Comparative effects of a series of prolactin inhibitors, 17beta-estradiol and 2alpha-methyldihydrotestosterone propionate, on growth of 7,12-dimethylbenz(a)anthracene-induced rat mammary carcinomas.
Eight ergot alkaloids and ergoline derivatives, effective prolactin inhibitors, were tested for activity against DMBA-induced rat mammary carcinomas. Compounds were administered daily, 5 times/week for 4 weeks, and rats were observed for an additional 4 weeks. Groups treated with androgen and estrogen were used as positive controls. Those ergot compounds and ergolines that proved to be highly effective in reducing tumor size or in inducing regression of tumors to nonpalpability were Deprenon (D-6-methyl-8-ergolin-I-ylacetic acid amide) and ergocryptine; effective to an intermediate degree were Dironyl [N-(D-6-methyl-8-isoergolin-I-yl)-N',N'-diethylurea], ergocornine, and Lysenyl [N-(D-6-methyl-8-isoergolenyl)-N',N'-diethyl-urea]; and effective to a minimal degree were Lergotrile (2-chloro-6-methylergoline-8beta-acetonitrile), CB-154, and 6605-VUFB (D-6-methyl-8-cyanomethylergolin-I). Remission of many individual carcinomas was brief, and duration of complete regression (all tumors in the rat were nonpalpable) was less than 10 weeks.
D015127:9,10-Dimethyl-1,2-benzanthracene; D000097:Acetonitriles / Q000627:therapeutic use; D000732:Androstanols / Q000031:analogs & derivatives* / Q000627:therapeutic use; D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy; D001971:Bromocriptine / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical; D004873:Ergolines / Q000627:therapeutic use; D004876:Ergot Alkaloids / Q000627:therapeutic use; D004958:Estradiol / Q000627:therapeutic use*; D005260:Female; D006801:Humans; D008090:Lisuride / Q000031:analogs & derivatives; D008325:Mammary Neoplasms, Experimental / Q000097:blood / Q000188:drug therapy*; D011388:Prolactin / Q000037:antagonists & inhibitors* / Q000097:blood; D051381:Rats; D014508:Urea / Q000031:analogs & derivatives
D000097:Acetonitriles; D000732:Androstanols; D004873:Ergolines; D004876:Ergot Alkaloids; C006208:dironyl; D001971:Bromocriptine; D004958:Estradiol; D015127:9,10-Dimethyl-1,2-benzanthracene; D014508:Urea; D011388:Prolactin; D008090:Lisuride