Coupar J M, Quinn M J
Unit of Addictive Drug Research, Victorian College of Pharmacy, Parkville, Australia.
J Pharm Pharmacol. 1988 May;40(5):378-80. doi: 10.1111/j.2042-7158.1988.tb05274.x.
The effects of the selective kappa-opioid agonist MR 2034 on the guinea-pig ileum were compared with those produced by the mu-agonist morphine. MR 2034 induced acute tolerance and inhibited electrically evoked contractions to the same extent as morphine. The slope of the concentration-effect curve to MR 2034 was not significantly different from that of morphine. However, MR 2034 and morphine may act at their respective receptors since naloxone was 6.57 times more effective at inhibiting responses to morphine than MR 2034. MR 2034, like morphine, induced acute dependence as revealed by naloxone-induced contractions of tissues that had been incubated with MR 2034 for 5 h. The functional properties of kappa-opoid receptors are the same as mu-receptors in the guinea-pig ileum.
将选择性κ-阿片受体激动剂MR 2034对豚鼠回肠的作用与μ-激动剂吗啡所产生的作用进行了比较。MR 2034诱导急性耐受性，并在与吗啡相同的程度上抑制电诱发的收缩。MR 2034浓度-效应曲线的斜率与吗啡的斜率无显著差异。然而，MR 2034和吗啡可能作用于各自的受体，因为纳洛酮抑制对吗啡反应的效力比抑制对MR 2034反应的效力高6.57倍。与吗啡一样，MR 2034也诱导急性依赖性，这可通过纳洛酮诱发经MR 2034孵育5小时的组织收缩来显示。在豚鼠回肠中，κ-阿片受体的功能特性与μ-受体相同。
