Introduction: Nicotinic acetylcholine receptors (nAChRs), pentameric ligand-gated cation channels, are potential targets for the development of therapeutics for a variety of disease states.
Areas covered: This article is reviewing recent advances in the development of small-molecule ligands for diverse nAChR subtypes and is a continuation of an earlier review in this journal.
Expert opinion: The development of nAChR ligands with preference for α4β2 or α7 subtypes for the treatment of central nervous system disorders are in the most advanced developmental stage. In addition, there is a fast growing interest to generate so-called PAMs, positive allosteric modulators, to influence the channels' functionalities.