Two Non-steroidal Anti-inflammatory Drugs, Niflumic Acid and Diclofenac, Inhibit the Human Glutamate Transporter EAAT1 Through Different Mechanisms

We investigated the effects of non-steroidal anti-inflammatory drugs on substrate-induced currents of l-glutamate (l-Glu) transporter EAAT1 expressed in Xenopus laevis oocytes. Niflumic acid (NFA) and diclofenac inhibited l-Glu-induced current through EAAT1 in a noncompetitive manner. NFA produced a...

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Main Authors: Kanako Takahashi (Author), Reiko Ishii-Nozawa (Author), Kouichi Takeuchi (Author), Ken Nakazawa (Author), Kaoru Sato (Author)
Format: Book
Published: Elsevier, 2010-01-01T00:00:00Z.
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100 1 0 |a Kanako Takahashi  |e author 
700 1 0 |a Reiko Ishii-Nozawa  |e author 
700 1 0 |a Kouichi Takeuchi  |e author 
700 1 0 |a Ken Nakazawa  |e author 
700 1 0 |a Kaoru Sato  |e author 
245 0 0 |a Two Non-steroidal Anti-inflammatory Drugs, Niflumic Acid and Diclofenac, Inhibit the Human Glutamate Transporter EAAT1 Through Different Mechanisms 
260 |b Elsevier,   |c 2010-01-01T00:00:00Z. 
500 |a 1347-8613 
500 |a 10.1254/jphs.09260SC 
520 |a We investigated the effects of non-steroidal anti-inflammatory drugs on substrate-induced currents of l-glutamate (l-Glu) transporter EAAT1 expressed in Xenopus laevis oocytes. Niflumic acid (NFA) and diclofenac inhibited l-Glu-induced current through EAAT1 in a noncompetitive manner. NFA produced a leftward shift in reversal potential (Erev) of l-Glu-induced current and increased current amplitude at the potentials more negative than −100 mV. Diclofenac had no effects on E rev and inhibited the current amplitude to the same extent at all negative potentials. These results indicate that NFA and diclofenac inhibit the l-Glu-induced EAAT1 current via different mechanisms.[Supplementary methods and Figure: available only at http://dx.doi.org/10.1254/jphs.09260SC] Keywords:: l-glutamate transporter, niflumic acid, diclofenac 
546 |a EN 
690 |a Therapeutics. Pharmacology 
690 |a RM1-950 
655 7 |a article  |2 local 
786 0 |n Journal of Pharmacological Sciences, Vol 112, Iss 1, Pp 113-117 (2010) 
787 0 |n http://www.sciencedirect.com/science/article/pii/S1347861319310643 
787 0 |n https://doaj.org/toc/1347-8613 
856 4 1 |u https://doaj.org/article/bae2bf9eef364241b6d46e083b10ab9d  |z Connect to this object online.