the forced swim test. |
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| 18439428 | Takeda H, Sadakane C, Hattori T, Katsurada T, Ohkawara T, Nagai K, Asaka M: Rikkunshito, an herbal medicine, suppresses cisplatin-induced anorexia in rats via 5-HT2 receptor antagonism. Gastroenterology. 2008 Jun;134(7):2004-13. Epub 2008 Feb 29. |
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| 17451674 | Obata H, Ito N, Sasaki M, Saito S, Goto F: Possible involvement of spinal noradrenergic mechanisms in the antiallodynic effect of intrathecally administered 5-HT2C receptor agonists in the rats with peripheral nerve injury. Eur J Pharmacol. 2007 Jul 12;567(1-2):89-94. Epub 2007 Mar 30. Taken together, these findings suggest that 5-HT (2A) and 5-HT (2C) receptors in the dorsal horn of the spinal cord might be involved in alleviating neuropathic pain by different mechanisms. Allodynia was produced by tight ligation of the fifth (L5) and sixth (L6) lumbar spinal nerves on the left side, and was measured by applying von Frey filaments to the left hindpaw. 6-chloro-2-(1-piperazinyl)-pyrazine (MK212; 100 microg) and 1-(m-chlorophenyl)-piperazine (mCPP; 300 microg) were used as 5-HT (2C) receptor agonists. |
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| 18644367 | Moran A, Ortiz de Urbina AV, Martin ML, Garcia M, Rodriguez-Barbero A, Dorado F, San Roman L: Characterization of contractile 5-hydroxytryptamine receptor subtypes in the in situ autoperfused kidney in the anaesthetized rat. Eur J Pharmacol. 2008 Sep 11;592(1-3):133-7. Epub 2008 Jul 4. The selective 5-HT2 receptor agonist alpha-methyl- (alpha-methyl- and the non-selective 5-HT2C receptor agonist (1-(3-chlorophenyl) piperazine), m-CPP, caused a local vasoconstrictor effect in the autoperfused rat kidney, whereas BW723C86, a selective 5-HT2B receptor agonist, the 5-HT1 receptor agonist 5-carboxamidotryptamine, 5-CT, and the selective 5-HT3 receptor agonist m-CPBG (1-(m-chlorophenyl)-biguanide) did not modify the renal perfusion pressure. |
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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 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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| 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. |
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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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| 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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| 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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| 12734389 | Hajos M, Hoffmann WE, Weaver RJ: Regulation of septo-hippocampal activity by 5-hydroxytryptamine (2C) receptors. J Pharmacol Exp Ther. 2003 Aug;306(2):605-15. Epub 2003 May 6. Intravenous administration of 5-HT2C receptor agonists 1-(3-chlorophenyl) piperazine dihydrochloride (m-CPP) and [S]-2-(chloro-5--indol-1-yl)-1-methyl-ethylamine (Ro 60-0175) dose dependently inhibited firing activity most of the recorded MS/DBv neurons and abolished theta oscillation in all tested MS/DBv and hippocampal neurons. |
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| 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. |
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| 17936345 | Yonezawa A, Yoshizumi M, Ebiko M, Ise SN, Watanabe C, Mizoguchi H, Kimura Y, Sakurada S: Ejaculatory response induced by a 5-HT2 receptor agonist m-CPP in rats: differential roles of 5-HT2 receptor subtypes. Pharmacol Biochem Behav. 2008 Feb;88(4):367-73. Epub 2007 Sep 18. It has been reported that systemic administration of m-CPP (1-[3-chlorophenyl] piperazine hydrochloride), a 5-HT (2) receptor agonist, produces a 5-HT (2C) receptor-mediated penile erections and self-grooming in rats. |
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| 15032678 | Poissonnet G, Parmentier JG, Boutin JA, Goldstein S: The emergence of selective 5-HT 2B antagonists structures, activities and potential therapeutic applications. Mini Rev Med Chem. 2004 Mar;4(3):325-30. 5-HT (2) receptors mediate a large array of physiological and behavioral functions in humans via three distinct subtypes: 5-HT (2A), 5-HT (2B) and 5-HT (2C). Indeed, four structural classes belonging to the piperazine, naphthylpyrimidine and tetrahydro-beta-carboline scaffolds were reported. |
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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. |
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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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| 11856898 | Gleason SD, Lucaites VL, Shannon HE, Nelson DL, Leander JD: m-CPP hypolocomotion is selectively antagonized by compounds with high affinity for 5-HT (2C) receptors but not 5-HT (2A) or 5-HT (2B) receptors. Behav Pharmacol. 2001 Dec;12(8):613-20. The ability of m-CPP [1-(m-chlorophenyl) piperazine] to produce hypolocomotion is well documented. We investigated the effects of the selective 5-HT (2A) antagonists, MDL 100,907 and ketanserin, the selective 5-HT (2B) antagonists, LY 202146 and LY 266097, the 5-HT (2B/2C) antagonist, SB 206553, and the selective 5-HT (2C) antagonist, SB 242084 on m-CPP-induced hypolocomotion and spontaneous locomotor activity in mice. |
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| 15109520 | Obata H, Saito S, Sakurazawa S, Sasaki M, Usui T, Goto F: Antiallodynic effects of intrathecally administered 5-HT (2C) receptor agonists in rats with nerve injury. Pain. 2004 Mar;108(1-2):163-9. Intrathecal administration of type 2 (5-HT (2)) receptor agonists, alpha-methyl- (alpha-m- or (+/-)-1-(4-iodo-2,5-dimethoxyphenyl)-2-aminopropane hydrochloride (DOI), produces antiallodynic effects in a rat model of neuropathic pain. Administration of the 5-HT (2C) receptor agonist, 6-chloro-2-(1-piperazinyl)-pyrazine (MK212; 3-100 microg), 1-(m-chlorophenyl)-piperazine (mCPP; 30-300 microg), or 1-(m-trifluoromethylphenyl)-piperazine (TFMPP; 30-300 microg), produced antiallodynic effects in a dose-dependent manner with no associated motor weakness. |
