Osawa Y, Yarborough C, Osawa Y
Science. 1982 Mar 5;215(4537):1249-51. doi: 10.1126/science.7058343.
Norethisterone (17 alpha-ethynyl-19-nortestosterone) is an effective irreversible inhibitor of estrogen synthetase (aromatase), the enzyme responsible for the conversion of androgens to estrogens, even at a 2 X 10(-6) molar concentration. This irreversible inactivation, which is directed toward the active site of aromatase and requires the cofactor-reduced nicotinamide adenine dinucleotide phosphate, is both time- and concentration-dependent. Ethisterone (17 alpha-ethynyltestosterone), in contrast, is not a suicide inhibitor of aromatase even at concentrations of 10(-4) molar.
炔诺酮（17α-乙炔基-19-去甲睾酮）是一种有效的雌激素合成酶（芳香化酶）不可逆抑制剂，该酶负责将雄激素转化为雌激素，即使在2×10⁻⁶摩尔浓度下也是如此。这种不可逆失活作用于芳香化酶的活性位点，且需要辅因子还原型烟酰胺腺嘌呤二核苷酸磷酸，它具有时间和浓度依赖性。相比之下，乙炔睾酮（17α-乙炔基睾酮）即使在10⁻⁴摩尔浓度下也不是芳香化酶的自杀性抑制剂。
