DGIdb - HTR4 Gene Record

HTR4 3360 Druggable Genome

Alternate Names:

3360
5-HYDROXYTRYPTAMINE RECEPTOR 4
HTR4
5-HT4
5-HT4R
602164
5299
ENSG00000164270
OTTHUMG00000129931
Serotonin receptor 4
5-HT-4
5-HYDROXYTRYPTAMINE 4 RECEPTOR (5-HT-4) (SEROTONIN RECEPTOR 4) (5- HT4). [SOURCE:UNIPROT/SWISSPROT;ACC:Q13639]
5HT4R_HUMAN
Q13639
5-HT 4 receptor
T59679

Gene Info:

Human Readable Name	G PROTEIN COUPLED RECEPTOR
Human Readable Name	DRUGGABLE GENOME
Interpro Short Name	7TM_GPCR_Rhodpsn
Interpro Acc	IPR000276
Interpro Type	Family
Uniprot Evidence	1: Evidence at protein level
Uniprot Status	Swiss-Prot
Interpro Name	GPCR, rhodopsin-like, 7TM
Target Subclass	Rhodopsin
Target Main Class	Receptors
Target Subclass	GPCR
Transmembrane Helix Count	7
Gene Biotype	PROTEIN_CODING

(6 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Briejer et al., 1993, Cisapride and a structural analogue, R 76,186, are 5-hydroxytryptamine4 (5-HT4) receptor agonists on the guinea-pig colon ascendens., Naunyn Schmiedebergs Arch. Pharmacol.
Yuan et al., 1994, Investigation of the role of 5-HT3 and 5-HT4 receptors in ascending and descending reflexes to the circular muscle of guinea-pig small intestine., Br. J. Pharmacol.
Katayama et al., 1995, [Cisapride, a gastroprokinetic agent, binds to 5-HT4 receptors]., Nippon Yakurigaku Zasshi
Meulemans et al., 1992, Is the action of cisapride on the guinea-pig ileum mediated via 5-HT4 receptors?, Eur. J. Pharmacol.
Cartier et al., 2003, Overexpression of serotonin4 receptors in cisapride-responsive adrenocorticotropin-independent bilateral macronodular adrenal hyperplasia causing Cushing's syndrome., J. Clin. Endocrinol. Metab.
Bharucha et al., 2000, Effects of a serotonin 5-HT(4) receptor antagonist SB-207266 on gastrointestinal motor and sensory function in humans., Gut
Crema et al., 1999, Intestinal prokinesia by two esters of 4-amino-5-chloro-2- methoxybenzoic acid: involvement of 5-hydroxytryptamine-4 receptors and dissociation from cardiac effects in vivo., J. Pharmacol. Exp. Ther.
Rahme et al., 1999, Electrophysiological and antiarrhythmic effects of the atrial selective 5-HT(4) receptor antagonist RS-100302 in experimental atrial flutter and fibrillation., Circulation
Nagakura et al., 1999, Pharmacological properties of a novel gastrointestinal prokinetic benzamide selective for human 5-HT4 receptor versus human 5-HT3 receptor., Pharmacol. Res.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Bach et al., 2001, 5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle., Naunyn Schmiedebergs Arch. Pharmacol.
Camilleri, 2001, Review article: tegaserod., Aliment. Pharmacol. Ther.
Cole et al., 2004, Tegaserod: a serotonin 5-HT4 receptor agonist for treatment of constipation-predominant irritable bowel syndrome., Drugs Today
Beattie et al., 2004, The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo., Br. J. Pharmacol.
Corsetti et al., 2002, Tegaserod: a new 5-HT(4) agonist in the treatment of irritable bowel syndrome., Expert Opin Pharmacother
Kamm, 2002, Review article: the complexity of drug development for irritable bowel syndrome., Aliment. Pharmacol. Ther.
Arranz et al., 1998, Characterization of the 5-HT4 binding site in human brain., J Neural Transm (Vienna)
Xu R et al., 2010, Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography., J Med Chem
Hedner E et al., 2008, Antifouling activity of a dibrominated cyclopeptide from the marine sponge Geodia barretti., J Nat Prod
Gobbi et al., 1997, Effects of chronic treatment with fluoxetine and citalopram on 5-HT uptake, 5-HT1B autoreceptors, 5-HT3 and 5-HT4 receptors in rats., Naunyn Schmiedebergs Arch. Pharmacol.
Camilleri M et al., 2007, Pharmacodynamic effects of a novel prokinetic 5-HT receptor agonist, ATI-7505, in humans., Neurogastroenterol Motil
Petrascheck M et al., 2007, An antidepressant that extends lifespan in adult Caenorhabditis elegans., Nature
Nakayama et al., 2005, Antiemetic activity of FK1052, a 5-HT3- and 5-HT4-receptor antagonist, in Suncus murinus and ferrets., J. Pharmacol. Sci.
Briejer et al., 2001, The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound., Eur. J. Pharmacol.
Raffa et al., 1996, Lack of binding of acetaminophen to 5-HT receptor or uptake sites (or eleven other binding/uptake assays)., Life Sci.
Craig et al., 1991, Peristalsis evoked by 5-HT and renzapride: evidence for putative 5-HT4 receptor activation., Br. J. Pharmacol.
Darblade et al., 2005, Piboserod (SB 207266), a selective 5-HT4 receptor antagonist, reduces serotonin potentiation of neurally-mediated contractile responses of human detrusor muscle., World J Urol
McCullough et al., 2006, The 5-HT2B antagonist and 5-HT4 agonist activities of tegaserod in the anaesthetized rat., Pharmacol. Res.

