Harris R A
J Pharmacol Exp Ther. 1980 Jun;213(3):497-503.
The effects of morphine, butorphanol, cyclazocine, ketocyclazocine, ethylketocyclazocine, and SKF-10,047 were tested, alone and in conjunction with naloxone or naltrexone, in rats responding under a fixed-interval, 5-min schedule of food presentation. Except for naloxone and naltrexone, all of the drugs decreased the average rate of responding in a dose-dependent manner. The rate-decreasing effects of morphine were markedly antagonized by naltrexone, while the effects of SKF-10,047 or high doses of cyclazocine were not antagonized by naltrexone or naloxone. Naltrexone and naloxone were able to antagonize the effects of butorphanol, ketocyclazocine, ethylketocyclazocine and low doses of cyclazocine, but these drugs were considerably more difficult to antagonize than was morphine. Thus, the interactions between these drugs and the narcotic antagonists allow the classification of the drugs into three groups, based on a marked shift, a moderate shift or no shift in the dose-response curve. This classification is consistent with the hypothesis of Martin et al., (Journal of Pharmacology and Experimental Therapeutics, 197: 517-532, 1976) regarding distinct receptors for morphine and related drugs (mu agonists), ketocyclazocine and ethylketocyclazocine (kappa agonists) and SKF-10,047 (sigma agonist).
在以固定间隔5分钟呈现食物的实验安排下，对大鼠测试了吗啡、布托啡诺、环唑辛、酮环唑辛、乙基酮环唑辛和SKF - 10,047单独使用以及与纳洛酮或纳曲酮联合使用时的效果。除纳洛酮和纳曲酮外，所有药物均以剂量依赖的方式降低了平均反应率。纳曲酮显著拮抗了吗啡的反应率降低作用，而纳曲酮或纳洛酮并未拮抗SKF - 10,047或高剂量环唑辛的作用。纳曲酮和纳洛酮能够拮抗布托啡诺、酮环唑辛、乙基酮环唑辛和低剂量环唑辛的作用，但这些药物比吗啡更难被拮抗。因此，根据剂量 - 反应曲线的显著偏移、适度偏移或无偏移，这些药物与麻醉拮抗剂之间的相互作用可将药物分为三组。这种分类与Martin等人（《药理学与实验治疗学杂志》，197: 517 - 532, 1976）关于吗啡及相关药物（μ激动剂）、酮环唑辛和乙基酮环唑辛（κ激动剂）以及SKF - 10,047（σ激动剂）的不同受体的假设一致。
