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1. 上海第二医科大学基础医学院
2. 浙江医科大学药学系
3. 上海第二医科大学基础医学院 90届毕业实习生
纸质出版日期:1991-05-01
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[1]胡雅儿,夏宗勤,卞以洁,潘镇球,潘晓红,易宁育.脑M受体生成和降解速率测定方法的建立[J].核技术,1991(05):285-290.
Hu Yaer Xia zongqin Bian Yijie Pan ZhenqiuPan Xiaohong Yi Ningyu. The determination of the production and degradation rate of brain M-cbolinergic receptors[J]. Nuclear techniques, 1991, (5): 285-290.
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.
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