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.
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页码：3938 / 3944
页数：7
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