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Martinez-Sanz 2015 ACS Chem Neurosci

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Martínez-Sanz FJ, Lajarín-Cuesta R, Moreno-Ortega AJ, González-Lafuente L, Fernández-Morales JC, López-Arribas R, Cano-Abad MF, de los Ríos C (2015) Benzothiazepine CGP37157 analogues exert cytoprotection in various in vitro models of neurodegeneration. ACS Chem Neurosci 6:1626-36.

» PMID: 26192029

Martinez-Sanz FJ, Lajarin-Cuesta R, Moreno-Ortega AJ, Gonzalez-Lafuente L, Fernandez-Morales JC, Lopez-Arribas R, Cano-Abad MF, de los Rios C (2015) ACS Chem Neurosci

Abstract: Mitochondria regulate cellular Ca(2+) oscillations, taking up Ca(2+) through its uniporter and releasing it through the mitochondrial sodium/calcium exchanger. The role of mitochondria in the regulation of Ca(2+) cycle has received much attention recently, as it is a central stage in neuronal survival and death processes. Over the last decades, the 4,1-benzothiazepine CGP37157 has been the only available blocker of the mitochondrial sodium/calcium exchanger, although it targets several other calcium transporters. We report the synthesis of 4,1-benzothiazepine derivatives with the goal of enhancing mitochondrial sodium/calcium exchanger blockade and selectivity, and the evaluation of their cytoprotective effect. The compound 4c presented an interesting neuroprotective profile in addition to an important blockade of the mitochondrial sodium/calcium exchanger. The use of this benzothiazepine could help to understand the physiological functions of the mitochondrial sodium/calcium exchanger. In addition, we hypothesize that a moderate blockade of the mitochondrial sodium/calcium exchanger would provide enhanced neuroprotection in neurons. Keywords: Benzothiazepines, NCLX, mNCX, Mitochondria, Neurodegeneration, Neuroprotection


Labels: Pathology: Neurodegenerative