胍丁胺抗大鼠身体依赖作用与阿片受体的关系

RELATIONSHIP BETWEEN INHIBITION OF AGMATINE ON RAT MORPHINE PHYSICAL DEPENDENCE AND OPIATE RECEPTORS

目的··：观察胍丁胺抗大鼠身体依赖作用与阿片受体间的关系。方法··：本文实验采用大鼠身体依赖实验和放射配体结合实验两种方法进行。结果··：胍丁胺虽然能剂量依赖性地抑制纳洛酮催促所引起的吗啡依赖大鼠戒断反应，但对３Ｈ－纳洛酮与大鼠前脑阿片受体结合反应无抑制作用（无直接作用），亦不能影响当身体依赖发生时阿片受体对配体的亲和力下降和受体数量下调等代偿性适应变化（无间接作用）。结论··：虽然胍丁胺能抑制阿片类药物身体依赖，但对阿片受体既无直接也无间接作用。

Objective: To observe the relationship between the inhibitory effects of agmatine on rat physical dependence and opioid receptors. Method: The experiments were performed with rat physical dependent test and radiant ligand binding assay. Result: Although agmatine could inhibit the abstinent syndromes of morphine dependent rats precipitated by naloxone in dose-dependent manner, it had neither effect on the binding of 3H-naloxone with opiate receptors in rat forebrain (direct effect) nor influence on the adaptation (indirect effect) characterized by the decrease in affinity of opiate receptors to ligand and down-regulation of receptors which took place in the formative process of physical dependence of opioids. Conclusion: Although agmatine can inhibit rat physical dependence on morphine, it has neither direct nor indirect action on opiate receptors.