New 5-HT1A receptor agonists possessing 1,4-benzoxazepine scaffold exhibit highly potent anti-ischemic effects.
作者信息
Kamei K, Maeda N, Ogino R, Koyama M, Nakajima M, Tatsuoka T, Ohno T, Inoue T
机构信息
Suntory Biomedical Research Limited, Osaka, Japan.
出版信息
Bioorg Med Chem Lett. 2001 Feb 26;11(4):595-8. doi: 10.1016/s0960-894x(01)00008-7.
Abstract
A series of new 3-substituted-4-(4-aminobutyl)-1,4-benzoxazepin-5(4H)-one derivatives (1-5) which showed a very high affinity for 5-HT1A receptor with good selectivity over dopamine D2 receptor was synthesized. Among these compounds, 3-chloro-4-[4-[4-(2-pyridinyl)-1,2,3,6-tetrahydropyridin-1-yl]butyl]-1,4-benzoxazepin-5(4H)-one (5: SUN N4057) exhibited remarkable neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model.
摘要
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