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HTR4 Gene Record

  • Summary
  • Interactions
  • Claims
  • 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
    BE0000084
    5-HT<sub>4</sub> receptor
    5-HT 4 receptor
    T59679
    9
    NM_000870
    NP_000861

    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
    GuideToPharmacology Gene Category Name 5-Hydroxytryptamine receptors
    GuideToPharmacology Gene Category ID 1
    (9 More Sources)

    Gene Categories: Category Details

    G PROTEIN COUPLED RECEPTOR
    DRUGGABLE GENOME

    Publications:

    Bharucha et al., 2000, Effects of a serotonin 5-HT(4) receptor antagonist SB-207266 on gastrointestinal motor and sensory function in humans., Gut
    Meulemans et al., 1992, Is the action of cisapride on the guinea-pig ileum mediated via 5-HT4 receptors?, Eur. J. Pharmacol.
    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.
    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.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    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.
    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.
    Katayama et al., 1995, [Cisapride, a gastroprokinetic agent, binds to 5-HT4 receptors]., Nippon Yakurigaku Zasshi
    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.
    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
    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.
    Corsetti et al., 2002, Tegaserod: a new 5-HT(4) agonist in the treatment of irritable bowel syndrome., Expert Opin Pharmacother
    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.
    Camilleri, 2001, Review article: tegaserod., Aliment. Pharmacol. Ther.
    Kamm, 2002, Review article: the complexity of drug development for irritable bowel syndrome., Aliment. Pharmacol. Ther.
    Cole et al., 2004, Tegaserod: a serotonin 5-HT4 receptor agonist for treatment of constipation-predominant irritable bowel syndrome., Drugs Today
    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
    van Wijngaarden et al., 1990, The concept of selectivity in 5-HT receptor research., Eur. J. 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.
    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.
    McCullough et al., 2006, The 5-HT2B antagonist and 5-HT4 agonist activities of tegaserod in the anaesthetized rat., Pharmacol. Res.
    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
    Guillemot et al., 2009, Metoclopramide stimulates catecholamine- and granin-derived peptide secretion from pheochromocytoma cells through activation of serotonin type 4 (5-HT4) receptors., Endocr. Relat. Cancer
    Bartolini A et al., 2011, Analgesic and antineuropathic drugs acting through central cholinergic mechanisms., Recent Pat CNS Drug Discov
    Lee A et al., 2010, Metoclopramide in the treatment of diabetic gastroparesis., Expert Rev Endocrinol Metab
    Alarcón de la Lastra et al., 1998, Effects of cinitapride on gastric ulceration and secretion in rats., Inflamm. Res.
    Alarcón-de-la-Lastra Romero et al., 1997, Cinitapride protects against ethanol-induced gastric mucosal injury in rats: role of 5-hydroxytryptamine, prostaglandins and sulfhydryl compounds., Pharmacology
  • CISAPRIDE   HTR4

    Interaction Score: 4.33

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Partial agonist
    Endogenous Drug? False
    Direct Interaction? True

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


    Sources:
    NCI TEND TTD DrugBank GuideToPharmacology

  • PIBOSEROD   HTR4

    Interaction Score: 4.06

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    16495076 15902472


    Sources:
    TTD DrugBank GuideToPharmacology

  • PF-04995274   HTR4

    Interaction Score: 3.25

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Details of the Assay for Interaction Measured at the 5-HT<sub>4d</sub> receptor.
    Specific Action of the Ligand Partial agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology

  • REVEXEPRIDE   HTR4

    Interaction Score: 3.25

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • PRUCALOPRIDE   HTR4

    Interaction Score: 3.25

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Partial agonist
    Endogenous Drug? False
    Mechanism of Interaction Serotonin 4 (5-HT4) receptor agonist

    PMIDs:
    11438309


    Sources:
    DrugBank GuideToPharmacology ChemblInteractions

  • VELUSETRAG   HTR4

    Interaction Score: 3.25

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Direct Interaction? True
    Endogenous Drug? False
    Specific Action of the Ligand Agonist

