Home
Resources
Publications
Benzothiazepine CGP37157 and Its 2'-isopropyl Analogue Modulate Ca²⁺ Entry Through CALHM1

Benzothiazepine CGP37157 and Its 2'-isopropyl Analogue Modulate Ca²⁺ Entry Through CALHM1

Ana J Moreno-Ortega, Francisco J Martínez-Sanz, Rocío Lajarín-Cuesta, Cristóbal de Los Rios, María F Cano-Abad

Neuropharmacology. 2015 Aug;95:503-10.

PMID: 25908402

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1802013086	ITH12575		1802013-08-6	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: