Marcus F I, Ryan J N, Stafford M G
J Lab Clin Med. 1975 Apr;85(4):610-20.
Derivatives of digoxin and digitoxin were measured by the Na-K-ATPase displacement assay and by radioimmunoassay and the data compared with biological potency of these compounds. There was a slightly higher affinity of digoxigenin-bis-digitoxoside as compared with digoxin using digoxin-specific antiserum and considerably less affinity of digoxigenin and dihydrodigoxin than the parent compound in the same system. A similar trend was observed for the derivatives of digitoxin using digoxin-specific antiserum. The recovery on extraction of some of the derivatives of digoxin and digitoxin differed from that of the parent compounds in the ATPase assay. The potency of the derivatives of these drugs in displacing 3H ouabain also differed from the parent compoundmboth the recovery on extraction and the potency for displacing ouabain must be considered in the estimation of the contribution of the derivatives of digoxin or digitoxin to the result of Na-K-ATPase assay. Quantitative information of the metabolites of digoxin and digitoxin in normal and pathological conditions is needed to properly interpret assay data obtained either by radioimmunoassay or by ATPase assay.
通过钠钾 - ATP酶置换试验和放射免疫分析法测定了地高辛和洋地黄毒苷的衍生物,并将数据与这些化合物的生物活性进行了比较。使用地高辛特异性抗血清时,洋地黄毒苷双洋地黄毒糖苷与地高辛相比具有略高的亲和力,而在同一系统中,洋地黄毒苷元和二氢地高辛与母体化合物相比亲和力明显较低。使用地高辛特异性抗血清时,洋地黄毒苷的衍生物也观察到类似趋势。在ATP酶试验中,地高辛和洋地黄毒苷的一些衍生物的提取回收率与母体化合物不同。这些药物衍生物置换3H哇巴因的效力也与母体化合物不同,在评估地高辛或洋地黄毒苷衍生物对钠钾 - ATP酶试验结果的贡献时,必须同时考虑提取回收率和置换哇巴因的效力。需要正常和病理条件下地高辛和洋地黄毒苷代谢物的定量信息,以正确解释通过放射免疫分析或ATP酶分析获得的试验数据。