Dykstra L A
J Pharmacol Exp Ther. 1985 Oct;235(1):20-5.
The effects of buprenorphine were examined under a shock titration procedure and compared to the effects of morphine. Under this procedure shock increased every 15 sec from 0 to 2.0 mA in 30 increments. Five responses within a 15-sec shock period decreased shock intensity by one increment. Both buprenorphine and morphine increased the level at which shock was maintained without decreasing rates of responding in the presence of shock. Buprenorphine-induced increases in median shock level occurred over a 10-fold dose range and were apparent for 6 to 12 hr. Dose-effect curves for morphine and buprenorphine were shifted to the right by prior administration of diprenorphine (0.001-1.0 mg/kg), naloxone (0.001-1.0 mg/kg) and beta-funaltrexamine (1.0-16.0 mg/kg), with the dose of antagonist required to restore responding to control levels being 1 to 2 log U larger for buprenorphine than for morphine. Buprenorphine-induced increases in median shock level were also restored to control levels when naloxone (1.0 mg/kg) was administered as much as 110 min after buprenorphine. Buprenorphine was not effective in antagonizing the effects of morphine. When a dose of buprenorphine which increased median shock level was administered once daily, median shock levels returned to control level within 6 to 15 days. When the morphine dose-effect curve was then redetermined in the presence of chronic buprenorphine, it exhibited a 10-fold shift to the right.
在休克滴定程序下研究了丁丙诺啡的作用，并与吗啡的作用进行了比较。在此程序中，休克强度每15秒从0增加到2.0毫安，共30个增量。在15秒的休克期内有五次反应可使休克强度降低一个增量。丁丙诺啡和吗啡均提高了休克维持水平，且在有休克存在时不降低反应率。丁丙诺啡引起的中位休克水平升高发生在10倍剂量范围内，且在6至12小时内明显。吗啡和丁丙诺啡的剂量-效应曲线在预先给予二丙诺啡（0.001 - 1.0毫克/千克）、纳洛酮（0.001 - 1.0毫克/千克）和β-氟纳曲胺（1.0 - 16.0毫克/千克）后向右移动，恢复反应至对照水平所需的拮抗剂剂量，丁丙诺啡比吗啡大1至2个对数单位。当在丁丙诺啡给药后长达110分钟给予纳洛酮（1.0毫克/千克）时，丁丙诺啡引起的中位休克水平升高也恢复到了对照水平。丁丙诺啡在拮抗吗啡的作用方面无效。当给予一次能提高中位休克水平的丁丙诺啡剂量时，中位休克水平在6至15天内恢复到对照水平。当随后在慢性丁丙诺啡存在的情况下重新测定吗啡的剂量-效应曲线时，它向右移动了10倍。
