洛贝林对强直和甲基苯丙胺诱导的多巴胺释放的影响。
Lobeline effects on tonic and methamphetamine-induced dopamine release.
作者信息
Wilhelm Clare J, Johnson Robert A, Eshleman Amy J, Janowsky Aaron
机构信息
Research Service, Veterans Affairs Medical Center, Portland, OR 97239, USA.
出版信息
Biochem Pharmacol. 2008 Mar 15;75(6):1411-5. doi: 10.1016/j.bcp.2007.11.019. Epub 2007 Dec 4.
Abstract
The mechanisms of interaction between lobeline and the dopamine transporter (DAT) or the vesicular monoamine transporter (VMAT-2) are not clear. The goal of this study was to elucidate the effects of lobeline on these transporters in a cell system co-expressing the DAT and VMAT-2. Lobeline caused release of [(3)H]dopamine to a similar extent as reserpine (VMAT-2 inhibitor), but was less efficacious than methamphetamine or dopamine. Additionally, lobeline decreased the [(3)H]dopamine-releasing effects of methamphetamine, unlike reserpine which increased release by methamphetamine. These results suggest that lobeline has unique properties at the DAT and VMAT-2 which may make it useful as a pharmacotherapeutic to treat methamphetamine abuse.
摘要
洛贝林与多巴胺转运体（DAT）或囊泡单胺转运体（VMAT-2）之间的相互作用机制尚不清楚。本研究的目的是在共表达DAT和VMAT-2的细胞系统中阐明洛贝林对这些转运体的影响。洛贝林引起的[³H]多巴胺释放程度与利血平（VMAT-2抑制剂）相似，但效力低于甲基苯丙胺或多巴胺。此外，与利血平增加甲基苯丙胺的释放不同，洛贝林降低了甲基苯丙胺的[³H]多巴胺释放作用。这些结果表明，洛贝林在DAT和VMAT-2上具有独特的性质，这可能使其成为治疗甲基苯丙胺滥用的有效药物。
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