Synthesis of (pGlu-5, MePhe-8, Sar-9) substance P (5-11) (DiMe-C7) using a polyacrylamide resin and biological activity on guinea pig ileum and tracheal smooth muscle

Abstract

DiMe-C7 (pGlu-Gln-Phe-MePhe-MeGly-Leu-MetNH2), a metabolically stable analogue of Substance P, was prepared by solid-phase peptide synthesis using a polyacrylamide resin and a labile anchorage derived from glycolic acid. Myotropic activities in guinea pig ileum (ED50 = 4.0 +/- 1.5 10(-8) M) and guinea pig trachea (ED50 = 8.6 +/- 3.5 10(-8) M) are discussed in comparison with the corresponding activities of Substance P.