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]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Irritable bowel syndrome [ICD9: 564.1, 787.91; ICD10: A09, K58, K59.1]
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 [1], [2]
HTF 919 Drug Info Approved Constipation [3], [4]
R0-93877 Drug Info Approved Constipation [5], [4]
Tegaserod Drug Info Approved Irritable bowel syndrome [4]
Mosapride Drug Info Phase 4 Discovery agent [6], [7]
Prucalopride Drug Info Phase 4 Discovery agent [8], [9]
Renzapride Drug Info Phase 3 Irritable bowel syndrome [10], [11]
DSP-6952 Drug Info Phase 2 Constipation [12]
Lintopride Drug Info Phase 2 Nausea [13]
PF-885706 Drug Info Phase 2 Gastroesophageal reflux disease [14]
Piboserod Drug Info Phase 2 Atrial fibrillation [15], [16]
PRX-3140 Drug Info Phase 2 Alzheimer disease; Post-traumatic stress disorder [17]
SB-207266A Drug Info Phase 2 Irritable bowel syndrome [18]
SPD-557 Drug Info Phase 2 Diabetic gastroparesis [19]
TD-5108 Drug Info Phase 2 Gastroparesis [20], [21]
YKP-GI Drug Info Phase 2 Constipation [22], [23]
TD-8954 Drug Info Phase 1/2 Alzheimer disease [24], [25]
BIMU-1 Drug Info Phase 1 Cognitive disorders [26], [27]
DA-6886 Drug Info Phase 1 Irritable bowel syndrome [28]
M-0004 Drug Info Phase 1 Gastroesophageal reflux disease [29]
PF-04995274 Drug Info Phase 1 Alzheimer disease [30]
SER-101 Drug Info Phase 1 Congestive heart failure [31]
Tegaserod Drug Info Withdrawn from market Dyspepsia; Gastro-oesophageal reflux; Irritable bowel syndrome [10], [32]
E-3620 Drug Info Discontinued in Phase 2 Gastric motility disorder [33]
Fabesetron Drug Info Discontinued in Phase 2 Irritable bowel syndrome [34]
Naronapride Drug Info Discontinued in Phase 2 Gastroesophageal reflux disease [35]
Norcisapride Drug Info Discontinued in Phase 2 Gastroesophageal reflux disease [36]
SL65.0155 Drug Info Discontinued in Phase 2 Parkinson's disease [37], [38]
TD-2749 Drug Info Discontinued in Phase 1 Gastrointestinal disease [39]
5-HT4/D2 antagonists Drug Info Terminated Schizophrenia [40]
DAU-6285 Drug Info Terminated Emesis [41], [42]
LY-353433 Drug Info Terminated Inflammatory bowel disease [43]
SB 203186 Drug Info Terminated Discovery agent [44], [45]
SC-53116 Drug Info Terminated Gastric motility disorder [46], [47]
SK-951 Drug Info Terminated Gastrointestinal disease [48]
Modulator (R)-zacopride Drug Info
BIMU-1 Drug Info [26]
DAU-6285 Drug Info
E-3620 Drug Info [49]
Fabesetron Drug Info
Lintopride Drug Info [13]
MDDR 287569 Drug Info [50], [4]
ML-10302 Drug Info
PRX-3140 Drug Info [51]
Renzapride Drug Info
SC-52491 Drug Info
SC-53116 Drug Info
SC-54750 Drug Info
SDZ-205-557 Drug Info
TD-8954 Drug Info [52]
VRX-03011 Drug Info
Inhibitor 1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info [53]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [54]
BARETTIN Drug Info [55]
GR-113808 Drug Info [56]
Norcisapride Drug Info [57]
SB-207710 Drug Info [58]
SEROTONIN Drug Info [55]
Antagonist 5-HT4/D2 antagonists Drug Info [40]
AF-3473 Drug Info [59]
GR 125487 Drug Info [60]
LY-353433 Drug Info [61]
ML 10375 Drug Info [62]
Piboserod Drug Info [63]
R-116712 Drug Info [64]
RO 116 1148 Drug Info [65]
RS 100235 Drug Info [66]
RS 116 0086 Drug Info [65]
SB 203186 Drug Info [67]
SB 204070 Drug Info [68]
SB-207266A Drug Info [63]
SER-101 Drug Info [69]
[11C]SB207145 Drug Info [70]
[123I]SB 207710 Drug Info [59]
Agonist alpha-methyl-5-HT Drug Info [68]
Cisapride Drug Info [71], [72]
DA-6886 Drug Info [59]
DSP-6952 Drug Info [73]
ER-21018 Drug Info [59]
HTF 919 Drug Info [67]
M-0004 Drug Info [59]
Mosapride Drug Info [74]
Naronapride Drug Info [75]
PF-04995274 Drug Info [76]
PF-885706 Drug Info [77]
Prucalopride Drug Info [63]
R0-93877 Drug Info [63]
RQ-00000010 Drug Info [59]
RS 57639 Drug Info [68]
RS 67333 Drug Info [78]
RS67506 Drug Info [79]
SK-951 Drug Info [80]
SL65.0155 Drug Info [81]
SPD-557 Drug Info [59]
SUVN-1004028 Drug Info [59]
TD-2749 Drug Info [82]
TD-5108 Drug Info [71], [74]
Tegaserod Drug Info [10]
YKP-GI Drug Info [83]
[3H]RS 57639 Drug Info [68]
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
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REF 7(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 8ClinicalTrials.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.
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REF 20ClinicalTrials.gov (NCT00391820) Evaluate the Safety and Efficacy of a 5-HT4 Agonist in Chronic Constipation (ACCORD Trial). U.S. National Institutes of Health.
REF 21(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 22ClinicalTrials.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.
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REF 28ClinicalTrials.gov (NCT01633723) Phase I Clinical Trial of DA-6886 in Healthy Male Subjects. U.S. National Institutes of Health.
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REF 51Clinical pipeline report, company report or official report of Nanotherapeutics.
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REF 54J 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.
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