Varenicline increases striatal dopamine D(2/3) receptor binding in rats.
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.
Crunelle
Cleo L
CL
Amsterdam Institute for Addiction Research and Department of Psychiatry, Academic Medical Center, University of Amsterdam, Amsterdam, the Netherlands.
Miller
Michelle L
ML
de Bruin
Kora
K
van den Brink
Wim
W
Booij
Jan
J
D000818:Animals; D001549:Benzamides / Q000493:pharmacokinetics; D001552:Benzazepines / Q000008:administration & dosage / Q000494:pharmacology*; D001665:Binding Sites; D002531:Cerebellum / Q000187:drug effects / Q000378:metabolism; D003342:Corpus Striatum / Q000187:drug effects* / Q000378:metabolism*; D008297:Male; D018722:Nicotinic Agonists / Q000008:administration & dosage / Q000494:pharmacology*; D011759:Pyrrolidines / Q000493:pharmacokinetics; D011810:Quinoxalines / Q000008:administration & dosage / Q000494:pharmacology*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D011897:Random Allocation; D051381:Rats; D017208:Rats, Wistar; D017448:Receptors, Dopamine D2 / Q000187:drug effects* / Q000378:metabolism*; D050637:Receptors, Dopamine D3 / Q000187:drug effects* / Q000378:metabolism*; D000068580:Varenicline
D001549:Benzamides; D001552:Benzazepines; D018722:Nicotinic Agonists; D011759:Pyrrolidines; D011810:Quinoxalines; D019275:Radiopharmaceuticals; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3; C055743:3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide; D000068580:Varenicline