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Overcoming the Psychiatric Side Effects of the Cannabinoid CB1 Receptor Antagonists: Current Approaches for

Thuy Nguyen1, Brian F Thomas1, Yanan Zhang1

  • 1Research Triangle Institute, Research Triangle Park, NC 27709, United States.

Current Topics in Medicinal Chemistry
|July 10, 2019
PubMed

Insights

Targeting the Cannabinoid CB1 Receptor (CB1R) shows promise for obesity and addiction, but side effects limit its use. New strategies aim to develop safer CB1R therapeutics.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Metabolic Disorders

Background:

  • The Cannabinoid CB1 Receptor (CB1R) is a key regulator of numerous physiological processes.
  • CB1R antagonism has demonstrated efficacy in preclinical and clinical studies for obesity, metabolic disorders, and addiction.
  • The first-in-class CB1R antagonist, rimonabant, was withdrawn due to severe psychiatric side effects.

Purpose of the Study:

  • To review the progress in developing therapeutics targeting the CB1R over the past two decades.
  • To explore strategies aimed at mitigating the adverse psychiatric effects associated with CB1R antagonism.
  • To highlight advancements in novel CB1R modulators.

Main Methods:

  • Literature review of studies on CB1R therapeutics from the last 20 years.
  • Analysis of strategies including neutral antagonists, peripherally restricted ligands, and allosteric modulators.
  • Examination of preclinical and clinical data regarding efficacy and safety profiles.

Main Results:

  • CB1R antagonism is effective for weight management and smoking cessation.
  • Psychiatric adverse events, such as anxiety and depression, are significant limitations of current CB1R antagonists.
  • Development is ongoing for safer CB1R-targeting drugs with improved side effect profiles.

Conclusions:

  • Despite challenges, the CB1R remains a significant therapeutic target.
  • Novel approaches are crucial for developing effective and safe CB1R-based medications.
  • Continued research into CB1R modulation holds potential for treating metabolic and addictive disorders.
Keywords:
Allosteric modulatorsCB1 receptorNeutral antagonistsPeripherally restricted antagonistsPsychiatric side effectsTherapeutics development.

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