Quantitative Fluorescence Measurement of Cardiac Na+/Ca2+ Exchanger Inhibition by Kinetic Analysis in Stably Transfected HEK293 Cells

Journal of Pharmacological Sciences

Hikaru Tanaka¹  Iyuki Namekata¹  Toru Kawanishi²  Naoko Iida-Tanaka¹  Koki Shigenobu¹ 

[1] Department of Pharmacology, Toho University Faculty of Pharmaceutical Sciences, Japan;Division of Biological Chemistry and Biologicals, National Institute of Health Sciences, Japan

关键词: Na+/Ca2+ exchanger;    fluorescence microscopy;    SEA0400;   

DOI  :  10.1254/jphs.SCJ06002X

学科分类：药学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(15)Cited-By(8)We developed a method to quantitatively evaluate the potency of Na+/Ca2+ exchanger (NCX) inhibitors with fluorescence microscopy in NCX1-transfected HEK 293 cells. The reverse mode and forward mode NCX activities were measured as the ascending slope of the early phase increase in cytoplasmic Ca2+ concentration after change to low Na+ extracellular solution and the descending rate (inverse of the exponential time constant) on return to normal solution, respectively. Both modes of NCX were inhibited by SEA0400 (2-[4-[(2,5-difluorophenyl)methoxy]phenoxy]-5-ethoxyaniline) and KB-R7943 (2-[2-[4-(4-nitrobenzyloxy)phenyl]ethyl]isothiourea methanesulfonate), and the concentration-inhibition relationships for both inhibitors were in good agreement with those previously reported in voltage clamped cardiomyocytes.

【 授权许可】

Unknown