Functional screening of α7 nicotinic receptor ligands.

Background: The α7 nicotinic acetylcholine receptor, a ligand-gated ion channel, is an attractive drug discovery target in schizophrenia and Alzheimer's disease. Objective: We have evaluated the various approaches to discovering ligands targeting the α7 nicotinic receptor to define the current paradigm driving drug discovery efforts in this area. Methods: Assays using functional read-outs as a consequence of α7 nicotinic receptor activation have been reviewed. Conclusion: Functional assays using fluorescence-based optical methods in combination with direct electrophysiological recordings of channel function currently provide an integrated approach to the discovery of α7 nicotinic receptor targeted ligands.