Nakayama R, Masuoka M, Masaki T, Shimamoto K
Acta Endocrinol Suppl (Copenh). 1979;229:2-23.
Anti-androgenic properties of newly synthesized steroidal compounds, TSAA-291 and its derivatives, were studied in the rat. (1) Subcutaneous administrations of TSAA-291 and TSAA-272 were effective in depressing the weight of seminal vesicles and ventral and dorsal prostates in the adult rat. (2) TSAA-291, TSAA-328 and TSAA-272 were shown to be anti-androgenic by the subcutaneous or oral route in the immature castrated male rat treated with testosterone propionate. The dose-response curves of all the test agents expressed in terms of percentage inhibition were approximately parallel to each other. Cyproterone acetate depressed the weight of levator ani muscle dose-dependently, whereas TSAA-291, TSAA-328 and TSAA-330 did not inhibit the muscle weight in a dose range sufficiently effective in inhibiting the weight of seminal vesicles and ventral and dorsal prostates. (3) TSAA-291 was also anti-androgenic against androstenedione and dehydroepiandrosterone. (4) Local administration of the anti-androgenic compounds into the left seminal vesicle or left testis of the young adult rat depressed the weight of the seminal vesicle or testis on the treated side as compared with the vehicle-injected contra-lateral side.
在大鼠中研究了新合成的甾体化合物TSAA - 291及其衍生物的抗雄激素特性。(1)皮下注射TSAA - 291和TSAA - 272可有效降低成年大鼠精囊、腹侧前列腺和背侧前列腺的重量。(2)在接受丙酸睾酮治疗的未成熟去势雄性大鼠中，通过皮下或口服途径显示TSAA - 291、TSAA - 328和TSAA - 272具有抗雄激素作用。所有受试药物以抑制百分比表示的剂量反应曲线大致相互平行。醋酸环丙孕酮剂量依赖性地降低提肛肌的重量，而TSAA - 291、TSAA - 328和TSAA - 330在对抑制精囊、腹侧前列腺和背侧前列腺重量足够有效的剂量范围内未抑制肌肉重量。(3)TSAA - 291对雄烯二酮和脱氢表雄酮也具有抗雄激素作用。(4)将抗雄激素化合物局部注射到年轻成年大鼠的左侧精囊或左侧睾丸中，与注射赋形剂的对侧相比，可降低治疗侧精囊或睾丸的重量。
