Peptide ligands for bombesin receptors.

摘要

Peptides of the formula A-B-Gln-Trp-Ala-Val-W-X-Y-T (A=H, Boc, Lys, Arg, B=valence bond, Asn, Thr, Glp, W=Gly, ala, X=valence bond, His(R1), his(R1), Phe, phe, Ser, Ser, Ala, ala, Y=valence bond, Leu, leu, Phe, phe, T=NH2, NH(CH2)4CH3, NHCH2-C6H5, Met-R2, Leu-R2, Ile-R2, Nle-R2, R1=H, Tos, Dnp, Bzl, R2=NH2, OH, OMe, NHNH2; if A=Lys, Arg then B NOTEQUAL Glp, if X=His,then Y-T NOTEQUAL Leu-Met-NH2, Phe-Met-NH2 if X=His(Dnp) and A=Boc, then B NOTEQUAL Asn) and their pharmaceutically acceptable salts show a high binding affinity to bombesin receptors. Their preparation and pharmaceutical compositions containing them are also decribed.