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D-丙氨酸2,D-亮氨酸5-脑啡肽可泛化为由芬太尼产生而非乙基酮环唑新产生的辨别性刺激。

D-Ala2,D-Leu5-enkephalin generalizes to a discriminative stimulus produced by fentanyl but not ethylketocyclazocine.

作者信息

Shearman G T, Herz A

出版信息

Pharmacol Biochem Behav. 1982 Feb;16(2):249-52. doi: 10.1016/0091-3057(82)90157-5.

Abstract

Male Sprague-Dawley rats were trained to discriminate between the effects of saline and either fentanyl (0.04 mg/kg) or ethylketocyclazocine (0.32 mg/kg) by responding on a FR 10 schedule of food reinforcement with a lever on one side of a food cup following a subcutaneous saline injection and responding with a lever on the alternate side following the subcutaneous injection of one of those drugs. The effects of an intracerebroventricular injection of either fentanyl (2.89-14.45 nmol) or D-Ala2,D-Leu5-enkephalin (0.172-1.72 nmol) dose-dependently generalized to the discriminative stimulus produced by fentanyl injected subcutaneously. Intracerebroventricular injection of ethylketocyclazocine (15.7-125.8 nmol) but not D-Ala2,D-Leu5-enkephalin (1.72-13.76 nmol) dose-dependently generalized to the discriminative stimulus produced by ethylketocyclazocine injected subcutaneously. These data demonstrate similarities in the discriminative stimulus properties of proposed micron and delta but not kappa and delta opiate receptor agonists.

摘要

雄性斯普拉格-道利大鼠经过训练,通过在皮下注射生理盐水后在食杯一侧的杠杆上按FR 10食物强化程序做出反应,以及在皮下注射上述药物之一后在另一侧杠杆上做出反应,来区分生理盐水与芬太尼(0.04毫克/千克)或乙基酮环唑辛(0.32毫克/千克)的作用。脑室内注射芬太尼(2.89 - 14.45纳摩尔)或D-丙氨酸2,D-亮氨酸5-脑啡肽(0.172 - 1.72纳摩尔)的作用呈剂量依赖性地泛化到皮下注射芬太尼所产生的辨别性刺激。脑室内注射乙基酮环唑辛(15.7 - 125.8纳摩尔)而非D-丙氨酸2,D-亮氨酸5-脑啡肽(1.72 - 13.76纳摩尔)的作用呈剂量依赖性地泛化到皮下注射乙基酮环唑辛所产生的辨别性刺激。这些数据表明,所提出的μ型和δ型而非κ型和δ型阿片受体激动剂在辨别性刺激特性方面存在相似性。

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