Action of a novel nonsteroidal antiandrogen, AA560.
The antiandrogenic properties of a new nonsteroidal antiandrogens, AA560 (N-2-chloromethyl-2-hydroxypropionyl)-3, 4, 5-trichloroaniline) were investigated. The ventral prostate, dorselateral prostate and coagulating gland weights in rats given AA560 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 AA560 there were significantly increases of serum FSH, LH and testosterone concentrations. In the in vivo experiment, the pretreatment with AA560 decreased the uptake of 3H-androgens in the nuclear fraction of the ventral prostate. On the other hand, a significant increase in the uptake of 3H-radioactivity in the cytosol fraction was observed. It was proved by the in vitro displacement study that AA560 inhibited the binding of 5 alpha-dihydrotestosterone with a receptor protein in the prostatic cytosol.
D000726:Androgen Antagonists / Q000494:pharmacology*; D000814:Aniline Compounds / Q000494:pharmacology*; D000818:Animals; D002369:Castration; D002715:Chlormadinone Acetate / Q000494:pharmacology; D003345:Corticosterone / Q000378:metabolism; D003600:Cytosol / Q000378:metabolism; D013196:Dihydrotestosterone; D005640:Follicle Stimulating Hormone / Q000097:blood; D007986:Luteinizing Hormone / Q000097:blood; D008297:Male; D011467:Prostate / Q000187:drug effects* / Q000378:metabolism; D051381:Rats; D013997:Time Factors
D000726:Androgen Antagonists; D000814:Aniline Compounds; D013196:Dihydrotestosterone; D002715:Chlormadinone Acetate; C025199:AA 560; D007986:Luteinizing Hormone; D005640:Follicle Stimulating Hormone; D003345:Corticosterone