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.
Publication types
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Evaluation Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Benzamides / pharmacokinetics
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Benzazepines / administration & dosage
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Benzazepines / pharmacology*
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Binding Sites
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Cerebellum / drug effects
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Cerebellum / metabolism
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Corpus Striatum / drug effects*
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Corpus Striatum / metabolism*
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Male
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Nicotinic Agonists / administration & dosage
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Nicotinic Agonists / pharmacology*
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Pyrrolidines / pharmacokinetics
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Quinoxalines / administration & dosage
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Quinoxalines / pharmacology*
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Radiopharmaceuticals / pharmacokinetics
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Random Allocation
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Rats
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Rats, Wistar
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Receptors, Dopamine D2 / drug effects*
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Receptors, Dopamine D2 / metabolism*
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Receptors, Dopamine D3 / drug effects*
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Receptors, Dopamine D3 / metabolism*
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Varenicline
Substances
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Benzamides
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Benzazepines
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Nicotinic Agonists
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Pyrrolidines
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Quinoxalines
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Radiopharmaceuticals
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Receptors, Dopamine D2
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Receptors, Dopamine D3
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3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide
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Varenicline