EMAIL THIS PAGE TO A FRIEND

Neuropharmacology

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


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.

Related Materials

Product #

Image

Description

Molecular Formula

Add to Cart

SML1947
ITH12575, ≥98% (HPLC)
C18H18ClNOS