Abstract：
: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 IC(50) value of 6.44 x 10(-4) M, followed by fleroxacin, ofloxacin and levofloxacin, their IC(50) 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 (IC(50)=2.86 x 10(-3) M) and fleroxacin (IC(50)=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).
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Zhang LR,Li MH,Cheng NN,Chen BY,Wang YMdoi
10.1016/s0014-2999(03)01316-5keywords:
subject
Has Abstractpub_date
2003-02-21 00:00:00pages
9-13issue
1-3eissn
0014-2999issn
1879-0712pii
S0014299903013165journal_volume
462pub_type
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