Recent developments in neuronal nicotinic acetylcholine receptor antagonists

Abstract

Neuronal nicotinic acetylcholine receptors (nAChRs) belong to a superfamily of ligand-gated ion channel receptors and are distributed extensively throughout the central and peripheral nervous systems. The structural and functional diversity of these receptors has stimulated interest in the development of subtype-selective agonists, as a result of a greater understanding of the role of these receptors in neuropathology and disease, including Alzheimer’s and Parkinson’s disease, Tourette’s syndrome, drug addiction and pain. Surprisingly, much less attention has been focused on the development of subtype-selective antagonists, which may also be useful as therapeutic agents. This article reviews the published patent literature on neuronal nicotinic receptor antagonists, with particular attention to receptor subtype selectivity of novel compounds that have been recently disclosed in the patent literature.