Spealman R D
Harvard Medical School, New England Regional Primate Research Center, Southborough, MA 01772-9102, USA.
Pharmacol Biochem Behav. 1995 Aug;51(4):661-5. doi: 10.1016/0091-3057(94)00434-k.
The effects of cocaine alone and after pretreatment with the dopamine D2 partial agonists terguride, SDZ 208-911, and SDZ 208-912 were determined in squirrel monkeys trained to discriminate cocaine from saline using a two-lever drug discrimination procedure. When tested alone, cocaine engendered dose-related increases in the percentage of responses on the cocaine-associated lever, reaching virtually exclusive cocaine-appropriate responding after a dose of 1.0 mg/kg. Pretreatment with terguride (0.003-0.03 mg/kg), SDZ 208-911 (0.001-0.01), and SDZ 208-912 (0.003-0.018 mg/kg) did not consistently alter the discriminative stimulus effects of cocaine. Although some doses of each D2 partial agonist either increased (notably SDZ 208-911) or decreased (notably SDZ 208-912) the level of cocaine-appropriate responding engendered by low to intermediate doses of cocaine, none of the drugs reduced the percentage of cocaine-appropriate responding engendered by low to intermediate doses of cocaine, none of the drugs reduced the percentage of cocaine-appropriate responses engendered by 1.0 mg/kg cocaine. The results do not support the view that terguride, SDZ 208-911, or SDZ 208-912 would serve as functional antagonists of the subjective effects of cocaine.
在松鼠猴中，使用双杠杆药物辨别程序训练其区分可卡因和生理盐水，从而确定单独使用可卡因以及用多巴胺D2部分激动剂特谷利特、SDZ 208 - 911和SDZ 208 - 912预处理后的效果。单独测试时，可卡因使与可卡因相关杠杆上的反应百分比呈剂量相关增加，在剂量为1.0 mg/kg后几乎完全出现对可卡因的正确反应。用特谷利特（0.003 - 0.03 mg/kg）、SDZ 208 - 911（0.001 - 0.01）和SDZ 208 - 912（0.003 - 0.018 mg/kg）预处理并没有始终如一地改变可卡因的辨别刺激效果。尽管每种D2部分激动剂的某些剂量要么增加（特别是SDZ 208 - 911）要么降低（特别是SDZ 208 - 912）低至中等剂量可卡因所引起的对可卡因的正确反应水平，但没有一种药物能降低低至中等剂量可卡因所引起的对可卡因的正确反应百分比，也没有一种药物能降低1.0 mg/kg可卡因所引起的对可卡因的正确反应百分比。结果不支持特谷利特、SDZ 208 - 911或SDZ 208 - 912可作为可卡因主观效应功能拮抗剂的观点。
