Bourne G R, Moss S R, Phillips P J, Shuker B
Biomed Mass Spectrom. 1980 May;7(5):226-30. doi: 10.1002/bms.1200070509.
The metabolic fate of the synthetic prostaglandin cloprostenol ('Estrumate') in the cow has been studied. Following intramuscular administration of 0.5 mg and 10 mg of [14C]cloprostenol to cows urinary excretion accounted for 58.2% and 56.3% of the dose respectively. Unchanged cloprostenol and its tetranor acid, probably formed by beta-oxidation, were the major components identified in urine. The tetranor acid was also present as a glucuronide conjugate. This synthetic prostaglandin analogue is apparently a poor substrate for the enzymes 15-hydroxyprostaglandin dehydrogenase and 13,14-reductase, which are responsible for the rapid metabolic deactivation of endogenous prostaglandins, as no components identified in urine were found to have undergone metabolic attack at the C-15 atom in the cloprostenol molecule.
已对合成前列腺素氯前列醇(“ Estrumate”)在奶牛体内的代谢命运进行了研究。给奶牛肌肉注射0.5毫克和10毫克[14C]氯前列醇后,尿液排泄分别占剂量的58.2%和56.3%。未变化的氯前列醇及其四降酸(可能由β-氧化形成)是尿液中鉴定出的主要成分。四降酸也以葡糖醛酸苷结合物的形式存在。这种合成前列腺素类似物显然是15-羟基前列腺素脱氢酶和13,14-还原酶的不良底物,这两种酶负责内源性前列腺素的快速代谢失活,因为在尿液中鉴定出的成分在氯前列醇分子的C-15原子上未发生代谢攻击。