| Name | 5 HT 3 |
|---|---|
| Synonyms | 5 HT 3; 5 hydroxytryptamine 3 receptor; serotonin receptor; HTR 3; HTR3; 5 HT3; 5 HT3A; 5 HT3R… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 19425598 | Morelli E, Gemma S, Budriesi R, Campiani G, Novellino E, Fattorusso C, Catalanotti B, Coccone SS, Ros S, Borrelli G, Persico M, Fiorini I, Nacci V, Ioan P, Chiarini A, Hamon M, Cagnotto A, Mennini T, Fracasso C, Colovic M, Caccia S, Butini S: Specific targeting of peripheral serotonin 5-HT (3) receptors. J Med Chem. 2009 Jun 11;52(11):3548-62. The unique properties of 4h and 4n, compared to their previously described centrally active N-methyl analogue 5a, are mainly due to the hydrophilic groups at the distal piperazine |
5(0,0,0,5) | 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). |
5(0,0,0,5) | Details |
| 12885436 | Castro L, Athanazio R, Barbetta M, Ramos AC, Angelo AL, Campos I, Varjao B, Ferreira H, Fregoneze J, de Castro e Silva E: Central 5-HT2B/2C and 5-HT3 receptor stimulation decreases salt intake in -depleted rats. Brain Res. 2003 Aug 15;981(1-2):151-9. |
4(0,0,0,4) | Details |
| 12079499 | Venkataraman P, Joshi P, Venkatachalan SP, Muthalagi M, Parihar HS, Kirschbaum KS, Schulte MK: Functional group interactions of a 5-HT3R antagonist. . BMC Biochem. 2002 Jun 13;3:16. Epub 2002 Jun 13. Analog 1 lacks the N1 benzyl group of lerisetron and analog 2 contains in place of the distal piperazine |
3(0,0,0,3) | Details |
| 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. |
2(0,0,0,2) | Details |
| 19122313 | Asagarasu A, Matsui T, Hayashi H, Tamaoki S, Yamauchi Y, Sato M: Design and synthesis of piperazinylpyridine derivatives as novel 5-HT1A agonists/5-HT3 antagonists for the treatment of irritable bowel syndrome (IBS). Chem Pharm Bull. 2009 Jan;57(1):34-42. These compounds, which were designed by pharmacophore analysis, bind to both subtype 1A (5-HT1A) and subtype 3 (5-HT3) receptors. The atom of the isoquinoline, a methoxy group and piperazine were essential to the pharmacophore for binding to these receptors. |
2(0,0,0,2) | Details |
| 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. We investigated the involvement of 5-HT1, 5-HT2, and 5-HT3 receptor subtypes in the regulation of spinal release. 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. |
2(0,0,0,2) | Details |
| 18238859 | Minato K, Suzuki R, Asagarasu A, Matsui T, Sato M: Biotransformation of 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl) piperazin-1-yl] butyl}qui nazolin-4 (3H)-one (TZB-30878), a novel (5-HT) 1A agonist/5-HT3 antagonist, in human hepatic cytochrome P450 enzymes. Drug Metab Dispos. 2008 May;36(5):831-40. Epub 2008 Jan 31. This compound has quinazoline, piperazine, and quinoline rings. |
2(0,0,0,2) | Details |
| 11305607 | Fujikawa M, Teratani F, Nakada Y: Enzyme immunoassay for 6-amino-5-chloro-1-isopropyl-2-(4-methyl-1-piperazinyl) benzimidazole, a novel 5-HT3 receptor antagonist. Biol Pharm Bull. 2001 Apr;24(4):422-4. The modification at the 4-methyl group of the piperazine moiety of KB-6806 significantly decreased the binding affinity to the antibody. |
2(0,0,0,2) | Details |
| 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-HT3 agonist SR57227A and the releaser/reuptake inhibitor d-fenfluramine increased the duration of avoidance behaviour in both types of rat. |
2(0,0,0,2) | Details |
| 11745625 | Hu HZ, Gao N, Lin Z, Gao C, Liu S, Ren J, Xia Y, Wood JD: P2X (7) receptors in the enteric nervous system of guinea-pig small intestine. J Comp Neurol. 2001 Nov 19;440(3):299-310. Rapidly activating depolarizing responses evoked by application of nicotinic, serotonergic 5-HT (3), or A (A)) receptor agonists were unaffected by brilliant blue G. The P2X (7) antagonists 1-[N,O-bis (1,5-isoquinolinesulfonyl)-N-methyl-l-tyrosyl]-4-piperazine (KN-62) and oxidized ATP also suppressed the BzBzATP-activated current. |
1(0,0,0,1) | 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. These data indicate that the central antinociceptive activity of ASA is modulated in a different manner by serotonin receptor antagonists, and that 5-HT (2) and 5-HT (3) receptors may exert a pivotal role in nociception, alone or in association. |
1(0,0,0,1) | 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 |
| 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. Because we observed that inhibited the increases in perfusion pressure induced by electrical stimulation of the lumbar chains, we used different agonists and antagonists to analyse the mechanism of action of 5-HT. 3. 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). |
