Psychopharmacology Laboratory, Department of Psychology, American University, Washington, D.C., USA.
Pharmacol Biochem Behav. 2010 Feb;94(4):580-7. doi: 10.1016/j.pbb.2009.11.014. Epub 2009 Dec 4.
Although cocaine is primarily known for its powerful hedonic effects, there is evidence that its affective experience has a notable aversive component that is less well understood. A variety of pharmacological and molecular approaches have implicated enhanced monoamine (MA) neurotransmission in the aversive effects of cocaine. Although numerous studies have yielded data supportive of the role of the monoamines (indirectly and directly), the specific system suggested to be involved differs across studies and paradigms (Freeman et al., 2005b; Grupp, 1997; Roberts and Fibiger, 1997). Monoamine transporter knockout mice have been useful in the study of many different aspects of cocaine effects relevant to human drug use and addiction, yet an assessment of the effects of deletion of the genes for the dopamine, norepinephrine and serotonin transporters (DAT, NET, and SERT, respectively) on cocaine's aversive properties has yet to be performed (Uhl et al., 2002). In the current investigation, the strength of cocaine-induced aversions was compared among three groups of transgenic mice with deletions of the genes responsible for the production of one of the monoamine transporters. When compared to their respective WT controls, dopamine transporter deletion slightly attenuated cocaine-induced aversion while deletion of SERT or NET resulted in a more significant delay in the onset and strength of cocaine-induced taste aversions. The data lead us to conclude that the action of cocaine to inhibit NET contributes most substantially to its aversive effects, with some involvement of SERT and minimal contribution of DAT.
尽管可卡因主要以其强大的愉悦效果而闻名,但有证据表明,它的情感体验具有显著的厌恶成分,而这一成分还不太为人理解。各种药理学和分子方法都表明,增强单胺(MA)神经递质传递与可卡因的厌恶效应有关。尽管许多研究都提供了支持单胺作用的数据(间接和直接),但在不同的研究和范式中,所涉及的特定系统也不同(Freeman 等人,2005b;Grupp,1997;Roberts 和 Fibiger,1997)。单胺转运体敲除小鼠在研究与人类药物使用和成瘾相关的可卡因作用的许多不同方面非常有用,但尚未对多巴胺、去甲肾上腺素和 5-羟色胺转运体(DAT、NET 和 SERT)基因缺失对可卡因厌恶特性的影响进行评估(Uhl 等人,2002)。在当前的研究中,对三组单胺转运体基因缺失的转基因小鼠进行了比较,以评估可卡因诱导的厌恶强度。与各自的 WT 对照相比,多巴胺转运体缺失略微减弱了可卡因诱导的厌恶,而 SERT 或 NET 的缺失导致可卡因诱导的味觉厌恶的发生和强度出现更显著的延迟。这些数据使我们得出结论,可卡因抑制 NET 的作用对其厌恶效应的贡献最大,SERT 也有一定的参与,而 DAT 的贡献最小。