A comprehensive patents review on cannabinoid 1 receptor antagonists as antiobesity agents

Abstract

Introduction: Obesity is a rapidly expanding worldwide health problem. Various targets are investigated presently for the treatment of obesity, but there remains an unmet need for an effective drug therapy with acceptable efficacy levels and reduced side effects. Targeting peripherally located cannabinoid 1 (CB1) receptors is an attractive strategy as these receptors play a vital role in energy homeostasis.

Areas covered: CB1 receptor antagonists constitute one of the most important categories of compounds of interest for the control of obesity. In this review, the authors focus on recent advances (since 2007) in diverse chemical classes of patented compounds belonging to the category of CB1 receptor antagonists.

Expert opinion: Safer CB1 receptor antagonists for the treatment of obesity can be discovered by developing such compounds that act peripherally. Increasing the polar service area, decreasing the lipophilicity and designing of neutral antagonists and allosteric inhibitors are some interesting strategies that could offer promising results.

Keywords:

• cannabinoid
• CB1 receptor antagonists
• endocannabinoid system
• obesity
• peripherally acting
• rimonabant

Acknowledgments

MK Sharma is thankful to University Grants Commission, New Delhi, for awarding Junior Research Fellowships (JRF) under the RFSMS-BSR programme [No.F. 7-129/2007 (BSR)].

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Notes

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