Yaksh T L, Rudy T A
Eur J Pharmacol. 1977 Nov 15;46(2):83-92. doi: 10.1016/0014-2999(77)90243-6.
Dose-response curves for morphine (0.5-20 mg/kg) were obtained in 4 rhesus monkeys performing the discrete trials shock titration task. Naloxone (5-500 microgram/kg) uniformly produced a dose dependent, parallel shift of the morphine dose-response curves to right. Plots for the 4 animals of the Log (dose ratio--1) versus --Log (naloxone) revealed that the line had a slope of -0.96. The value of the pA2 was 7.2. Similar experiments were carried out in two rhesus monkeys using cyclazocine. Naloxone (50-1000 microgram) similarly produced a rightward dose dependent, parallel shift of the cyclazocine dose response curves. Unlike the results obtained with morphine, the pA2 for naloxone obtained with cyclazocine was 6.3 and the slope of the dose ratio line was -1.6.
在4只恒河猴执行离散试验电击滴定任务时,获得了吗啡(0.5 - 20毫克/千克)的剂量-反应曲线。纳洛酮(5 - 500微克/千克)一致地使吗啡剂量-反应曲线产生剂量依赖性、平行向右移位。对4只动物绘制的Log(剂量比 - 1)与 - Log(纳洛酮)的图显示,该线的斜率为 - 0.96。pA2值为7.2。使用环唑辛在2只恒河猴中进行了类似实验。纳洛酮(50 - 1000微克)同样使环唑辛剂量-反应曲线产生向右的剂量依赖性、平行移位。与用吗啡获得的结果不同,用环唑辛获得的纳洛酮的pA2为6.3,剂量比线的斜率为 - 1.6。