Spealman R D, Bergman J, Madras B K
Harvard Medical School, New England Regional Primate Research Center, Southborough, MA 01772-9102.
Pharmacol Biochem Behav. 1991 Aug;39(4):1011-3. doi: 10.1016/0091-3057(91)90067-c.
Self-administration of the high-affinity cocaine analog 2 beta-carbomethoxy-3 beta-(4-fluorophenyl)tropane (CFT) and cocaine were compared in squirrel monkeys responding under a second-order schedule of IV drug injection. Both CFT and cocaine maintained self-administration in all subjects. As the dose of either drug was increased, the rate of responding first increased and then decreased. Although the two drugs had qualitatively similar effects, CFT was approximately six times more potent than cocaine. This potency relation corresponds closely with the potency relations reported for CFT and cocaine in studies of dopamine uptake inhibition and binding at cocaine recognition sites. The results are consistent with the view that the reinforcing effects of cocaine-like drugs are mediated at cocaine recognition sites associated with the dopamine uptake system, and suggest that radioligand probes based on CFT may be suitable markers for these sites.
在松鼠猴按静脉注射药物的二阶程序做出反应的过程中，对高亲和力可卡因类似物2β-甲氧羰基-3β-（4-氟苯基）托烷（CFT）和可卡因的自我给药情况进行了比较。CFT和可卡因在所有受试动物中均维持了自我给药行为。随着两种药物剂量的增加，反应率先升高后降低。尽管这两种药物在性质上有相似的作用，但CFT的效力约为可卡因的六倍。这种效力关系与在多巴胺摄取抑制和可卡因识别位点结合研究中报道的CFT和可卡因的效力关系密切对应。这些结果与如下观点一致，即可卡因样药物的强化作用是在与多巴胺摄取系统相关的可卡因识别位点介导的，并表明基于CFT的放射性配体探针可能是这些位点的合适标记物。
