Synthesis and pharmacological evaluation of piperidinoalkanoyl-1,2,3,4-tetrahydroisoquinoline derivatives as novel specific bradycardic agents

被引：14

作者：

Kubota, H ^{[1
]}

Watanabe, T ^{[1
]}

Kakefuda, A ^{[1
]}

Masuda, N ^{[1
]}

Wada, K ^{[1
]}

Ishii, N ^{[1
]}

Sakamoto, S ^{[1
]}

Tsukamoto, S ^{[1
]}

机构：

[1] Yamanouchi Pharmaceut Co Ltd, Inst Drug Discovery Res, Tsukuba, Ibaraki 3058585, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 12期

关键词：

cardiac disease; myocardial ischemia; bradycardic agent; zatebradine;

D O I：

10.1016/j.bmcl.2004.04.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of piperidinoalkanoyl-1,2,3,4-tetrahydroisoquinoline derivatives were synthesized, and their bradycardic activities were investigated in the isolated right atria of guinea pigs and in conscious rats. These efforts identified the achiral compound 2f, which exhibited potent and long-lasting bradycardic activity with minimal effects on mean blood pressure in conscious rats. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：3049 / 3052

页数：4

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