Recent developments in neuronal nicotinic acetylcholine receptor antagonists

Neuronal nicotinic acetylcholine receptors (nAChRs) belong to a superfamily of ligand-gated ion channel receptors and are distributed extensively thro ughout the central and peripheral nervous systems. The structural and funct ional diversity of these receptors has stimulated interest in the developme nt of subtype-selective agonists, as a result of a greater understanding of the role of these receptors in neuropathology and disease, including Alzhe imer's and Parkinson's disease, Tourette's syndrome, drug addiction and pai n. Surprisingly, much less attention has been focused on the development of subtype-selective antagonists, which may also be useful as therapeutic age nts. This article reviews the published patent literature on neuronal nicot inic receptor antagonists, with particular attention to receptor subtype se lectivity of novel compounds that have been recently disclosed in the paten t literature.