MR2266和MR2267对大鼠脊髓水平吗啡或纳布啡镇痛的拮抗作用。

Antagonistic effect of MR2266 and MR2267 on morphine or nalbuphine analgesia at the spinal levels in rats.

作者信息

Kmieciak-Kołada K, Spiewak Z, Urbanowicz A, Pawłowski J, Herman Z S

机构信息

Department of Clinical Pharmacology, Silesian Academy of Medicine, Katowice, Poland.

出版信息

Pol J Pharmacol. 1995 Nov-Dec;47(6):509-18.

PMID:8868373

Abstract

The aim of this paper was to study the effect of two benzomorphan derivatives MR2266 and MR2267 with predominant antagonism to kappa-opioid receptors administered intrathecally on the analgesic action of morphine and nalbuphine. Both compounds attenuated the analgesia elicited by examined opioid agonists. Our results support the hypothesis that the spinal opioid receptors take part in analgesic effect of morphine and nalbuphine. It was for the first time described that MR2267, considered as inactive enantiomer of MR2266, is an active opioid antagonist when administered intrathecally.

摘要

本文的目的是研究鞘内注射两种主要拮抗κ-阿片受体的苯并吗啡烷衍生物MR2266和MR2267对吗啡和纳布啡镇痛作用的影响。两种化合物均减弱了受试阿片类激动剂引起的镇痛作用。我们的结果支持以下假设：脊髓阿片受体参与吗啡和纳布啡的镇痛作用。首次报道，被认为是MR2266无活性对映体的MR2267在鞘内给药时是一种活性阿片拮抗剂。