Varenicline increases striatal dopamine D2/3 receptor binding in rats

被引：20

作者：

Crunelle, Cleo L. ^{[1
,2
,3
]}

Miller, Michelle L. ^{[1
,2
,3
]}

de Bruin, Kora ^{[3
]}

van den Brink, Wim ^{[1
,2
]}

Booij, Jan ^{[3
]}

机构：

[1] Univ Amsterdam, Amsterdam Inst Addict Res, Acad Med Ctr, NL-1070 AW Amsterdam, Netherlands

[2] Univ Amsterdam, Dept Psychiat, Acad Med Ctr, NL-1070 AW Amsterdam, Netherlands

[3] Univ Amsterdam, Dept Nucl Med, Acad Med Ctr, NL-1070 AW Amsterdam, Netherlands

来源：

ADDICTION BIOLOGY | 2009年 / 14卷 / 04期

关键词：

123I-IB2M storage phosphor imaging; dopamine receptor; drug partial agonism; nicotric receptor alpha 4 beta 2; striatum; varenicline;

D O I：

10.1111/j.1369-1600.2009.00168.x

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Increasing dopamine D-2/3 receptor availability is postulated to be a treatment for drug addiction. Varenicline, an alpha 4 beta 2-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 I-123-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.

引用

页码：500 / 502

页数：3

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