Abstract
The antiandrogenic properties of AA560 (N- (2'-chloromethy1-2 '-hydroxypropionyl) -3, 4, 5-trichloroaniline) and the mechanism of its action were investigated. The following results were obtained.
1. The antagonistic effect of AA560 against exogeneous androgen was stronger than SCH 13521, cyproterone acetate or chlormadinone acetate.
2. The antagonistic affect of AA560 against endogeneous androgen was stronger than SCH13521 or chlormadinone acetate.
3. In intact male rats given AA560 orally there was significant increase of serum LH, FSH and testosterone levels.
4. In the in vivo experiment, the pretreatment with AA560 decreased the uptake of 3H-androgens in the nuclear fraction. On the other hand, 145°C of increase in the uptake of 3H-radioactivity in the cytosol fraction was observed.
5. It was observed in the in vitro displacement study that AA560 inhibited the formation of 5α-DHT-Receptor complex in the cytosol of rat ventral prostate.
