Cariporide

Cariporide (HOE-642) is a selective Na⁺/H⁺ exchange inhibitor. In Vitro: Cariporide significantly suppresses markers of cell death, such as TUNEL positivity and caspase-3 cleavage, at 8 or 16 hours. Cariporide remarkably suppresses cytosolic Na⁺ and Ca²⁺ accumulation. Cariporide prevents mitochondrial membrane potential loss induced by H²⁺O^2+[1]. Cariporide (HOE-642) ameliorates myocardial ischemia/reperfusion injury, by the well-established reduction of cytosolic Ca²⁺ in cardiac myocytes through inhibition of Na⁺/H⁺ exchange^[2]. Cariporide (HOE-642), has inhibitory effects on the degranulation of human platelets, the formation of platelet–leukocyte-aggregates, and the activation of the GPIIb/IIIa receptor (PAC-1)^[3]. In Vivo: Intravenous administration of cariporide significantly decreases brain Na⁺ uptake and reduces cerebral edema, brain swelling, and infarct volume^[4].