    PMIDs:
    None found


    Sources:
    TTD DrugBank GuideToPharmacology ChemblInteractions

  • TAK-954   HTR4

    Interaction Score: 3.25

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Agonist
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology

  • CHEMBL401607   HTR4

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18271554


    Sources:
    DTC

  • CHEMBL114112   HTR4

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20812727


    Sources:
    DTC

  • TEGASEROD   HTR4

    Interaction Score: 2.92

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

    Interaction Info:
    Specific Action of the Ligand Partial agonist
    Endogenous Drug? False

    PMIDs:
    12150698 15466450 11207504 11752352 11876686 15645012


    Sources:
    TTD DrugBank GuideToPharmacology

  • NARONAPRIDE   HTR4

    Interaction Score: 2.43

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    17187586


    Sources:
    DrugBank ChemblInteractions

  • SUVN-D4010   HTR4

    Interaction Score: 1.62

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • CINITAPRIDE   HTR4

    Interaction Score: 1.62

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    9562338 9211565


    Sources:
    DrugBank

  • MOSAPRIDE   HTR4

    Interaction Score: 1.62

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Full agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology

  • DA-6886   HTR4

    Interaction Score: 1.62

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ZACOPRIDE   HTR4

    Interaction Score: 1.62

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Full agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CISAPRIDE   HTR4

    Interaction Score: 1.62

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RENZAPRIDE   HTR4

    Interaction Score: 1.3

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Full agonist
    Endogenous Drug? False

    PMIDs:
    1364818


    Sources:
    TTD DrugBank GuideToPharmacology

  • TICALOPRIDE   HTR4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • LINTOPRIDE   HTR4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • METOCLOPRAMIDE HYDROCHLORIDE   HTR4

    Interaction Score: 0.54

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RELENOPRIDE   HTR4

    Interaction Score: 0.54

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Partial agonist
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • TROPISETRON   HTR4

    Interaction Score: 0.49

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    9826103


    Sources:
    NCI GuideToPharmacology

  • METOCLOPRAMIDE   HTR4

    Interaction Score: 0.46

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    18948374 21585331 21278804


    Sources:
    DrugBank

  • CAPESEROD   HTR4

    Interaction Score: 0.36

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

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Serotonin 4 (5-HT4) receptor partial agonist
    Specific Action of the Ligand Partial agonist

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • TEGASEROD MALEATE   HTR4

    Interaction Score: 0.27

    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

  • ONDANSETRON   HTR4

    Interaction Score: 0.25

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    2164935


    Sources:
    DrugBank

  • VILAZODONE   HTR4

    Interaction Score: 0.23

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Agonist
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • ZOLMITRIPTAN   HTR4

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TEND

  • METITEPINE   HTR4

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18033297


    Sources:
    DTC

  • MIANSERIN   HTR4

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18033297


    Sources:
    DTC

  • FLUOXETINE   HTR4

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9228186


    Sources:
    NCI

  • ACETAMINOPHEN   HTR4

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    8699917


    Sources:
    NCI

  • SEROTONIN   HTR4

    Interaction Score: 0.07

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? True
    Specific Action of the Ligand Full agonist

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CISPLATIN   HTR4

    Interaction Score: 0.02

    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:

  • GuideToPharmacology: 3360

    • Version: 29-September-2020

    Alternate Names:
    5299 HUGO Gene ID
    5299 HUGO Gene Symbol
    5-hydroxytryptamine receptor 4 HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name 5-Hydroxytryptamine receptors
    GuideToPharmacology Gene Category ID 1

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR

    Publications:

  • DrugBank: BE0000084

    • Version: 5.1.7

    Alternate Names:
    HTR4 DrugBank Gene Name
    Q13639 UniProt Accession
    3360 Entrez Gene Id

    Gene Info:

    Publications:
    Bharucha et al., 2000, Effects of a serotonin 5-HT(4) receptor antagonist SB-207266 on gastrointestinal motor and sensory function in humans., Gut
    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.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.

  • 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:

  • GO: HTR4

    • Version: 05-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21