Moreno-Ortega 2015 Neuropharmacology
| Moreno-Ortega AJ, Martínez-Sanz FJ, Lajarín-Cuesta R, de Los Rios C, Cano-Abad MF (2015) Benzothiazepine CGP37157 and its 2'-isopropyl analogue modulate Ca2+ entry through CALHM1. Neuropharmacology 95:503-10. |
Moreno-Ortega AJ, Martínez-Sanz FJ, Lajarín-Cuesta R, de Los Rios C, Cano-Abad MF (2015) Neuropharmacology
Abstract: CALHM1 is a Ca2+ channel discovered in 2008, which plays a key role in the neuronal electrical activity, among other functions. However, there are no known efficient blockers able to modulate its Ca2+ handling ability. We herein describe that benzothiazepine CGP37157 and its newly synthesized analogue ITH12575 reduced Ca2+ influx through CALHM1 at low micromolar concentrations. These results could serve as a starting point for the development of more selective CALHM1 ligands using CGP37157 as a hit compound, which would help to study the physiological role of CALHM1 in the control of [2+]cyt in excitable cells, as well as its implication in CNS diseases.
Copyright © 2015 Elsevier Ltd. All rights reserved. • Keywords: Benzothiazepines, CGP37157, Calcium homeostasis modulator 1 (CALHM1), Carbonyl cyanide-p-trifluoromethoxyphenylhydrazone, Dimebolin, FCCP, ITH12575, Neurodegenerative diseases, PubChem CID: 197033, PubChem CID: 2688, PubChem CID: 3330
Labels:
