کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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2011231 | 1066999 | 2015 | 6 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Inhibitory effects of imperatorin on voltage-gated K+ channels and ATP-sensitive K+ channels Inhibitory effects of imperatorin on voltage-gated K+ channels and ATP-sensitive K+ channels](/preview/png/2011231.png)
BackgroundImperatorin is a furocoumarin isolated from Angelica archangelica and Cnidium monnieri. It has multiple neuromodulatory actions such as anticonvulsant effects, anxiolytic effects and anti-nociceptive effects. Although there have been reports demonstrating its effects on voltage-gated Na+ channels (VGSC) and transient reversal potential (TRP) V1 channels in neurons, there is hitherto no work showing whether this compound affects voltage-gated K+ (Kv) channels and ATP-sensitive K+ (KATP) channels.MethodsWe investigated the effects of imperatorin on K+ channels using whole-cell configuration voltage-clamp technique.ResultsImperatorin inhibited Kv channels in differentiated neuronal NG108-15 cells, and caused a left shift in the steady-state inactivation curve without affecting activation gating. Imperatorin also inhibited heterologously expressed wild type Kv1.2 and Kv2.1 channels, but became much less potent in inhibiting Kv1.2 V370G, a mutant defective in C-type inactivation, implying that drug inhibition depends on C-type inactivation. At a high concentration (100 μM), imperatorin also suppressed KATP channels.ConclusionOur results suggest that imperatorin inhibited both Kv and KATP channels.
Journal: Pharmacological Reports - Volume 67, Issue 1, February 2015, Pages 134–139