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应用放射配体受体结合试验观察梭曼对[~3H]QNB与大鼠脑组织匀浆和P_2膜制备结合的影响。结果显示,[~3H]QNB与P_2膜制备的结合具有受体与配体结合的典型特征:特异性与饱和性,其K_D=1.03nmol/L,B_(max)=0.16Pmol/mg蛋白,Hill系数~nH=1.0。对于[~3H]QNB与大鼠脑匀浆结合,梭曼在10~(-9)～10~(-7)mol/L浓度时对结合计数有轻度抑制,但没有实际意义,对于[~3H]QNB与大鼠脑组织P_2膜制备结合,梭曼在10~(-13)～10~(-3)mol/L范围内各浓度对结合计数均无明显影响。由此表明,梭曼对放射配体[~3H]QNB与大鼠中枢M-AChR的结合没有竞争抑制作用,从而说明梭曼不与大鼠中枢M-AChR发生直接作用。
Radioligand binding assay was used to observe the effect of soman on the binding of [~ 3H] QNB to rat brain homogenate and P_2 membrane preparation. The results showed that the binding of [~ 3H] QNB and P_2 membrane preparation showed typical characteristics of receptor-ligand binding: specificity and saturation, K_D = 1.03nmol / L, Bmax = 0.16Pmol / mg protein, Hill coefficient ~ nH = 1.0. For the binding of [~ 3H] QNB to rat brain homogenates, somatostatin had a mild inhibitory effect on the binding counts at concentrations of 10 ~ (-9) ~ 10 ~ (-7) mol / L, but no practical significance. ~ 3H] QNB combined with the preparation of P_2 membrane in rat brain tissue. Soman’s concentration in the range of 10 ~ (-13) ~ 10 ~ (-3) mol / L had no significant effect on the binding assay. Thus, soman has no competitive inhibition on the binding of radiosensitizer [-3H] QNB to rat central M-AChR, indicating that soman does not directly interact with rat central M-AChR.