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. Administration of either 5-HT (1A) antagonist (NAN-190), 5-HT (2) antagonist (ketanserin) or 5-HT (3 ) antagonist (3-(4-Allylpiperazin-1-yl)-2-quinoxalinecarbonitrile) blocked suanzaorentang-induced NREMS increase. |
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 |
| 15084129 | Berardi F, Ferorelli S, Abate C, Colabufo NA, Contino M, Perrone R, Tortorella V: 4-(tetralin-1-yl)- and 4-(naphthalen-1-yl) alkyl derivatives of 1-cyclohexylpiperazine as sigma receptor ligands with agonist sigma2 activity. J Med Chem. 2004 Apr 22;47(9):2308-17. Moreover, homologues of compound 33 displayed also satisfactory selectivities over D (2)-like, 5-HT (3), and adrenergic alpha (1) receptors. |
1(0,0,0,1) | Details |
| 12486804 | Tsai CL, Wang LH, Tsai CC: Role of and in the behavioral thermoregulation of female tilapia during the prespawning phase. J Exp Zool. 2002 Oct 1;293(5):443-9. Intrahypothalamic microinjection with (5-HT, 3 microliters of 1.0 x 10 (-6) M) resulted in a significant increase in the selected temperature. This effect was mimicked by the agonist of 5-HT1A, 1B, and 2C receptors, N-3-trifluoromethylphenyl piperazine. |
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 |
| 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). |
0(0,0,0,0) | 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. |
0(0,0,0,0) | 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. |
0(0,0,0,0) | 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. |
0(0,0,0,0) | Details |
| 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. |
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 |
| 14517765 | Sugimoto Y, Inoue K, Yamada J: Involvement of 5-HT (2) receptor in -induced hyperglycemia in mice. Horm Metab Res. 2003 Sep;35(9):511-6. i. p.-induced hyperglycemia was antagonized by the 5-HT (2C/2B) receptor agonist 1-(3-chlorophenyl) piperazine (mCPP), while the 5-HT (2B) receptor agonist BW 723C86 had no effect. |
0(0,0,0,0) | Details |
| 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 |
| 12218511 | Miranda F, Orozco G, Velazquez-Martinez DN: Full substitution of the discriminative cue of a 5-HT (1A/1B/2C) agonist with the combined administration of a 5-HT (1B/2C) and a 5-HT (1A) agonist. Behav Pharmacol. 2002 Jul;13(4):303-11. In generalization tests, INDO, 8--2-(di-n-propylamino) tetralin (8-OH-DPAT, a 5-HT (1A) agonist), 1-(3-trifluoromethylphenyl) piperazine (TFMPP, a 5-HT (1B) agonist), alpha-methyl- (a 5-HT (2C) agonist) or 2-methyl- (a 5-HT (3) agonist), were administered alone or in combination. |
31(0,1,1,1) | Details |
| 19831400 | Butini S, Budriesi R, Hamon M, Morelli E, Gemma S, Brindisi M, Borrelli G, Novellino E, Fiorini I, Ioan P, Chiarini A, Cagnotto A, Mennini T, Fracasso C, Caccia S, Campiani G: Novel, potent, and selective quinoxaline-based 5-HT (3) receptor ligands. 1. J Med Chem. 2009 Nov 12;52(21):6946-50. We investigated the pharmacological profile of a novel series of quinoxaline-based 5-HT (3) receptor ligands bearing an extra basic moiety on the piperazine N-4. |
82(1,1,1,2) | Details |
| 12560138 | Horiuchi H, Ogata T, Morino T, Takeba J, Yamamoto H: Serotonergic signaling inhibits hyperalgesia induced by spinal cord damage. Brain Res. 2003 Feb 14;963(1-2):312-20. The spinal cord injury-induced thermal-hyperalgesia was mimicked by the intrathecal application of metergoline, a non-selective antagonist, 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl]-piperazine hydrobromide (NAN190), a selective 5-HT1 antagonist, and 3-tropanyl-3,5-dichlorobenzoate (MDL72222), a selective 5-HT3 antagonist. |
31(0,1,1,1) | Details |
| 11557597 | Fu XW, Wang D, Pan J, Farragher SM, Wong V, Cutz E: Neuroepithelial bodies in mammalian lung express functional type 3 receptor. Am J Physiol Lung Cell Mol Physiol. 2001 Oct;281(4):L931-40. (5-HT) type 3 receptor (5-HT (3)-R) is a ligand-gated ion channel found primarily in the central and peripheral nervous system. |
8(0,0,0,8) | Details |
| 19735696 | Naumenko VS, Kondaurova EM, Popova NK: Central 5-HT3 receptor-induced hypothermia in mice: interstrain differences and comparison with hypothermia mediated via 5-HT1A receptor. Neurosci Lett. 2009 Nov 6;465(1):50-4. Epub 2009 Sep 6. |
6(0,0,0,6) | Details |