A new class of diamine-based human histamine H3 receptor antagonists:: 4-(aminoalkoxy)benzylamines

被引：112

作者：

Apodaca, R ^{[1
]}

Dvorak, CA ^{[1
]}

Xiao, W ^{[1
]}

Barbier, AJ ^{[1
]}

Boggs, JD ^{[1
]}

Wilson, SJ ^{[1
]}

Lovenberg, TW ^{[1
]}

Carruthers, NI ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, San Diego, CA 92121 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 18期

关键词：

D O I：

10.1021/jm030185v

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

4-(Aminoalkoxy)benzylamines were prepared and screened for in vitro activity at the human histamine H-3 receptor. Some members of this series exhibited subanomolar binding affinities. Analogues in which one nitrogen atom was replaced with a methine group showed greatly reduced binding affinities. Six members of this series were found to be antagonists in a cell-based model of human histamine H-3 receptor activation. One member of this series, 1-[4-(3-piperidin-1-ylpropoxy)benzyljpiperidine (7b), was found to be a selective and potent human H-3 receptor antagonist.

引用

页码：3938 / 3944

页数：7

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