Biologically active octapeptides

Abstract

Abstract Novel compositions of the formula ##STR1## wherein A represents an L, D or DL amino-acid selected from the group consisting of Ala, Val, Phe, p-Cl-Phe, Trp, Pro, Ser, Thr, Glu, Gly, Beta Ala, Abu, N-Me Ala, 5-F-Trp, 5-Br-Trp, 5-Cl-Trp, their acetylated derivatives or a pharmaceutically acceptable acid addition salt thereof; B represents an L, D or DL amino acid amide selected from the group consisting of Thr NH 2 , Val NH 2 , Pro NH 2 , HO-Pro NH 2 , Ser NH 2 , Tyr NH 2 , Trp NH 2 , 5-F-Trp NH 2 , For-Trp NH 2 , Ala NH 2 , Gly NH 2 , Me Ala NH 2 ; X represents L-Phe or L-Tyr, Y represents L-Thr or L-Val; Z is L, D or DL-5-F-Trp, 5-Br-Trp, 5-Cl-Trp, 5-I-Trp or D-Trp; and C" and C' represent L or D Cys, Abu, Asp or Lys; and the pharmaceutically acceptable acid addition salts thereof; are useful as agents for inhibiting the release of growth hormone, for the treatment of gastrointestinal disorders and for therapy of certain cancers and the management of diabetes. These biologically active octapeptides all possess a terminal amino acid amide at position 8 and are prepared by solid phase methods.

Inventors

• 👤 Andrew V. Schally
• 👤 Ren Z. Cai

Bibliographic Details