Nicotinic acetylcholine receptors: an overview on drug discovery.

BACKGROUND: Nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels that participate in many physiological functions. Receptors result from the assembly of five homologous or heterologous subunits that form the ligand-binding site and an ionic pore. In vertebrates, 17 subunits have been identified, alpha (1 - 10), beta (1 - 4), gamma, delta and epsilon. Assembly of different subunit combinations allows a diversity of physiological and pharmacological properties.

OBJECTIVE: To review the putative involvement of nAChRs in several diseases.

METHODS: We discuss the expression pattern of the subunits, the pharmacological tools for distinguishing them and their role in pathogenesis.

RESULTS/CONCLUSION: Long-standing efforts in this field should soon result in the finding of new molecules that might be applicable to situations ranging from neurological diseases to immune treatments.