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. 2016 Apr 20;6:24575. doi: 10.1038/srep24575

Figure 7. 3D53, W54011 and JJ47 are orally active anti-inflammatory compounds that inhibit C5a agonist-induced paw oedema in male Wistar rats.

Figure 7

Paw oedema was induced in male Wistar rats by intraplantar administration of C5aR-PA (350 μg per paw in 100 μL of saline control). Paw swelling (% area change from baseline) was recorded at indicated timepoints. To determine comparative in vivo residence times, (A) 3D53 (5 mg/kg, p.o., n = 3 per group), (B) W54011 (30 mg/kg, p.o., n = 2 per group) and (C) JJ47 (30 mg/kg, p.o., n = 2 per group) were given orally 1 h prior to injection of C5aR-PA at specific time-points post-antagonism. Oral bioavailabilities of (D) 3D53 (F ~ 2%), (E) W54011 (F ~ 74%) and (F) JJ47 (F ~ 12%) were measured using LCMS to quantify plasma concentrations. C5aR antagonist was administering as an intravenous dose (1 mg/kg via an implanted jugular vein catheter in 50:50 DMSO/saline) versus an oral dose (10 mg/kg in olive oil, via gavage). Plasma was collected at various time points and analyzed. Error bars are means ± SEM normalized to maximal swelling of saline control. *p < 0.05, **p < 0.01 and ***p < 0.001 by student t-test.