Target Information

Target General Infomation
Target ID
T59679
Former ID
TTDS00107
Target Name
5-hydroxytryptamine 4 receptor
Gene Name
HTR4
Synonyms
5-HT-4; 5-HT4; 5-HT4 receptor; Serotonin receptor; Serotonin receptor 4; HTR4
Target Type
Successful
Disease Atrial fibrillation [ICD9: 272, 427.31; ICD10: E78, I48]
Alzheimer disease; Post-traumatic stress disorder [ICD9:331, 309.81; ICD10: G30, F43.1]
Alzheimer disease [ICD9: 331; ICD10: G30]
Constipation [ICD9: 564; ICD10: K59.0]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Congestive heart failure [ICD9: 428; ICD10: I50]
Diabetic gastroparesis [ICD9: 250, 536.3; ICD10: E08-E13, K31.8]
Dyspepsia; Gastro-oesophageal reflux; Irritable bowel syndrome [ICD9:536.8, 530, 564.1, 787.91; ICD10: K30, K21, A09, K58, K59.1]
Emesis [ICD9: 787; ICD10: R11]
Gastrointestinal disease [ICD10: K00-K93]
Gastroparesis [ICD9: 536.3; ICD10: K31.8]
Gastroesophageal reflux disease [ICD9: 140-229, 530; ICD10: K21]
Gastric motility disorder [ICD10: K22.4]
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Neurodegenerative disease [ICD9: 330-337; ICD10: G30-G32]
Nausea [ICD10: R11]
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Parkinson's disease [ICD9: 332; ICD10: G20]
Schizophrenia [ICD9: 295; ICD10: F20]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Unspecified [ICD code not available]
Function
Thisis 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.
BioChemical Class
GPCR rhodopsin
Target Validation
T59679
UniProt ID
Q13639
Sequence
MDKLDANVSSEEGFGSVEKVVLLTFLSTVILMAILGNLLVMVAVCWDRQLRKIKTNYFIV
SLAFADLLVSVLVMPFGAIELVQDIWIYGEVFCLVRTSLDVLLTTASIFHLCCISLDRYY
AICCQPLVYRNKMTPLRIALMLGGCWVIPTFISFLPIMQGWNNIGIIDLIEKRKFNQNSN
STYCVFMVNKPYAITCSVVAFYIPFLLMVLAYYRIYVTAKEHAHQIQMLQRAGASSESRP
QSADQHSTHRMRTETKAAKTLCIIMGCFCLCWAPFFVTNIVDPFIDYTVPGQVWTAFLWL
GYINSGLNPFLYAFLNKSFRRAFLIILCCDDERYRRPSILGQTVPCSTTTINGSTHVLRD
AVECGGQWESQCHPPATSPLVAAQPSDT
Drugs and Mode of Action
Drug(s) Cisapride Drug Info Approved Gastroesophageal reflux disease [538540], [539528]
HTF 919 Drug Info Approved Constipation [546112], [551871]
R0-93877 Drug Info Approved Constipation [546610], [551871]
Tegaserod Drug Info Approved Irritable bowel syndrome [551871]
Mosapride Drug Info Phase 4 Discovery agent [524637], [539549]
Prucalopride Drug Info Phase 4 Discovery agent [524070], [539559]
Renzapride Drug Info Phase 3 Irritable bowel syndrome [536224], [539568]
DSP-6952 Drug Info Phase 2 Constipation [549293]
Lintopride Drug Info Phase 2 Nausea [534100]
PF-885706 Drug Info Phase 2 Gastroesophageal reflux disease [522400]
Piboserod Drug Info Phase 2 Atrial fibrillation [521950], [539424]
PRX-3140 Drug Info Phase 2 Alzheimer disease; Post-traumatic stress disorder [548095]
SB-207266A Drug Info Phase 2 Irritable bowel syndrome [551422]
SPD-557 Drug Info Phase 2 Diabetic gastroparesis [523512]
TD-5108 Drug Info Phase 2 Gastroparesis [521907], [543127]
YKP-GI Drug Info Phase 2 Constipation [524531], [543129]
TD-8954 Drug Info Phase 1/2 Alzheimer disease [524450], [543128]
BIMU-1 Drug Info Phase 1 Cognitive disorders [533870], [539484]
DA-6886 Drug Info Phase 1 Irritable bowel syndrome [523965]
M-0004 Drug Info Phase 1 Gastroesophageal reflux disease [548565]
PF-04995274 Drug Info Phase 1 Alzheimer disease [523152]
SER-101 Drug Info Phase 1 Congestive heart failure [549179]
Tegaserod Drug Info Withdrawn from market Dyspepsia; Gastro-oesophageal reflux; Irritable bowel syndrome [536224], [539432]
