CGP-37157
MPTP inhibitor / Inhibits the mitochondrial Na+-Ca2+ exchanger (NCX) in isolated heart mitochondria, IC50=0.36 μM.1 Does not inhibit the plasmalemmal NCX.2 Also inhibits voltage-gated Ca2+ channels in intact cells and therefore its use in cellular studies must employ adequate controls.3 Prevents sudden death in a Guinea pig model of heart failure.4 Displays pronounced cytoprotective effects in chromaffin cells5 and in neuronal injury models.6 Blood-brain barrier permeant.
Biochemicals & reagents
75450-34-9
1) Cox et al. (1993), Selectivity of inhibition of Na(+)-CA2+ exchange of heart mitochondria by benzothiazepine CGP-37157; J. Cardiovasc. Phamracol., 21 595 2) Namekata et al. (2015), Pharmacological discrimination of plasmalemmal and mitochondrial sodium-calcium exchanger in cardiomyocyte-derived H9c2 cells; Biol. Pharm. Bull, 38 147 3) Baron & Thayer (1997), CGP37157 modulates mitochondrial Ca2+ homeostasis in cultured rat dorsal root ganglion neurons; Eur. J. Pharmacol., 340 295 4) Liu et al. (2014), Inhibiting mitochondrial Na+/Ca2+ exchange prevents sudden death in a guinea pig model of heart failure; Circ. Res., 115 44 5) Nicolau et al. (2009), Mitochondrial Na+/Ca2+-exchanger vlocker CGP37157 protects against chromaffin cell death elicited by veratridine; J. Pharmacol. Exp. Ther., 330 844 6) Ruiz et al. (2014), CGP37157, an inhibitor of the mitochondrial Na+/CA2+ exchanger, protects neurons from excitotoxicity by blocking voltage gated Ca2+ channels; Cell Death Dis., 5 e1156
RT
TARGET: Ion channel -- PATHWAY: Mitochondrial function; Calcium signaling -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Heart disease