Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.

ID: ALA1147511

Journal: Bioorg Med Chem Lett

Title: Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.

Authors: Wei ZL, Xiao Y, Kellar KJ, Kozikowski AP.

Abstract: A series of bivalent ligands 6a-d of epibatidine were synthesized. All four ligands showed nanomolar binding affinities at six neuronal nicotinic acetylcholine receptor (nAChR) subtypes in competition binding assays. In contrast to epibatidine, these bivalent ligands are weak partial agonists at the alpha3beta4 nAChR as shown by functional assays.

CiteXplore: 15050615

DOI: 10.1016/j.bmcl.2003.10.071

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