Will the new CB1 cannabinoid receptor antagonist SR-147778 have advantages over rimonabant?

Doggrell, Sheila A. (2005) Will the new CB1 cannabinoid receptor antagonist SR-147778 have advantages over rimonabant?. Expert Opinion On Investigational Drugs, 14 3: 339-342.


Author Doggrell, Sheila A.
Title Will the new CB1 cannabinoid receptor antagonist SR-147778 have advantages over rimonabant?
Journal name Expert Opinion On Investigational Drugs  (ERA 2012 Listed)    (ERA 2010 Rank A)   Check publisher's open access policy
Publication date 2005-03
Sub-type Article
DOI 10.1517/13543784.14.3.339
Volume number 14
Issue number 3
ISSN 1744-7658
1354-3784
Start page 339
End page 342
Total pages 4
Place of publication London
Publisher Informa Healthcare
Collection year 2005
Language eng
Subject C1
11 Medical and Health Sciences
1115 Pharmacology and Pharmaceutical Sciences
Abstract Obesity and alcoholism are two common modern-day diseases. The cannabinoid CB, receptor antagonist rimonabant is in Phase III clinical trial for the treatment of obesity with preliminary results showing that it decreases appetite and body weight. Animal studies have shown that rimonabant is effective in the treatment of alcoholism. SR-147778 is a new potent and selective CB1 receptor antagonist. In animals, SR-147778 has been shown to inhibit CB1 receptor-mediated hypothermia, analgesia and slowing of gastrointestinal transit. In rats trained to drink sucrose, the oral administration of SR-147778 3 mg/kg, before the presentation of sucrose, decreased the consumption of sucrose. SR-147778 3 mg/kg also reduced spontaneous feeding in rats deprived of food and also in non-deprived rats. In Sardinian alcohol-preferring (sP) rats, in the alcohol-naive state, SR-147778 slowed the development of a preference for alcohol. in alcohol-experienced sP rats SR-147778 (2.5, 5 and 10 mg/kg p.o.) reduced the alcohol intake. When alcohol-experienced sP rats are deprived of alcohol for 15 days, there is a large intake of alcohol on reintroduction of alcohol, and this response was almost abolished by treatment with SR-147778. From the preclinical studies published to date, there is no obvious major point of difference between rimonabant and SR-147778, and both are promising agents for the treatment of obesity and alcoholism.
Keyword Alcoholism
Cb1 Receptor Antagonist
Cb1 Receptor
Obesity
Rimonabant
Sardinian Alcohol-preferring Rats
Sr-147778
Pharmacology & Pharmacy
Selective Antagonist
Alcohol Dependence
Sr-141716
Sr147778
Potent
Rats
Q-Index Code C1

 
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