کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9425855 | 1295895 | 2005 | 13 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Inhibition of the cloned delayed rectifier K+ channels, Kv1.5 and Kv3.1, by riluzole
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کلمات کلیدی
PTXIMDMKv1.5Kv3.1I–V - I - VIscove’s Modified Dulbecco’s Medium - اصلاح شده Dulbecco Medium Iscove استCho - برایChinese Hamster Ovary - تخمدان هامستر چینیcurrent-voltage - جریان ولتاژriluzole - ریلوزولpertussis toxin - سموم سورافنیhigh voltage-activated - ولتاژ بالا فعال می شودG-proteins - پروتئین GHVA - چه
موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب (عمومی)
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The action of riluzole, a neuroprotective drug, on cloned delayed rectifier K+ channels (Kv1.5 and Kv3.1) was examined using the whole-cell patch-clamp technique. Riluzole reversibly inhibited Kv1.5 currents in a concentration-dependent manner with an IC50 of 39.69±2.37μM. G-protein inhibitors (pertussis toxin and GDPβS) did not prevent this inhibition of riluzole on Kv1.5. No voltage-dependent inhibition by riluzole was found over the voltage range in which channels are fully activated. Riluzole shifted the steady-state inactivation curves of Kv1.5 in a hyperpolarizing direction in a concentration-dependent manner. It accelerated the deactivation kinetics of Kv1.5 in a concentration dependent-manner, but had no effect on the steady-state activation curve. Riluzole exhibited a use-independent inhibition of Kv1.5. The effects of riluzole on Kv3.1, the Shaw-type K+ channel were also examined. Riluzole caused a concentration-dependent inhibition of Kv3.1 currents with an IC50 of 120.98±9.74μM and also shifted the steady-state inactivation curve of Kv3.1 in the hyperpolarizing direction. Thus, riluzole inhibits both Kv1.5 and Kv3.1 currents in a concentration-dependent manner and interacts directly with Kv1.5 by preferentially binding to the inactivated and to the closed states of the channel.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Neuroscience - Volume 133, Issue 4, 2005, Pages 1007-1019
Journal: Neuroscience - Volume 133, Issue 4, 2005, Pages 1007-1019
نویسندگان
H.S. Ahn, J.-S. Choi, B.H. Choi, M.-J. Kim, D.-J. Rhie, S.-H. Yoon, Y.-H. Jo, M.-S. Kim, K.-W. Sung, S.J. Hahn,