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纳洛芬对慢性脊髓犬的西格玛效应。

Sigma effects of nalorphine in the chronic spinal dog.

作者信息

Gilbert P E, Martin W R

出版信息

Drug Alcohol Depend. 1976 Oct;1(6):373-6. doi: 10.1016/0376-8716(76)90001-6.

Abstract

The effects of graded doses of nalorphine and morphine were studied in nondependent chronic spinal dogs. Morphine and low doses of nalorphine produced behavioral changes characterized by indifference, whereas the largest dose of nalorphine produced canine delirium indistinguishable from that produced by SKF-10, 047 or cyclazocine. Nalorphine depressed the flexor reflex; however, a plateau was observed. The data suggest that nalorphine is a partial agonist of the kappa type and a sigma agonist in addition to being a competitive antagonist at the mu receptor, and further, that the dysphoric and hallucinogenic effects of nalorphine-like drugs are due to their sigma activity.

摘要

在非依赖性慢性脊髓犬中研究了不同剂量纳洛啡和吗啡的作用。吗啡和低剂量纳洛啡产生以淡漠为特征的行为变化,而最大剂量的纳洛啡产生的犬谵妄与SKF-10,047或环唑辛产生的难以区分。纳洛啡抑制屈肌反射;然而,观察到一个平台期。数据表明,纳洛啡除了是μ受体的竞争性拮抗剂外,还是κ型部分激动剂和σ激动剂,此外,纳洛啡样药物的烦躁不安和致幻作用归因于它们的σ活性。

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