摘要

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 alpha 4b2 or alpha 7 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.

  • 出版日期2011-12