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麻醉拮抗剂喷他佐辛的刺激特性:与吗啡相似及纳洛酮的拮抗作用

Stimulus properties of the narcotic antagonist pentazocine: similarity to morphine and antagonism by naloxone.

作者信息

Kuhn D M, Greenberg I, Appel J B

出版信息

J Pharmacol Exp Ther. 1976 Jan;196(1):121-7.

PMID:1246006
Abstract

Pentazocine (10 mg/kg) and saline were used as discriminative stimuli in rats. After pentazocine administration, reinforcement could be obtained contingent on pressing one particular lever (left or right) in a two-lever operant chamber. Responding on the opposite lever was reinforced only after saline injections; a drug-lever combination was always held constant for each animal. Discriminated choice responding between pentazocine and saline was learned to an 80% correct criterion. Test injections of morphine produced dose-related responding on the pentazocine lever. Choice responding after 7.5 mg/kg of morphine was not significantly different from choice responding after 10 mg/kg of pentazocine. The discriminable ED50 values for both pentazocine and morphine were estimated from dose-response curves and when given in combination (pentazocine ED50 + morphine ED50), more drug-related responding occurred than occurred after either drug (ED50) alone. Naloxone produced saline-like responding but antagonized the stimulus properties of both pentazocine and morphine. However, the antagonism of the morphine cue by naloxone was significantly greater than the antagonism of the pentazocine cue. The results indicate that pentazocine and morphine are similar in at least one important respect suggesting that these drugs may share a common site of action.

摘要

喷他佐辛(10毫克/千克)和生理盐水被用作大鼠的辨别性刺激物。给予喷他佐辛后,在双杠杆操作性条件反射箱中按压一个特定杠杆(左或右)即可获得强化。只有在注射生理盐水后,对另一侧杠杆的反应才会得到强化;每种动物的药物-杠杆组合始终保持不变。以80%正确标准学会了对喷他佐辛和生理盐水的辨别性选择反应。吗啡的测试注射在喷他佐辛杠杆上产生了剂量相关的反应。7.5毫克/千克吗啡后的选择反应与10毫克/千克喷他佐辛后的选择反应没有显著差异。根据剂量-反应曲线估计了喷他佐辛和吗啡的可辨别半数有效剂量(ED50)值,当联合给药时(喷他佐辛ED50+吗啡ED50),与单独给予任何一种药物(ED50)相比,出现了更多与药物相关的反应。纳洛酮产生了类似生理盐水的反应,但拮抗了喷他佐辛和吗啡的刺激特性。然而,纳洛酮对吗啡线索的拮抗作用明显大于对喷他佐辛线索的拮抗作用。结果表明,喷他佐辛和吗啡在至少一个重要方面相似,这表明这些药物可能有共同的作用位点。

相似文献

1
Stimulus properties of the narcotic antagonist pentazocine: similarity to morphine and antagonism by naloxone.麻醉拮抗剂喷他佐辛的刺激特性:与吗啡相似及纳洛酮的拮抗作用
J Pharmacol Exp Ther. 1976 Jan;196(1):121-7.
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Intermediate efficacy mu opioids: examination of their morphine-like stimulus effects and response rate-decreasing effects in morphine-tolerant rats.中等效力的μ阿片类药物:在吗啡耐受大鼠中对其吗啡样刺激效应和反应率降低效应的研究。
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The discriminative stimulus properties of cyclazocine: generalization studies involving nalorphine, morphine and LSD.环唑辛的辨别刺激特性:涉及烯丙吗啡、吗啡和麦角酸二乙胺的泛化研究。
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Pentazocine, cyclazocine, and nalorphine as discriminative stimuli.喷他佐辛、环唑辛和烯丙吗啡作为辨别刺激物。
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Morphine, pentazocine and naloxone effects on responding under a multiple schedule of reinforcement in rhesus monkeys and pigeons.吗啡、喷他佐辛和纳洛酮对恒河猴和鸽子在多重强化程序下反应的影响。
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Discriminative effects of morphine in the squirrel monkey.吗啡对松鼠猴的辨别效应。
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Effects of morphine, pentazocine and cyclazocine alone and in combination with naloxone on electric shock titration in the squirrel monkey.吗啡、喷他佐辛和环佐辛单独及与纳洛酮联合应用对松鼠猴电击滴定的影响。
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引用本文的文献

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Empirical evidence that the state dependence and drug discrimination paradigms can generate different outcomes.有经验证据表明状态依赖性和药物辨别范式会产生不同的结果。
Psychopharmacology (Berl). 1995 Aug;120(3):272-9. doi: 10.1007/BF02311174.
2
Asymmetrical effects of morphine and naloxone on reward mechanisms.吗啡和纳洛酮对奖赏机制的不对称作用。
Psychopharmacology (Berl). 1982;78(3):219-24. doi: 10.1007/BF00428154.
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Psilocybin as a discriminative stimulus: lack of specificity in an animal behavior model for 'hallucinogens'.
裸盖菇素作为一种辨别刺激物:在“致幻剂”动物行为模型中缺乏特异性。
Psychopharmacology (Berl). 1982;76(2):130-5. doi: 10.1007/BF00435266.
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Discriminative stimulus properties of narcotic and non-narcotic drugs in rats trained to discriminate opiate kappa-receptor agonists.在经训练以辨别阿片κ受体激动剂的大鼠中,麻醉性和非麻醉性药物的辨别刺激特性。
Psychopharmacology (Berl). 1982;78(1):63-6. doi: 10.1007/BF00470590.
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Discriminative stimulus properties of naloxone.纳洛酮的辨别刺激特性。
Psychopharmacology (Berl). 1982;77(4):305-8. doi: 10.1007/BF00432760.
6
Effects of pentazocine and other opiates on shock detection in the rat: involvement of opiate and dopamine receptors.喷他佐辛及其他阿片类药物对大鼠休克检测的影响:阿片受体和多巴胺受体的作用
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7
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Stimulus effects of delta(9)-THC and its interaction with naltrexone and catecholamine blockers in rats.大鼠中δ-9-四氢大麻酚的刺激作用及其与纳曲酮和儿茶酚胺阻滞剂的相互作用
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