Dhar J D, Setty B S
Department of Endocrinology, Central Drug Research Institute, Lucknow, India.
Contraception. 1990 Jul;42(1):121-38. doi: 10.1016/0010-7824(90)90096-e.
The effect of Anandron, a nonsteroidal antiandrogen, on the reproductive system and fertility of adult male rats was studied. Administered at a daily oral dose of 5 mg and 10 mg (per rat) for 30 days, it caused a significant increase in the plasma testosterone levels. Spermatogenic arrest in about 20 to 50% of the tubules in 9 out of 16 rats and stimulation of Leydig cells was observed in rats treated with the higher dose. Although a reduction occurred in accessory sex organ (epididymis, seminal vesicles, SV; ventral prostate, VP; dorsal prostate, DP and coagulating gland, CG) weight, no parallel reduction was evident in the secretory indices of the epididymis (glycerylphosphorylcholine and sialic acid), VP (alkaline phosphatase) and CG (fructose). However, there was a reduction in the total content per organ of these constituents. Females mated with treated males showed postimplantation loss indicating an adverse effect of Anandron during spermiogenesis. The results suggest that the peripheral antiandrogenic potency of Anandron in intact animals is insufficient to completely neutralize the elevated levels of androgens. A microdose (1 microgram) of estradiol efficiently neutralized the central stimulatory effect of Anadron and potentiated its antiandrogenic action. The potential use of such a combination for 'Fertility Regulation' in male is discussed.
研究了非甾体类抗雄激素药物阿那雄酮对成年雄性大鼠生殖系统和生育能力的影响。以每日口服剂量5毫克和10毫克（每只大鼠）给药30天，导致血浆睾酮水平显著升高。在16只大鼠中的9只中，约20%至50%的曲细精管出现生精停滞，且在接受较高剂量治疗的大鼠中观察到睾丸间质细胞受到刺激。尽管附属性器官（附睾、精囊、SV；腹侧前列腺、VP；背侧前列腺、DP和凝固腺、CG）重量有所减轻，但附睾（甘油磷酸胆碱和唾液酸）、VP（碱性磷酸酶）和CG（果糖）的分泌指标并未出现相应下降。然而，这些成分在每个器官中的总含量有所降低。与经处理的雄性大鼠交配的雌性大鼠出现植入后丢失，表明阿那雄酮在精子发生过程中产生了不良影响。结果表明，阿那雄酮在完整动物中的外周抗雄激素效力不足以完全中和升高的雄激素水平。微量（1微克）雌二醇可有效中和阿那雄酮的中枢刺激作用，并增强其抗雄激素作用。讨论了这种组合在男性“生育调节”中的潜在用途。
