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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

LoVerme J,Duranti A,Tontini A,Spadoni G,Mor M,Rivara S,Stella N,Xu C,Tarzia G,Piomelli D

doi

10.1016/j.bmcl.2008.12.059

subject

Has Abstract

pub_date

2009-02-01 00:00:00

pages

639-43

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)01582-5

journal_volume

19

pub_type

杂志文章

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