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酮唑新、乙基酮唑新和非那佐辛对程序控制行为的影响:纳洛酮的拮抗作用。

Effects of ketazocine, ethylketazocine and phenazocine on schedule-controlled behavior: antagonism by naloxone.

作者信息

Leander J D

出版信息

Neuropharmacology. 1982 Sep;21(9):923-8. doi: 10.1016/0028-3908(82)90085-5.

Abstract

Dose-effect curves were determined for phenazocine (0.64-2.5 mg/kg), ketazocine (1.25-80 mg/kg) and ethylketazocine (1.25-80 mg/kg) in pigeons responding under a multiple fixed-ratio 30-response, fixed-interval 5-min schedule of grain presentation. All three opioid agonists decreased responding with the larger doses. The effects of phenazocine were completely antagonized by small doses of naloxone (0.01-1 mg/kg), whereas the effects of ethylketazocine required larger doses of naloxone (1-10 mg/kg) to be completely antagonized. The behavioral effects of ketazocine were partially attenuated by naloxone, but were not antagonized completely even by a 10 mg/kg dose of naloxone. These data from the pigeon are consistent with previous interpretations that the effects of phenazocine are mediated by actions at a mu opioid receptor, whereas the effects of ketazocine and ethylketazocine are mediated by actions at a kappa opioid receptor.

摘要

在鸽子按照多重固定比率30次反应、固定间隔5分钟的谷物呈现时间表做出反应的情况下,测定了非那佐辛(0.64 - 2.5毫克/千克)、凯他佐辛(1.25 - 80毫克/千克)和乙基凯他佐辛(1.25 - 80毫克/千克)的剂量效应曲线。所有三种阿片类激动剂在较大剂量时都会减少反应。小剂量的纳洛酮(0.01 - 1毫克/千克)可完全拮抗非那佐辛的作用,而乙基凯他佐辛的作用需要较大剂量的纳洛酮(1 - 10毫克/千克)才能完全拮抗。凯他佐辛的行为效应被纳洛酮部分减弱,但即使给予10毫克/千克剂量的纳洛酮也不能完全拮抗。来自鸽子的这些数据与先前的解释一致,即非那佐辛的作用是通过对μ阿片受体的作用介导的,而凯他佐辛和乙基凯他佐辛的作用是通过对κ阿片受体的作用介导的。

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