Benzothiazepine CGP37157 and its 2′-isopropyl analogue modulate Ca2+ entry through CALHM1

Autor:	Rocío Lajarín-Cuesta, Francisco J. Martínez-Sanz, Cristóbal de los Ríos, María F. Cano-Abad, Ana J. Moreno-Ortega
Rok vydání:	2015
Předmět:	Pharmacology Cellular and Molecular Neuroscience chemistry.chemical_compound Chemistry Biophysics CALHM1 Carbonyl cyanide-p-trifluoromethoxyphenylhydrazone Combinatorial chemistry Isopropyl
Zdroj:	Neuropharmacology. 95:503-510
ISSN:	0028-3908
DOI:	10.1016/j.neuropharm.2015.02.016
Popis:	CALHM1 is a Ca(2+) 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 Ca(2+) handling ability. We herein describe that benzothiazepine CGP37157 and its newly synthesized analogue ITH12575 reduced Ca(2+) 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 [Ca(2+)]cyt in excitable cells, as well as its implication in CNS diseases.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::14731caefa28f6d00a80f2ae2c3d63ab https://doi.org/10.1016/j.neuropharm.2015.02.016 Zobrazit plný text záznamu Full Text from ScienceDirect