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Nicotinic acetylcholine receptor ligands as potential therapeutics

The nicotinic acetylcholine receptors (nAChRs) belong to a superfamily of ligand-gated ion channels. Neuronal nAChRs are involved in a variety of complex cognitive processes (learning and memory) and therefore in CNS disorders. These include, for example, Alzheimer’s and Parkinson’s disease, attention deficit hyperactivity disorder, Tourette’s syndrome, schizophrenia, depression, pain and tobacco dependence. Thus, nAChRs present a rational target for the treatment of these pathological processes. Over the past years an increasing number of ligands, especially for the α4β2 subtype has been synthesised. Recent developments reveal increased interest in α7 ligands for the treatment of CNS diseases as well as for pain and inflammation. Unfortunately, only a few companies provide biological data in detail, especially regarding subtype selectivity and functionality. This review provides an overview of the recent patent literature focusing mainly on small molecule ligands.