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中缝正中核参与吗啡、丁丙诺啡和替利定诱导的大鼠抗伤害感受作用。

Involvement of the median raphe nucleus in antinociception induced by morphine, buprenorphine and tilidine in the rat.

作者信息

Bryant R M, Olley J E, Tyers M B

出版信息

Br J Pharmacol. 1982 Dec;77(4):615-24. doi: 10.1111/j.1476-5381.1982.tb09339.x.

Abstract

1 Antinociception induced by three analgesics with differing profiles of activity, morphine, buprenorphine and tilidine, have been evaluated in the hot plate and paw pressure tests after administration by the subcutaneous route and directly into the median raphe nucleus in the conscious rat. 2 Behavioural and neurological effects of the three analgesics were also assessed. 3 The typical profiles of antinociceptive activity induced by the three analgesics were qualitatively similar after either route of administration. Morphine induced naloxone-sensitive dose-dependent effects in both tests. Buprenorphine showed naloxone-sensitive effects with a bell-shaped dose-response curve in the thermal test but dose-dependent activity in the pressure test. Tilidine induced naloxone-sensitive dose-dependent effects in the thermal test but demonstrated naloxone-insensitive activity in the paw pressure test. 4 The behavioural and neurological effects of the analgesics in the dose range used would not have affected the animals' ability to respond to the nociceptive stimuli. 5 The results suggest that the median raphe could participate in drug-induced antinociception. The mechanisms by which this might occur are discussed.

摘要
  1. 通过皮下给药以及直接注入清醒大鼠的中缝核,在热板试验和爪压试验中评估了吗啡、丁丙诺啡和替利定这三种具有不同活性特征的镇痛药所诱导的抗伤害感受作用。2. 还评估了这三种镇痛药的行为和神经学效应。3. 两种给药途径后,三种镇痛药诱导的抗伤害感受活性的典型特征在性质上相似。吗啡在两项试验中均诱导出对纳洛酮敏感的剂量依赖性效应。丁丙诺啡在热试验中表现出对纳洛酮敏感的效应,剂量 - 反应曲线呈钟形,但在压力试验中呈剂量依赖性活性。替利定在热试验中诱导出对纳洛酮敏感的剂量依赖性效应,但在爪压试验中表现出对纳洛酮不敏感的活性。4. 所用剂量范围内的镇痛药的行为和神经学效应不会影响动物对伤害性刺激作出反应的能力。5. 结果表明中缝核可能参与药物诱导的抗伤害感受作用。讨论了这种情况可能发生的机制。

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本文引用的文献

8
The role of the gut in the metabolism of strong analgesics.肠道在强效镇痛药代谢中的作用。
Biochem Pharmacol. 1976 Mar 15;25(6):735-41. doi: 10.1016/0006-2952(76)90255-0.

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