For the purpose of obtaining hormonal spectra of anti-
androgen TSAA-291 and its derivatives, a variety of endocrine characteristics were studied. (1) Androgenic and anabolic activity : Subcutaneous administration of anti-
androgen TSAA-291 and its
acetate, TSAA-328, to the immature orchiectomized rat resulted in significant weight increase of the levator ani but in only a nominal response of seminal vesicles and prostates even at a large daily dose of 9.6 mg. The resultant anabolic/androgenic ratio was estimated to be extremely high. (2) Oestrogenic activity : Uterine weight in response to these anti-
androgens were sluggishly dose-dependent, and the maximal plateau response remained considerably lower than that induced by oestradiol-17 beta. The oestrogenic activity of these anti-
androgens was estimated to be 1/200 000 or less as that of oestradiol-17 beta. A single subcutaneous dose of 100 mg of
TSAA-291 or its
caproate, TSAA-330, did not induce the vaginal cornification in the adult ovariectomized rat. (3) Anti-oestrogenic activity : Antagonistic effect of these anti-
androgenic compounds on the uterine weight response to oestradiol-17 beta was found in the immature ovariectomized rat. A single subcutaneous dose of 100 mg of
TSAA-291 or TSAA-330 also induced the antagonism against the cornification caused by daily treatments with 1 microgram oestrone in the adult ovariectomized rat. (4) Progestational activity : These anti-
androgenic compounds proved to be less active than
progesterone in the McPhail's test. (5) Anti-inflammatory activity : Daily subcutaneous dose of 20 mg of
TSAA-291 for 6 days did not significantly depress the weight of
granuloma developed around the cotton-pellet implanted in the young male rat.
TSAA-291 did not affect the anti-inflammatory action of 1/6 mg of
prednisolone phosphate. Combination of both agents seemed to be effective in enhancing the anti-androgenic action of
TSAA-291, whereas
prednisolone phosphate alone rather increased the weight of the accessory sex organs. (6)
Liver glycogen deposition activity : Daily intramuscular doses up to 38.4 mg of
TSAA-291 for 5 days did not increase the
liver glycogen level in the adrenalectomized rat.