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Inhibition of L-type Ca2+ channel by mitochondrial Na+-Ca2+ exchange inhibitor CGP-37157 in rat atrial myocytes.
Eur J Pharmacol. 2006 Dec 15; 552(1-3):15-9.EJ

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.

Authors+Show Affiliations

College of Pharmacy, Chungnam National University, 220 Gungdong, Yuseong-Gu, Daejeon, 305-764, South Korea. shwoo@cnu.ac.krNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17054940

Citation

Thu, Le Thi, et al. "Inhibition of L-type Ca2+ Channel By Mitochondrial Na+-Ca2+ Exchange Inhibitor CGP-37157 in Rat Atrial Myocytes." European Journal of Pharmacology, vol. 552, no. 1-3, 2006, pp. 15-9.
Thu le T, Ahn JR, Woo SH. Inhibition of L-type Ca2+ channel by mitochondrial Na+-Ca2+ exchange inhibitor CGP-37157 in rat atrial myocytes. Eur J Pharmacol. 2006;552(1-3):15-9.
Thu, l. e. . T., Ahn, J. R., & Woo, S. H. (2006). Inhibition of L-type Ca2+ channel by mitochondrial Na+-Ca2+ exchange inhibitor CGP-37157 in rat atrial myocytes. European Journal of Pharmacology, 552(1-3), 15-9.
Thu le T, Ahn JR, Woo SH. Inhibition of L-type Ca2+ Channel By Mitochondrial Na+-Ca2+ Exchange Inhibitor CGP-37157 in Rat Atrial Myocytes. Eur J Pharmacol. 2006 Dec 15;552(1-3):15-9. PubMed PMID: 17054940.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Inhibition of L-type Ca2+ channel by mitochondrial Na+-Ca2+ exchange inhibitor CGP-37157 in rat atrial myocytes. AU - Thu,Le Thi, AU - Ahn,Joung Real, AU - Woo,Sun-Hee, Y1 - 2006/09/23/ PY - 2006/06/17/received PY - 2006/09/06/revised PY - 2006/09/07/accepted PY - 2006/10/24/pubmed PY - 2007/1/5/medline PY - 2006/10/24/entrez SP - 15 EP - 9 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 552 IS - 1-3 N2 - 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. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/17054940/Inhibition_of_L_type_Ca2+_channel_by_mitochondrial_Na+_Ca2+_exchange_inhibitor_CGP_37157_in_rat_atrial_myocytes_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0014-2999(06)01033-8 DB - PRIME DP - Unbound Medicine ER -