Therapeutic Targets Database
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TTD Target ID: TTDS00399

Target Information
Name5-hydroxytryptamine receptor 3A    
Type of targetSuccessful target    
Synonyms5-HT-3    
5-HT3A    
5-HT3R    
5HT3R    
HTR3    
HTR3A    
Serotonin receptor 3A    
Serotonin-gated ion channel receptor    
DiseaseChemotherapy-induced nausea and vomiting    [1]
Diarrhea    [2]
Irritable bowel syndrome    [3]
Postoperative nausea and vomiting    [4]
Drug(s)AlosetronApprovedIrritable bowel syndrome[3][2]
DolasetronApprovedNausea and vomiting[1]
LevetriacetamApprovedFibromyalgia[5]
PalonosetronApprovedNausea and vomiting[4]
ProcaineApprovedAnesthetic[6]
TropisetronApprovedFibromyalgia[5]
RenzapridePhase III completedIrritable bowel syndrome[7]
ArverapamilPhase II completedIrritable bowel syndrome[7]
DDP-225Phase IIIrritable bowel syndrome[7]
DDP-225Terminated in Phase IIChronic functional vomiting[7]
ATI-17000PreclinicalIrritable bowel syndrome[7]
BioChemical ClassIon transport    
UniProt IDP46098
SequenceMLLWVQQALLALLLPTLLAQGEARRSRNTTRPALLRLSDYLLTNYRKGVRPVRDWRKPTT VSIDVIVYAILNVDEKNQVLTTYIWYRQYWTDEFLQWNPEDFDNITKLSIPTDSIWVPDI LINEFVDVGKSPNIPYVYIRHQGEVQNYKPLQVVTACSLDIYNFPFDVQNCSLTFTSWLH TIQDINISLWRLPEKVKSDRSVFMNQGEWELLGVLPYFREFSMESSNYYAEMKFYVVIRR RPLFYVVSLLLPSIFLMVMDIVGFYLPPNSGERVSFKITLLLGYSVFLIIVSDTLPATAI GTPLIGVYFVVCMALLVISLAETIFIVRLVHKQDLQQPVPAWLRHLVLERIAWLLCLREQ STSQRPPATSQATKTDDCSAMGNHCSHMGGPQDFEKSPRDRCSPPPPPREASLAVCGLLQ ELSSIRQFLEKRDEIREVARDWLRVGSVLDKLLFHIYLLAVLAYSITLVMLWSIWQYA
Target ValidationClick to Find Target Validation Information.    
Inhibitor (4-Quinolin-2-ylpiperazin-1-yl)acetic Acid[8]
1- (biphenyl-4-yl)-3-[9]
10,11-dihydro-5H-dibenzo[b,f]azepine[10]
2- (1H-Imidazol-4-ylmethyl)-4-phenyl-thiazole[11]
2- (4-Benzyl-piperazin-1-yl)-benzothiazole[12]
2- (4-Methyl-piperazin-1-yl)-quinoline[13]
3- (2-Amino-ethyl)-2-methyl-1H-indol-5-ol[11]
3alpha- (1'-Methyl-2'-Indolecarbonyloxy)-tropane[14]
3alpha- (2'-Indolecarbonyloxy)-nortropane[14]
4- ([15]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[16]
4-Benzoxazo-2-yl-1,4-diazabicyclo[3.2.2]nonane[17]
5,6-dichloro-3,4-dihydroquinazolin-2-amine[18]
5-chloro-3,4-dihydroquinazolin-2-amine[18]
6- (4-Methyl-piperazin-1-yl)-phenanthridine[13]
7- (piperidin-4-ylmethoxy)-2-naphthonitrile[15]
A-987306[19]
BEMESETRON[20]
BRL-24682[21]
BRL-46470[22]
CP-810123[17]
FLUPENTIXOLE[10]
MESULERGINE[23]
ML-10302[24]
Norcisapride[25]
PH-709829[26]
PHA-543613[26]
QUIPAZINE[27]
SC-52491[28]
SC-53116[28]
SDZ-205557[24]
SEROTONIN[13]
ZACOPRIDE[24]
AntagonistAS-8112[29]
ATI-17000[7]
Alosetron[3][2]
Arverapamil[7]
CR-3124[29]
DDP-225[7]
Dolasetron[1]
Levetriacetam[5]
Palonosetron[4]
Procaine[6]
Renzapride[7]
Tropisetron[5]
MultitargetRenzapride[7]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Palonosetron plus dexamethasone versus granisetron plus dexamethasone for prevention of nausea and vomiting during chemotherapy: a double-blind, double-dummy, randomised, comparative phase III trial. Lancet Oncol. 2009 Feb;10(2):115-24. Epub 2009 Jan 8. To Reference
Ref 2Role of serotonin in gastrointestinal motility and irritable bowel syndrome. Clin Chim Acta. 2009 May;403(1-2):47-55. Epub 2009 Feb 4. To Reference
Ref 3Efficacy of 5-HT3 antagonists and 5-HT4 agonists in irritable bowel syndrome: systematic review and meta-analysis. Am J Gastroenterol. 2009 Jul;104(7):1831-43; quiz 1844. Epub 2009 May 26. To Reference