TEGASEROD HTR4

Interaction Score: 8.01

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

antagonist (inhibitory)

Interaction Info:

PMIDs:
11207504 15645012 15466450 12150698 11752352 11876686

Sources:
TTD
PIBOSEROD HTR4

Interaction Score: 6.87

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
15902472 16495076

Sources:
TTD
CISAPRIDE HTR4

Interaction Score: 6.41

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
8321323 7952869 7557734 1555639 12519861 11034583 10027842 10556228 10328995 11752352 11218067

Sources:
NCI TEND TTD
REVEXEPRIDE HTR4

Interaction Score: 4.58

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
CHEMBL401607 HTR4

Interaction Score: 4.58

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18271554

Sources:
DTC
CHEMBL114112 HTR4

Interaction Score: 4.58

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20812727

Sources:
DTC
SUVN-D4010 HTR4

Interaction Score: 2.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PF-04995274 HTR4

Interaction Score: 2.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
None found

Sources:
TTD
DA-6886 HTR4

Interaction Score: 2.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PRUCALOPRIDE HTR4

Interaction Score: 2.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

Direct Interaction yes

PMIDs:
11438309

Sources:
ChemblInteractions
VELUSETRAG HTR4

Interaction Score: 2.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
NARONAPRIDE HTR4

Interaction Score: 2.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

Direct Interaction yes

PMIDs:
17187586

Sources:
ChemblInteractions
TAK-954 HTR4

Interaction Score: 2.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
None found

Sources:
TTD
CISAPRIDE HTR4

Interaction Score: 2.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
CAPESEROD HTR4

Interaction Score: 2.29

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 4 (5-HT4) receptor partial agonist

PMIDs:
None found

Sources:
ChemblInteractions
LINTOPRIDE HTR4

Interaction Score: 1.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
MOSAPRIDE HTR4

Interaction Score: 1.14

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
None found

Sources:
TTD
RENZAPRIDE HTR4

Interaction Score: 0.92

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
1364818

Sources:
TTD
METOCLOPRAMIDE HYDROCHLORIDE HTR4

Interaction Score: 0.76

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TROPISETRON HTR4

Interaction Score: 0.65

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
9826103

Sources:
NCI
METITEPINE HTR4

Interaction Score: 0.46

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18033297

Sources:
DTC
MIANSERIN HTR4

Interaction Score: 0.46

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18033297

Sources:
DTC
ZOLMITRIPTAN HTR4

Interaction Score: 0.46

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TEND
TEGASEROD MALEATE HTR4

Interaction Score: 0.38

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 4 (5-HT4) receptor partial agonist

PMIDs:
None found

Sources:
ChemblInteractions
FLUOXETINE HTR4

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9228186

Sources:
NCI
ACETAMINOPHEN HTR4

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8699917

Sources:
NCI
CISPLATIN HTR4

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16079468

Sources:
NCI

Ensembl: ENSG00000164270
- Version: 101_38
Alternate Names:

HTR4 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
RussLampel: ENSG00000164270
- Version: 26-July-2011
Alternate Names:

ENSG00000164270 Ensembl Gene Id

5-HYDROXYTRYPTAMINE 4 RECEPTOR (5-HT-4) (SEROTONIN RECEPTOR 4) (5- HT4). [SOURCE:UNIPROT/SWISSPROT;ACC:Q13639] Description

HTR4 Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TEND: Q13639
- Version: 01-August-2011
Alternate Names:

Q13639 Uniprot Accession

3360 Entrez Gene Id

HTR4 Gene Symbol

Gene Info:

