Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00106

Target Information
Name5-hydroxytryptamine 3 receptor    
Type of targetSuccessful target    
Synonyms5-HT-3    
5-HT3 receptor    
5-HT3R    
5-hydroxytryptamine receptor 3    
5-hydroxytryptamine receptor type 3    
Serotonin-gated ion channel receptor    
DiseaseAlcohol dependence
[ICD9: 303   ICD10: F10.2]
[1]
Alcoholism
[ICD9: 303   ICD10: F10.2]
[1]
Irritable bowel syndrome
[ICD9: 564.1   ICD10: K58]
[2]
Nausea and vomiting
[ICD9: 787, 787.0   ICD10: R11]
[3][4][5]
Pruritus
[ICD9: 698   ICD10: L29]
[6]
Drug(s)GranisetronApprovedNausea and vomiting[7][8]
OndansetronApprovedChemotherapy-induced nausea and vomiting[6]
LerisetronPhase IIINausea and Vomiting, Testicular Germ Cell Tumor, Emesis[9]
KB-6806Phase IIChemotherapyinduced emesis[9]
OndansetronPhase IIAlcohol use disorders[10]
YM060Japan FiledDiarrhea-predominant irritable bowel syndrome in male (Orally-disintegrating tablet)
BioChemical ClassIon transport    
UniProt IDP46098
FunctionThis is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel.    
SequenceMLLWVQQALLALLLPTLLAQGEARRSRNTTRPALLRLSDYLLTNYRKGVRPVRDWRKPTT VSIDVIVYAILNVDEKNQVLTTYIWYRQYWTDEFLQWNPEDFDNITKLSIPTDSIWVPDI LINEFVDVGKSPNIPYVYIRHQGEVQNYKPLQVVTACSLDIYNFPFDVQNCSLTFTSWLH TIQDINISLWRLPEKVKSDRSVFMNQGEWELLGVLPYFREFSMESSNYYAEMKFYVVIRR RPLFYVVSLLLPSIFLMVMDIVGFYLPPNSGERVSFKITLLLGYSVFLIIVSDTLPATAI GTPLIGVYFVVCMALLVISLAETIFIVRLVHKQDLQQPVPAWLRHLVLERIAWLLCLREQ STSQRPPATSQATKTDDCSAMGNHCSHMGGPQDFEKSPRDRCSPPPPPREASLAVCGLLQ ELSSIRQFLEKRDEIREVARDWLRVGSVLDKLLFHIYLLAVLAYSITLVMLWSIWQYA
Related US Patent6,333,328
6,384,042
6,440,453
6,451,808
6,462,065
6,552,057
6,555,546
6,770,655
QSAR ModelClick to Find Target QSAR Model.    
AgonistOndansetron[10]
Ondansetron[6]
AntagonistBRL 43694A[11]
Ciproxifan[12]
Granisetron[7][8]
KB-6806[9]
LY278584[1]
Lerisetron[9]
Y-25130[5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 15-HT(3A) receptor subunit is required for 5-HT3 antagonist-induced reductions in alcohol drinking. Neuropsychopharmacology. 2004 Oct;29(10):1807-13. To Reference
Ref 2Drug treatment options for irritable bowel syndrome: managing for success. Drugs Aging. 2001;18(3):201-11. To Reference
Ref 3Effects of ondansetron on postoperative emesis in Chinese children. Acta Anaesthesiol Sin. 1998 Jun;36(2):87-91. To Reference
Ref 4Use of ondansetron, a 5-HT3 receptor antagonist, as a new type of antiemetic in pediatric oncology. Orv Hetil. 1993 Jun 20;134(25):1363-7. To Reference
Ref 5The antiemetic profile of Y-25130, a new selective 5-HT3 receptor antagonist. Eur J Pharmacol. 1991 Apr 24;196(3):299-305. To Reference
Ref 6Treatment of pruritus in chronic liver disease with the 5-hydroxytryptamine receptor type 3 antagonist ondansetron: a randomized, placebo-controlled, double-blind cross-over trial. Eur J Gastroenterol Hepatol. 1998 Oct;10(10):865-70. To Reference
Ref 7New approaches to chemotherapy-induced nausea and vomiting: from neuropharmacology to clinical investigations. Cancer J. 2006 Sep-Oct;12(5):341-7. To Reference
Ref 8Reduction of rectal sensitivity and post-prandial motility by granisetron, a 5 HT3-receptor antagonist, in patients with irritable bowel syndrome. Aliment Pharmacol Ther. 1993 Apr;7(2):175-80. To Reference
Ref 9Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51. To Reference
Ref 10Development of medications for alcohol use disorders: recent advances and ongoing challenges. Expert Opin Emerg Drugs. 2005 May;10(2):323-43. To Reference
Ref 11BRL 43694A--a 5-hydroxytryptamine receptor blocker as an antiemetic in cytostatic therapy. Schweiz Med Wochenschr. 1989 Jun 10;119(23):831-4. To Reference
Ref 12The histamine H3 receptor: from gene cloning to H3 receptor drugs. Nat Rev Drug Discov. 2005 Feb;4(2):107-20. To Reference



 

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