2-Furoyl-LIGRLO-amide: A potent and selective proteinase-activated receptor 2 agonist

John J. McGuire, Mahmoud Saifeddine, Chris R. Triggle, Kimberly Sun, Morley D. Hollenberg

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Abstract

A peptide corresponding to a proteinase-activated receptor 2 (PAR 2)-activating peptide with an N-terminal furoyl group modification, 2-furoyl-LIGRLO-NH2, was assessed for PAR2-dependent and -independent biological activities. 2-Furoyl-LIGRLO-NH2 was equally effective to and 10 to 25 times more potent than SLIGRL-NH2 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-NH2 was 10 to 300 times more potent than SLIGRL-NH2. Unlike trans-cinnamoyl-LIGRLO-NH2, 2-furoyl-LIGRLO-NH2 did not cause a prominent non-PAR 2-mediated contraction of murine femoral arteries. In conclusion, 2-furoyl-LIGRLO-NH2 represents the most potent and selective activator of PAR2 in biological systems described to date.

Original languageEnglish
Pages (from-to)1124-1131
Number of pages8
JournalJournal of Pharmacology and Experimental Therapeutics
Volume309
Issue number3
DOIs
Publication statusPublished - 1 Jun 2004

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ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

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