Abstract
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-methyl-1-piperazinyl)-4-oxo-3- quinolinecarboxylic acid hydrochloride], competitively inhibits the receptor bindings of [3H]GABA and [3H]muscimol. In conclusion, our findings suggest that the inhibition of GABA binding to receptors (including uptake sites) in the brain may be involved in the induction of epileptogenic neurotoxicities by quinolones.
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- Antoniadis A., Müller W. E., Wollert U. Inhibition of GABA and benzodiazepine receptor binding by penicillins. Neurosci Lett. 1980 Jul;18(3):309–312. doi: 10.1016/0304-3940(80)90302-x. [DOI] [PubMed] [Google Scholar]
- Asano T., Ogasawara N. Solubilization of gamma-aminobutyric acid receptor from rat brain. Life Sci. 1980 Apr 7;26(14):1131–1137. doi: 10.1016/0024-3205(80)90652-9. [DOI] [PubMed] [Google Scholar]
- Bensadoun A., Weinstein D. Assay of proteins in the presence of interfering materials. Anal Biochem. 1976 Jan;70(1):241–250. doi: 10.1016/s0003-2697(76)80064-4. [DOI] [PubMed] [Google Scholar]
- Borea P. A., Bonora A. Brain receptor binding and lipophilic character of benzodiazepines. Biochem Pharmacol. 1983 Feb 15;32(4):603–607. doi: 10.1016/0006-2952(83)90482-3. [DOI] [PubMed] [Google Scholar]
- Falch E., Hedegaard A., Nielsen L., Jensen B. R., Hjeds H., Krogsgaard-Larsen P. Comparative stereostructure-activity studies on GABAA and GABAB receptor sites and GABA uptake using rat brain membrane preparations. J Neurochem. 1986 Sep;47(3):898–903. doi: 10.1111/j.1471-4159.1986.tb00695.x. [DOI] [PubMed] [Google Scholar]
- Hill D. R., Bowery N. G. 3H-baclofen and 3H-GABA bind to bicuculline-insensitive GABA B sites in rat brain. Nature. 1981 Mar 12;290(5802):149–152. doi: 10.1038/290149a0. [DOI] [PubMed] [Google Scholar]
- Hirose T., Okezaki E., Kato H., Ito Y., Inoue M., Mitsuhashi S. In vitro and in vivo activity of NY-198, a new difluorinated quinolone. Antimicrob Agents Chemother. 1987 Jun;31(6):854–859. doi: 10.1128/aac.31.6.854. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hori S., Kurioka S., Matsuda M., Shimada J. Inhibitory effect of cephalosporins on gamma-aminobutyric acid receptor binding in rat synaptic membranes. Antimicrob Agents Chemother. 1985 Apr;27(4):650–651. doi: 10.1128/aac.27.4.650. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Tsuji A., Kubo O., Miyamoto E., Yamana T. Physicochemical properties of beta-lactam antibiotics: oil-water distribution. J Pharm Sci. 1977 Dec;66(12):1675–1679. doi: 10.1002/jps.2600661205. [DOI] [PubMed] [Google Scholar]
- Zukin S. R., Young A. B., Snyder S. H. Gamma-aminobutyric acid binding to receptor sites in the rat central nervous system. Proc Natl Acad Sci U S A. 1974 Dec;71(12):4802–4807. doi: 10.1073/pnas.71.12.4802. [DOI] [PMC free article] [PubMed] [Google Scholar]
- de Boer T., Stoof J. C., van Duyn H. Effect of penicillin on transmitter release from rat cortical tissue. Brain Res. 1980 Jun 16;192(1):296–300. doi: 10.1016/0006-8993(80)91033-1. [DOI] [PubMed] [Google Scholar]