Cannabinoid-1 receptor antagonist rimonabant (SR141716) increases striatal dopamine D2 receptor availability

Addict Biol. 2013 Nov;18(6):908-11. doi: 10.1111/j.1369-1600.2011.00369.x. Epub 2011 Sep 29.

Abstract

The cannabinoid 1 receptor antagonist rimonabant (SR141716) alters rewarding properties and intake of food and drugs. Additionally, striatal dopamine D2 receptor (DRD2) availability has been implicated in reward function. This study shows that chronic treatment of rats with rimonabant (1.0 and 3.0 mg/kg/day) dose-dependently increased DRD2 availability in the dorsal striatum (14 and 23%) compared with vehicle. High-dose rimonabant also increased DRD2 availability in the ventral striatum (12%) and reduced weight gain. Thus, up-regulation of striatal DRD2 by chronic rimonabant administration may be an underlying mechanism of action and confirms the interactions of the endocannabinoid and dopaminergic systems.

Keywords: Cannabinoid 1 receptor; IBZM; dopamine D2 receptor; nucleus accumbens; rimonabant; striatum.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Basal Ganglia / drug effects*
  • Basal Ganglia / metabolism
  • Cannabinoid Receptor Antagonists / pharmacology*
  • Dose-Response Relationship, Drug
  • Male
  • Piperidines / pharmacology*
  • Pyrazoles / pharmacology*
  • Random Allocation
  • Rats
  • Receptors, Dopamine D2 / metabolism*
  • Reward
  • Rimonabant
  • Up-Regulation / drug effects
  • Weight Gain / drug effects

Substances

  • Cannabinoid Receptor Antagonists
  • Piperidines
  • Pyrazoles
  • Receptors, Dopamine D2
  • Rimonabant