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本文用去势大鼠和小鼠研究17α-甲基睾丸素(Ⅰ)及一些衍生物的同化和雄性素样作用。同化作用指标是观察大、小鼠提肛肌和小鼠腎脏重量的增加,雄性素样作用是以精囊重量的增加来表示。結果指出,I的双氫衍生物——17α-甲基-(5α-雄甾烷-17β-羥-3-酮(Ⅱ)和17α-甲基-(5α)-雄甾烷-3β,17β-二羥(Ⅲ)的口服剂量为30毫克/公斤时,在去势大鼠的同化和雄性素样作用与I无显著不同。剂量12.5毫克/公斤肌肉注射时,則Ⅱ对去势小鼠的同化作用比I显著增强,雄性素样作用与I无显著不同;而Ⅲ的同化作用和雄性素样作用均有减弱。17α-甲基-(5α)-雄甾烷-17β-羥(Ⅳ)系I的3位脫氧衍生物,当給去势大鼠口服30毫克/公斤时,其同化作用比I显著增强;給去势小鼠肌肉注射12.5毫克/公斤时,其同化作用与I大致相同,但雄性素样作用只有I的1/3,因之,同化与雄性素样作用比值高至3.63—4.50。睾丸素17位脫氧衍生物——5α-雄甾烷-3-羥(Ⅴ)和5α-雄甾烷-3-酮(Ⅵ)的剂量为30—40毫克/公斤时,无論口服或注射,在去势大鼠和小鼠均不出現同化和雄性素样作用。以上結果表明,将化合物I 4,5位氫化和3位脫氧,可使同化作用:雄性素样作用比值明显提高,17位脫氧則失去同化和雄性素样作用。
In this paper, ovariectomized rats and mice 17α-methyl testosterone (Ⅰ) and some derivatives of the assimilation and the male-like effect. The indicators of assimilation were observed in rats and mice with levator ani and kidney weight increase in mice. The male-like effect was expressed as an increase in seminal vesicle weight. The results indicate that the 17-methyl- (5α-androstane-17β-hydroxy-3-keto (II) and 17α-methyl- (5α) -androstane-3β, 17β - When the oral dose of dihydroxy (III) was 30 mg / kg, the assimilation and androgens in ovariectomized rats were not significantly different from those of I. The intramuscular injection of 12.5 mg / kg intramuscular injection of Was significantly higher than that of I, and the male-like effect was not significantly different from that of I, while the assimilation of Ⅲ and the male-like effect were weakened.17α-methyl- (5α) -androstane-17β- ) Department I deoxynucleotidyl derivative 3, when given orally to rats orally 30 mg / kg, the assimilation ratio was significantly enhanced than I; castrate mice intramuscular injection of 12.5 mg / kg, its assimilation and I roughly The same, but only 1/3 of the role of male and therefore, the assimilation and the ratio of male-like effect as high as 3.63-4.50. Testosterone 17 deoxy derivative - 5a-androstane-3-hydroxy (Ⅴ ) And 5α-androstan-3-one (Ⅵ) dose of 30-40 mg / kg, regardless of oral or injection, in ovariectomized rats and mice showed no assimilation and androgen-like effect. The results show that compound I 4,5 is hydrogenated 3-deoxy enable assimilation: androgen-like effects were significantly improved, the loss of the 17-deoxy-like effect in male and assimilation.