Discovery of novel α7 nicotinic receptor antagonists

被引：19

作者：

Peng, Youyi ^{[1
]}

Zhang, Qiang ^{[1
]}

Snyder, Gretchen L. ^{[1
]}

Zhu, Hongwen ^{[1
]}

Yao, Wei ^{[1
]}

Tomesch, John ^{[1
]}

Papke, Roger L. ^{[2
]}

O'Callaghan, James P. ^{[3
]}

Welsh, William J. ^{[4
]}

Wennogle, Lawrence P. ^{[1
]}

机构：

[1] Intracellular Therapies Inc, New York, NY 10032 USA

[2] Univ Florida, Coll Med, Dept Pharmacol & Therapeut, Gainesville, FL 32610 USA

[3] NIOSH, Ctr Dis Control & Prevent, Morgantown, WV 26505 USA

[4] Univ Med & Dent New Jersey, Robert Wood Johnson Med Sch, Dept Pharmacol, Piscataway, NJ 08854 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 16期

关键词：

Nicotinic acetylcholine receptors; alpha; 7; antagonists; Pharmacophore; Neuroprotection; ACETYLCHOLINE-RECEPTORS; DRUG DISCOVERY; RAT-BRAIN; BINDING; AGONIST; SCHIZOPHRENIA; MEMORY;

D O I：

10.1016/j.bmcl.2010.06.103

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two distinct families of small molecules were discovered as novel alpha 7 nicotinic acetylcholine receptor (nAChR) antagonists by pharmacophore-based virtual screening. These novel antagonists exhibited selectivity for the neuronal alpha 7 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. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：4825 / 4830

页数：6

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