Varenicline increases striatal dopamine D(2/3) receptor binding in rats.

Author(s): Crunelle CL, Miller ML, de Bruin K, van den Brink W, Booij J

Affiliation(s): Amsterdam Institute for Addiction Research and Department of Psychiatry, Academic Medical Center, University of Amsterdam, Amsterdam, the Netherlands.

Publication date & source: 2009-09, Addict Biol., 14(4):500-2. Epub 2009 Jul 24.

Publication type: Research Support, Non-U.S. Gov't

Increasing dopamine D(2/3) receptor availability is postulated to be a treatment for drug addiction. Varenicline, an alpha4beta2-nicotinic partial agonist, is effective for nicotine dependence. We hypothesize that varenicline increases dopamine D(2/3) receptor availability. Twenty male drug-naive rats were randomized to varenicline (2 mg/kg) or placebo for 14 days, and then injected with the dopamine D(2/3) radiotracer 123I-IBZM. We found significantly higher striatum-to-cerebellum binding ratios in both dorsal and ventral striatum for the varenicline group compared with placebo. Varenicline increases dopamine D(2/3) receptor availability in drug-naive rats. Therefore, varenicline may be an effective treatment for addictions other than smoking.