A new class of diamine-based human histamine H-3 receptor antagonists: 4-(aminoalkoxy)benzylamines

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. Si...

Full description

Saved in:
Bibliographic Details
Published inJournal of medicinal chemistry Vol. 46; no. 18; pp. 3938 - 3944
Main Authors Apodaca, R, Dvorak, CA, Xiao, W, Barbier, AJ, Boggs, JD, Wilson, SJ, Lovenberg, TW, Carruthers, NI
Format Journal Article
LanguageEnglish
Published WASHINGTON Amer Chemical Soc 28.08.2003
Subjects
Chemistry, Medicinal
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Science & Technology
LIGANDS
RAT
CLONING
AMINO-ACIDS
CHEMISTRY
ALDEHYDES
PART 2
MODEL
BINDING
H-3-RECEPTORS
Online AccessGet full text

Cover

More Information
Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm030185v