Английская Википедия:17β-Methyl-17α-dihydroequilenin

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17β-Methyl-17α-dihydroequilenin (developmental code name NCI-122), also known as 17β-methyl-6,8-didehydro-17α-estradiol, is a synthetic steroidal estrogen which was never marketed.[1][2] It is the C17β methylated derivative of 17α-dihydroequilenin, an equine estrogen and constituent of conjugated estrogens (Premarin).[1][2] 17α-Dihydroequilenin itself is an analogue of 17α-estradiol, the C17 epimer of estradiol (or 17β-estradiol).[1][2] NCI-122 has respective relative binding affinities of about 8.1% and 16% for the ERα and ERβ when compared to estradiol.[2] It is far less potent as an estrogen in comparison to estradiol, with relative estrogenic potencies at the ERα and ERβ of 1.4% and 0.81%, respectively.[1] Nonetheless, NCI-122 acts as a full agonist of the ERα (ERβ was not assessed) and has estrogenic activity similar to that of estradiol at sufficiently high concentrations.[2] The mechanisms of the lower potency of NCI-122 and related estrogens (e.g., 17α-estradiol and equilenin) relative to estradiol have been studied.[1]

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Шаблон:Estrogen receptor modulators


Шаблон:Steroid-stub Шаблон:Genito-urinary-drug-stub