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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
    465
    nicotinic acetylcholine receptor α4 subunit
    NICOTINIC ACETYLCHOLINE RECEPTOR
    BE0000849
    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
    NM_000744
    NP_000735

    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
    GuideToPharmacology Gene Category Name Nicotinic acetylcholine receptors
    GuideToPharmacology Gene Category ID 76
    (11 More Sources)

    Gene Categories: Category Details

    DNA REPAIR
    ION CHANNEL
    EXTERNAL SIDE OF PLASMA MEMBRANE
    DRUGGABLE GENOME

    Publications:

    Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.
    Arias et al., 2005, Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors., Curr. Protein Pept. Sci.
    Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.
    Stauderman KA et al., 1998, Characterization of human recombinant neuronal nicotinic acetylcholine receptor subunit combinations alpha2beta4, alpha3beta4 and alpha4beta4 stably expressed in HEK293 cells., J Pharmacol Exp Ther
    Espeseth et al., 2007, Nicotine receptor gene CHRNA4 modulates early event-related potentials in auditory and visual oddball target detection tasks., Neuroscience
    De Luca et al., 2006, Genetic interaction between alpha4 and beta2 subunits of high affinity nicotinic receptor: analysis in schizophrenia., Exp Brain Res
    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
    Winterer et al., 2007, Association of attentional network function with exon 5 variations of the CHRNA4 gene., Hum. Mol. Genet.
    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
    Mansvelder et al., 2009, Nicotinic modulation of synaptic transmission and plasticity in cortico-limbic circuits., Semin. Cell Dev. Biol.
    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.
    Narahashi et al., 2000, Symposium overview: mechanism of action of nicotine on neuronal acetylcholine receptors, from molecule to behavior., Toxicol. 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.
    Matera C et al., 2015, Bifunctional compounds targeting both D2 and non-α7 nACh receptors: design, synthesis and pharmacological characterization., Eur J Med Chem
    Gu F et al., 2020, Association Between Nicotine-dependent Gene Polymorphism and Smoking Cessation in Patients With Lung Cancer., Clin Lung Cancer
    Jackson et al., 2010, Role of alpha5 nicotinic acetylcholine receptors in pharmacological and behavioral effects of nicotine in mice., J. Pharmacol. Exp. Ther.
    Zaniewska et al., Nicotine dependence - human and animal studies, current pharmacotherapies and future perspectives., Pharmacol Rep
    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)
    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
    Rollema et al., 2007, Rationale, pharmacology and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessation., Trends Pharmacol. Sci.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    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.
    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
    Hendrickson et al., 2013, Neuronal nicotinic acetylcholine receptors: common molecular substrates of nicotine and alcohol dependence., Front Psychiatry
    Dopico et al., 2009, Acute alcohol action and desensitization of ligand-gated ion channels., Pharmacol. Rev.
    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
    Damaj et al., 2005, Effect of dextrometorphan and dextrorphan on nicotine and neuronal nicotinic receptors: in vitro and in vivo selectivity., J. Pharmacol. Exp. Ther.
    Smulders CJ et al., 2005, Cholinergic drugs potentiate human nicotinic alpha4beta2 acetylcholine receptors by a competitive mechanism., Eur J Pharmacol
    Matsubayashi H et al., 1997, Amantadine inhibits nicotinic acetylcholine receptor function in hippocampal neurons., J Pharmacol Exp Ther
    Flood P et al., 2002, Isoflurane hyperalgesia is modulated by nicotinic inhibition., Anesthesiology
    Yamashita M et al., 2005, Isoflurane modulation of neuronal nicotinic acetylcholine receptors expressed in human embryonic kidney cells., Anesthesiology
    Brannigan G et al., 2010, Multiple binding sites for the general anesthetic isoflurane identified in the nicotinic acetylcholine receptor transmembrane domain., Proc Natl Acad Sci U S A
    Jin X et al., 2011, A portable site: a binding element for 17β-estradiol can be placed on any subunit of a nicotinic α4β2 receptor., J Neurosci
    Paradiso K et al., 2001, The C terminus of the human nicotinic alpha4beta2 receptor forms a binding site required for potentiation by an estrogenic steroid., J Neurosci
    Talka R et al., 2015, Methadone's effect on nAChRs--a link between methadone use and smoking?, Biochem Pharmacol
    Talka R et al., 2015, Methadone is a non-competitive antagonist at the α4β2 and α3* nicotinic acetylcholine receptors and an agonist at the α7 nicotinic acetylcholine receptor., Basic Clin Pharmacol Toxicol
    Ortells MO et al., 2002, Molecular modelling of the interactions of carbamazepine and a nicotinic receptor involved in the autosomal dominant nocturnal frontal lobe epilepsy., Br J Pharmacol
    Bertrand D, 2002, Neuronal Nicotinic Acetylcholine Receptors and Epilepsy., Epilepsy Curr
    Di Resta C et al., 2010, Effect of carbamazepine and oxcarbazepine on wild-type and mutant neuronal nicotinic acetylcholine receptors linked to nocturnal frontal lobe epilepsy., Eur J Pharmacol
  • VARENICLINE   CHRNA4

