Laurent S, Schmitt H
Eur J Pharmacol. 1983 Dec 9;96(1-2):165-9. doi: 10.1016/0014-2999(83)90547-2.
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.
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。