Synthesis and biological activity of Substance P C‐terminal hexapeptide and heptapeptide analogues

GEORGE STAVROPOULOS*, KOSTAS KARAGIANNIS, PAUL CORDOPATIS, DAVID HALLE, CHAIM GILON, GIORA BAR‐AKIVA, ZVI SELINGER, MICHAEL CHOREV

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

7 Scopus citations

Abstract

The analogues [Glu(OBzl)11]SP6–11 and [Glu(OBzl)11]SP5–11 of the C‐terminal hexapeptide and heptapeptide of Substance P have been synthesized by conventional solution methods. In each analogue the SCH3 group of Met11 is replaced by the COOCH2C6H5 group. The in vitro activity of both analogues has been determined on three biological preparations: guinea pig ileum (GPI), rat vas deferens (RVD), and rat portal vein (RPV). The selectivity for the different receptors has been studied by utilizing atropine‐treated guinea pig ileum (GPI + At). The results showed that both analogues are mainly active on GPI through the NK‐1 receptor and that both analogues are equipotent to Substance P.

Original languageEnglish
Pages (from-to)180-184
Number of pages5
JournalInternational Journal of Peptide and Protein Research
Volume37
Issue number3
DOIs
StatePublished - Mar 1991

Keywords

  • guinea pig ileum assay
  • methionine replacement
  • NK‐1 receptor
  • Substance P
  • Substance P C‐terminal analogues

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