THE SEROTONIN 5-HT4 RECEPTOR .3. DESIGN AND PHARMACOLOGICAL EVALUATION OF A NEW CLASS OF ANTAGONISTS

被引：9

作者：

BUCHHEIT, KH ^{[1
]}

KLEIN, F ^{[1
]}

KLOPPNER, E ^{[1
]}

PFANNKUCHE, HJ ^{[1
]}

MATTES, H ^{[1
]}

机构：

[1] SANDOZ PHARMA LTD,PRECLIN RES,CH-4002 BASEL,SWITZERLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 21期

关键词：

D O I：

10.1016/0960-894X(95)00434-U

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design, synthesis and pharmacological activity of a new class of potent and selective 5-HT4 receptor antagonists containing an indole nucleus linked to a carbazimidamide are presented. 4c, a representative member of our new class is a potent competitive antagonist at 5-HT4 receptors with a pA(2) value of 8.4, displaying selectivity (ranging from 20 to over 1000 fold) versus other serotonin receptor subtypes.

引用

页码：2495 / 2500

页数：6

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