E-3620 Drug Info Discontinued in Phase 2 Gastric motility disorder [545633]
Fabesetron Drug Info Discontinued in Phase 2 Irritable bowel syndrome [544894]
Naronapride Drug Info Discontinued in Phase 2 Gastroesophageal reflux disease [547851]
Norcisapride Drug Info Discontinued in Phase 2 Gastroesophageal reflux disease [546263]
SL65.0155 Drug Info Discontinued in Phase 2 Parkinson's disease [539921], [547240]
TD-2749 Drug Info Discontinued in Phase 1 Gastrointestinal disease [548098]
5-HT4/D2 antagonists Drug Info Terminated Schizophrenia [536463]
DAU-6285 Drug Info Terminated Emesis [539587], [545063]
LY-353433 Drug Info Terminated Inflammatory bowel disease [546330]
SB 203186 Drug Info Terminated Discovery agent [539648], [545117]
SC-53116 Drug Info Terminated Gastric motility disorder [539515], [545444]
SK-951 Drug Info Terminated Gastrointestinal disease [546979]
Modulator (R)-zacopride Drug Info
BIMU-1 Drug Info [533870]
DAU-6285 Drug Info
E-3620 Drug Info [1572591]
Fabesetron Drug Info
Lintopride Drug Info [534100]
MDDR 287569 Drug Info [544189], [551871]
ML-10302 Drug Info
PRX-3140 Drug Info [551175]
Renzapride Drug Info
SC-52491 Drug Info
SC-53116 Drug Info
SC-54750 Drug Info
SDZ-205-557 Drug Info
TD-8954 Drug Info [531522]
VRX-03011 Drug Info
Inhibitor 1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info [527952]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
BARETTIN Drug Info [528498]
GR-113808 Drug Info [528977]
Norcisapride Drug Info [530330]
SB-207710 Drug Info [531144]
SEROTONIN Drug Info [528498]
Antagonist 5-HT4/D2 antagonists Drug Info [536463]
AF-3473 Drug Info [543971]
GR 125487 Drug Info [534287]
LY-353433 Drug Info [534112]
ML 10375 Drug Info [525774]
Piboserod Drug Info [535146]
R-116712 Drug Info [525710]
RO 116 1148 Drug Info [526322]
RS 100235 Drug Info [527202]
RS 116 0086 Drug Info [526322]
SB 203186 Drug Info [535385]
SB 204070 Drug Info [534429]
SB-207266A Drug Info [535146]
SER-101 Drug Info [550359]
[11C]SB207145 Drug Info [531597]
[123I]SB 207710 Drug Info [543971]
Agonist alpha-methyl-5-HT Drug Info [534429]
Cisapride Drug Info [536685], [536898]
DA-6886 Drug Info [543971]
DSP-6952 Drug Info [550349]
ER-21018 Drug Info [543971]
HTF 919 Drug Info [535385]
M-0004 Drug Info [543971]
Mosapride Drug Info [536689]
Naronapride Drug Info [531812]
PF-04995274 Drug Info [550239]
PF-885706 Drug Info [548442]
Prucalopride Drug Info [535146]
R0-93877 Drug Info [535146]
RQ-00000010 Drug Info [543971]
RS 57639 Drug Info [534429]
RS 67333 Drug Info [525888]
RS67506 Drug Info [534265]
SK-951 Drug Info [525467]
SL65.0155 Drug Info [535516]
SPD-557 Drug Info [543971]
SUVN-1004028 Drug Info [543971]
TD-2749 Drug Info [544307]
TD-5108 Drug Info [536685], [536689]
Tegaserod Drug Info [536224]
YKP-GI Drug Info [532929]
[3H]RS 57639 Drug Info [534429]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
cAMP signaling pathway
Neuroactive ligand-receptor interaction
Serotonergic synapse
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
5HT4 type receptor mediated signaling pathway
PathWhiz Pathway Excitatory Neural Signalling Through 5-HTR 4 and Serotonin
Reactome Serotonin receptors
G alpha (s) signalling events
WikiPathways Serotonin Receptor 4/6/7 and NR3C Signaling
Monoamine GPCRs
GPCRs, Class A Rhodopsin-like
GPCR ligand binding
GPCR downstream signaling
References
Ref 521907ClinicalTrials.gov (NCT00391820) Evaluate the Safety and Efficacy of a 5-HT4 Agonist in Chronic Constipation (ACCORD Trial). U.S. National Institutes of Health.
