A comprehensive patents review on cannabinoid 1 receptor antagonists as antiobesity agents
Mayank Kumar Sharma1, Prashant R Murumkar1, Mahesh A Barmade1
1a The M. S. University of Baroda, Pharmacy Department, Faculty of Technology and Engineering, Kalabhavan Vadodara - 390 001, India mryadav11@yahoo.co.in.
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.
Insights
Developing peripherally acting cannabinoid 1 (CB1) receptor antagonists offers a promising strategy for effective obesity treatment with fewer side effects. Research focuses on novel compounds targeting CB1 receptors to improve energy homeostasis.
Area of Science:
- Pharmacology
- Medicinal Chemistry
- Endocrinology
Background:
- Obesity presents a significant global health challenge with an ongoing need for effective pharmacotherapies.
- Cannabinoid 1 (CB1) receptors, crucial for energy balance, are a key therapeutic target for obesity management.
- Current obesity treatments often lack sufficient efficacy or acceptable side effect profiles.
Purpose of the Study:
- To review recent advancements (post-2007) in patented CB1 receptor antagonist compounds for obesity treatment.
- To explore diverse chemical classes of CB1 receptor antagonists.
- To identify strategies for developing safer and more effective anti-obesity drugs.
Main Methods:
- Literature review of scientific publications and patents since 2007.
- Focus on compounds targeting peripherally located CB1 receptors.
- Analysis of chemical structures and properties of CB1 receptor antagonists.
Main Results:
- Identification of various chemical classes of CB1 receptor antagonists patented since 2007.
- Highlighting the role of peripheral CB1 receptor antagonism in energy homeostasis.
- Discussion of challenges and opportunities in developing selective CB1 antagonists.
Conclusions:
- Peripherally acting CB1 receptor antagonists represent a viable strategy for safer obesity treatment.
- Strategies such as increasing polar surface area and decreasing lipophilicity can enhance drug safety.
- Development of neutral antagonists and allosteric inhibitors shows potential for improved therapeutic outcomes.
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