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.