张均田, 雷海鹏. 17α-甲基睾丸素及其某些衍生物对去势大鼠和小鼠同化作用的观察J. 药学学报, 1964, 11(10): 659-664.
引用本文: 张均田, 雷海鹏. 17α-甲基睾丸素及其某些衍生物对去势大鼠和小鼠同化作用的观察J. 药学学报, 1964, 11(10): 659-664.
CHANG CHUN-T'IEN LEI HAI-P'ENG, . THE ANABOLIC AND ANDROGENIC ACTIVITIES OF 17α-METHYLTESTOSTERONE AND RELATED STEROIDS IN CASTRATED RATS AND MICEJ. Acta Pharmaceutica Sinica, 1964, 11(10): 659-664.
Citation: CHANG CHUN-T'IEN LEI HAI-P'ENG, . THE ANABOLIC AND ANDROGENIC ACTIVITIES OF 17α-METHYLTESTOSTERONE AND RELATED STEROIDS IN CASTRATED RATS AND MICEJ. Acta Pharmaceutica Sinica, 1964, 11(10): 659-664.

17α-甲基睾丸素及其某些衍生物对去势大鼠和小鼠同化作用的观察

THE ANABOLIC AND ANDROGENIC ACTIVITIES OF 17α-METHYLTESTOSTERONE AND RELATED STEROIDS IN CASTRATED RATS AND MICE

  • 摘要: 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。

     

    Abstract: 17α-Methyltestosterone (Ⅰ) and related steroids were studied for their anabolic and androgenic activities in castrated rats and mice. For rats the levator ani weight was taken as the criterion of anabolic activity, and the weight of the seminal vesicles served as a measure of androgenic activity. For mice the same parameters were used and, besides, the kidney weight was employed as an additional measure of anabolic activity. Results indicated that the anabolic and androgenic activities of 17α-methyl-(5α)-androstane-17β-ol-3-one (Ⅱ) or 17α-methyl-(5α)-androstane-3β, 17β-diol (Ⅲ), 4,5-hydro-genated analogues of (Ⅰ), at a dosage of 30 mg/kg by garage in castrated rats, were not significantly different from those of Ⅰ. However, when the doses were reduced to 12.5 mg/kg, the anabolic activity of Ⅱ in castrated mice was much greater than that of Ⅰ, while the androgenic activity of the two compounds was approximately equal. The anabolic and androgenic activities.of Ⅲ were weaker as compared with those of Ⅰ.The compound 17α-methyl-(5α)-androstane-17β-ol (Ⅳ) (3-deoxy-analog of Ⅰ) at a daily dosage of 30 mg/kg by gavage in castrated rats was shown to be more active on the levator ani and the seminal vesicles than Ⅰ. In castrated mice, Ⅳ caused similar anabolic effects as Ⅰ in doses of 12.5 mg/kg, while its androgenic potency was only one third of that of Ⅰ. Castrated rats and mice were treated with 5α-androstane-3-ol and 5α-androstane-3-one (17-deoxy analogue of testosterone) by gavage or by injection at a dosage of 30 and 40 mg/kg. Neither anabolic nor androgenic activities were observed. From the above results, it may be concluded that removal of the oxygen atom from C3 and hydrogenation at C4 and C5 in 17α-methyltestosterone molecule may increase anabolic and/or decrease androgenic activity, while removal of the oxygen from C17 of testosterone results in loss of both anabolic and androgenic activities. In view of the increase in anabolic activity by removal of the oxygen at C3, synthesis of and pharmacological studies on a series of 3-deoxy analogues of testosterone and cortisone are in progress and will be reported in due course.

     

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