脑M受体生成和降解速率测定方法的建立

The determination of the production and degradation rate of brain M-cbolinergic receptors

本文报道整体应用M胆碱能受体的选择性烷化剂BCM不可逆地阴断已存在的脑M受体,然后用放射配基结合分析法观察脑内新生M受体的时相变化,计算代谢动力学参数。实验测得三批正常成年Balb-c小鼠脑M受体的动力学参数甚为接近,平均生成速率(Pr)=37.34fmol/(mg·h),半更新时间(t_(1/2)=19.82h,降解速率常数(Kd)=0.03501/h。脑M受体的生或降解速率测定方法系首次报道,对探讨疾病时脑M受体变化的机理及药物作用机制是一种有用的技术。

A technique for the determination of the production and degradation rates of mouse brain M-receptors was established. The selective alkylating ager.t BCM was given in vivo to irreversibly inhibit the M-receptors and the 3H-QNB binding assay was used to monitor the time-related increase of newly synthesized receptors. A tracer kinetics mathematical model was used to calculate the parameters. The results of three separate experiments with Balb-C mice were close to each other, the average production rate being 37.34fmol/mg protein/h, the average degradation rate constant being 0.035/h, and the half-time being 19.82h. The significance of this technique in the study of the mechanism of pathological changes in brain M-receptors and drug actions was discussed.