封锁腺苷triphosphate-sensitive thiamylal钾离子通道的鼠心室细胞。

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呢堤Y, Oshita年代,Kitahata H,黑田Y,【T, Nakaya Y

封锁腺苷triphosphate-sensitive thiamylal钾离子通道的鼠心室细胞。

麻醉学。2000年4月,92 (4):1154 - 9。

PubMed ID

10754636 (在PubMed

]

文摘

背景:三磷酸腺苷(ATP)敏感的钾()诱导通道保护细胞在缺血和再灌注。本研究调查的影响thiamylal atp敏感性钾通道活动在孤立在模拟缺血大鼠心室细胞。方法:雄性Wistar鼠与乙醚麻醉。单身,静心室细胞分散酶学。膜电流使用膜片钳技术记录。cell-attached配置中,诱导通道电流进行评估之前和期间激活这些渠道的2,4-dinitrophenol管理25后,50和100 mg / l thiamylal。从current-amplitude直方图开放概率确定。由内而外的配置,得到的电流电压关系之前和之后的应用thiamylal(50毫克/ 1)。结果:在cell-attached配置2 4-dinitrophenol引起频繁的通道打开。2,4-Dinitrophenol-induced通道活动显著减少了格列本脲,这表明渠道研究诱导通道。 Open probability of KATP channels was reduced by thiamylal in a concentration-dependent manner. KATP channels could be activated in the inside-out configuration because of the absence of ATP. Thiamylal inhibited KATP channel activity without changing the single-channel conductance. CONCLUSIONS: The results obtained in this study indicate that thiamylal inhibits KATP channel activities in cell-attached and inside-out patches, suggesting a direct action of this drug on these channels.

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药物靶点

药物	目标	类	生物	药理作用	行动
Thiamylal	ATP-sensitive内向整流钾通道11	蛋白质	人类	是的	抑制剂	细节
Thiamylal	ATP-sensitive内向整流钾通道8	蛋白质	人类	是的	抑制剂	细节