Effects of KRN4884, a novel K+ channel opener, on ionic currents in rabbit femoral arterial myocytes.
Effects of KRN4884, a novel K+ channel opener, on ionic currents in rabbit femoral arterial myocytes.
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KRN4884（一种新型 K 通道开放剂）对兔股动脉肌细胞离子电流的影响。
DOI：
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发表时间：
2003
影响因子：
3.5
通讯作者：
Y. Imaizumi
中科院分区：
文献类型：
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作者：
K. Muraki;Akiko Sasaoka;S. Ohya;Minoru Watanabe;Y. Imaizumi
在兔股动脉肌细胞（RFAM）上观察了新型钾通道开放剂KRN 4884（5-amino-N-[2-（2-chlorophenyl）ethyl]-N '-cyano-3-pyridinecarboxamidine）对离子电流的影响。在全细胞钳条件下，细胞灌流5.9 mM K（+）浴溶液，KRN 4884引起一个外向电流在-30 mV。KRN 4884诱导的电流具有-78 mV的逆转电位，并通过应用格列本脲（glib）消除。KRN 4884在激活ATP敏感性K（+）电流（I（K-ATP））方面的效力约为左克罗卡林的43倍。另一方面，KRN 4884既不影响电压依赖性Ca（2+）通道电流，也不影响延迟整流型K（+）通道电流。在由内而外的膜片钳配置中，细胞用对称的140 mM K（+）溶液灌流，KRN 4884在腺苷二磷酸存在下激活47 pS K（+）通道。类似的47 pS K（+）通道，这是可逆的抑制glib，记录在外向补丁条件下。RT-PCR分析发现，内向整流钾通道6.1（Kir6.1）和磺酰脲2B（SUR 2B）转录本主要表达于兔股动脉。这些结果表明KRN 4884有效地激活RFAM中的I（K-ATP）。KRN 4884敏感性47 pS K（+）通道活性是I（K-ATP）的基础，是一种血管型K（ATP）通道，由Kir6.1和SUR 2B组成，与其他类型平滑肌中K（+）通道开放剂激活的ATP敏感性K（+）通道具有相似的特征。
Effects of KRN4884 (5-amino-N-[2-(2-chlorophenyl)ethyl]-N'-cyano-3-pyridinecarboxamidine), a novel K(+) channel opener, on ionic currents were examined in rabbit femoral arterial myocytes (RFAMs). Under whole-cell clamp conditions where cells were superfused with 5.9 mM K(+) bathing solution, KRN4884 elicited an outward current at -30 mV. KRN4884-induced current had a reversal potential of -78 mV and was abolished by application of glibenclamide (glib). KRN4884 was approximately 43 times more potent than levcromakalim in activating an ATP-sensitive K(+) current (I(K-ATP)). On the other hand, KRN4884 affected neither voltage-dependent Ca(2+) nor delayed rectifier K(+) channel currents. In the inside-out patch clamp configuration where cells were superfused with the symmetrical 140 mM K(+) solution, KRN4884 activated 47 pS K(+) channels in the presence of adenosine diphosphate. Similar 47 pS K(+) channels, which were reversibly inhibited by glib, were recorded under outside-out patch conditions. Using RT-PCR analysis, we found that inward rectifier K channel 6.1 (Kir6.1) and sulfonylurea 2B (SUR2B) transcripts were predominantly expressed in rabbit femoral artery. These results indicate that KRN4884 potently activates I(K-ATP) in RFAMs. The KRN4884-sensitive 47 pS K(+) channel activity underlying I(K-ATP) is a vascular type K(ATP) channel consisting of Kir6.1 and SUR2B and has similar characteristics to those of ATP-sensitive K(+) channels activated by K(+) channel openers in other types of smooth muscles.
影响因子：
56.9
作者：
STANDEN, NB;QUAYLE, JM;NELSON, MT
通讯作者：
NELSON, MT