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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Functional screening of α7 nicotinic receptor ligands
John Dunlop1, Ravikumar Peri, Georg C Terstappen
1Neuroscience Discovery Research, Wyeth Research, CN-8000, Princeton, NJ 08543, USA +1 732 274 4193 ; +1 732 274 4755 ; Dunlopj@wyeth.com.
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.
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