Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 46, Issue 18, Pages 3938-3944Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm030185v
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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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