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Research ArticleArticle

Specific Activation of the α7 Nicotinic Acetylcholine Receptor by a Quaternary Analog of Cocaine

Michael M. Francis, Elaine Y. Cheng, Gregory A. Weiland and Robert E. Oswald
Molecular Pharmacology July 2001, 60 (1) 71-79; DOI: https://doi.org/10.1124/mol.60.1.71
Michael M. Francis
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Elaine Y. Cheng
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Gregory A. Weiland
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Robert E. Oswald
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Abstract

Effects of cocaine and cocaine methiodide were evaluated on the homomeric α7 neuronal nicotinic receptor (nAChR). Whereas cocaine itself is a general nAChR noncompetitive antagonist, we report here the characterization of cocaine methiodide, a novel selective agonist for the α7 subtype of nAChR. Data from125I-α-bungarotoxin binding assays indicate that cocaine methiodide binds to α7 nAChR with aK i value of approximately 200 nM while electrophysiology studies indicate that the addition of a methyl group at the amine moiety of cocaine changes the drug's activity profile from inhibitor to agonist. Cocaine methiodide activates α7 nAChR with an EC50 value of approximately 50 μM and shows comparable efficacy to ACh in oocyte experiments. While agonist effects are specific for the α7 neuronal nAChR and are not observed with heteromeric neuronal or skeletal muscle nAChR, antagonist effects are present for heteromeric nAChR combinations. Studies of PC12 cells transiently transfected with human α7 cDNA and expressing a variety of functional nicotinic receptor subtypes confirm the specificity of cocaine methiodide agonist effects. Our results indicate that a quaternary structural derivative of cocaine can be used as a specific agonist for the α7 subtype of neuronal nicotinic receptor.

  • Abbreviations

    nAChR
    nicotinic acetylcholine receptor
    FBS
    fetal bovine serum
    GFP
    green fluorescent protein
    MLA
    methyllycaconitine
    HEK
    human embryonic kidney
    DMEM
    Dulbecco's modified Eagle's medium
    • Received January 31, 2001.
    • Accepted March 12, 2001.
    • The American Society for Pharmacology and Experimental Therapeutics
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    Molecular Pharmacology: 60 (1)
    Molecular Pharmacology
    Vol. 60, Issue 1
    1 Jul 2001
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    Research ArticleArticle

    Specific Activation of the α7 Nicotinic Acetylcholine Receptor by a Quaternary Analog of Cocaine

    Michael M. Francis, Elaine Y. Cheng, Gregory A. Weiland and Robert E. Oswald
    Molecular Pharmacology July 1, 2001, 60 (1) 71-79; DOI: https://doi.org/10.1124/mol.60.1.71

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    Research ArticleArticle

    Specific Activation of the α7 Nicotinic Acetylcholine Receptor by a Quaternary Analog of Cocaine

    Michael M. Francis, Elaine Y. Cheng, Gregory A. Weiland and Robert E. Oswald
    Molecular Pharmacology July 1, 2001, 60 (1) 71-79; DOI: https://doi.org/10.1124/mol.60.1.71
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