A novel class of Na+ and Ca2+ channel dual blockers with highly potent anti-ischemic effects

被引：18

作者：

Annoura, H ^{[1
]}

Nakanishi, K ^{[1
]}

Uesugi, M ^{[1
]}

Fukunaga, A ^{[1
]}

Miyajima, A ^{[1
]}

Tamura-Horikawa, Y ^{[1
]}

Tamura, S ^{[1
]}

机构：

[1] Suntory Inst Biomed Res, Osaka 6188503, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(99)00516-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel arylpiperidines (4a-d) which have highly potent blocking effects for both neuronal Na+ and T-type Ca2+ channels with extremely low affinity for dopamine D-2 receptors were synthesized. Among these compounds, 1-(2-hydroxy-3-phenoxy)propyl-4-(4-phenoxyphenyl)-piperidine hydrochloride (4c; SUN N5030) exhibited remarkable neuroprotective activity in a transient middle cerebral artery occlusion (MCAO) model. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：2999 / 3002

页数：4

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