| abstract |
Peptides of formula A-B-C-D-Gln-Trp-Ala-Val-X-Y-T-W (either A = H, Boc; AC; one of B and C = pMel, mMel; the other of B and C = valence bond, Gly, Leu-Gly, E-Leu-Gly, Gln-E-Leu-Gly,E,E-Gly with E = Arg(A), arg(A), Lys(A), lys(A), Orn(A), orn(A) or A = H, B = Glp-Arg-Leu-Gly, C = pMel or mMel; and D = valence bond, Asn, Thr; X = Gly, ala; Y = valence bond, His(R1), his(R1), Phe, phe, Ser, ser, Ala, ala; T = valence bond, Leu, leu, Phe, phe; W = OH, NH2NH(CH2)4CH3, NH(CH2)2C6H5, Met-R2, Leu-R2, Ile-R2, Nle-R2; R1 = H, Tos, Dnp, Bzl; R2 = NH2, OH, OCH3, NHNH2) and their pharmaceutically acceptbale salts are irreversible peptide ligands for Bombesin receptors. Their preparation and pharmaceutical compositions containing them are also described. |