李仪奎, 金若敏, 陈长勋, 王筠默. 氯甲左箭毒的受体动力学研究J. 药学学报, 1984, 19(4): 241-244.
引用本文: 李仪奎, 金若敏, 陈长勋, 王筠默. 氯甲左箭毒的受体动力学研究J. 药学学报, 1984, 19(4): 241-244.
LI Yi-kui, JIN Ruo-min, CHEN Chang-xun , WANG Yun-mo, . STUDIES ON THE DRUG-RECEPTOR KINETICS OF DIMETHYLCURINE METHYLCHLORIDEJ. Acta Pharmaceutica Sinica, 1984, 19(4): 241-244.
Citation: LI Yi-kui, JIN Ruo-min, CHEN Chang-xun , WANG Yun-mo, . STUDIES ON THE DRUG-RECEPTOR KINETICS OF DIMETHYLCURINE METHYLCHLORIDEJ. Acta Pharmaceutica Sinica, 1984, 19(4): 241-244.

氯甲左箭毒的受体动力学研究

STUDIES ON THE DRUG-RECEPTOR KINETICS OF DIMETHYLCURINE METHYLCHLORIDE

  • 摘要: 本文研究了氯甲左箭毒(DMC)对N2受体的拮抗作用,并以氯化筒箭毒碱(d-TC)为对照。在DMC作用下,ACh对蟾蜍腹直肌的累积剂量—效应%曲线平行右移,测得其pA2=5.472,KB=0.363±0.011(±SE),而d-TC则分别为5.635和0.258±0.010。以log(x-1)对DMC对M的负对数(-logB)作图,其回归线斜率=-0.96,同竞争性拮抗剂的理论斜率-1十分接近。此外,不管DMC的浓度如何,所计算得的KB值基本不变。上述结果证明,DMC对N2受体的拮抗性质确为竞争性拮抗,其对N2受体的亲和力约为d-TC的70%。

     

    Abstract: The drug-receptor interactions of dimethylcurine methylchloride (DMC) with toad rectus abdominis N2-receptor were studied and compared with that of dtubocurarine chloride (d-TC). The antagonism of DMC to the ACh induced muscle contractions was completely overcome by increasing the concentration of ACh and the dose-cumulative-effect curves were parallel. The pA2 values of DMC and d-TC were 5.472 and 5.635 respectively. The KB 's of DMC and d-TC were 0.363±0.011 (±SE) and 0.258±0.010 respectively. When the dose ratios log (X-1) were plotted versus negative log molar values of DMC (Schild plot), the regression slope was -0.96, very close to the theoretical value -1.0 of competitive antagonist. The calculated KB's of different concentrations of DMC were approximately the same. These results strongly suggest that the DMC is a competitive antagonist and its affinity is about 70% that of d-TC on toad rectus abdominis.

     

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