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Beschreibung

Native proteinase activated receptor-2- (PAR-2) specific agonist, SLIGRL-NH2, modified with an N-terminal furoyl group to increase its potency and resistance to metabolic degradation. Shown to activate [Ca2+]i mobilization in PAR-2-expressing cells (EC50 = 253 nM in HCT-15 cells) in vitro. Also induces PAR-2-mediated salivation (ED50 = 30 nmol/kg, i.v.) in vivo. Exhibits no effects on PAR-2-/- mice. Reactive towards human, rat, and mouse PAR-2., The native PAR-2-specific agonist, SLIGRL-NH2, is modified with an N-terminal furoyl group to increase its potency and resistance to metabolic degradation. Shown to activate [Ca2+]i mobilization in PAR-2-expressing cells (EC50 = 253 nM using HCT-15 cells) in vitro and induce PAR-2 mediated salivation (ED50 = 30 nmol/kg, i.v.) in vivo, while exhibiting no effect on PAR-2-/- mice. Reactive towards human, rat, and murine PAR-2.