| 摘要 |
<p>The invention relates to novel peptides and peptide derivatives which act as antagonists of natural LH-RH and have the general formula: X-R1-R2-R3-Ser-Tyr-R4-R5-R6-R7-R8-NH2 wherein X represents hydrogen or a lower acyl(1-6 C) group, R1 and R2 represent either the same or different groups selected from D-Bal(2), D-Bal(3), D-Nal(1), D-Nal(2), D-Phe or D-Phe substittted at the phenyl moiety by one or more halogen,alkyl(1-4 C),alkoxy (1-4 C) or nitro groups; R3 represents D-Trp, D-Bal(2), D-Bal(3), D-Nal(1), D-Nal(2) or D-Pal, with the proyiso that at least one of the symbols R1 or R3 represents a D-Bal(2) or D-Bal(3) group; R represents D-Arg, D-Lys, D-homo Arg or D-dialkyl (1-4 C)-homo Arg; R5 represents L-Leu, L-Met or the alkyl(1-4C) or phenylalkyl(7-10C) ether of L-Cys, L-Ser or L-homo Ser ; R6 represents L-Lys or L-Arg; R7 represents L-Pro or L-thiaprolyl, and R8 represents D-Ala or Gly. The invention also includes the acid addition salts of the above defined peptides.</p> |
