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目的:用表达人μ受体的Sf9昆虫细胞(Sf9-μ细胞)研究二氢埃托啡、芬太尼、海洛因和哌替啶对μ受体亲和力与依赖性。方法:竞争结合实验检测受体亲和力;放免法删定cAMP;热板法测痛;纳洛酮催促跳跃评价身体依赖性。结果:Sf9-μ细胞经上述药物孵育后,纳洛酮引起cAMP超射,以结合实验中K_i值与cAMP超射实验中的EC_(50)值之比作为药物在Sf9-μ细胞的依赖性指数,以镇痛FD_(50)与戒断反应中累积剂量的ED_(50)之比作为小鼠身体依赖性指数,上述药物的两种依赖性指数之间以及受体亲和力与镇痛活性之间有较好的相关性。结论:Sf9-μ细胞可用来评价阿片类约物的受体亲和力及依赖潜能。
OBJECTIVE: To investigate the affinity and dependence of dihydroetorphine, fentanyl, heroin and pethidine on μ receptors using Sf9 insect cells (Sf9-μ cells) expressing the human μ receptor. METHODS: The competitive binding assay was used to detect the receptor affinity. The cAMP was removed by radioimmunoassay. The analgesic was measured by hot plate method. Naloxone was used to evaluate the body dependence. RESULTS: Naloxone caused cAMP hyperosmolarity after Sf9-μ cells were incubated with the above drugs. The ratio of K_i in the binding assay to the value of EC 50 in the cAMP superinjection assay was used as the drug’s dependence on Sf9-μ cells The ratio of analgesic FD_ (50) to cumulative dose ED_ (50) in withdrawal response was used as the mouse body-dependence index, and the dependence between the two drugs and the receptor affinity and analgesic activity There is a good correlation between. Conclusion: Sf9-μ cells can be used to assess the receptor affinity and reliance potential of opioid.