Forefront of Na+/Ca2+ Exchanger Studies: Molecular Pharmacology of Na+/Ca2+ Exchange Inhibitors
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- Iwamoto Takahiro
- Department of Pharmacology, School of Medicine, Fukuoka University
Bibliographic Information
- Other Title
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- Molecular Pharmacology of Na〔+〕/Ca〔2+〕 Exchange Inhibitors
- Molecular Pharmacology of Na Ca 2 Exchange Inhibitors
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Abstract
The Na+/Ca2+ exchanger (NCX) is an ion transporter that exchanges Na+ and Ca2+ in either Ca2+ efflux or Ca2+ influx mode, depending on membrane potential and transmembrane ion gradients. In myocytes, neurons, and nephron cells, NCX is thought to play an important role in the regulation of intracellular Ca2+ concentration. Recently, the benzyloxyphenyl derivatives KB-R7943, SEA0400, and SN-6 have been developed as selective NCX inhibitors. Currently, SEA0400 is the most potent and selective inhibitor. These inhibitors possess different isoform-selectivities, although they have similar properties, such as Ca2+ influx mode-selectivity and I1 inactivation-dependence. Recent site-directed mutagenesis has revealed that these inhibitors possess some molecular determinants (Phe-213, Val-227, Tyr-228, Gly-833, and Asn-839) for interaction with NCX1. These benzyloxyphenyl derivatives are expected to be useful tools to study the physiological roles of NCX. Moreover, such inhibitors may have therapeutic potential as a new remedy for ischemic disease, arrhythmias, heart failure, and hypertension.<br>
Journal
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- Journal of Pharmacological Sciences
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Journal of Pharmacological Sciences 96 (1), 27-32, 2004
The Japanese Pharmacological Society
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Keywords
Details 詳細情報について
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- CRID
- 1390282680151871744
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- NII Article ID
- 10014166162
- 130000074341
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- NII Book ID
- AA11806667
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- ISSN
- 13478648
- 13478613
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- NDL BIB ID
- 7084185
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- PubMed
- 15359084
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed