Vojtísková M, Polácková M, Viklický V, Khoda M E
Endokrinologie. 1978 Apr;71(2):135-42.
The effects of a prolonged subcutaneous administration of SCH 13521 dissolved in 0.3% hydroxypropyl cellulose (2-8 weeks in daily doses of 0.2 or 1.0 mg amounting to an estimated equivalent of experimental and curative doses used by others in laboratory animals and men) were studied in males of the mouse inbred strain C57BL/6. Following the treatment, the activity of spermatogenesis (expressed as the mean number of seminiferous tubules containing mature sperm and epididymal sperm count) was inhibited while the testis weight was not reduced, obviously due to an absolute increase of the interstitial tissue which was a marked histological feature of the testes, particularly following the higher doses of SCH 13521. Lower doses and shorter-lasting administration of the compound seem to inhibit the activity more effectively because after a prolonged administration reparatory processes tend to be triggered via a stimulatory effect on the synthesis of testosterone in Leydig cells. The solvent alone, hydroxypropyl cellulose, had some inhibitory effect on spermatogenesis. The lymphoid system remained both morphologically and functionally unaffected by SCH 13521 unlike the steroidal antiandrogen cyproterone actetate.
在近交系C57BL/6雄性小鼠中研究了皮下长期给予溶解于0.3%羟丙基纤维素的SCH 13521的作用（每日剂量0.2或1.0毫克，持续2 - 8周，估计相当于其他研究者在实验动物和人类中使用的实验剂量和治疗剂量）。治疗后，精子发生活性（以含有成熟精子的生精小管平均数量和附睾精子计数表示）受到抑制，而睾丸重量未降低，这显然是由于间质组织绝对增加所致，这是睾丸的一个显著组织学特征，尤其是在给予较高剂量的SCH 13521后。较低剂量和较短时间给予该化合物似乎更有效地抑制活性，因为长期给药后，通过对睾丸间质细胞睾酮合成的刺激作用，往往会引发修复过程。单独的溶剂羟丙基纤维素对精子发生有一定的抑制作用。与甾体类抗雄激素醋酸环丙孕酮不同，SCH 13521对淋巴系统的形态和功能均无影响。
