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用3H—QNB测定体外培养心肌细胞的M受体,得到典型的饱和曲线,培养2至8天内M受体密度稳定在一定水平。培养液中加三碘甲状原氨酸使M受体密度降低,且有剂量依赖关系;同时加知母皂甙元的琥珀酰衍生物S-ZMS,浓度递增至10 ̄(-5)mol/L以上时,能使降低的M受体密度提高到接近正常水平。S-ZMS单独加于培养液中对M受体无上调或下调作用,对 ̄3H-QNB与心肌M受体的结合也无竞争作用,所以是不同于激动剂或拮抗剂的心肌M受体调节药
The 3M-QNB was used to measure the M receptor of cultured cardiomyocytes in vitro and a typical saturation curve was obtained. The M receptor density was stable at a certain level within 2 to 8 days of culture. The addition of triiodothyronine to the culture medium reduced the M-receptor density in a dose-dependent manner; at the same time, it added the S-ZMS, a succinyl derivative of saponin, to the concentration of 10 ( (-5) mol/L. Above, the reduced M receptor density can be increased to near normal levels. S-ZMS alone added to the culture medium did not up-regulate or down-regulate M-receptors, nor did it have a competitive effect on the binding of 3H-QNB to the myocardium M-receptor, so it is a differentiating cardiomyocyte M-receptor than an agonist or antagonist. Regulatory drugs