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CHRNA4 Gene Record

  • Summary
  • Interactions
  • Claims
  • CHRNA4 1137 Druggable Genome

    Alternate Names:

    1137
    CHOLINERGIC RECEPTOR NICOTINIC ALPHA 4 SUBUNIT
    CHRNA4
    BFNC
    EBN
    EBN1
    NACHR
    NACHRA4
    NACRA4
    118504
    1958
    ENSG00000101204
    OTTHUMG00000033080
    P43681
    ACHA4_HUMAN
    NICOTINIC ACETYLCHOLINE RECEPTOR
    NEURONAL ACETYLCHOLINE RECEPTOR SUBUNIT ALPHA-4
    NEURONAL ACETYLCHOLINE RECEPTOR PROTEIN, ALPHA-4 SUBUNIT PRECURSOR. [SOURCE:UNIPROT/SWISSPROT;ACC:P43681]
    PA26490
    T78111
    Neuronal acetylcholine receptor alpha-4
    T70967

    Gene Info:

    Target Class Receptors
    Target Subclass TC:1.A.9
    Uniprot Status Swiss-Prot
    Interpro Type Domain
    Interpro Name Neurotransmitter-gated ion-channel ligand-binding
    Human Readable Name DRUGGABLE GENOME
    Interpro Short Name Neur_chan_lig-bd
    Interpro Name Neurotransmitter-gated ion-channel
    Interpro Type Family
    Uniprot Evidence 1: Evidence at protein level
    Interpro Acc IPR006202
    Interpro Short Name Neur_channel
    Human Readable Name ION CHANNEL
    Interpro Acc IPR006201
    Transmembrane Helix Count 4
    Target Subclass Ligand_gated_ion_channels
    Target Subclass Channels
    Target Subclass cys-loop
    Target Main Class Receptors
    Gene Biotype PROTEIN_CODING
    (9 More Sources)

    Gene Categories: Category Details

    DNA REPAIR
    ION CHANNEL
    EXTERNAL SIDE OF PLASMA MEMBRANE
    DRUGGABLE GENOME

    Publications:

    Arias et al., 2005, Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors., Curr. Protein Pept. Sci.
    Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.
    Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.
    Klaassen et al., 2006, Seizures and enhanced cortical GABAergic inhibition in two mouse models of human autosomal dominant nocturnal frontal lobe epilepsy., Proc. Natl. Acad. Sci. U.S.A.
    Ehringer et al., 2007, Association of the neuronal nicotinic receptor beta2 subunit gene (CHRNB2) with subjective responses to alcohol and nicotine., Am. J. Med. Genet. B Neuropsychiatr. Genet.
    Mansvelder et al., 2009, Nicotinic modulation of synaptic transmission and plasticity in cortico-limbic circuits., Semin. Cell Dev. Biol.
    Zaniewska et al., Nicotine dependence - human and animal studies, current pharmacotherapies and future perspectives., Pharmacol Rep
    Espeseth et al., 2007, Nicotine receptor gene CHRNA4 modulates early event-related potentials in auditory and visual oddball target detection tasks., Neuroscience
    Winterer et al., 2007, Association of attentional network function with exon 5 variations of the CHRNA4 gene., Hum. Mol. Genet.
    Narahashi et al., 2000, Symposium overview: mechanism of action of nicotine on neuronal acetylcholine receptors, from molecule to behavior., Toxicol. Sci.
    De Luca et al., 2006, Genetic interaction between alpha4 and beta2 subunits of high affinity nicotinic receptor: analysis in schizophrenia., Exp Brain Res
    Jackson et al., 2010, Role of alpha5 nicotinic acetylcholine receptors in pharmacological and behavioral effects of nicotine in mice., J. Pharmacol. Exp. Ther.
    Gu F et al., 2020, Association Between Nicotine-dependent Gene Polymorphism and Smoking Cessation in Patients With Lung Cancer., Clin Lung Cancer
    Chu CJ et al., 2011, Association of nicotinic acetylcholine receptor subunit alpha-4 polymorphisms with smoking behaviors in Chinese male smokers., Chin Med J (Engl)
    Hoft NR et al., 2011, CHRNB2 promoter region: association with subjective effects to nicotine and gene expression differences., Genes Brain Behav
    Breitling LP et al., 2009, Association of nicotinic acetylcholine receptor subunit alpha 4 polymorphisms with nicotine dependence in 5500 Germans., Pharmacogenomics J
    Li MD et al., 2005, Ethnic- and gender-specific association of the nicotinic acetylcholine receptor alpha4 subunit gene (CHRNA4) with nicotine dependence., Hum Mol Genet
    Matera C et al., 2015, Bifunctional compounds targeting both D2 and non-α7 nACh receptors: design, synthesis and pharmacological characterization., Eur J Med Chem
    Rollema et al., 2007, Rationale, pharmacology and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessation., Trends Pharmacol. Sci.
    Steensland et al., 2007, Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, selectively decreases ethanol consumption and seeking., Proc. Natl. Acad. Sci. U.S.A.
    McColl et al., 2008, Human abuse liability of the smoking cessation drug varenicline in smokers and nonsmokers., Clin. Pharmacol. Ther.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Nakamura et al., 2007, Efficacy and tolerability of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, in a 12-week, randomized, placebo-controlled, dose-response study with 40-week follow-up for smoking cessation in Japanese smokers., Clin Ther
    Rocha Santos J et al., 2015, CHRNA4 rs1044396 is associated with smoking cessation in varenicline therapy., Front Genet
    Walker et al., 2014, Cytisine versus nicotine for smoking cessation., N. Engl. J. Med.
    Houlihan et al., 2001, Activity of cytisine and its brominated isosteres on recombinant human alpha7, alpha4beta2 and alpha4beta4 nicotinic acetylcholine receptors., J. Neurochem.
    Eaton JB et al., 2003, Characterization of human alpha 4 beta 2-nicotinic acetylcholine receptors stably and heterologously expressed in native nicotinic receptor-null SH-EP1 human epithelial cells., Mol Pharmacol
    Kim SA et al., 2004, Association of polymorphisms in nicotinic acetylcholine receptor alpha 4 subunit gene (CHRNA4), mu-opioid receptor gene (OPRM1), and ethanol-metabolizing enzyme genes with alcoholism in Korean patients., Alcohol
    Dopico et al., 2009, Acute alcohol action and desensitization of ligand-gated ion channels., Pharmacol. Rev.
    Hendrickson et al., 2013, Neuronal nicotinic acetylcholine receptors: common molecular substrates of nicotine and alcohol dependence., Front Psychiatry
  • VARENICLINE   CHRNA4

