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Discovery of novel alpha7 nicotinic receptor antagonists.

Authors
Peng-Y; Zhang-Q; Snyder-GL; Zhu-H; Yao-W; Tomesch-J; Papke-RL; O'Callaghan-JP; Welsh-WJ; Wennogle-LP
Source
Bioorg Med Chem Lett 2010 Aug; 20(16):4825-4830
NIOSHTIC No.
20037273
Abstract
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
Molecular-biology; Molecular-structure; Nerves; Neuropharmacology; Organo-phosphorus-compounds; Biological-warfare-agents; Intoxicants; Alpha-particles; Brain-function; Neurological-reactions; Author Keywords: Nicotinic; acetylcholine receptors; alpha7 antagonists; Pharmacophore; Neuroprotection
Contact
L.P. Wennogle, Intra-Cellular Therapies, Inc., New York, NY, 10032
CODEN
BMCLE8
Publication Date
20100815
Document Type
Journal Article
Email Address
wennogle@intracellulartherapies.com
Fiscal Year
2010
NTIS Accession No.
NTIS Price
Issue of Publication
16
ISSN
0960-894X
NIOSH Division
HELD
Priority Area
Manufacturing
Source Name
Bioorganic & Medicinal Chemistry Letters
State
NY; FL; WV; NJ
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