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Discovery of novel alpha7 nicotinic receptor antagonists.
Bioorganic & medicinal chemistry letters 2010 Jun 25; In press
Peng Y, Zhang Q, Snyder G GL, Zhu H, Yao W, Tomesch J, Papke R RL, O'callaghan J JP, Welsh W WJ, Wennogle L LP
Intra-Cellular Therapies, Inc., New York, NY, 10032, United States.
Two distinct families of small molecules were discovered as novel alpha7 nicotinic acetylcholine receptor (nAChR) antagonists by pharmacophore-based virtual screening. These novel antagonists exhibited selectivity for the neuronal alpha7 subtype over other nAChRs and good brain penetration. Neuroprotection was demonstrated by representative compounds 7i and 8 in a mouse seizure-like behavior model induced by the nerve agent diisopropylfluorophosphate (DFP). These novel nAChR antagonists have potential use as antidote for organophosphorus nerve agent intoxication.
Keywords: nicotinic