    Interaction Score: 1.37

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

    Interaction Info:
    Trial Name varenicline, CP-526
    Novel drug target Established target
    Details of the Assay for Interaction <i>In vitro</i> affinity for recombinant human &alpha;4&beta;2 receptors in membranes from transfected CHO-K1 cells, determined by displacement of [<sup>3</sup>H]-(−)-cytisine.

    PMIDs:
    17692720 25774163 17573127 11752352 17626178 18288085


    Sources:
    TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

  • ISPRONICLINE   CHRNA4

    Interaction Score: 1.0

    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: 1.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • DEXMECAMYLAMINE   CHRNA4

    Interaction Score: 1.0

    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

  • POZANICLINE   CHRNA4

    Interaction Score: 0.75

    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 DrugBank ChemblInteractions

  • HEXOBARBITAL   CHRNA4

    Interaction Score: 0.6

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11264449 16248797 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank

  • BUTETHAL   CHRNA4

    Interaction Score: 0.6

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11264449 16248797 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank

  • CYTISINICLINE   CHRNA4

    Interaction Score: 0.57

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    25517706 11553677


    Sources:
    TTD DrugBank

  • SECOBARBITAL   CHRNA4

    Interaction Score: 0.54

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    11264449 16248797 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank

  • TRIMETHAPHAN   CHRNA4

    Interaction Score: 0.5

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • TEBANICLINE   CHRNA4

    Interaction Score: 0.5

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • AZD1446   CHRNA4

    Interaction Score: 0.5

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • VARENICLINE TARTRATE   CHRNA4

    Interaction Score: 0.5

    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: 0.5

    Interaction Types & Directionality:
    modulator

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • NICOTINE POLACRILEX   CHRNA4

    Interaction Score: 0.5

    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: 0.5

    Interaction Types & Directionality:
    antagonist (inhibitory)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • THIOPENTAL   CHRNA4

    Interaction Score: 0.5

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11264449 16248797 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank

  • ALTINICLINE   CHRNA4

    Interaction Score: 0.5

    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: 0.5

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • TC-6499   CHRNA4

    Interaction Score: 0.5

    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

  • MEPHOBARBITAL   CHRNA4

    Interaction Score: 0.46

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11264449 16248797 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank

  • NICOTINE   CHRNA4

    Interaction Score: 0.42

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Details of the Assay for Interaction <i>In vitro</i> affinity for recombinant human &alpha;4&beta;2 receptors in membranes from transfected CHO-K1 cells, determined by displacement of [<sup>3</sup>H]-(−)-cytisine.
    Specific Action of the Ligand Agonist
    Details of Interaction &alpha;4&beta;2

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


    Sources:
    TEND DTC PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

  • AMOBARBITAL   CHRNA4

    Interaction Score: 0.4

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    11264449 16248797 10487207


    Sources:
    DrugBank

  • BARBITAL   CHRNA4

    Interaction Score: 0.4

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    11264449 16248797 10487207


    Sources:
    DrugBank

  • HEPTABARBITAL   CHRNA4

    Interaction Score: 0.4

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    11264449 16248797 10487207


    Sources:
    DrugBank

  • ATRACURIUM   CHRNA4

    Interaction Score: 0.4

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Antagonism of ACh activation of human &alpha;4&beta;2 nACh receptors expressed in <i>Xenopus</i> oocytes, at different ACh concentrations.
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology

  • APROBARBITAL   CHRNA4

    Interaction Score: 0.4

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    11264449 16248797 10487207


    Sources:
    DrugBank

  • MECAMYLAMINE   CHRNA4

    Interaction Score: 0.36

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Specific Action of the Ligand None
    Details of Interaction &alpha;4&beta;4
    Endogenous Drug? False

