Biochem/physiol Actions

SCH 79797 aids protection during ischemic injury. During subarachnoid hemorrhage (SAH), it plays a key role in the maintenance of microvascular integrity. SCH 79797 also elicits pro‐apoptotic and antiproliferative effects.

SCH 79797 is a nonpeptidic antagonist that targets protease activated receptor-1 (PAR-1) with high affinity (IC50 = 70 nM against 10 nM haTRAP in competitive binding assay; Ki = 35 nM) and selectively inhibits PAR-1 agonists-induced human platelet aggregation (IC50 = 300 nM and 3 μM against 300 nM haTRAP and 0.1 U/mL A-thrombin, respectively), while exhibiting little potency against platelet aggregation induced by ADP, collagen, or PAR-4 agonist γ-thrombin. SCH-79797 is shown to display neuroprotective and antiepileptogenic efficacy in a rat model of lithium/pilocarpine-induced status epilepticus (SE) in vivo (25 μg/kg via daily i.p. 20-30 min after SE termination).