Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDS00107

Target Information
Name5-hydroxytryptamine 4 receptor    
Type of targetSuccessful target    
5-HT4 receptor    
Serotonin receptor    
Serotonin receptor 4    
DiseaseAlzheimer's disease
[ICD9: 331.0   ICD10: G30]
Cardiac arrhythmias
[ICD9: 427   ICD10: I47-I49]
[ICD9: 290-294   ICD10: F01-F07]
Diarrhoea-predominant irritable bowel syndrome
[ICD9: 564.1   ICD10: K58]
Drug dependence
[ICD9: 303-304   ICD10: F10.2-F19.2]
Irritable bowel syndrome
[ICD9: 564.1   ICD10: K58]
Psychiatric illness[4]
Drug(s)CisaprideApprovedGastroesophageal reflux disease[6][7]
TegaserodApprovedIrritable bowel syndrome[8]
RenzapridePhase III completedIrritable bowel syndrome[8]
TegaserodPhase IIIDyspepsia[8]
Fluphenazine DecanoatePhase IIPsoriasis[9]
PRX-3140Phase IIAlzheimer's disease
PumosetragPhase IIIrritable bowel syndrome[8]
TegaserodPhase IIGastro-oesophagal reflux[8]
PumosetragPhase IGastro-oesophageal reflux[8]
TD-8954Phase ICognitive impairment associated with Alzheimer's disease
5-HT4/D2 antagonistsNo development reportedSchizophrenia[10]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
UniProt IDQ13639
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. The activity of this receptor is mediated by G proteins that stimulates adenylate cyclase.    
Target ValidationClick to Find Target Validation Information.    
Inhibitor1- ([11]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[12]
HTF 919[18]
Antagonist5-HT4/D2 antagonists[10]
Fluphenazine Decanoate[9]
SB 203186[18]
SDZ 205,557[4]
MultitargetFluphenazine Decanoate[9]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The serotonin 5-HT4 receptor and the amyloid precursor protein processing. Exp Gerontol. 2003 Jan-Feb;38(1-2):159-66. To Reference
Ref 2Agonist-like activity of antibodies directed against the second extracellular loop of the human cardiac serotonin 5-HT4(e) receptor in transfected COS-7 cells. Receptors Channels. 2002;8(2):113-21. To Reference
Ref 3SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties. J Pharmacol Exp Ther. 2002 Aug;302(2):731-41. To Reference
Ref 4Antagonism of 5-hydroxytryptamine(4) receptors attenuates hyperactivity induced by cocaine: putative role for 5-hydroxytryptamine(4) receptors in the nucleus accumbens shell. J Pharmacol Exp Ther. 1999 Oct;291(1):300-7. To Reference
Ref 5Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32. To Reference
Ref 6Metoclopramide stimulates catecholamine- and granin-derived peptide secretion from pheochromocytoma cells through activation of serotonin type 4 (5-HT4) receptors. Endocr Relat Cancer. 2009 Mar;16(1):281-90. Epub 2008 Oct 23. To Reference
Ref 7The in vivo gastrointestinal activity of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):139-47. Epub 2008 Apr 12. To Reference
Ref 8Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313. To Reference
Ref 9Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63. To Reference
Ref 10The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31. To Reference
Ref 11J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity. To Reference
Ref 12J 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 13J Nat Prod. 2006 Oct;69(10):1421-4.Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands. To Reference
Ref 14J Med Chem. 2007 Sep 6;50(18):4482-92. Epub 2007 Aug 3.Synthesis of specific bivalent probes that functionally interact with 5-HT(4) receptor dimers. To Reference
Ref 15J Med Chem. 2009 Apr 23;52(8):2214-25.Design, synthesis, and biological evaluation of new 5-HT4 receptor agonists: application as amyloid cascade modulators and potential therapeutic utility in Alzheimer's disease. To Reference
Ref 16Bioorg Med Chem Lett. 2009 Oct 1;19(19):5679-83. Epub 2009 Aug dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I). To Reference
Ref 17J Med Chem. 2010 Oct 14;53(19):7035-47.Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography. To Reference
Ref 185-Hydroxytryptamine mediated contractions in isolated preparations of equine ileum and pelvic flexure: pharmacological characterization of a new 5-HT(4) agonist. J Vet Pharmacol Ther. 2002 Feb;25(1):49-58. To Reference
Ref 19The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):125-37. Epub 2008 Apr 16. To Reference


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