Increased vascular permeability by a specific agonist of protease-activated receptor-2 in rat hindpaw.
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.
Kawabata
A
A
Department of Pathophysiology & Therapeutics, Faculty of Pharmaceutical Sciences, Kinki University, Higashi-Osaka, Japan.
Kuroda
R
R
Minami
T
T
Kataoka
K
K
Taneda
M
M
D000287:Administration, Topical; D000818:Animals; D002199:Capillary Permeability / Q000187:drug effects*; D010450:Endopeptidases / Q000502:physiology*; D008297:Male; D009842:Oligopeptides / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D003189:p-Methoxy-N-methylphenethylamine / Q000494:pharmacology
D009842:Oligopeptides; C112356:seryl-leucyl-isoleucyl-glycyl--arginyl-leucinamide; D003189:p-Methoxy-N-methylphenethylamine; D010450:Endopeptidases