Vinogradov V A, Polonskiĭ V M
Farmakol Toksikol. 1986 Jan-Feb;49(1):79-81.
The influence of dinorphine 1-6 and naloxone on the appearance of experimental duodenal ulcers, induced by cysteamine, was studied in rats. It was revealed that the 15 micrograms/kg dose of dinorphine 1-6 distinctly blocks the formation of ulcers. Naloxone prevents dose-dependently the effect of dinorphine 1-6 on ulcer-formation, indicating that dinorphine acts through specific opiate receptors. Naloxone itself also shows moderate anti-ulcer activity, that disappears with the increase of the preparation dose. Mechanisms of the paradoxical naloxone action in the given experimental model from the point of view of existence of its own pharmacological activity are being discussed.
研究了二氢吗啡酮1-6和纳洛酮对大鼠半胱胺诱发的实验性十二指肠溃疡外观的影响。结果表明,15微克/千克剂量的二氢吗啡酮1-6能明显阻止溃疡形成。纳洛酮能剂量依赖性地阻止二氢吗啡酮1-6对溃疡形成的作用,表明二氢吗啡酮通过特定的阿片受体起作用。纳洛酮本身也显示出适度的抗溃疡活性,且随着制剂剂量的增加而消失。从其自身药理活性存在的角度,讨论了在给定实验模型中纳洛酮矛盾作用的机制。