硝苯地平对肝细胞膜胰岛素受体的影响
Effects of nifedipine on insulin receptors in rat hepatocytic membrane
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摘要: 目的: 观察钙拮抗剂硝苯地平(NF)对正常大鼠肝细胞膜胰岛素受体的作用,探讨NF对胰岛素生物学效应的影响。方法: 不同浓度(0 5 μmol/L、1 0 μmol/L和10.0 μmol/L) NF灌注大鼠肝脏,或在胰岛素与大鼠肝细胞膜受体结合的反应体系中加入加入上述浓度NF,用放免法测定受体的结合能力。结果: NF灌注后大鼠肝细胞膜高亲和力胰岛素受体亲和常数(K1)及结合位点浓度(Q1)无显著变化;NF作用于反应体系,高亲和力胰岛素受体亲和常数(K1)及结合位点浓度(Q1)下降。结论: NF直接作用于反应体系,对大鼠肝细胞膜胰岛素受体的结合能力产生一定程度影响。Abstract: Objective: To investigate the effects of calcium antagonist nifedipine(NF)on insulin receptors in rat hepatocytic membrane and explore the effects of NF on biological action of insulin.Methods: Exp 1: The rat livers were perfused with different concentrations of NF(0.5,1 0,and 1 0.0μmol/L),and the preparation of hepatocytic membrane was produced for measuring the binding capacity of insulin receptors by radioimmunoassay Exp 2: The hepatocytic membrane samples from non NF treated were reacted with different concentrations of NF for measuring the binding capacity of insulin receptor.Results: Exp 1 showed that the maximal binding capacity (Bmax),affinity constant (K 1) and binding sites(Q 1) of higher affinity receptor were not influenced by 3 scale concentrations of NF,whereas,the affinity constant(K 2)of lower affinity receptor was elevated in manner of NF dose dependence,and the binding sites(Q 2)of lower affinity receptor were reduced Exp 2 showed that the Bmax,Q 1,Q 2 and K 2 were decreased by 3 scale concentrations of NF in a manner of dose dependence,and the higher concentrations of NF lowered K 1 either.Conclusion: NF influenced the binding capacity of insulin receptor in the hepatocytic membrane at some extent by means of the direct reaction.
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