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Inhibition of L-type Ca2+ Channel by Mitochondrial Na+-Ca2+ Exchange Inhibitor CGP-37157 in Rat Atrial Myocytes

Inhibition of L-type Ca2+ Channel by Mitochondrial Na+-Ca2+ Exchange Inhibitor CGP-37157 in Rat Atrial Myocytes

Le Thi Thu, Joung Real Ahn, Sun-Hee Woo

Eur J Pharmacol. 2006 Dec 15;552(1-3):15-9.

PMID: 17054940

Abstract:

7-chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one (CGP-37157) inhibits mitochondrial Na(+)-Ca(2+) exchange. It is often used as an experimental tool for studying the role of the mitochondrial Na(+)-Ca(2+) exchanger in Ca(2+) signaling. Because the selectivity of CGP-37157 in adult cardiomyocytes has not been confirmed, we tested whether CGP-37157 affects the L-type Ca(2+) channel using a whole-cell patch-clamp in adult rat atrial myocytes. We found that CGP-37157 suppressed L-type Ca(2+) current (I(Ca)) with IC(50) of approximately 0.27 microM, without altering the voltage dependence of the current-voltage relationships. CGP-37157 inhibited the Ba(2+) current (I(Ba)) through the Ca(2+) channel with a similar dose-response. The inhibitory effects of CGP-37157 on I(Ca) or I(Ba) were resistant to the intracellular Ca(2+) buffering. Intracellular application of CGP-37157 did not significantly alter I(Ca). The combination of CGP-37157 with known Ca(2+) channel inhibitor diltiazem yielded antagonism consistent with additivity of response. Our data suggest that CGP-37157 directly suppresses the L-type Ca(2+) channel in intact adult cardiomyocytes.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP75450349-A	CGP-37157		75450-34-9	Price

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