Inhibitory effects of quinolone antibacterial agents on gamma-aminobutyric acid binding to receptor sites in rat brain membranes

@article{Tsuji1988InhibitoryEO,
  title={Inhibitory effects of quinolone antibacterial agents on gamma-aminobutyric acid binding to receptor sites in rat brain membranes},
  author={Akira Tsuji and H. Sato and Yuki Kume and Ikumi Tamai and Eiichi Okezaki and Osamu Nagata and Hideo Kato},
  journal={Antimicrobial Agents and Chemotherapy},
  year={1988},
  volume={32},
  pages={190 - 194}
}
  • A. Tsuji, H. Sato, +4 authors H. Kato
  • Published 1 February 1988
  • Biology, Medicine
  • Antimicrobial Agents and Chemotherapy
The specific binding of 3H-labeled gamma-aminobutyric acid ([3H]GABA) to synaptic plasma membranes from rat brains was inhibited by various quinolonecarboxylic acid derivatives (quinolones), and these inhibitions were concentration dependent. The binding of [3H]muscimol to GABAA sites was also inhibited. These inhibitory potencies differed widely among the quinolones examined. The Dixon plots showed that a newly developed difluorinated quinolone, NY-198 [1-ethyl-6,8-difluoro-1,4-dihydro-7-(3… 
Possible intermolecular interaction between quinolones and biphenylacetic acid inhibits gamma-aminobutyric acid receptor sites.
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The findings suggested that the blockade of GABA-ersic neurotransmission in CNS is a dominant mechanism of convulsion induced by NQs and that the convulsant-adverse reaction of Nqs in vivo may be predicted from the inhibitory effect on the GABA(A) receptor in vitro using the Xenopus oocytes translation system of exogenous mRNA.
Involvement of inhibitory and excitatory neurotransmitters in levofloxacin- and ciprofloxacin-induced convulsions in mice.
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It is suggested that LVFX has fewer effects on the brains than CPFX and that convulsions induced by these quinolones alone and by thesequinolones administered with BPAA may be mediated largely through glutamate and GABA(B) rather than GABA(A) receptors in mice.
Selective antagonism of the GABAA receptor by ciprofloxacin and biphenylacetic acid
TLDR
The data indicate that ciprofloxacin and BPAA are selective antagonists of GABAA receptors, an action that may contribute to their excitatory effects in vivo and suggest that the molecular properties of GabAA receptors in different regions of the CNS influence the extent to which these drugs synergistically inhibit the GAB AA receptor.
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