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Updated: Jun 21, 2026

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Published on: August 6, 2013
Varenicline increases striatal dopamine D(2/3) receptor binding in rats
Cleo L Crunelle1, Michelle L Miller, Kora de Bruin
1Amsterdam Institute for Addiction Research and Department of Psychiatry, Academic Medical Center, University of Amsterdam, Amsterdam, the Netherlands.
Abstract:
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-naïve 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-naïve rats. Therefore, varenicline may be an effective treatment for addictions other than smoking.
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