| Name | serotonin receptor |
|---|---|
| Synonyms | 5 hydroxytryptamine receptor 6; serotonin receptor; 5 HT 6; 5 HT6; 5 hydroxytryptamine (serotonin) receptor 6; 5 hydroxytryptamine 6 receptor; HTR 6; HTR6… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 12558977 | Cobb WS, Abercrombie ED: Differential regulation of somatodendritic and nerve terminal release by serotonergic innervation of substantia nigra. J Neurochem. 2003 Feb;84(3):576-84. The non-selective serotonin receptor agonist 1-(m-chlorophenyl)-piperazine (100 micro m) elicited a similar pattern of release in substantia nigra and striatum. |
81(1,1,1,1) | Details |
| 11800033 | Tierney AJ, Mangiamele LA: Effects of and analogs on posture and agonistic behavior in crayfish. J Comp Physiol A. 2001 Dec;187(10):757-67. In our second experiment, we tested and four serotonin receptor agonists [1-(3-chlorophenyl) piperazine dihydrochloride, 2-methyl- 5-carboxamidotryptamine and alpha-methyl- and measured the ability of each agonist to mimic the actions of the amine. |
81(1,1,1,1) | Details |
| 15745826 | Lee M, Rangisetty JB, Pullagurla MR, Dukat M, Setola V, Roth BL, Glennon RA: 1-(1-Naphthyl) piperazine as a novel template for 5-HT6 serotonin receptor ligands. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1707-11. 4-Sulfonyl analogs of 1-(1-naphthyl) piperazine bind at human 5-HT6 receptors and represent a novel class of human 5-HT6 receptor ligands. |
112(1,2,2,2) | 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. |
31(0,1,1,1) | Details |
| 20078106 | de la Fuente T, Martin-Fontecha M, Sallander J, Benhamu B, Campillo M, Medina RA, Pellissier LP, Claeysen S, Dumuis A, Pardo L, Lopez-Rodriguez ML: Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. J Med Chem. 2010 Feb 11;53(3):1357-69. Thus, we propose that D3.32 in TM 3 anchors the protonated piperazine ring, the benzimidazole ring expands parallel to EL 2 to bond N6.55 in TM 6, and the aromatic ring is placed between TMs 3 and 5 in CH (2)-containing compounds and between TMs 3 and 6 in CO-containing compounds. |
4(0,0,0,4) | Details |
| 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. Serotonin receptor sensitivity is likely to be an important determinant of this fatigue. |
3(0,0,0,3) | Details |
| 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. |
2(0,0,0,2) | Details |
| 11347881 | Van Craenenbroeck E, Vercammen J, Matthys G, Beirlant J, Marot C, Hoebeke J, Strobbe R, Engelborghs Y: Heuristic statistical analysis of fluorescence fluctuation data with bright spikes: application to ligand binding to the human serotonin receptor expressed in Escherichia coli cells. Biol Chem. 2001 Mar;382(3):355-61. |
2(0,0,0,2) | Details |
| 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. |
2(0,0,0,2) | Details |
| 15467976 | Feuchtl A, Bagli M, Stephan R, Frahnert C, Kolsch H, Kuhn KU, Rao ML: Pharmacokinetics of m-chlorophenylpiperazine after intravenous and oral administration in healthy male volunteers: implication for the pharmacodynamic profile. Pharmacopsychiatry. 2004 Jul;37(4):180-8. Seven different major serotonin receptor subtypes have been described. |
2(0,0,0,2) | Details |
| 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). |
1(0,0,0,1) | Details |
| 17691920 | Caccia S: N-dealkylation of arylpiperazine derivatives: disposition and metabolism of the 1-aryl-piperazines formed. Curr Drug Metab. 2007 Aug;8(6):612-22. These metabolites are best known for the variety of serotonin receptor-related effects they cause in man and animals, although some have affinity for other neurotransmitter receptors; others, however, are still largely unexplored despite uncontrolled use as amphetamine-like designer drugs. Once formed they distribute extensively in tissues, including brain which is the target site of most arylpiperazine derivatives, and are then primarily biotransformed by CYP2D6-dependent oxidation to hydroxylates which are excreted as conjugates; only 1-(2-benzisothiazolyl)-piperazine is more susceptible to oxidation than to aromatic hydroxylation. |
