2-Furoyl-LIGRLO-amide: A potent and selective proteinase-activated receptor 2 agonist Academic Article uri icon

Overview

MeSH Major

  • Oligopeptides
  • Receptor, PAR-2

abstract

  • A peptide corresponding to a proteinase-activated receptor 2 (PAR(2))-activating peptide with an N-terminal furoyl group modification, 2-furoyl-LIGRLO-NH(2), was assessed for PAR(2)-dependent and -independent biological activities. 2-Furoyl-LIGRLO-NH(2) was equally effective to and 10 to 25 times more potent than SLIGRLNH(2) for increasing intracellular calcium in cultured human and rat PAR(2)-expressing cells, respectively. In bioassays of tissue PAR(2) activity, measured as arterial vasodilation and hyperpolarization, 2-furoyl-LIGRLO-NH(2) was 10 to 300 times more potent than SLIGRL-NH(2). Unlike trans-cinnamoyl-LIGRLO-NH(2), 2-furoyl-LI-GRLO-NH(2) did not cause a prominent non-PAR(2)-mediated contraction of murine femoral arteries. In conclusion, 2-furoyl-LI-GRLO-NH(2) represents the most potent and selective activator of PAR(2) in biological systems described to date.

publication date

  • June 2004

Research

keywords

  • Academic Article

Identity

Language

  • eng

Digital Object Identifier (DOI)

  • 10.1124/jpet.103.064584

PubMed ID

  • 14976230

Additional Document Info

start page

  • 1124

end page

  • 31

volume

  • 309

number

  • 3