Background: The alpha7 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 alpha7 nicotinic receptor to define the current paradigm driving drug discovery efforts in this area. Methods: Assays using functional read-outs as a consequence of alpha7 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 alpha7 nicotinic receptor targeted ligands.
        
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Dunlop J, Peri R, Terstappen GC, Bowlby M (2008) Functional screening of alpha7 nicotinic receptor ligands Expert Opin Drug Discov3: 623-8
Dunlop J, Peri R, Terstappen GC, Bowlby M (2008) Expert Opin Drug Discov3: 623-8