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对μ或δ受体有选择性的阿片肽的行为效应。II. 非依赖性和吗啡依赖性大鼠的运动活性

Behavioral effects of opioid peptides selective for mu or delta receptors. II. Locomotor activity in nondependent and morphine-dependent rats.

作者信息

Locke K W, Holtzman S G

出版信息

J Pharmacol Exp Ther. 1986 Sep;238(3):997-1003.

PMID:3018231
Abstract

The i.c.v. administration of opioid peptides having selectivity for the mu receptor (D-Ala2-NMePhe4-Gly5(ol)enkephalin and FK 33,824) produced effects on the locomotor activity of nondependent and morphine-dependent rats that differed both quantitatively and qualitatively from those effects produced by peptides having selectivity for the delta receptor (D-Ala2-D-Leu5enkephalin and metkephamid) and beta-endorphin, which has similar affinity for both receptors. Peptides selective for the mu receptor: had a biphasic effect on locomotor activity of nondependent rats, inducing an increase at low doses and an initial decrease followed by a later increase at higher doses and had an enhanced stimulant effect on locomotor activity with tolerance to the depressant effect in morphine-dependent rats. Peptides selective for the delta receptor and beta-endorphin: induced only a dose-related increase in the locomotor activity of nondependent rats and had effects on the locomotor activity of morphine-dependent rats that did not differ substantially from those in nondependent rats. Naltrexone (0.1 mg/kg s.c.) and beta-funaltrexamine (5.0 micrograms/rat i.c.v.), an irreversible antagonist, each blocked to a comparable extent the effects of D-Ala2-NMePhe4-Gly5(ol)enkephalin and DAla2-D-Leu5enkephalin on the locomotor activity of nondependent rats. Thus, effects of opioid peptides that act predominantly at mu or delta receptors on locomotor activity cannot be differentiated in nondependent rats by antagonists but can be differentiated in morphine-dependent rats. These results suggest that the depressant and stimulant effects of opioid peptides on locomotor activity are mediated by distinct neuronal sites.

摘要

向脑室内注射对μ受体具有选择性的阿片肽（D - Ala2 - NMePhe4 - Gly5(ol)脑啡肽和FK 33,824），对非依赖性和吗啡依赖性大鼠的运动活性产生的影响，在数量和质量上都不同于对δ受体具有选择性的肽（D - Ala2 - D - Leu5脑啡肽和甲硫啡肽）以及对两种受体具有相似亲和力的β - 内啡肽所产生的影响。对μ受体具有选择性的肽：对非依赖性大鼠的运动活性有双相作用，低剂量时诱导增加，高剂量时最初降低随后增加，并且对吗啡依赖性大鼠的运动活性具有增强的刺激作用，同时对其抑制作用产生耐受性。对δ受体具有选择性的肽和β - 内啡肽：仅在非依赖性大鼠中诱导与剂量相关的运动活性增加，并且对吗啡依赖性大鼠运动活性的影响与非依赖性大鼠相比没有实质性差异。纳曲酮（0.1 mg/kg皮下注射）和不可逆拮抗剂β - 氟纳曲胺（5.0微克/大鼠脑室内注射），在相当程度上阻断了D - Ala2 - NMePhe4 - Gly5(ol)脑啡肽和D - Ala2 - D - Leu5脑啡肽对非依赖性大鼠运动活性的影响。因此，在非依赖性大鼠中，拮抗剂无法区分主要作用于μ或δ受体的阿片肽对运动活性的影响，但在吗啡依赖性大鼠中可以区分。这些结果表明，阿片肽对运动活性的抑制和刺激作用是由不同的神经元位点介导的。

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