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Bioorg Med Chem Lett
2007 Sep 01;1717:4855-60. doi: 10.1016/j.bmcl.2007.06.047.
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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.
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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.
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