Bedford J A, Borne R F, Wilson M C
Pharmacol Biochem Behav. 1980 Jul;13(1):69-75. doi: 10.1016/0091-3057(80)90122-7.
The effects of cocaine and norcocaine were compared using locomotor activity, fixed-ratio 100 (FR 100) and fixed-interval 4 min (FI 4 min) food reinforcement and free feeding paradigms in rat and intravenous self-administration tests in rhesus monkeys. Cocaine was shown to significantly increase locomotor activity at doses of 20 and 40 mg/kg, while norcocaine had no effect at these doses and produced convulsions and death at 60 and 80 mg/kg. Both compounds significantly reduced food consumption at one or more of the doses tested. Cocaine and norcocaine at doses of 20 and 40 mg/kg, produced decreases in FR responding. Cocaine at doses of 10, 20, and 40 mg/kg, produced increases in FI responding; norcocaine had no effect following 10 mg/kg and decreased responding at 20 and 40 mg/kg. Cocaine (0.2 mg/kg/inj) and norcocaine (0.5, 0.2, 0.8 mg/kg/inj) maintained intravenous self-administration in all three monkeys tested. The data indicate that norcocaine is a pharmacologically active metabolite of cocaine which could account for some of the activity heretofore attributed to cocaine. However, the lack of any stimulatory effect of norcocaine or locomotor activity and the lack of increased responding produced by norcocaine on fixed-interval behavior suggest that norcocaine differs qualitatively from cocaine.
使用大鼠的自主活动、固定比率100（FR 100）和固定间隔4分钟（FI 4分钟）食物强化及自由进食范式以及恒河猴的静脉自我给药试验，比较了可卡因和去甲可卡因的作用。结果显示，可卡因在20和40毫克/千克剂量时可显著增加自主活动，而去甲可卡因在这些剂量下无作用，在60和80毫克/千克时会引发惊厥和死亡。两种化合物在一个或多个测试剂量下均显著减少食物消耗。20和40毫克/千克剂量的可卡因和去甲可卡因可使FR反应减少。10、20和40毫克/千克剂量的可卡因可使FI反应增加；10毫克/千克的去甲可卡因无作用，20和40毫克/千克时反应减少。可卡因（0.2毫克/千克/注射）和去甲可卡因（0.5、0.2、0.8毫克/千克/注射）在所有三只受试猴子中均维持静脉自我给药。数据表明，去甲可卡因是可卡因的一种具有药理活性的代谢产物，这可以解释一些迄今归因于可卡因的活性。然而，去甲可卡因对自主活动缺乏任何刺激作用，且对固定间隔行为没有产生反应增加，这表明去甲可卡因在性质上与可卡因不同。
