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CGP 37157 is a potent and selective antagonist of the mitochondrial Na+-Ca2+ exchanger with IC50 value of 0.4 μM [1].

The mitochondrial Na+-Ca2+ exchanger (mNCE) is an antiporter membrane protein and removes a single Ca2+ in exchange for the import of three Na+. Mitochondrial Ca2+ uptake plays a critical role in the control of apoptosis, regulation of metabolic activity and Ca2+ shaping and buffering of Ca2+ signals [2].

CGP 37157 is a selective mNCE antagonist. In isolated heart mitochondria, CGP-37157 inhibited the activity of mNCE with IC50 value of 0.36 μM in a dose-dependent way [1]. In human and mouse β-cells, CGP-37157 inhibited KCl- and glucose-stimulated Ca2+ signals in a dose-dependent way and decreased insulin secretion from perifused islets [2]. In rat forebrain neurons, CGP-37157 consistently caused a rapid fall in Ca2+ influx stimulated by glutamate, which suggested the recovery of Ca2+ influx induced by glutamate was regulated via mNCE [3]. In rat dorsal root ganglion neurons, CGP37157 inhibited depolarization-induced Ca2+ influx and mitochondrion-mediated Ca2+ influx [4].

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