1-(6-AMino-1-oxohexyl)-4-(3-Methyl-1-oxobutyl)piperazine-d8 Monohydrobromide: Labelled ENMD 547, a selective PAR-2 antagonist. Dose dependently inhibits calcium signaling in Lewis lung carcinoma cells stimulated with a soluble peptide PAR-2 agonist or trypsin, but not with a so luble PAR-1 agonist. Does not inhibit platelet aggregation stimulated by thrombin suggesting that it does not inhibit PAR-3 or PAR-4 signaling. Reduces TNF-a and IL-1β production from rheumatoid arthr itis synovial primary cell culture and reduces joint swelling in a carageenan/kaloin-injected mouse model.
