Английская Википедия:17α-Ethynyl-3α-androstanediol

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Шаблон:Short description Шаблон:Drugbox

17α-Ethynyl-3α-androstanediol (developmental code names HE-3235, Apoptone), also known as 17α-ethynyl-5α-androstane-3α,17β-diol, is a synthetic androstane steroid and a 17α-substituted derivative of 3α-androstanediol which was never marketed.[1][2][3] It was under development for the treatment of prostate cancer but was discontinued.[1][2][3]

17α-Ethynyl-3α-androstanediol itself shows very low affinity for steroid receptors, including the Шаблон:Abbrlink, Шаблон:Abbrlink, Шаблон:Abbrlink, Шаблон:Abbrlink, and Шаблон:Abbrlink, and its mechanism of action is not well-characterized.[1][4] It produces 5α-dihydroethisterone (5α-dihydro-17α-ethynyltestosterone), a ligand of several steroid hormone receptors, and 17α-ethynyl-3β-androstanediol, an estrogen, as active metabolites.[1][5] These metabolites may contribute importantly to the biological activity of 17α-ethynyl-3α-androstanediol, with 17α-ethynyl-3α-androstanediol potentially serving as a prodrug.[1][5]

Шаблон:Affinities of estrogen receptor ligands for the ERα and ERβ

Analogues of 17α-ethynyl-3α-androstanediol include 17α-ethynyl-3β-androstanediol, ethinylandrostenediol (17α-ethynyl-5-androstenediol), ethandrostate (17α-ethynyl-5-androstenediol 3β-cyclohexanepropionate), ethinylestradiol (17α-ethynylestradiol), ethisterone (17α-ethynyltestosterone), and 5α-dihydroethisterone (17α-ethynyldihydrotestosterone).

References

Шаблон:Reflist

Шаблон:Androgen receptor modulators Шаблон:Estrogen receptor modulators


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