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丁丙诺啡的阿片类激动剂和拮抗剂行为效应

Opioid agonist and antagonist behavioural effects of buprenorphine.

作者信息

Leander J D

出版信息

Br J Pharmacol. 1983 Apr;78(4):607-15. doi: 10.1111/j.1476-5381.1983.tb09410.x.

Abstract

1 The agonist and antagonist effects of a range of buprenorphine doses (0.08-20 mg/kg) were studied on the responding of pigeons under a multiple fixed-ratio, fixed-interval schedule of grain presentation. Various doses (0.02-10 mg/kg) of buprenorphine were also tested in pigeons trained to discriminate between injections of 0.05 mg/kg of fentanyl and injections of distilled water. 2 Buprenorphine, over a broad dose range (0.08-5 mg/kg), increased the rates of responding in the fixed-interval component of the multiple schedule and disrupted patterning of responding within the fixed-interval, without affecting fixed-ratio responding even at a dose of 40 mg/kg. The effects of some of the high doses on fixed-interval responding were still evident one and two days after buprenorphine injection. 3 Doses of buprenorphine which produced increases in fixed-interval responding were also effective as antagonists of the behavioural depression produced by 40 mg/kg of morphine, and were discriminated as fentanyl-like by pigeons trained to discriminate between injections of fentanyl and injections of water. 4 These results show that buprenorphine produces marked agonist and antagonist effects over an extremely broad dose range without producing behavioural depressant effects.

摘要
  1. 研究了一系列丁丙诺啡剂量(0.08 - 20毫克/千克)对鸽子在多种固定比率、固定间隔谷物投喂时间表下反应的激动剂和拮抗剂作用。还对经训练能区分注射0.05毫克/千克芬太尼和注射蒸馏水的鸽子测试了各种剂量(0.02 - 10毫克/千克)的丁丙诺啡。2. 在很宽的剂量范围(0.08 - 5毫克/千克)内,丁丙诺啡增加了多种时间表中固定间隔部分的反应率,并扰乱了固定间隔内的反应模式,即使在40毫克/千克的剂量下也不影响固定比率反应。丁丙诺啡注射后一天和两天,一些高剂量对固定间隔反应的影响仍然明显。3. 产生固定间隔反应增加的丁丙诺啡剂量,也可作为40毫克/千克吗啡所致行为抑制的拮抗剂,并且经训练区分芬太尼注射和水注射的鸽子将其辨别为类似芬太尼。4. 这些结果表明,丁丙诺啡在极宽的剂量范围内产生明显的激动剂和拮抗剂作用,而不产生行为抑制作用。

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