Targeting the endocannabinoid system in diabesity: Fact or fiction?

Drug Discov Today. 2021 Jul;26(7):1750-1758. doi: 10.1016/j.drudis.2021.03.022. Epub 2021 Mar 27.


'Diabesity' refers to a rising epidemic indicated by the intricate relationship between obesity and diabetes. The global prevalence of these coexisting, insidious diseases increases social and economic health burdens at a rapid pace. Numerous reports delineate the involvement of the underlying endocannabinoid (EC) signaling system through the cannabinoid-1 (CB1) receptor in the regulation of metabolism and adiposity. Conversely, EC inverse agonists can result in severe depression and suicidal thoughts through interactions with CB1/2 receptors in the brain. This review attempts to elucidate a possible mechanism for the amelioration of diabesity. Moreover, we also highlight the available targets of the CB1 receptor, which could pave the way for safe and effective therapy.

Keywords: Cannabinoid receptor; Diabesity; Diabetes mellitus; Endocannabinoid; Obesity.

Publication types

  • Review

MeSH terms

  • Animals
  • Cannabinoid Receptor Antagonists / therapeutic use
  • Diabetes Mellitus / drug therapy*
  • Diabetes Mellitus / metabolism
  • Endocannabinoids / metabolism*
  • Humans
  • Obesity / drug therapy*
  • Obesity / metabolism
  • Receptors, Cannabinoid / metabolism


  • Cannabinoid Receptor Antagonists
  • Endocannabinoids
  • Receptors, Cannabinoid