کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8318604 | 1539012 | 2014 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Inhibition of the cardiac ATP-dependent potassium current by KB-R7943
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کلمات کلیدی
ATP-sensitive K+ currentCCCPIKAChNCXKB-R7943IKrIK1IncXIKATPiKIRdelayed rectifier K+ current - تکرار K + کنتاکتورFish heart - قلب ماهیCardiomyocytes - قلب و عروقSodium–calcium exchanger - مبدل سدیم کلسیمIon channels - کانال های یونیcarbonyl cyanide m-chlorophenyl hydrazone - کربونیل سیانید m-کلروفنیل هیدرازونglibenclamide - گلی بن کلامید
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Inhibition of the cardiac ATP-dependent potassium current by KB-R7943 Inhibition of the cardiac ATP-dependent potassium current by KB-R7943](/preview/png/8318604.png)
چکیده انگلیسی
KB-R7943 (2-[2-[4-(4-nitrobenzyloxy)phenyl]ethyl]isothiourea) was developed as a specific inhibitor of the sarcolemmal sodium-calcium exchanger (NCX) with potential experimental and therapeutic use. However, in cardiomyocytes KB-R7943 also effectively blocks several K+ currents including the delayed rectifier, IKr, and background inward rectifier, IK1. In the present study we analyze the effects of KB-R7943 on the ATP-dependent potassium current (IKATP) recorded by whole-cell patch-clamp in ventricular cardiomyocytes from a mammal (mouse) and a fish (crucian carp). IKATP was induced by external application of a mitochondrial uncoupler CCCP (3 Ã 10â 7 M) and internal perfusion of the cell with ATP-free pipette solution. A weakly inwardly rectifying current with a large outward component, recorded in the presence of CCCP, was blocked with 10â 5 M glibenclamide by 56.1 ± 4.6% and 56.9 ± 3.6% in crucian carp and mouse ventricular myocytes, respectively. In fish cardiomyocytes IKATP was blocked by KB-R7943 with an IC50 value of 3.14 Ã 10â 7 M, while in mammalian cells IC50 was 2.8 Ã 10â 6 M (P < 0.05). 10â 5 M KB-R7943 inhibited CCCP-induced IKATP by 99.9 ± 0.13% and 97.5 ± 1.2% in crucian carp and mouse ventricular myocytes, respectively. In crucian carp the IKATP is about an order of magnitude more sensitive to KB-R7943 than the background IK1, but in mammals IKATP and IK1 are almost equally sensitive to KB-R7943. Therefore, the ability of KB-R7943 to block IKATP should be taken into account together with INCX inhibition when investigating possible cardioprotective effects of this compound.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Comparative Biochemistry and Physiology Part A: Molecular & Integrative Physiology - Volume 175, September 2014, Pages 38-45
Journal: Comparative Biochemistry and Physiology Part A: Molecular & Integrative Physiology - Volume 175, September 2014, Pages 38-45
نویسندگان
Denis V. Abramochkin, Matti Vornanen,