    Interaction Score: 2.09

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

    Interaction Info:
    Trial Name varenicline, CP-526
    Novel drug target Established target

    PMIDs:
    17573127 17626178 18288085 11752352 17692720 25774163


    Sources:
    TdgClinicalTrial TEND PharmGKB

  • ISPRONICLINE   CHRNA4

    Interaction Score: 1.63

    Interaction Types & Directionality:
    partial agonist (activating)

    Interaction Info:
    Novel drug target Established target
    Trial Name TC-1734, AZD-3480, ispronicline
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 partial agonist

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • CHEMBL59986   CHRNA4

    Interaction Score: 1.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • DEXMECAMYLAMINE   CHRNA4

    Interaction Score: 1.63

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name TC-5214
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 antagonist

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • CYTISINICLINE   CHRNA4

    Interaction Score: 0.98

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    25517706 11553677


    Sources:
    TTD

  • TRIMETHAPHAN   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • TEBANICLINE   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • HEXOBARBITAL   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    16248797 11264449 10487207


    Sources:
    TdgClinicalTrial TEND

  • PANCURONIUM   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • AZD1446   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CP-601927   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    partial agonist (activating)

    Interaction Info:
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 partial agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PENTOLINIUM   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • VARENICLINE TARTRATE   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ABT-560   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    modulator

    Interaction Info:
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 modulator
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • POZANICLINE   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    partial agonist (activating)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Nicotinic acetylcholine receptor alpha4/beta2/alpha5 partial agonist
    Trial Name pozanicline , ABT-089

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • NICOTINE POLACRILEX   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TC-2216   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 antagonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • ATRACURIUM   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • SECOBARBITAL   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    16248797 11264449 10487207


    Sources:
    TdgClinicalTrial TEND

  • ALTINICLINE   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • SOFINICLINE   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BUTETHAL   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    16248797 11264449 10487207


    Sources:
    TdgClinicalTrial TEND

  • TC-6499   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name TC-6499
    Novel drug target Established target
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • BUTABARBITAL   CHRNA4

    Interaction Score: 0.81

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    16248797 11264449 10487207


    Sources:
    TdgClinicalTrial TEND

  • THIOPENTAL   CHRNA4

    Interaction Score: 0.74

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    16248797 11264449 10487207


    Sources:
    TdgClinicalTrial TEND

  • NICOTINE   CHRNA4

    Interaction Score: 0.71

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Mechanism of Interaction Neuronal acetylcholine receptor; alpha4/beta2 agonist
    Direct Interaction yes
    Trial Name -

    PMIDs:
    17146052 17226798 19560048 20081230 17590520 17613539 11006350 16636791 20400469 31402126 21740768 20854418 19290018 15790597 26164842


    Sources:
    DTC TdgClinicalTrial ChemblInteractions TEND PharmGKB TTD

  • MEPHOBARBITAL   CHRNA4

    Interaction Score: 0.68

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    16248797 11264449 10487207


    Sources:
    TdgClinicalTrial TEND

  • DEXEFAROXAN   CHRNA4

    Interaction Score: 0.54

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • MECAMYLAMINE   CHRNA4

    Interaction Score: 0.54

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:

    PMIDs:
    14645658


    Sources:
    TTD

  • PENTOBARBITAL   CHRNA4

    Interaction Score: 0.41

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    16248797 11264449 10487207


    Sources:
    TdgClinicalTrial TEND

  • TALBUTAL   CHRNA4

    Interaction Score: 0.41

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    16248797 11264449 10487207


