British Journal of Pharmacology · 1998 · 118 citations · 17 references
MedicineImmunologyPharmacologyInflammationPharmacodynamicsSignal TransductionInflammatory MediatorsInflammatory ProcessesMast Cell PharmacologyPermeability EnhancementVascular Changes In InflammationVascular PermeabilityAgonist ActivityAmino AcidsMast Cell Degranulation InhibitionMast Cell Degranulation PathwaysMast Cell ExocytosisPretreatment
The present study examined the effect of intraplantar (i.pl.) administration of a selective agonist of protease-activated receptor (PAR)-2, SLIGRL-NH2(PP6-NH2), on vascular permeability in rat hindpaw. PP6-NH2, administered i.pl. at 10-100 nmol per paw, enhanced vascular permeability and caused oedema formation in rat hindpaw. SLIGRL (PP6-OH) and trypsin, by i.pl. administration, also elicited an increase in vascular permeability, although i.pl. administration of the mixture of constituent amino acids of PP6-OH at an equivalent dose did not. The PP6-NH2-induced increase in vascular permeability was abolished by repeated pretreatment with compound 48/80 to deplete bioactive amines in mast cells. These findings suggest that the activation of PAR-2 induces acute inflammation, at least partially, via mast cell degranulation in rat hindpaw.
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Protease-activated receptor 3 is a second thrombin receptor in humans
Hiroaki Ishihara, Andrew J. Connolly, Dewan Zeng et al. · Nature · 1997 · 875 citations
Interactions of Mast Cell Tryptase with Thrombin Receptors and PAR-2
Marina Molino, Elliot S. Barnathan, Robert P. Numerof et al. · Journal of Biological Chemistry · 1997 · 591 citations · Full text