1(0,0,0,1) | 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. Remarkably, these responses were unaffected by the antagonists rauwolscine (5-HT (2B)), SB204741 (5-HT (2B/2C)) or Ro 04-6790 (5-ht (6)) (300 and 1000 microg kg (-1) each). 4. 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. |
1(0,0,0,1) | Details |
| 18762217 | Lam DD, Zhou L, Vegge A, Xiu PY, Christensen BT, Osundiji MA, Yueh CY, Evans ML, Heisler LK: Distribution and neurochemical characterization of neurons within the nucleus of the solitary tract responsive to agonist-induced hypophagia. Behav Brain Res. 2009 Jan 3;196(1):139-43. Epub 2008 Aug 13. Here we investigated whether the classic anorectic serotonin receptor agonist m-chloro-phenylpiperazine (mCPP) enhances the activity of metabolically sensitive NTS neurons. |
2(0,0,0,2) | Details |
| 17892934 | Tasler S, Kraus J, Wuzik A, Muller O, Aschenbrenner A, Cubero E, Pascual R, Quintana-Ruiz JR, Dordal A, Merce R, Codony X: Discovery of 5-HT6 receptor ligands based on virtual HTS. . Bioorg Med Chem Lett. 2007 Nov 15;17(22):6224-9. Epub 2007 Sep 8. |
2(0,0,0,2) | Details |
| 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. |
1(0,0,0,1) | Details |
| 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. Treatment with the selective 5-HT (1A) serotonin receptor agonist 8-OH-DPAT (0.1, 0.25, 0.5 and 2.0 mg/kg) induced a dose-dependent decrease in the amount of time spent by the males near the partition, or "partition time", which is considered the main pattern of sexual motivation. |
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 |
| 16307611 | Guitton MJ, Pujol R, Puel JL: m-Chlorophenylpiperazine exacerbates perception of -induced tinnitus in rats. Eur J Neurosci. 2005 Nov;22(10):2675-8. The serotonin receptor 5-HT2c agonist m-chlorophenylpiperazine (mCPP) has been widely used to induce anxiety-like states in animals and anxiety in humans. |
1(0,0,0,1) | Details |
| 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. The serotonin receptor agonist mCPP induces hyperlocomotion in 5-HT2C receptor knockout (KO) mice or in the presence of a 5-HT2C receptor antagonist. |
1(0,0,0,1) | Details |
| 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. The resulting MIP P (WAY) was evaluated as an affinity matrix in the screening of serotonin receptor antagonists with known affinities for the native receptor. |
1(0,0,0,1) | 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. |
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 |
| 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. |
1(0,0,0,1) | Details |
| 15113845 | Schlag BD, Lou Z, Fennell M, Dunlop J: Ligand dependency of 5-hydroxytryptamine 2C receptor internalization. J Pharmacol Exp Ther. 2004 Sep;310(3):865-70. Epub 2004 Apr 27. The (5-HT) 2C subtype of serotonin receptor is a GPCR that we have shown to internalize upon agonist incubation. In this study, we have examined the effects of 5-HT2C receptor agonists Ro 60-0175 [(S)-2-(6-chloro-5-fluoroindol-1-yl)-1-methylethylamine], and WAY-161503 [(4aR)-8,9-dichloro-2,3,4,4a-tetrahydro-1H-pyrazino [1,2-a] quinoxalin-5 (6H) -one]; partial agonists mCPP [1-(m-chlorophenyl) piperazine] and DOI [(+)-1-(2,5-dimethoxy-4-iodophenyl)-2-amino-propane]; inverse agonists SB-206553 [N-3-pyridinyl-3,5-dihydro-5-methylbenzo (1,2-b:4,5-b') dipyrrole-1 (2H) carbo xamide] and mianserin; and neutral antagonists SB-242084 [6-chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl) oxy]-5-pyridyl] carbamoyl]-in doline] and 5-methoxygramine on the internalization of a C-terminal green fluorescent protein (GFP)-tagged 5-HT2C receptor (VSV isoform) expressed in transiently transfected human embryonic kidney cells. |
1(0,0,0,1) | 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. |
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. |
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. |
1(0,0,0,1) | 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 |
| 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. |
0(0,0,0,0) | Details |