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本文研究了氯甲左箭毒(DMC)对N_2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pA_2=5.472,K_B=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(-log[B])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K_B值基本不变。上述结果证明,DMC对N_2受体的拮抗性质确为竞争性拮抗,其对N_2受体的亲和力约为d-TC的70%。
In this paper, we studied the antagonistic effect of DMC on N 2 receptor, and used myostatin (d-TC) as control. Under the action of DMC, the cumulative dose-response curve of ACh to the rectus abdominis muscles of right toad parallel to the right, measured pA_2 = 5.472, K_B = 0.363 ± 0.011 (± SE), while d-TC was 5.635 and 0.258 ± 0.010. The negative logarithm (-log [B]) of DMC versus M was plotted against log (x-1) with a slope of regression line = -0.96, very close to the theoretical slope of competitive antagonist -1. In addition, the calculated K_B value remains essentially the same regardless of the DMC concentration. The above results demonstrate that the antagonistic nature of DMC to N 2 receptor is indeed competitive antagonism and its affinity for N 2 receptor is about 70% of d-TC.