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目的 :观察 ZMA ,QST,QT对 M1 受体及其偶联 G-蛋白结合功能的影响。方法 :以 CH Om 1细胞为模型在使用不同药时 ,用放射配基结合分析法检测 M1 受体密度 ,以非 GTP ase水解的 [35 S] GTPγS与 G-蛋白的不可逆结合检测 G-蛋白的结合活性 ,并计算偶联比率 ;以 Western blot方法检测 Gq/1 1α的量。结果 :ZMA10 - 5 m ol/L 及 QST10 - 5 m ol/L 能够提高M1 受体、M1 受体偶联的 G-蛋白的活性。并改善其偶联比率。Q ST10 - 5 m ol/L 还能够提高 Gq/1 1α的量。结论 :ZMA和 QST作用机理可能不同 :ZMA促进偶联的机理很可能主要是提高 M1 受体后 G -蛋白的结合活性提高 ,并且改善 M1 受体和Gq/1 1α的偶联。Q ST可能还与促进 Gq/1 1α合成有关。
Objective: To observe the effect of ZMA, QST and QT on the binding function of M1 receptor and its coupling G-protein. METHODS: Using CH Om 1 cells as models, M1 receptor densities were measured using radioligand binding assays, and G-proteins were detected by irreversible binding of [35 S] GTPγS and G-proteins hydrolyzed by non-GTP ases. The binding activity was calculated and the coupling ratio was calculated; the amount of Gq/1 1α was detected by Western blot. RESULTS: ZMA10 - 5 m ol/L and QST10 - 5 m ol/L could increase the activity of M1 receptor and M1 receptor-coupled G-protein. And improve its coupling ratio. Q ST10 - 5 m ol/L can also increase the amount of Gq/1 1α. Conclusion: The mechanism of action of ZMA and QST may be different: The mechanism of ZMA promoting coupling is likely to increase the binding activity of G-protein after M1 receptor, and improve the coupling of M1 receptor and Gq/1 1α. Q ST may also be involved in promoting the synthesis of Gq/1 1α.