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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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| 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 elevation in plasma and back muscle contractions evoked by the 5-HT (2A) agonist DOI (1 mg/kg ip) were attenuated, whilst wet-dog shakes were enhanced by treatment. 5-HT (2B) agonist-induced behaviour and the hypolocomotion and hypophagia induced by the 5-HT (2C) agonist m-CPP (2.5 mg/kg ip) were unaltered but the mCPP-induced elevation in was abolished by treatment. |
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| 12231467 | Arjona AA, Pooler AM, Lee RK, Wurtman RJ: Effect of a 5-HT (2C) agonist, dexnorfenfluramine, on amyloid precursor protein metabolism in guinea pigs. Brain Res. 2002 Sep 27;951(1):135-40. Chronic administration of mCPP (1-(m-chlorophenyl) piperazine) (2 mg/kg bid, i.p.), a 5-HT (2B/2C) agonist, for 9 days also increased CSF APP (s) levels (P <0.5) when measured 2 h after the drug's last administration; hippocampal and cortical APP (h) levels were unaffected. Stimulation of serotonin receptor subtypes 5-HT (2A) or 5-HT (2C) in stably transfected 3T3 cells by dexnorfenfluramine (DEXNOR) or increases secretion of the APP metabolite APP (s). |
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| 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. |
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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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| 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. 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. |
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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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| 20118542 | Hess S, Padoani C, Scorteganha LC, Holzmann I, Malheiros A, Yunes RA, Delle Monache F, de Souza MM: Assessment of mechanisms involved in antinociception caused by myrsinoic acid B. Biol Pharm Bull. 2010 Feb;33(2):209-15. The antinociception caused by AMB in the test was significantly attenuated by i.p. treatment of mice with precursor, 600 mg/kg), alpha2 and alpha1-adrenoceptor antagonists (yohimbine, 0.2 mg/kg/prazosin, 0.2 mg/kg), p-chlorophenylalanine (PCPA) an inhibitor of synthesis (100 mg/kg), 1-(2-methoxyphenyl)-4-(4-phthalimidobutyl) piperazine (NAN 190), a 5-HT1 (A) selective receptor antagonist (0.5 mg/kg) and a non-selective cholinergic antagonist (atropine, 10 mg/kg). |
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| 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. |
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| 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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| 11504649 | McCort G, Hoornaert C, Aletru M, Denys C, Duclos O, Cadilhac C, Guilpain E, Dellac G, Janiak P, Galzin AM, Delahaye M, Guilbert F, O'Connor S: Synthesis and SAR of 3- and 4-substituted quinolin-2-ones: discovery of mixed 5-HT (1B)/5-HT (2A) receptor antagonists. Bioorg Med Chem. 2001 Aug;9(8):2129-37. Quinolin-2-ones bearing a heteroaryl-piperazine linked by a two carbon chain at the 3- or 4-position were synthesised and evaluated as mixed 5-HT (1B)/5-HT (2A) receptor antagonists. |
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| 12482418 | Gonzalez-Gomez JC, Santana L, Uriarte E, Brea J, Villazon M, Loza MI, De Luca M, Rivas ME, Montenegro GY, Fontenla JA: New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors. Bioorg Med Chem Lett. 2003 Jan 20;13(2):175-8. Most of the new compounds showed high affinity for the three types of receptors alpha (1A), D (2) and 5-HT (2A) which depends, fundamentally, on the substitution of the N (4) of the piperazine ring. |
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| 12726823 | Mitchell PJ, Fairhall SJ, Fletcher A, Redfern PH: Effects of single and repeated electroconvulsive shock on the social and agonistic behaviour of resident rats. Neuropharmacology. 2003 Jun;44(7):911-25. Additional studies showed that bi-daily ECS treatment nearly abolished 5-HT (2C) receptor-mediated hypolocomotion induced by acute m-chlorophenylpiperazine (mCPP, 2.5 mg/kg sc) challenge 24 h following 2 ECSs, while 4 ECSs only enhanced 5-HT (2A) receptor-mediated head shakes induced by 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI, 2.0 mg/kg sc). |
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| 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. |
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| 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). |
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| 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. |
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| 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. |
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| 15507224 | Adamec R, Creamer K, Bartoszyk GD, Burton P: Prophylactic and therapeutic effects of acute systemic injections of EMD 281014, a selective 2A receptor antagonist on anxiety induced by predator stress in rats. Eur J Pharmacol. 2004 Nov 3;504(1-2):79-96. We examined the effect of the selective 2A (5-HT (2A)) receptor antagonist 7-[4-[2-(4--phenyl)-ethyl]-piperazine-1-carbonyl]-1H-indole-3-carbon itrile HCl (EMD 281014) [Bartoszyk, G.D., van Amsterdam, C., Bottcher, H., Seyfried, C.A., 2003. |
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| 12119448 | Sandrini M, Vitale G, Pini LA: Central antinociceptive activity of is modulated by brain serotonin receptor subtypes. Pharmacology. 2002 Aug;65(4):193-7. Binding experiments indicate that both and ketanserin completely prevented the decrease in the maximum number of 5-HT (2) receptors (B (max)) provoked by ASA. |
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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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