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κ阿片受体激动剂强啡肽-(1-13)和乙基酮环唑新对麻醉大鼠的中枢心血管效应

Central cardiovascular effects of kappa agonists dynorphin-(1-13) and ethylketocyclazocine in the anaesthetized rat.

作者信息

Laurent S, Schmitt H

出版信息

Eur J Pharmacol. 1983 Dec 9;96(1-2):165-9. doi: 10.1016/0014-2999(83)90547-2.

Abstract

Opiate kappa agonists were administered into the cisterna magna of normotensive urethane-anaesthetized artificially ventilated rats: ethylketocyclazocine (78.7 nM) (EKC) and dynorphin-(1-13) (62.3 nM) produced significant and long-lasting decreases in both blood pressure and heart rate. High doses of naloxone (1 mg/kg i.v.) were required to partially antagonize these effects. The central cardiovascular effects of EKC and dynorphin-(1-13) were compared to those of fentanyl (3 nM), [D-Ala2,Met5]enkephalinamide (17 nM) and beta-endorphin (2.9 nM) which induced increases in blood pressure and heart rate. These results suggest that opposite central cardiovascular effects could be induced by activation of various opiate receptors.

摘要

将阿片κ受体激动剂注入血压正常、经乌拉坦麻醉并人工通气的大鼠的脑池:乙基酮环唑辛(78.7 nM)(EKC)和强啡肽 -(1 - 13)(62.3 nM)可使血压和心率显著且持久地降低。需要高剂量的纳洛酮(1 mg/kg静脉注射)才能部分拮抗这些作用。将EKC和强啡肽 -(1 - 13)的中枢心血管效应与芬太尼(3 nM)、[D - Ala2,Met5]脑啡肽酰胺(17 nM)和β - 内啡肽(2.9 nM)的效应进行比较,后三者可使血压和心率升高。这些结果表明,激活各种阿片受体可诱发相反的中枢心血管效应。

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