Hypothalamic CB1 cannabinoid receptors regulate energy balance in mice

Endocrinology. 2012 Sep;153(9):4136-43. doi: 10.1210/en.2012-1405. Epub 2012 Jul 9.

Abstract

Cannabinoid type 1 (CB(1)) receptor activation is generally considered a powerful orexigenic signal and inhibition of the endocannabinoid system is beneficial for the treatment of obesity and related metabolic diseases. The hypothalamus plays a critical role in regulating energy balance by modulating both food intake and energy expenditure. Although CB(1) receptor signaling has been implicated in the modulation of both these mechanisms, a complete understanding of its role in the hypothalamus is still lacking. Here we combined a genetic approach with the use of adeno-associated viral vectors to delete the CB(1) receptor gene in the adult mouse hypothalamus and assessed the impact of such manipulation on the regulation of energy balance. Viral-mediated deletion of the CB(1) receptor gene in the hypothalamus led to the generation of Hyp-CB(1)-KO mice, which displayed an approximately 60% decrease in hypothalamic CB(1) receptor mRNA levels. Hyp-CB(1)-KO mice maintained on a normocaloric, standard diet showed decreased body weight gain over time, which was associated with increased energy expenditure and elevated β(3)-adrenergic receptor and uncoupling protein-1 mRNA levels in the brown adipose tissue but, surprisingly, not to changes in food intake. Additionally, Hyp-CB(1)-KO mice were insensitive to the anorectic action of the hormone leptin (5 mg/kg) and displayed a time-dependent hypophagic response to the CB(1) inverse agonist rimonabant (3 mg/kg). Altogether these findings suggest that hypothalamic CB(1) receptor signaling is a key determinant of energy expenditure under basal conditions and reveal its specific role in conveying the effects of leptin and pharmacological CB1 receptor antagonism on food intake.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calorimetry, Indirect
  • Eating / drug effects
  • Energy Metabolism / genetics
  • Energy Metabolism / physiology*
  • Genetic Vectors / genetics
  • Hypothalamus / metabolism*
  • In Situ Hybridization, Fluorescence
  • Leptin / pharmacology
  • Male
  • Mice
  • Mice, Knockout
  • Piperidines / pharmacology
  • Pyrazoles / pharmacology
  • Real-Time Polymerase Chain Reaction
  • Receptor, Cannabinoid, CB1 / genetics
  • Receptor, Cannabinoid, CB1 / metabolism*
  • Rimonabant

Substances

  • Leptin
  • Piperidines
  • Pyrazoles
  • Receptor, Cannabinoid, CB1
  • Rimonabant