Inhibition by fluoroquinolones of K+ currents in rat dissociated hippocampal neurons
文献类型：期刊论文
| 作者 | Zhang, LR; Li, MH; Cheng, NN; Chen, BY; Wang, YM |
| 刊名 | EUROPEAN JOURNAL OF PHARMACOLOGY
 |
| 出版日期 | 2003-02-21 |
| 卷号 | 462期号:1-3页码:9-13 |
| 关键词 | fluoroquinolone hippocampus K+ current, transient K+ current, delayed rectifier |
| ISSN号 | 0014-2999 |
| DOI | 10.1016/S0014-2999(03)01316-5 |
| 文献子类 | Article |
| 英文摘要 | The effects of four fluoroquinolones (sparfloxacin, fleroxacin, ofloxacin and levofloxacin) on K+ currents were investigated in pyramidal neurons acutely isolated from rat hippocampus, to evaluate their relative, potencies for inhibiting these channels. Using patch-clamp electrophysiological techniques, we found that all four compounds inhibited the delayed rectifier K+ current (I-K), but with different potencies. Sparfloxacin was the most potent compound, displaying an IC50 value of 6.44 x 10(-4) M, followed by fleroxacin, ofloxacin and levofloxacin, their IC50 values being 7.09 X 10(-3), 8.42 x 10(-3) and 1.10 x 10(-2) M, respectively. In contrast, the fast transient K+ current (I-A) was blocked only by sparfloxacin (IC50 = 2.86 x 10(-3) M) and fleroxacin (IC50=4.38 x 10(-3) M), but not by ofloxacin and levofloxacin even at concentrations up to 1 mM. The K+ current inhibition was reversible after washout of the compounds. Further study is needed to clarify the possible involvement of this novel action in the adverse effects of fluoroquinolones in the central nervous system (CNS). (C) 2003 Elsevier Science B.V. All rights reserved. |
| WOS关键词 | AMINOBUTYRIC-ACID RECEPTOR ; QUINOLONES ; TOXICITY ; GABA(A) ; SITES ; CIPROFLOXACIN ; SPARFLOXACIN ; LEVOFLOXACIN ; OFLOXACIN ; BINDING |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000181088700002 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274261]  |
| 专题 | 新药研究国家重点实验室 中科院受体结构与功能重点实验室 |
| 通讯作者 | Cheng, NN |
| 作者单位 | 1.Fudan Univ, Sch Pharm, Dept Pharmacol, Shanghai 200032, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 200032, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, LR,Li, MH,Cheng, NN,et al. Inhibition by fluoroquinolones of K+ currents in rat dissociated hippocampal neurons[J]. EUROPEAN JOURNAL OF PHARMACOLOGY,2003,462(1-3):9-13. |
| APA | Zhang, LR,Li, MH,Cheng, NN,Chen, BY,&Wang, YM.(2003).Inhibition by fluoroquinolones of K+ currents in rat dissociated hippocampal neurons.EUROPEAN JOURNAL OF PHARMACOLOGY,462(1-3),9-13. |
| MLA | Zhang, LR,et al."Inhibition by fluoroquinolones of K+ currents in rat dissociated hippocampal neurons".EUROPEAN JOURNAL OF PHARMACOLOGY 462.1-3(2003):9-13. |
入库方式： OAI收割
来源：上海药物研究所
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