Tarpley W G, Sun F F
J Med Chem. 1978 Mar;21(3):288-91. doi: 10.1021/jm00201a011.
The metabolic transformation and excretion of tritium-labeled cis-delta4-15(S)-15-methylprostaglandin F1alpha methyl ester (1) have been investigated in rats after chronic and single dose oral administration. Three metabolites have been identified from a partially purified urinary extract. They were the cis-delta4-15-methylprostaglandin F1alpha (2), 15-methyl-2,3-dinorprostaglandin F1alpha (3), and 15-methyl-2,3,4,5-tetranorprostaglandin F1alpha (4). The excretion of the drug-related species was significantly slower than that of the natural prostaglandin F2alpha. The slow excretion rate and the presence of unchanged cis-delta4-15-methylprostaglandin F1alpha in urine suggested that the metabolically protected prostaglandin could persist in the body and, therefore, exhibit longer duration of action.
对氚标记的顺式δ4-15(S)-15-甲基前列腺素F1α甲酯（1）在大鼠经慢性和单次口服给药后的代谢转化及排泄情况进行了研究。从部分纯化的尿液提取物中鉴定出了三种代谢物。它们分别是顺式δ4-15-甲基前列腺素F1α（2）、15-甲基-2,3-二去甲前列腺素F1α（3）和15-甲基-2,3,4,5-四去甲前列腺素F1α（4）。与药物相关物质的排泄明显慢于天然前列腺素F2α。排泄速度缓慢以及尿液中存在未变化的顺式δ4-15-甲基前列腺素F1α表明，这种代谢保护的前列腺素能够在体内持续存在，因此具有更长的作用持续时间。
