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Bioorg Med Chem Lett. 2009 Feb 1;19(3):639-43. doi: 10.1016/j.bmcl.2008.12.059. Epub 2008 Dec 24.

Synthesis and characterization of a peripherally restricted CB1 cannabinoid antagonist, URB447, that reduces feeding and body-weight gain in mice.

Author information

1
Department of Pharmacology, 360 MedScience II, University of California, Irvine, CA 92697-4625, USA.

Abstract

Cannabinoid CB(1) receptor antagonists reduce body weight in rodents and humans, but their clinical utility as anti-obesity agents is limited by centrally mediated side effects. Here, we describe the first mixed CB(1) antagonist/CB(2) agonist, URB447 ([4-amino-1-(4-chlorobenzyl)-2-methyl-5-phenyl-1H-pyrrol-3-yl](phenyl)methanone), which lowers food intake and body-weight gain in mice without entering the brain or antagonizing central CB(1)-dependent responses. URB447 may provide a useful pharmacological tool for investigating the cannabinoid system, and might serve as a starting point for developing clinically viable CB(1) antagonists devoid of central side effects.

PMID:
19128970
PMCID:
PMC3690177
DOI:
10.1016/j.bmcl.2008.12.059
[Indexed for MEDLINE]
Free PMC Article

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