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 p...

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Veröffentlicht in:	International Journal of Peptide and Protein Research 1987-02, Vol.29 (2), p.170-176
Hauptverfasser:	CALAS, B., MICHELOT, R., LECAER, J.P., CAVE, A., PARELLO, J., POTIER, P.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Chemistry conformation analysis DiMe-C7 Exact sciences and technology Guinea Pigs Ileum - physiology In Vitro Techniques Male Muscle Contraction - drug effects Muscle, Smooth - drug effects Muscle, Smooth - physiology n.m.r Organic chemistry Peptide Fragments peptide synthesis Peptides polyacrylamide polyacrylamide resin Preparations and properties Protein Conformation Pyrrolidonecarboxylic Acid - analogs & derivatives resins Substance P Substance P - analogs & derivatives Substance P - chemical synthesis Substance P - pharmacology Trachea - physiology
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Beschreibung
Zusammenfassung:	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.
ISSN:	0367-8377 1399-3011
DOI:	10.1111/j.1399-3011.1987.tb02243.x