Inhibition of GABAA receptor-mediated current responses by enoxacin (new quinolone) and felbinac (non-steroidal anti-inflammatory drug) in Xenopus oocytes injected with mouse-brain messenger RNA.
The convulsant interaction between enoxacin (ENX), a new quinolone antibacterial agent (NQ), and felbinac (FLB), a non-steroidal anti-inflammatory drug (NSAID), in vivo was reproduced as the change of GABA-induced current response in Xenopus oocytes injected with mouse brain mRNA. GABA (10 microM) response was inhibited by ENX in a dose-dependent manner, and IC50 of ENX was 96 microM. Moreover, the inhibitory effect of ENX was 80-fold potentiated in the presence of 10 microM FLB. The GABAA-antagonistic interaction between these two drugs in vitro was considered a possible mechanism of convulsant reaction after concomitant administration of NQs and NSAIDs in vivo.
Kawakami
J
J
Department of Pharmacy, University of Tokyo Hospital, Faculty of Medicine, Japan.
Shimokawa
M
M
Yamamoto
K
K
Sawada
Y
Y
Asanuma
A
A
Yanagisawa
K
K
Iga
T
T
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D001923:Brain Chemistry; D004357:Drug Synergism; D004594:Electrophysiology; D015365:Enoxacin / Q000494:pharmacology*; D051379:Mice; D009865:Oocytes / Q000187:drug effects / Q000378:metabolism*; D010648:Phenylacetates / Q000494:pharmacology*; D011061:Poly A / Q000378:metabolism; D012313:RNA / Q000378:metabolism; D012333:RNA, Messenger / Q000378:metabolism*; D018079:Receptors, GABA / Q000187:drug effects*; D014982:Xenopus laevis; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D010648:Phenylacetates; D012333:RNA, Messenger; D018079:Receptors, GABA; D011061:Poly A; D015365:Enoxacin; C012776:biphenylylacetic acid; D005680:gamma-Aminobutyric Acid; D012313:RNA