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KMID : 0811720070110000087
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Korean Journal of Physiology & Pharmacology
2007 Volume.11 No. 0 p.87 ~ p.0
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Inhibition of L-type Ca2+ Channel by Mitochondrial Na+-Ca2+ Exchange Inhibitor CGP-37157 in Rat Atrial Myocytes
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Thu Le Thi
Son Min-Jeong
Woo Sun-Hee
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Abstract
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7-chloro-5-(2-chlorophenyl)-1,5-dihydro-4,1-benzothiazepine-2(3H)-one (CGP-37157) inhibits mitochondrial Na+-Ca2+ exchange. It is often used as an experimental tool for studying the role of the mitochondrial Na+-Ca2+ exchanger in Ca2+ signaling. Because the selectivity of CGP-37157 in adult cardiomyocytes has not been confirmed, we tested whether CGP-37157 affects the L-type Ca2+ channel using a whole-cell patch-clamp in adult rat atrial myocytes. We found that CGP-37157 suppressed L-type Ca2+ current (ICa) with IC50 of ∼0.27μM, without altering the voltage dependence of the current-voltage relationships. CGP-37157 inhibited the Ba2+ current (IBa) through the Ca2+ channel with a similar dose-response. The inhibitory effects of CGP-37157 on ICa or IBa were resistant to the intracellular Ca2+ buffering. Intracellular application of CGP-37157 did not significantly alter ICa. The combination of CGP-37157 with known Ca2+ channel inhibitor diltiazem yielded antagonism consistent with additivity of response. Our data suggest that CGP-37157 directly suppresses the L-type Ca2+ channel in intact adult cardiomyocytes.
Source: Korean Journal of Physiology & Pharmacology.2007 Oct;11(Suppl II):S82-S82
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KEYWORD
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CGP-37157, L-type Ca2+ current, Atrial myocyte
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