Reznikov A G, Demchenko V N, Varga S V, Bozhok Y M
Endokrinologie. 1978 Nov;72(3):276-84.
Influence of the competitive testosterone antagonist 4-nitro-3-trifluoromethylisobutyranilide (NFBA) on the hypothalamo-hypophyseal-gonadal system in male Wistar rats and guinea pigs was studied. NFBA as well as nonlabelled testosterone diminished 3H-testosterone uptake in hypothalamus and hypophysis of castrated animals. Increase of plasma testosterone level was obtained after the antiandrogen treatment in a dose of 10 or 25 mg/kg per os during 3, 10 and 48 days. Maximal level of the hormone was noticed on the 10th day. The contents of 17-ketosteroids in testes had not changed, but the testosterone content and steroid-delta5-3beta-ol-dehydrogenase activity were high during the treatment period. After 10 days of NFBA administration increased plasma LH level was found. Increase in size and number of gonadotropocytes was revealed by histological and histochemical methods as well as Leydig cell hypertrophy. High plasma testosterone level and Leydig cell activation were obtained in guinea pigs as a result of NFBA subcutaneous injections in a dose of 10 mg/kg during 30 days. The suggestion is made that prolonged NFBA treatment produces changes in the testosterone metabolism. Short-term administration of NFBA may be used for the estimation of the hypothalamo-hypophyseal functional abilities.
研究了竞争性睾酮拮抗剂4-硝基-3-三氟甲基异丁酰苯胺（NFBA）对雄性Wistar大鼠和豚鼠下丘脑-垂体-性腺系统的影响。NFBA以及未标记的睾酮均可降低去势动物下丘脑和垂体对3H-睾酮的摄取。在以10或25 mg/kg的剂量口服抗雄激素药物3天、10天和48天后，血浆睾酮水平升高。在第10天观察到激素的最高水平。睾丸中17-酮类固醇的含量没有变化，但在治疗期间睾酮含量和类固醇-δ5-3β-醇脱氢酶活性较高。在给予NFBA 10天后，发现血浆LH水平升高。通过组织学和组织化学方法显示促性腺细胞的大小和数量增加，以及睾丸间质细胞肥大。由于在30天内以10 mg/kg的剂量皮下注射NFBA，豚鼠出现了高血浆睾酮水平和睾丸间质细胞活化。有人提出，长期使用NFBA会导致睾酮代谢发生变化。短期给予NFBA可用于评估下丘脑-垂体的功能能力。
