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. 2012 Mar;165(5):1413–1423. doi: 10.1111/j.1476-5381.2011.01610.x

Figure 5.

Figure 5

GB88 is a PAR2-selective antagonist of PAR2-induced inflammation in rat paws. (A) GB88 attenuates the acute paw oedema induced by PAR2 agonists. Intraplantar (i.pl.) administration of 2f-LIGRLO-NH2 (350 µg per paw in 100 µL of saline control) induces paw oedema (% area change from baseline) after 30 min (reducing to baseline after 24 h) that is inhibited (≤80%) by prophylactic GB88 (10 mg·kg−1, p.o. in olive oil) given orally 120 min prior to 2f-LIGRLO-NH2 (n = 5 per group, *P < 0.01, significant effect of GB88; anova). (B) GB88 blocks PAR2, but not PAR1, agonist-induced paw oedema. GB88 (10 mg·kg−1 p.o.) significantly reduces paw swelling induced by PAR2 agonists trypsin (20 µg per paw), SLIGRL-NH2 (2 mg per paw) or GB110 (350 µg per paw), but not by oedema induced by PAR1 agonists thrombin (5 U per paw) or TFLLR-NH2 (2 mg per paw) or by PAR4 agonist AYPGKF-NH2 (2 mg per paw). Data (means + SEM) normalized to maximal swelling of controls. *P < 0.01, significant effect of GB88; n = 6 per group.