    PMIDs:
    14645658


    Sources:
    TTD DrugBank GuideToPharmacology

  • PHYSOSTIGMINE   CHRNA4

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14645658


    Sources:
    DrugBank

  • DECAMETHONIUM   CHRNA4

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14645658


    Sources:
    DrugBank

  • CP-601927   CHRNA4

    Interaction Score: 0.33

    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

  • DEXEFAROXAN   CHRNA4

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • CHEMBL490153   CHRNA4

    Interaction Score: 0.33

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Specific Action of the Ligand None
    Details of Interaction &alpha;4&beta;2
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • RIVANICLINE   CHRNA4

    Interaction Score: 0.33

    Interaction Types & Directionality:
    agonist (activating)

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

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • TALBUTAL   CHRNA4

    Interaction Score: 0.3

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11264449 16248797 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank

  • METHARBITAL   CHRNA4

    Interaction Score: 0.3

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -

    PMIDs:
    11264449 16248797 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank

  • BUTALBITAL   CHRNA4

    Interaction Score: 0.3

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11264449 16248797 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank

  • EPIBATIDINE   CHRNA4

    Interaction Score: 0.28

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    9454827


    Sources:
    DrugBank

  • BUTABARBITAL   CHRNA4

    Interaction Score: 0.28

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11264449 16248797 10487207


    Sources:
    TEND TdgClinicalTrial

  • PENTOBARBITAL   CHRNA4

    Interaction Score: 0.27

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11264449 16248797 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank

  • SCOPOLAMINE   CHRNA4

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15733544


    Sources:
    DrugBank

  • HEXAMETHONIUM   CHRNA4

    Interaction Score: 0.25

    Interaction Types & Directionality:
    blocker (inhibitory)

    Interaction Info:
    Specific Action of the Ligand None
    Details of Interaction &alpha;4&beta;2
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PENTOLINIUM   CHRNA4

    Interaction Score: 0.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • AMANTADINE   CHRNA4

    Interaction Score: 0.2

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    9152392


    Sources:
    DrugBank

  • PANCURONIUM   CHRNA4

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • PRIMIDONE   CHRNA4

    Interaction Score: 0.19

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11264449 16248797 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank

  • PHENOBARBITAL   CHRNA4

    Interaction Score: 0.16

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    11264449 16248797 10487207


    Sources:
    TEND TdgClinicalTrial DrugBank

  • ESTRADIOL BENZOATE   CHRNA4

    Interaction Score: 0.15

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11517245


    Sources:
    DrugBank

  • ASM-024   CHRNA4

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ATROPINE   CHRNA4

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15733544


    Sources:
    DrugBank

  • ISOFLURANE   CHRNA4

    Interaction Score: 0.12

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    12131122 15618790 20660787


    Sources:
    DrugBank

  • DEXTROMETHORPHAN   CHRNA4

    Interaction Score: 0.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    15356218


    Sources:
    DrugBank

  • COTININE   CHRNA4

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • METHADONE   CHRNA4

    Interaction Score: 0.09

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    26231941 25196810


    Sources:
    DrugBank

  • ESTRADIOL   CHRNA4

    Interaction Score: 0.09

    Interaction Types & Directionality:
    binder

    Interaction Info:

    PMIDs:
    21451042 11517245


    Sources:
    DrugBank

  • CARBAMAZEPINE   CHRNA4

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12110613 15309115 20561518


    Sources:
    DrugBank

  • ALCOHOL   CHRNA4

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23641218 19270242 15902904


    Sources:
    PharmGKB DrugBank

  • 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:

  • GuideToPharmacology: 1137

    • Version: 29-September-2020

    Alternate Names:
    1958 HUGO Gene ID
    1958 HUGO Gene Symbol
    cholinergic receptor nicotinic alpha 4 subunit HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name Nicotinic acetylcholine receptors
    GuideToPharmacology Gene Category ID 76

    Gene Categories:
    ION CHANNEL

    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

  • DrugBank: BE0000849

    • Version: 5.1.7

    Alternate Names:
    CHRNA4 DrugBank Gene Name
    P43681 UniProt Accession
    1137 Entrez Gene Id

    Gene Info:

    Publications:
    Espeseth et al., 2007, Nicotine receptor gene CHRNA4 modulates early event-related potentials in auditory and visual oddball target detection tasks., Neuroscience
    De Luca et al., 2006, Genetic interaction between alpha4 and beta2 subunits of high affinity nicotinic receptor: analysis in schizophrenia., Exp Brain Res
    Winterer et al., 2007, Association of attentional network function with exon 5 variations of the CHRNA4 gene., Hum. Mol. Genet.

  • 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:

  • Pharos: CHRNA4

    • Version: 03-September-2020

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

    Gene Info:

    Gene Categories:
    ION CHANNEL

    Publications:

  • GO: CHRNA4

    • Version: 05-September-2020

    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:

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