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.
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.
D000818:Animals; D006168:Guinea Pigs; D007082:Ileum / Q000502:physiology; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology*; D010446:Peptide Fragments; D011487:Protein Conformation; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives; D013373:Substance P / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D014132:Trachea / Q000502:physiology
D010446:Peptide Fragments; D013373:Substance P; C032720:substance P (5-11), pGlu(5)-MePhe(8)-MeGly(9)-; D011761:Pyrrolidonecarboxylic Acid