Ref 521950ClinicalTrials.gov (NCT00421746) A Clinical Study Assessing the Potential of Piboserod for the Treatment of Heart Failure. U.S. National Institutes of Health.
Ref 522400ClinicalTrials.gov (NCT00730665) Efficacy And Safety Of PF-00885706 For The Relief Of Symptoms In Subjects With Gastro-esophageal Reflux Disease (GERD). U.S. National Institutes of Health.
Ref 523152ClinicalTrials.gov (NCT01193062) Study In Healthy Subjects To Evaluate The Changes In The Protein sAPP-Alpha In Cerebrospinal Fluid Following A Single Oral Dose Of PF-04995274. U.S. National Institutes of Health.
Ref 523512ClinicalTrials.gov (NCT01370863) An Explorative Trial to Evaluate the Pharmacodynamic Effect of SPD557 on Reflux Parameters in Refractory GERD Patients. U.S. National Institutes of Health.
Ref 523965ClinicalTrials.gov (NCT01633723) Phase I Clinical Trial of DA-6886 in Healthy Male Subjects. U.S. National Institutes of Health.
Ref 524070ClinicalTrials.gov (NCT01692132) A Post Marketing Surveillance Study on the Safety and Effectiveness of Prucalopride in the Treatment of Chronic Constipation. U.S. National Institutes of Health.
Ref 524450ClinicalTrials.gov (NCT01953081) A Randomized, Double-Blind Study to Evaluate the Safety, Tolerability, and Pharmacodynamics of a Single Dose of Intravenous TD-8954 Compared With Metoclopramide in Critically Ill Patients With Enteral Feeding Intolerance. U.S. National Institutes of Health.
Ref 524531ClinicalTrials.gov (NCT01989234) A Multicenter, Double-Blind, Randomized, Placebo-Controlled, 12-Week, Dose-Range-Finding Trial of YKP10811 Capsules Administered Once Daily to Subjects With Chronic Idiopathic Constipation. U.S. National Institutes of Health.
Ref 524637ClinicalTrials.gov (NCT02056405) Effect of Mosapride on Postoperative Ileus in Patients Undergoing Colorectal Surgery. U.S. National Institutes of Health.
Ref 533870Gastroprokinetic properties of the benzimidazolone derivative BIMU 1, an agonist at 5-hydroxytryptamine4 and antagonist at 5-hydroxytryptamine3 receptors. Naunyn Schmiedebergs Arch Pharmacol. 1994 Apr;349(4):338-45.
Ref 534100The effects of lintopride, a 5HT-4 antagonist, on oesophageal motility. Aliment Pharmacol Ther. 1995 Oct;9(5):563-9.
Ref 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 538540FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020210.
Ref 539424(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 225).
Ref 539432(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 226).
Ref 539484(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 234).
Ref 539515(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 238).
Ref 539528(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 240).
Ref 539549(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 242).
Ref 539559(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 243).
Ref 539568(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 244).
Ref 539587(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 246).
Ref 539648(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 255).
Ref 539921(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 29).
Ref 543127(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8425).
Ref 543128(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8426).
Ref 543129(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8427).
Ref 544894Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001434)
Ref 545063Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002002)
Ref 545117Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002177)
Ref 545444Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003270)
Ref 545633Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004004)
Ref 546112Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006410)
Ref 546263Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007174)
Ref 546330Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007508)
Ref 546610Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009175)
Ref 546979Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011740)
Ref 547240Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014352)
Ref 547851Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019926)
Ref 548095Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021864)
Ref 548098Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021879)
Ref 548565Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026666)
Ref 549179Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033318)
Ref 549293Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034751)
Ref 551422Clinical pipeline report, company report or official report of Department of Pharmacology University of Wisconsin School of Medicine.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref
Ref 525467Identification of SK-951, a novel benzofuran derivative, as an agonist to 5-HT4 receptors. Jpn J Pharmacol. 1999 Feb;79(2):203-12.
Ref 525710Mapping of serotonin 5-HT(4) receptor mRNA and ligand binding sites in the post-mortem human brain. Synapse. 2000 Apr;36(1):35-46.
Ref 525774Exploration of the ligand binding site of the human 5-HT(4) receptor by site-directed mutagenesis and molecular modeling. Br J Pharmacol. 2000 Jun;130(3):527-38.
