Ruenitz P C
Drug Metab Dispos. 1981 Sep-Oct;9(5):456-60.
Metabolism of the triarylethylene antiestrogen enclomiphene (EC) has been studied in rabbit liver. Incubation of EC with microsomes in the presence of NADPH gave two metabolites, EC-1 and EC-2, as determined by thin-layer chromatography (TLC). EC-1 had mass-spectral features that were identical to those of synthetic desethylenclomiphene, and was indistinguishable from this compound by TLC and gas-liquid chromatography (GLC). EC-2 was similarly identical to synthetic 4-hydroxyclomiphene, but was separable from 3-hydroxyclomiphene by TLC ang GLC. EC-2 methyl ether was homogeneous with 4-methoxyclomiphene, but not with 4'-methoxyclomiphene, in GLC. These results suggest that enclomiphene is metabolized in a manner qualitatively similar to that reported for other structurally related antiestrogens.
已对三芳基乙烯类抗雌激素药物氯米芬（EC）在兔肝脏中的代谢情况进行了研究。在存在NADPH的情况下，将EC与微粒体一起温育，通过薄层色谱法（TLC）测定得到了两种代谢产物，即EC-1和EC-2。EC-1的质谱特征与合成的去乙基氯米芬相同，通过TLC和气液色谱法（GLC）无法将其与该化合物区分开来。EC-2同样与合成的4-羟基氯米芬相同，但通过TLC和GLC可将其与3-羟基氯米芬分离。在GLC中，EC-2甲醚与4-甲氧基氯米芬同质，但与4'-甲氧基氯米芬不同质。这些结果表明，氯米芬的代谢方式在质量上与其他结构相关抗雌激素药物的报道相似。
