Kiiatkin E A, Zhukov V N
Biull Eksp Biol Med. 1987 Dec;104(12):692-5.
A significant enhancement of the analgetic effect of morphine (6 mg/kg, subcutaneously; tail withdrawal reflex at 60 degrees C) was observed in rats 3-4 hours after single naloxone (1 mg/kg) administration. Periodical naloxone injection (0.5 mg/kg, subcutaneously, 3 times per day at 3.5-hour intervals for 3 days) led to a prominent and long-term (testing on the 20th and 105th hour after the last naloxone administration) enhancement of morphine analgesia (2.6 mg/kg subcutaneously) and insignificant inhibition of stress analgesia during two-hour immobilization of animals. These modifications of morphine and stress analgetic effects are considered a result of adaptive changes of opiate receptors after their blockade.
单次给予纳洛酮(1毫克/千克)3至4小时后,观察到大鼠吗啡(6毫克/千克,皮下注射;60摄氏度热尾甩反射)镇痛效果显著增强。定期注射纳洛酮(0.5毫克/千克,皮下注射,每天3次,间隔3.5小时,共3天)导致吗啡镇痛(2.6毫克/千克,皮下注射)显著且长期增强(在最后一次给予纳洛酮后第20小时和105小时进行测试),并且在动物两小时固定过程中对应激镇痛的抑制作用不显著。吗啡和应激镇痛作用的这些改变被认为是阿片受体阻断后适应性变化的结果。