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- Title
Modulation of Glutamate and Glycine Transporters by Niflumic, Flufenamic and Mefenamic Acids.
- Authors
Habjan, Suzanne; Vandenberg, Robert J.
- Abstract
Three fenamates—niflumic, flufenamic and mefenamic acids—were tested for effects on substrate-induced currents of glutamate and glycine transporters (EAAT1, EAAT2, GLYT1b and GLYT2a) expressed in Xenopus laevis oocytes. All fenamates inhibited EAAT1 currents; 100 μM flufenamic acid produced the most inhibition, decreasing the Imax by 53 ± 4% ( P < 0.001). EAAT2 currents were less sensitive, but 100 μM flufenamic acid inhibited the Imax by 34 ± 5% ( P = 0.006). All fenamates inhibited GLYT1b currents; 100 μM flufenamic acid produced the most inhibition, decreasing the Imax by 61 ± 1% ( P < 0.001). At 100 μM, effects on the GLYT2a Imax were mixed: 13 ± 2% inhibition by flufenamic acid ( P = 0.002), 30 ± 6% enhancement by niflumic acid ( P = 0.002), and no effect by mefenamic acid. Minor effects on substrate affinity suggested non-competitive mechanisms. These data could contribute to the development of selective transport modulators.
- Subjects
MEFENAMIC acid; GLUTAMIC acid; GLYCINE; RESPONSE inhibition; IMMUNOMODULATORS; ACETIC acid; NONSTEROIDAL anti-inflammatory agents; ANALGESICS
- Publication
Neurochemical Research, 2009, Vol 34, Issue 10, p1738
- ISSN
0364-3190
- Publication type
Article
- DOI
10.1007/s11064-009-9983-y