Biological activities of 17α-hydroxyprogesterone derivatives such as 17α-hydroxyprogesterone (HP), 17α-hydroxyprogesterone acetate (HPA), 17α-hydroxyprogesterone capronate (HPC), 6α-methyl-17α-acetoxyprogesterone (Provera) and 6α-chloro-17α-acetoxyprogesterone (chlovera) were investigated. The results are summarized as follows.
1. Androgenic and anabolic activity : Spayed rats were injected with the Steroids daily 7 days and seminal vesicles, prostates and m. levator ani were weighed. 2000mcg. of progesterone, HP, HPA or HPC was all inactive, showing that thier activities were less than 1/80 of testosterone propionate, while 500mcg. of Provera and 1000mcg. of Chlovera were inactive, showing thier activities less than 1/20 to 1/40 of testosterone propionate.
2. Estrogenic activity : By the uterine weight method 1000mcg. of HP, HPA, HPC or Chlovera and 500mcg. of Provera were quite inactive, thier activities being less than 1/500 to 1/1000 of estrone, while 500mcg. of progesterone was active, corresponding to 1/500 of estrone. By smear test HPA, HP and HPC corresponded to 1/5000, 1/10000 and 1/10000 of estrone in activity. However, 1000mcg. of Provera and Chlovera were inactive, their activity being less than 1/10000 of estrone.
3. Inhibiting action on the pituitary : Gonadotropic potency of the pituitary was somewhat inhibited by Provera, but it was not influenced by HP, HPC and Chlovera.
4. Influences on the suprarenal gland : When male rats were injected with 1mg of Provera daily 7 to 20 days, of suprarenal gland in weight was confirmed only in the group of Provera. Histologically atrophy of zona fasciculata was distinct in the same group.
5. Progestational activity : These steroids were compared on progestational activity by the scale of Mc Phail, and relative potency can be tabulated as follows, when the potency of progesterone is assumed to be 100 in case of parenteral adminiatration and that of ethinyl-testosterone 100 in case of oral treatment.
6. Maintenance of pregnancy : On the 10th day of pregnancy of albino-rats bilateral ovaries were removed and maintenance of pregnancy was observed, treating with various steroid compounds. The rate of successful treatment was briefly as follows.
7. As for the toxic and side effect there were observed neither water retention in various organs nor impairement of general conditions, although rats and mice were treated with as much as 1mg of Provera or Chlovera daily 30 days by injection or mouth and 2.5mg daily 3 days intraperitoneally, respectively.
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