Cannabinoid-1 receptor inhibition prevents the reduction of 24-hour energy expenditure with weight loss

Metabolism. 2012 Apr;61(4):546-53. doi: 10.1016/j.metabol.2011.09.002. Epub 2011 Oct 14.

Abstract

Pharmacologic inhibition of the cannabinoid-1 receptor (CB1R) in rodent models leads to weight loss and time-dependent changes in energy balance. This study evaluated the effects of CB1R inhibition on weight loss, energy expenditure (EE), and food intake (FI) in an obese canine model following 4 weeks of treatment. Eighteen maintenance-fed obese beagles were evenly and randomly allocated to a CB1R inverse agonist (AM251) (2 mg/kg), a 70% food-restricted (FR) diet, or a control group (C). Evaluations included body weight and composition (dual-energy x-ray absorptiometry scan), EE (doubly labeled water), and FI. Change in body mass at week 4 was significantly greater (P < .050) in the AM251 (-1476.7 g) and FR groups (-1100.0 g) than in the C group (-228.3 g). Food intake was decreased from week 2 onward in the FR and AM251 groups (P < .05). Absolute and lean mass-adjusted EEs were decreased only in the FR group (P < .01); EE in the AM251 group was greater (P < .05) than that in the FR group. Pharmacologic inhibition of CB1R in a canine model led to sustained effects on FI and EE. Weight loss was greater with AM251 than could be accounted for by food restriction (∼25%), an effect likely mediated by the EE response to CB1R inhibition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Absorptiometry, Photon
  • Animals
  • Disease Models, Animal
  • Dogs
  • Eating / drug effects
  • Eating / physiology
  • Energy Metabolism / physiology*
  • Female
  • Glucose Tolerance Test
  • Obesity / drug therapy*
  • Obesity / metabolism*
  • Piperidines / pharmacology*
  • Pyrazoles / pharmacology*
  • Random Allocation
  • Receptor, Cannabinoid, CB1 / antagonists & inhibitors*
  • Receptor, Cannabinoid, CB1 / metabolism
  • Weight Loss / drug effects*
  • Weight Loss / physiology

Substances

  • Piperidines
  • Pyrazoles
  • Receptor, Cannabinoid, CB1
  • AM 251