Paris J, Fournau P, Granero M, Lanquetin A, Thévenot R
Arzneimittelforschung. 1986 Jul;36(7):1069-74.
17 beta-Acetoxy-5 alpha, 17 alpha-pregn-2-ene-20-yne (TX 380) strongly suppresses the hypophyso-gonadic axis at central and peripheral levels. Depending on the dosage and on the hormonal status at the time of treatment, this combined inhibition results in major disturbances of the estrus cycle and in impaired ovulation. TX 380 shows minimal androgenic activity. It exerts no effect on the fetal female urogenital tract during gestation. TX 380 possesses only weak estrogenic properties, and does not promote endometrial proliferation in the female rabbit. Moreover, it markedly opposes the action of progesterone. Given this pharmacological profile, TX 380 stands as a candidate drug in the treatment of gynecologic affections, such as endometriosis and benign breast disease, and as a potential contraceptive agent.
17β-乙酰氧基-5α,17α-孕甾-2-烯-20-炔（TX 380）在中枢和外周水平强烈抑制垂体-性腺轴。根据治疗时的剂量和激素状态，这种联合抑制会导致发情周期的重大紊乱和排卵受损。TX 380的雄激素活性极小。在妊娠期，它对雌性胎儿泌尿生殖道无影响。TX 380仅具有微弱的雌激素特性，且不会促进雌性兔子宫内膜增殖。此外，它明显拮抗孕酮的作用。鉴于这种药理学特性，TX 380可作为治疗子宫内膜异位症和良性乳腺疾病等妇科疾病的候选药物，以及作为一种潜在的避孕药。