Ref 525888Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells. Br J Pharmacol. 2000 Oct;131(4):827-35.
Ref 526322A 5-HT4 receptor transmembrane network implicated in the activity of inverse agonists but not agonists. J Biol Chem. 2002 Jul 12;277(28):25502-11. Epub 2002 Apr 25.
Ref 527202New insights into the human 5-HT4 receptor binding site: exploration of a hydrophobic pocket. Br J Pharmacol. 2004 Oct;143(3):361-70. Epub 2004 Sep 6.
Ref 527952J 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.
Ref 528498J Nat Prod. 2006 Oct;69(10):1421-4.Brominated cyclodipeptides from the marine sponge Geodia barretti as selective 5-HT ligands.
Ref 528977J 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.
Ref 530330Bioorg 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).
Ref 531079J 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.
Ref 531144J 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.
Ref 531522The Pharmacology of TD-8954, a Potent and Selective 5-HT(4) Receptor Agonist with Gastrointestinal Prokinetic Properties. Front Pharmacol. 2011 May 30;2:25.
Ref 531597Mass dose effects and in vivo affinity in brain PET receptor studies--a study of cerebral 5-HT4 receptor binding with [11C]SB207145. Nucl Med Biol. 2011 Nov;38(8):1085-91.
Ref 531812Systematic review: cardiovascular safety profile of 5-HT(4) agonists developed for gastrointestinal disorders. Aliment Pharmacol Ther. 2012 Apr;35(7):745-67.
Ref 532929A randomized trial of 5-hydroxytryptamine4-receptor agonist, YKP10811, on colonic transit and bowel function in functional constipation. Clin Gastroenterol Hepatol. 2015 Apr;13(4):701-8.e1.
Ref 533870Gastroprokinetic properties of the benzimidazolone derivative BIMU 1, an agonist at 5-hydroxytryptamine4 and antagonist at 5-hydroxytryptamine3 receptors. Naunyn Schmiedebergs Arch Pharmacol. 1994 Apr;349(4):338-45.
Ref 534100The effects of lintopride, a 5HT-4 antagonist, on oesophageal motility. Aliment Pharmacol Ther. 1995 Oct;9(5):563-9.
Ref 534112LY353433, a potent, orally effective, long-acting 5-HT(4) receptor antagonist: comparison to cisapride and RS23597-190. J Pharmacol Exp Ther. 1996 Apr;277(1):97-104.
Ref 534265Peripheral 5-HT4 receptors. FASEB J. 1996 Oct;10(12):1398-407.
Ref 534287Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor. FEBS Lett. 1996 Nov 25;398(1):19-25.
Ref 534429[3H]RS 57639, a high affinity, selective 5-HT4 receptor partial agonist, specifically labels guinea-pig striatal and rat cloned (5-HT4S and 5-HT4L) receptors. Neuropharmacology. 1997 Apr-May;36(4-5):671-9.
Ref 535146Irritable bowel syndrome: new agents targeting serotonin receptor subtypes. Drugs. 2001;61(3):317-32.
Ref 5353855-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.
Ref 535516SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties. J Pharmacol Exp Ther. 2002 Aug;302(2):731-41.
Ref 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 536463The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22. Epub 2007 Jul 31.
Ref 536685The 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.
Ref 536689The 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.
Ref 536898Metoclopramide 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.
Ref 543971(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 9).
Ref 544189Phase II study of Cilengitide (EMD 121974, NSC 707544) in patients with non-metastatic castration resistant prostate cancer, NCI-6735. A study by the DOD/PCF Prostate Cancer Clinical Trials Consortium. Invest New Drugs. 2012 April; 30(2): 749-757.
Ref 544307A Hybrid Structural Approach to Analyze Ligand Binding by the Serotonin Type 4 Receptor (5-HT4). Mol Cell Proteomics. 2013 May; 12(5): 1259-1271.
Ref 548442Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025579)
Ref 550239Pharmacokinetics, safety and tolerability of PF04995274: A 5HT4 partial agonist being developed for the treatment of Alzheimer's disease. Alzheimer's and Dementia.
Ref 550349DSP-6952, a high affinity serotonin (5-HT4) receptor partial agonist. Sumitomo Dainippon Pharma Co. Ltd.
Ref 550359Phase I clinical trail of SER101 (RO1160367) for treating heart failure leukemia. Roche.
Ref 551175Clinical pipeline report, company report or official report of Nanotherapeutics.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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