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Chinfloxacin hydrochloride inhibits HERG potassium channel at open state
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 12
- DOI:
- No doi available
- Key Word:
- 盐酸昌欣沙星;HERG钾离子通道;氟喹诺酮
Abstract： 探讨一种新型氟喹诺酮类抗菌剂盐酸昌欣沙星(chinfloxacin hydrochloride,CFX)对HERG(human ether-(a)-go-go-related gene)钾离子通道动力学的影响.利用全细胞膜片钳技术,在HEK293细胞中记录异源表达的HERG钾电流,观察CFX对通道的抑制作用,分析其对通道激活、失活和去激活等动力学过程的影响.结果表明,CFX作用于HERG钾离子通道的开放状态,以浓度依赖的方式抑制HERG钾电流,半有效抑制浓度(IC50)为(162.1±14.2)μmol·L-1,是其改造前体盐酸莫西沙星的2倍,但CFX不改变通道动力学特性.由于改变细胞外液K+浓度,CFX对HERG钾电流抑制作用增强.
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