| Name | 5 hydroxytryptamine receptor (protein family or complex) |
|---|---|
| Synonyms | 5 Hydroxytryptamine receptor; 5 Hydroxytryptamine receptors; 5 hydroxytryptamine 3 receptor; 5 hydroxytryptamine 3 receptors; serotonin receptor; serotonin receptors |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 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. |
81(1,1,1,1) | 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. The combination of structural elements (heterocyclic nucleus, oxyalkyl chain and 4-substituted piperazine) known to be critical in order to have affinity on serotonin receptors and the proper selection of substituents led to compounds with higher receptor specificity and affinity. |
81(1,1,1,1) | Details |
| 11516887 | de Boer D, Bosman IJ, Hidvegi E, Manzoni C, Benko AA, dos Reys LJ, Maes RA: Piperazine-like compounds: a new group of designer drugs-of-abuse on the European market. Forensic Sci Int. 2001 Sep 15;121(1-2):47-56. 1-Aryl-piperazine compounds are, depending on their substituents, selective for certain serotonin receptors and together with their easy availability and their so-called legal status, this group of psychoactive compounds are potential designer drugs-of-abuse. |
6(0,0,1,1) | 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. |
2(0,0,0,2) | 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. Mutagenesis and modeling studies point out that the ligand-binding sites in serotonin receptors are located in the transmembrane domain. |
1(0,0,0,1) | Details |
| 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. |
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. |
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. A series of 52 conformationally constrained butyrophenones have been synthesized and pharmacologically tested as antagonists at 5-HT (2A), 5-HT (2B), and 5-HT (2C) serotonin receptors, useful for dissecting the role of each 5-HT (2) subtype in pathophysiology. Significant selectivity at the 5-HT (2B) receptor vs 5-HT (2C) was observed with 1-1 [(1-oxo-1,2,3,4-tetrahydro-3-naphthyl) methyl]-4-[3-(p-fluorobenzoyl) pro pyl] piperazine (more than 100-fold higher). |
1(0,0,0,1) | Details |
| 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. |
1(0,0,0,1) | Details |
| 16005846 | Pucadyil TJ, Chattopadhyay A: modulates the antagonist-binding function of hippocampal serotonin1A receptors. Biochim Biophys Acta. 2005 Aug 1;1714(1):35-42. The serotonin1A receptor is the most extensively studied member of the family of seven transmembrane domain G-protein coupled serotonin receptors. |
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. |
1(0,0,0,1) | Details |
| 15849995 | Maksay G, Simonyi M, Bikadi Z: Subunit rotation models activation of 5-HT3AB receptors by agonists. J Comput Aided Mol Des. 2004 Oct;18(10):651-64. The N-terminal extracellular regions of heterooligomeric 3AB-type human 5-hydroxytryptamine receptors (5-HT3ABR) were modelled based on the crystal structure of snail binding protein AChBP. AB subunit dimers with different rotations were applied for docking of ligands with different efficacies: m-chlorophenylbiguanide, SR 57227, quinolinyl piperazine and lerisetron derivatives. |
1(0,0,0,1) | Details |
| 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 (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. |
1(0,0,0,1) | 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. We used rat isolated brainstem block preparations to analyze the functional roles of serotonin receptors in the generation of trigeminal rhythmic activities. 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. |
1(0,0,0,1) | Details |
| 12770569 | Gannon RL: Serotonergic (1A) mixed agonists/antagonists elicit large-magnitude phase shifts in hamster circadian wheel-running rhythms. Neuroscience. 2003;119(2):567-76. The serotonergic ligands 8-(2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl)-8-azaspiro (4.5) decane-7,9-d ione dihydrochloride (BMY 7378), S 15535, and 8-[2-(1,4-benzodioxan-2-ylmethylamino) ethyl]-8-azaspiro [4.5] decane-7,9-dio ne hydrochloride (MDL 73005 EF) can all be classified as mixed agonists/antagonists at type 1A serotonin receptors. |
1(0,0,0,1) | Details |
| 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. |
1(0,0,0,1) | Details |
| 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. |
1(0,0,0,1) | Details |
| 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. |
1(0,0,0,1) | 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. |
1(0,0,0,1) | Details |
| 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. |
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. |
1(0,0,0,1) | Details |
| 16256082 | Gatch MB: substitutes for the discriminative stimulus effects of m-chlorophenylpiperazine. Brain Res. 2005 Nov 16;1062(1-2):161-5. Epub 2005 Oct 26. These findings suggest an important role of serotonin receptors in mediating the discriminative stimulus effects of |
1(0,0,0,1) | 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. A series of 15 new 2-H- and 2-substituted 5-[omega-[4-(2-methoxyphenyl)-piperazinyl]-alkyl]-1,2,3,4-tetrahydro-gamma -carboline derivatives were prepared, and their affinity for 5-HT1A and 5-HT2A serotonin receptors was determined. |
1(0,0,0,1) | 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. These results raise significant concerns about studies using NAN-190 and SB 269970 as specific antagonists of serotonin receptors. |
1(0,0,0,1) | Details |
| 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. |
1(0,0,0,1) | Details |
| 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. |
1(0,0,0,1) | Details |
| 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. It is only recently that the tools necessary to clearly delineate which serotonin receptors are involved in the mediation of m-CPP hypolocomotion have become available. |
1(0,0,0,1) | 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. 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 |