Ref 4Management of postoperative nausea and vomiting: focus on palonosetron. Ther Clin Risk Manag. 2009 Feb;5(1):21-34. Epub 2009 Mar 26. To Reference
Ref 5Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62. To Reference
Ref 6Local anesthetics have different mechanisms and sites of action at recombinant 5-HT3 receptors. Reg Anesth Pain Med. 2007 Nov-Dec;32(6):462-70. To Reference
Ref 7Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313. To Reference
Ref 8J Med Chem. 2009 Jun 11;52(11):3548-62.Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships. To Reference
Ref 9J Med Chem. 2010 Jun 10;53(11):4379-89.Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914). To Reference
Ref 10Eur J Med Chem. 2009 Jun;44(6):2667-72. Epub 2008 Dec 16.Molecular properties of psychopharmacological drugs determining non-competitive inhibition of 5-HT3A receptors. To Reference
Ref 11J Med Chem. 1990 Jan;33(1):13-6.Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists. To Reference
Ref 12J Med Chem. 1994 Apr 29;37(9):1320-5.Synthesis of 2-piperazinylbenzothiazole and 2-piperazinylbenzoxazole derivatives with 5-HT3 antagonist and 5-HT4 agonist properties. To Reference
Ref 13J Med Chem. 1999 May 6;42(9):1556-75.Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors. To Reference
Ref 14Bioorg Med Chem. 2009 Oct 1;17(19):6872-8. Epub 2009 Aug 20.Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors. To Reference
Ref 15Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32. Epub 2009 Feb 20.Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. To Reference
Ref 16J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. To Reference
Ref 17J Med Chem. 2010 Feb 11;53(3):1222-37.Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models. To Reference
Ref 18Bioorg Med Chem Lett. 2008 Jan 1;18(1):256-61. Epub 2007 Oct 30.Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: structure-activity relationship elucidation. To Reference
Ref 19J Med Chem. 2008 Nov 27;51(22):7094-8.cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. To Reference
Ref 20J Med Chem. 1992 Jan 24;35(2):310-9.Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships. To Reference
Ref 21J Med Chem. 2003 Feb 27;46(5):702-15.Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity. To Reference
Ref 22J Med Chem. 1997 Oct 10;40(21):3369-80.Phenylimidazolidin-2-one derivatives as selective 5-HT3 receptor antagonists and refinement of the pharmacophore model for 5-HT3 receptor binding. To Reference
Ref 23J Med Chem. 1997 Oct 24;40(22):3670-8.Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure. To Reference
Ref 24Bioorg. Med. Chem. Lett. 4(12):1433-1436 (1994) To Reference
Ref 25Bioorg Med Chem Lett. 2009 Oct 1;19(19):5679-83. Epub 2009 Aug 8.mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I). To Reference
Ref 26Bioorg Med Chem Lett. 2008 Jun 15;18(12):3611-5. Epub 2008 May 1.Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity. To Reference
Ref 27J Med Chem. 2009 Nov 12;52(21):6946-50.Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization. To Reference
Ref 28J Med Chem. 2006 Feb 9;49(3):1125-39.Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists. To Reference
Ref 29Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51. To Reference



 

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