    Sources:
    TdgClinicalTrial TEND

  • METHARBITAL   CHRNA4

    Interaction Score: 0.41

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    16248797 11264449 10487207


    Sources:
    TdgClinicalTrial TEND

  • BUTALBITAL   CHRNA4

    Interaction Score: 0.41

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    16248797 11264449 10487207


    Sources:
    TdgClinicalTrial TEND

  • PRIMIDONE   CHRNA4

    Interaction Score: 0.26

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    16248797 11264449 10487207


    Sources:
    TdgClinicalTrial TEND

  • ASM-024   CHRNA4

    Interaction Score: 0.23

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • PHENOBARBITAL   CHRNA4

    Interaction Score: 0.22

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    16248797 11264449 10487207


    Sources:
    TdgClinicalTrial TEND

  • COTININE   CHRNA4

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ALCOHOL   CHRNA4

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15902904 19270242 23641218


    Sources:
    PharmGKB

  • Ensembl: ENSG00000101204

    • Version: 101_38

    Alternate Names:
    CHRNA4 Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • TdgClinicalTrial: P43681

    • Version: January-2014

    Alternate Names:
    CHRNA4 Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass TC:1.A.9

    Publications:

  • RussLampel: ENSG00000101204

    • Version: 26-July-2011

    Alternate Names:
    ENSG00000101204 Ensembl Gene Id
    CHRNA4 Display Id
    NEURONAL ACETYLCHOLINE RECEPTOR PROTEIN, ALPHA-4 SUBUNIT PRECURSOR. [SOURCE:UNIPROT/SWISSPROT;ACC:P43681] Description

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • HopkinsGroom: P43681

    • Version: 11-September-2012

    Alternate Names:
    ACHA4_HUMAN Uniprot Id
    CHRNA4 Uniprot Gene Name
    ENSG00000101204 Ensembl Gene Id

    Gene Info:
    Uniprot Status Swiss-Prot
    Interpro Type Domain
    Interpro Name Neurotransmitter-gated ion-channel ligand-binding

    Gene Categories:
    ION CHANNEL, DRUGGABLE GENOME

    Publications:

  • TEND: P43681

    • Version: 01-August-2011

    Alternate Names:
    ACHA4_HUMAN Uniprot Id
    ENSG00000101204 Ensembl Gene Id
    1137 Entrez Gene Id

    Gene Info:
    Transmembrane Helix Count 4
    Target Subclass Ligand_gated_ion_channels
    Target Subclass Channels

    Publications:

  • PharmGKB: CHRNA4

    • Version: 18-August-2020

    Alternate Names:
    PA26490 PharmGKB ID

    Gene Info:

    Publications:
    Rocha Santos J et al., 2015, CHRNA4 rs1044396 is associated with smoking cessation in varenicline therapy., Front Genet
    Breitling LP et al., 2009, Association of nicotinic acetylcholine receptor subunit alpha 4 polymorphisms with nicotine dependence in 5500 Germans., Pharmacogenomics J
    Hoft NR et al., 2011, CHRNB2 promoter region: association with subjective effects to nicotine and gene expression differences., Genes Brain Behav

  • TTD: Nicotinic acetylcholine receptor

    • Version: 2020.06.01

    Alternate Names:
    nAChR TTD Gene Abbreviation
    T78111 TTD Target ID

    Gene Info:

    Publications:
    Sunaga H et al., 2010, Gantacurium and CW002 do not potentiate muscarinic receptor-mediated airway smooth muscle constriction in guinea pigs., Anesthesiology
    Casella G et al., 2010, Therapeutic advances in the treatment of nicotine addiction: present and future., Ther Adv Chronic Dis

  • DTC: CHRNA4

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Matera C et al., 2015, Bifunctional compounds targeting both D2 and non-α7 nACh receptors: design, synthesis and pharmacological characterization., Eur J Med Chem

  • HingoraniCasas: ENSG00000101204

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000101204 Gene Symbol
    CHRNA4 Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • ChemblInteractions: NACRA4

    • Version: chembl_23

    Alternate Names:
    NACRA4 GENE_SYMBOL
    CHRNA4 GENE_SYMBOL
    Neuronal acetylcholine receptor subunit alpha-4 UNIPROT

    Gene Info:

    Publications:

  • GO: CHRNA4

    • Version: 01-February-2022

    Alternate Names:
    NACRA4 GO Gene Synonym

    Gene Info:

    Gene Categories:
    DNA REPAIR, EXTERNAL SIDE OF PLASMA MEMBRANE

    Publications:

  • TTD: Neuronal acetylcholine receptor alpha-4

    • Version: 2020.06.01

    Alternate Names:
    CHRNA4 TTD Gene Abbreviation
    T70967 TTD Target ID

    Gene Info:

    Publications:

  • Pharos: CHRNA4

    • Version: 01-February-2022

    Alternate Names:
    Neuronal acetylcholine receptor subunit alpha-4 Gene Name
    P43681 UniProt ID

    Gene Info:

    Gene Categories:
    ION CHANNEL

    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