Williams J G, Longcope C, Williams K I
Steroids. 1975 Mar;25(3):343-54. doi: 10.1016/0039-128x(75)90091-4.
A mixture of 4-3-H and 4-14-C-mestranol was administered orally to four women. Reactions involving position 4 were no greater than 1.7-3% of the dose as measured by liberation of 3-H into body water. The extent of de-ethynylation in vivo was no greater than 1-2% of the dose as measured by urinary estrone metabolites. Mestranol (0.7 and 0.32% of the dose), 17alpha-ethynylestradiol (6.6 and 11.3%) and 2-hydroxy-17alpha-ethynylestradiol (0.64 and 0.7%) were identified as metabolite aglycons by reverse isotope dilution after Ketodase hydrolysis of the urine from two of the women.
将4 - ³H和4 - ¹⁴C美雌醇的混合物口服给予四名女性。通过³H释放到体内水中来测量，涉及4位的反应不超过剂量的1.7 - 3%。通过尿雌酮代谢物测量，体内去乙炔基化程度不超过剂量的1 - 2%。通过对两名女性尿液进行酮酶水解后，采用反向同位素稀释法鉴定出美雌醇（分别为剂量的0.7%和0.32%）、17α - 乙炔雌二醇（分别为6.6%和11.3%）以及2 - 羟基 - 17α - 乙炔雌二醇（分别为0.64%和0.7%）作为代谢产物苷元。
