SCH79797

SCH 79797 is a non-peptide antagonist of proteinase-activated receptor 1 (PAR1).¹ It blocks binding of the high affinity thrombin receptor-activating peptide (haTRAP) (IC₅₀ = 70 nM) as well as platelet aggregation induced by either haTRAP or α-thrombin (IC₅₀ = 0.3 and 3 ?M, respectively).² SCH 79797 has no activity against PAR2, PAR4, or other receptors involved in platelet activation.² It also blocks PAR1 activation on vascular smooth muscle cells and endothelial cells.^2,3

1.Ahn, H.S., Arik, L., Boykow, G., et al.Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonistsBioorg. Med. Chem. Lett.9(14)2073-2078(1999) 2.Ahn, H.S., Foster, C., Boykow, G., et al.Inhibition of cellular action of thrombin by N3-cyclopropyl-7-{[4-(1-methylethyl)phenyl]methyl}-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonistBiochem. Pharmacol.60(10)1425-1434(2000) 3.Lidington, E.A., Steinberg, R., Kinderlerer, A.R., et al.A role for proteinase-activated receptor 2 and PKC-ε in thrombin-mediated induction of decay-accelerating factor on human endothelial cellsAm. J. Physiol. Cell Physiol.289(6)1437-1447(2005)