Kriván M, Szabó G, Sarnyai Z, Kovács G L, Telegdy G
Department of Pathophysiology, Albert Szent-Györgyi Medical University, Szeged, Hungary.
Pharmacol Biochem Behav. 1992 Sep;43(1):187-92. doi: 10.1016/0091-3057(92)90656-z.
The development of cross-tolerance to an analgesic effect has been observed between a mu-receptor agonist, heroin, and a delta-receptor agonist, Met2-Pro5-enkephalinamide. Repeated treatments with heroin twice a day for 4 days resulted in a decreased nociceptive effect to enkephalin on day 5. The enkephalin dose-response line was shifted to the right, considered a sign of the development of cross-tolerance. Peripheral treatment with oxytocin blocked the development of heroin-enkephalin cross-tolerance. A similar effect was observed after intracerebroventricular administration of oxytocin, supporting our assumption that oxytocin blocks the development of heroin-enkephalin cross-tolerance via CNS mechanisms.
已观察到μ受体激动剂海洛因和δ受体激动剂甲硫氨酸脑啡肽之间对镇痛作用产生了交叉耐受性。每天两次用海洛因重复治疗4天,导致在第5天对脑啡肽的伤害感受作用降低。脑啡肽剂量反应线向右移动,这被认为是交叉耐受性发展的标志。外周给予催产素可阻断海洛因 - 脑啡肽交叉耐受性的发展。脑室内给予催产素后也观察到类似效果,这支持了我们的假设,即催产素通过中枢神经系统机制阻断海洛因 - 脑啡肽交叉耐受性的发展。