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Comparative Effects of a Series of Prolactin Inhibitors, 17ß-Estradiol and 2-Methyldihydrotestosterone Propionate, on Growth of 7,12-Dimethylbenz(a)anthracene-induced Rat Mammary Carcinomas¹

Memorial Sloan-Kettering Cancer Center, New York, New York 10021 [M. N. T., C. C. S., L. H., I. M. M., M. B.]; Department of Oncology, Montefiore Hospital and Medical Center, Bronx, New York 10467 [L. H., B. J. R., R. M. B.]; and Department of Pathology, Lawrence Hospital, Bronxville, New York 10708 [J. M. B.]

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-1-ylacetic acid amide) and ergocryptine; effective to an intermediate degree were Dironyl [N-(D-6-methyl-8-isoergolin-1-yl)-N',N'-diethylurea], ergocornine, and Lysenyl [N-(D-6-methyl-8-isoergolenyl)-N',N'-diethylurea]; and effective to a minimal degree were Lergotrile (2-chloro-6-methylergoline-8ß-acetonitrile), CB-154, and 6605-VUFB (D-6-methyl-8-cyanomethylergolin-1). Remission of many individual carcinomas was brief, and duration of complete regression (all tumors in the rat were nonpalpable) was less than 10 weeks.

¹ Supported in part by National Cancer Institute Grants CA-08748, CA-18856, and CA-07304 from NIH, Department of Health, Education, and Welfare. Presented in part at the Sixty-sixth Annual Meeting of the American Association for Cancer Research, San Diego, Calif., May 7 to 11, 1975 (43).

² To whom requests for reprints should be addressed, at Donald S. Walker Laboratory, Sloan-Kettering Institute for Cancer Research, 145 Boston Post Road, Rye, N. Y. 10580.

³ Present address: J. T. Baker Diagnostics Division, Bethlehem, Pa. 18017.

⁴ Present address: Department of Internal Medicine, University of Texas Health Science Center at Dallas, Dallas, Texas 75235.

Received 9/16/76. Accepted 7/26/77.

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