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    Bioorg Med Chem Lett. 2007 Sep 1;17(17):4855-60. Epub 2007 Jun 14.

    Synthesis of desformylflustrabromine and its evaluation as an alpha4beta2 and alpha7 nACh receptor modulator.

    Kim JS, Padnya A, Weltzin M, Edmonds BW, Schulte MK, Glennon RA.

    Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA.

    Desformylflustrabromine (dFBr; 1) and desformylflustrabromine-B (dFBr-B; 2) have been previously isolated from natural sources, and the former has been demonstrated to be a novel and selective positive allosteric modulator of alpha4beta2 nicotinic acetylcholine (nACh) receptors. The present study describes the synthesis of water-soluble salts of 1 and 2, and confirms and further investigates the actions of 1 and 2 using two-electrode voltage clamp recordings.

    PMID: 17604168 [PubMed - indexed for MEDLINE]

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