Target Main Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
HopkinsGroom: Q13639
- Version: 11-September-2012
Alternate Names:

5-HYDROXYTRYPTAMINE RECEPTOR 4 Uniprot Protein Name

5HT4R_HUMAN Uniprot Id

Q13639 Uniprot Accession

Gene Info:

Interpro Short Name 7TM_GPCR_Rhodpsn

Interpro Acc IPR000276

Human Readable Name DRUGGABLE GENOME

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:

NCI: HTR4

Version: 14-September-2017

Alternate Names:

Gene Info:

Publications:

Gobbi et al., 1997, Effects of chronic treatment with fluoxetine and citalopram on 5-HT uptake, 5-HT1B autoreceptors, 5-HT3 and 5-HT4 receptors in rats., Naunyn Schmiedebergs Arch. Pharmacol.

Nakayama et al., 2005, Antiemetic activity of FK1052, a 5-HT3- and 5-HT4-receptor antagonist, in Suncus murinus and ferrets., J. Pharmacol. Sci.

Arranz et al., 1998, Characterization of the 5-HT4 binding site in human brain., J Neural Transm (Vienna)

DTC: HTR4

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Petrascheck M et al., 2007, An antidepressant that extends lifespan in adult Caenorhabditis elegans., Nature

Hedner E et al., 2008, Antifouling activity of a dibrominated cyclopeptide from the marine sponge Geodia barretti., J Nat Prod

Xu R et al., 2010, Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography., J Med Chem

ChemblInteractions: HTR4
- Version: chembl_23
Alternate Names:

HTR4 GENE_SYMBOL

5-hydroxytryptamine receptor 4 UNIPROT

Serotonin receptor 4 UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000164270
- Version: 31-May-2017
Alternate Names:

ENSG00000164270 Gene Symbol

HTR4 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
dGene: HTR4
- Version: 27-Jun-2013
Alternate Names:

3360 Gene ID

5-HT4 dGene Synonym

5-HT4R dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TTD: 5-HT 4 receptor
- Version: 2020.06.01
Alternate Names:

HTR4 TTD Gene Abbreviation

T59679 TTD Target ID

Gene Info:

Publications:

Mechanism of Interaction	Serotonin 4 (5-HT4) receptor agonist
Direct Interaction	yes

Direct Interaction	yes
Mechanism of Interaction	Serotonin 4 (5-HT4) receptor partial agonist

ENSG00000164270	Ensembl Gene Id
5-HYDROXYTRYPTAMINE 4 RECEPTOR (5-HT-4) (SEROTONIN RECEPTOR 4) (5- HT4). [SOURCE:UNIPROT/SWISSPROT;ACC:Q13639]	Description
HTR4	Display Id

5-HYDROXYTRYPTAMINE RECEPTOR 4	Uniprot Protein Name
5HT4R_HUMAN	Uniprot Id
Q13639	Uniprot Accession

HTR4	GENE_SYMBOL
5-hydroxytryptamine receptor 4	UNIPROT
Serotonin receptor 4	UNIPROT

HTR4 Gene Record

HTR4 3360 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: partial agonist (activating) agonist (activating) antagonist (inhibitory)

Interaction Info:

PMIDs: 11207504 15645012 15466450 12150698 11752352 11876686

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 15902472 16495076

Sources: TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 8321323 7952869 7557734 1555639 12519861 11034583 10027842 10556228 10328995 11752352 11218067

Sources: NCI TEND TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18271554

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20812727

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist Direct Interaction yes

PMIDs: 11438309

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist Direct Interaction yes

PMIDs: 17187586

Sources: ChemblInteractions

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: partial agonist (activating) agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Serotonin 4 (5-HT4) receptor partial agonist

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 1364818

Sources: TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist Direct Interaction yes

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

antagonist (inhibitory)

PMIDs:
11207504 15645012 15466450 12150698 11752352 11876686

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
15902472 16495076

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

PMIDs:
8321323 7952869 7557734 1555639 12519861 11034583 10027842 10556228 10328995 11752352 11218067

Sources:
NCI TEND TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

n/a

PMIDs:
18271554

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20812727

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

Direct Interaction yes

PMIDs:
11438309

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

Direct Interaction yes

PMIDs:
17187586

Sources:
ChemblInteractions

Interaction Types & Directionality:

agonist (activating)

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 4 (5-HT4) receptor partial agonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

PMIDs:
1364818

Sources:
TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
9826103

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
18033297

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
18033297

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TEND

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Serotonin 4 (5-HT4) receptor partial agonist

PMIDs:
None found

Sources:
ChemblInteractions