Action of a novel nonsteroidal antiandrogen, AA560.

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Abstract
The ventral prostate, dorselateral prostate and coagulating gland weights in rats given AA 560 at 1-9 mg/head were significantly less than those in the intact rats. The seminal vesicle weights in rats given 3-9 mg/head were significantly less than those of the intact group. In intact animals given daily 3 or 9 mg of AA 560 there were significant increases of serum FSH [follitropin], LH [lutropin] and testosterone concentrations. In the in vivo experiment, the pretreatment with AA 560 decreased the uptake of 3H-androgens in the nuclear fraction of the ventral prostate. A significant increase in the uptake of 3H-radioactivity in the cytosol fraction was observed. The in vitro displacement study proved that AA 560 inhibited the binding of 5.alpha.-dihydrotestosterone with a receptor protein in the prostatic cytosol.