Literature DB >> 14647531

Pharmacology of KB-R7943: a Na+-Ca2+ exchange inhibitor.

Md Shah Amran1, Nobuo Homma, Keitaro Hashimoto.   

Abstract

The Na+-Ca2+ exchange (NCX) system plays a pivotal role in regulating intracellular Ca2+ concentration in cardiomyocytes, neuronal cells, kidney and a variety of other cells. It performs a particularly important function in regulating cardiac contractility and electrical activity. One of the leading NCX inhibitors is KB-R9743 (KBR) that appears to exhibit selectivity for Ca2+-influx-mode NCX activity (reverse mode of NCX). In this article we reviewed pharmacology of KBR and provide a brief summary of studies with other NCX inhibitors, such as SEA0400 (SEA) and SN-6 (SN). Potential clinical usefulness of KBR and other NCX inhibitors is still controversial but the reviewed findings may be helpful in designing more selective and clinically useful NCX inhibitors for the treatment of cardiac, neuronal and kidney diseases.

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Year:  2003        PMID: 14647531     DOI: 10.1111/j.1527-3466.2003.tb00121.x

Source DB:  PubMed          Journal:  Cardiovasc Drug Rev        ISSN: 0897-5957


  23 in total

1.  High potency inhibition of hERG potassium channels by the sodium-calcium exchange inhibitor KB-R7943.

Authors:  Hongwei Cheng; Yihong Zhang; Chunyun Du; Christopher E Dempsey; Jules C Hancox
Journal:  Br J Pharmacol       Date:  2012-04       Impact factor: 8.739

2.  The Na+/Ca2+ exchanger inhibitor, KB-R7943, blocks a nonselective cation channel implicated in chemosensory transduction.

Authors:  A Pezier; Y V Bobkov; B W Ache
Journal:  J Neurophysiol       Date:  2008-12-31       Impact factor: 2.714

3.  Neuroprotective effect of KB-R7943 against glutamate excitotoxicity is related to mild mitochondrial depolarization.

Authors:  T P Storozhevykh; Ya E Senilova; T Brustovetsky; V G Pinelis; N Brustovetsky
Journal:  Neurochem Res       Date:  2009-09-22       Impact factor: 3.996

4.  Regional genomic regulation of cardiac sodium-calcium exchanger by oestrogen.

Authors:  Guojun Chen; Xiaoyan Yang; Sean Alber; Vladimir Shusterman; Guy Salama
Journal:  J Physiol       Date:  2011-01-04       Impact factor: 5.182

5.  Inhibitory effect of YM-244769, a novel Na+/Ca2+ exchanger inhibitor on Na+/Ca2+ exchange current in guinea pig cardiac ventricular myocytes.

Authors:  Kanna Yamashita; Yasuhide Watanabe; Satomi Kita; Takahiro Iwamoto; Junko Kimura
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2016-08-01       Impact factor: 3.000

6.  p21-Activated kinase1 (Pak1) is a negative regulator of NADPH-oxidase 2 in ventricular myocytes.

Authors:  Jaime DeSantiago; Dan J Bare; Lei Xiao; Yunbo Ke; R John Solaro; Kathrin Banach
Journal:  J Mol Cell Cardiol       Date:  2013-12-28       Impact factor: 5.000

7.  Reverse-mode Na+/Ca2+ exchange is an important mediator of venous contraction.

Authors:  Nathan R Tykocki; William F Jackson; Stephanie W Watts
Journal:  Pharmacol Res       Date:  2012-09-10       Impact factor: 7.658

8.  WITHDRAWN: Sex-differences in sodium/calcium exchange expression is a determinant of the arrhythmia phenotype in pre-pubertal rabbit hearts with Long QT type 2.

Authors:  Guojun Chen; Xiaoyan Yang; Laurie J Kerchner; Naomi R Salama; Sean Alber; Vladimir Shusterman; Barry London; Guy Salama
Journal:  Heart Rhythm       Date:  2010-12-27       Impact factor: 6.343

9.  Increased bone resorption by osteoclast-specific deletion of the sodium/calcium exchanger isoform 1 (NCX1).

Authors:  Giuseppe Albano; Silvia Dolder; Mark Siegrist; Annie Mercier-Zuber; Muriel Auberson; Candice Stoudmann; Willy Hofstetter; Olivier Bonny; Daniel G Fuster
Journal:  Pflugers Arch       Date:  2016-12-09       Impact factor: 3.657

Review 10.  Regulation of intracellular and mitochondrial sodium in health and disease.

Authors:  Elizabeth Murphy; David A Eisner
Journal:  Circ Res       Date:  2009-02-13       Impact factor: 17.367

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