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 soluble 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 arthritis synovial primary cell culture and reduces joint swelling in a carageenan/kaloin-injected mouse model.
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