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Cannabinoid receptor antagonists and obesity.

Shawn C Black¹

¹Cardiovascular and Metabolic Diseases, MS 8220-3119, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA. shawn_c_black@groton.pfizer.com

Current Opinion in Investigational Drugs (London, England : 2000)

|May 12, 2004

Summary

Blocking cannabinoid-1 (CB1) receptors reduces appetite and body weight. CB1 receptor antagonists, like rimonabant, show promise for treating obesity by decreasing food intake and promoting weight loss in both animals and humans.

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Area of Science:

Neuroscience
Pharmacology
Obesity Research

Background:

The cannabinoid-1 (CB1) receptor is implicated in regulating appetitive behaviors.
Agonists of the CB1 receptor stimulate food consumption, while endogenous agonists increase with food demand.

Purpose of the Study:

To investigate the role of CB1 receptor antagonists in modulating food intake and body weight.
To review the discovery and therapeutic potential of selective CB1 receptor antagonists.

Main Methods:

Administration of CB1 receptor agonists and antagonists in animal models.
Clinical trials evaluating CB1 receptor antagonists in humans.
Analysis of patent literature for CB1 antagonist discovery efforts.

Main Results:

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CB1 receptor antagonists inhibit both short-term and long-term food intake in rodents.
Chronic administration of CB1 antagonists leads to sustained body weight reduction in rodents and humans.
Rimonabant (SR-141716) has demonstrated appetite and weight reduction in human trials.

Conclusions:

CB1 receptor antagonists are effective in reducing appetite and body weight.
Selective CB1 receptor antagonists represent a potential therapeutic strategy for obesity management.
Ongoing research and development, including clinical trials for rimonabant, support the therapeutic value of CB1 receptor antagonism.