Flufenamic acid is a pH-dependent antagonist of TRPM2 channels

Neuropharmacology

Volumn 47, Issue 3, 2004, Pages 450-460

  Hill, K ^a   Benham, C D ^a   McNulty, S ^a   Randall, A D ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Calcium; Fenamate; Flufenamic acid; Transient receptor potential; TRPM2

Indexed keywords

ADENOSINE DIPHOSPHATE RIBOSE; FLUFENAMIC ACID; NONSTEROID ANTIINFLAMMATORY AGENT; RECOMBINANT PROTEIN; TRANSIENT RECEPTOR POTENTIAL CHANNEL;

ANIMAL CELL; ARTICLE; CELL LINE; CONCENTRATION RESPONSE; CONTROLLED STUDY; ELECTRIC CURRENT; ELECTROPHYSIOLOGY; EMBRYO; HUMAN; HUMAN CELL; INSULINOMA; KINETICS; NONHUMAN; PATCH CLAMP; PH; PRIORITY JOURNAL; PROTEIN FUNCTION; RAT; TIME;

ADENOSINE DIPHOSPHATE RIBOSE; ANIMALS; CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INTERACTIONS; EMBRYO; FLUFENAMIC ACID; HUMANS; HYDROGEN-ION CONCENTRATION; INSULINOMA; ION CHANNELS; KIDNEY; MEMBRANE POTENTIALS; MEMBRANE PROTEINS; PATCH-CLAMP TECHNIQUES; RATS; RECOMBINANT PROTEINS; TRPM CATION CHANNELS;

EID: 3242736642     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.neuropharm.2004.04.014     Document Type: Article

References (30)

1. Bevan S., Szolcsanyi J. Sensory neuron-specific actions of capsaicin: mechanisms and applications. Trends Pharmacol. Sci. 11:1990;330-333
2. Boland L.M., Morrill J.A., Bean B.P. Omega-conotoxin block of N-type calcium channels in frog and rat sympathetic neurons. J. Neurosci. 14:1994;5011-5027
3. Chen Q., Olney J.W., Lukasiewicz P.D., Almli T., Romano C. Fenamates protect neurons against ischemic and excitotoxic injury in chick embryo retina. Neurosci. Lett. 242:1998;163-166
4. Cho H., Kim M.S., Shim W.S., Yang Y.D., Koo J., Oh U. Calcium-activated cationic channel in rat sensory neurons. Eur. J. Neurosci. 17:2003;2630-2638
5. Clapham D.E., Montell C., Schultz G., Julius D. International Union of Pharmacology, XLIII. Compendium of voltage-gated ion channels: transient receptor potential channels. Pharmacol. Rev. 55:2003;591-596
6. Grimm C., Kraft R., Sauerbruch S., Schultz G., Harteneck C. Molecular and functional characterization of the melastatin-related cation channel TRPM3. J. Biol. Chem. 278:2003;21493-21501
7. 2+-permeable channel activated by changes in redox status confers susceptibility to cell death. Mol. Cell. 9:2002;163-173
8. Heiner I., Eisfeld J., Halaszovich C.R., Wehage E., Jungling E., Zitt C., Luckhoff A. Expression profile of the transient receptor potential (TRP) family in neutrophil granulocytes: evidence for currents through long TRP channel 2 induced by ADP-ribose and NAD. Biochem. J. 371:2003;1045-1053
9. Herson P.S., Lee K., Pinnock R.D., Hughes J., Ashford M.L. Hydrogen peroxide induces intracellular calcium overload by activation of a non-selective cation channel in an insulin-secreting cell line. J. Biol. Chem. 274:1999;833-841
10. Inamura K., Sano Y., Mochizuki S., Yokoi H., Miyake A., Nozawa K., Kitada C., Matsushime H., Furuichi K. Response to ADP-Ribose by Activation of TRPM2 in the CRI-G1 Insulinoma Cell Line. J. Membr. Biol. 191:2003;201-207
11. 2+- activated Cl-channel currents in rat ventral prostate epithelial cells. Prostate. 55:2003;118-127
12. Kraft R., Grimm C., Grosse K., Hoffmann A., Sauerbruch S., Kettenmann H., Schultz G., Harteneck C. Hydrogen peroxide and ADP-ribose induce TRPM2-mediated calcium influx and cation currents in microglia. Am. J. Physiol. Cell Physiol. 286:2004;C129-C137
13. Lee Y.T., Wang Q. Inhibition of hKv2.1, a major human neuronal voltage-gated K+ channel, by meclofenamic acid. Eur. J. Pharmacol. 378:1999;349-356
14. Lee R.J., Shaw T., Sandquist M., Partridge L.D. Mechanism of action of the non-steroidal anti-inflammatory drug flufenamate on [Ca2+]i and Ca(2+)-activated currents in neurons. Cell Calcium. 19:1996;431-438
15. Lee H.M., Kim H.I., Shin Y.K., Lee C.S., Park M., Song J.H. Diclofenac inhibition of sodium currents in rat dorsal root ganglion neurons. Brain Res. 992:2003;120-127
16. Maksay G., Korpi E.R., Uusi-Oukari M. Bimodal action of furosemide on convulsant [3H]EBOB binding to cerebellar and cortical GABA(A) receptors. Neurochem. Int. 33:1998;353-358
17. Martin R.L., Lee J.H., Cribbs L.L., Perez-Reyes E., Hanck D.A. Mibefradil block of cloned T-type calcium channels. J. Pharmacol. Exp. Ther. 295:2000;302-308
18. 2+ dependence of transient receptor potential melastatin 2 (TRPM2) cation channel activation. J. Biol. Chem. 278:2003;11002-11006
19. Meadows H.J., Randall A.D. Functional characterisation of human TASK-3, an acid-sensitive two-pore domain potassium channel. Neuropharmacology. 40:2001;551-559
20. Moffat A.C. Clarke's Isolation and Identification of Drugs. 1986;The Pharmaceutical Press
21. Perraud A.L., Fleig A., Dunn C.A., Bagley L.A., Launay P., Schmitz C., Stokes A.J., Zhu Q., Bessman M.J., Penner R., Kinet J.P., Scharenberg A.M. ADP-ribose gating of the calcium-permeable LTRPC2 channel revealed by Nudix motif homology. Nature. 411:2001;595-599
22. Perraud A.L., Schmitz C., Scharenberg A.M. TRPM2 Ca(2+) permeable cation channels: from gene to biological function. Cell Calcium. 33:2003;519-531
23. 2+]i. Proc. Natl. Acad. Sci. USA. 100:2003;15166-15171
24. Sinkkonen S.T., Mansikkamaki S., Moykkynen T., Luddens H., Uusi-Oukari M., Korpi E.R. Receptor subtype-dependent positive and negative modulation of GABA(A) receptor function by niflumic acid, a nonsteroidal anti-inflammatory drug. Mol. Pharmacol. 64:2003;753-763
25. Smith M.A., Herson P.S., Lee K., Pinnock R.D., Ashford M.L. Hydrogen-peroxide-induced toxicity of rat striatal neurones involves activation of a non-selective cation channel. J. Physiol. 547:2003;417-425
26. Srinivas M., Spray D.C. Closure of gap junction channels by arylaminobenzoates. Mol. Pharmacol. 63:2003;1389-1397
27. Tozzi A., Bengtson C.P., Longone P., Carignani C., Fusco F.R., Bernardi G., Mercuri N.B. Involvement of transient receptor potential-like channels in responses to mGluR-I activation in midbrain dopamine neurons. Eur. J. Neurosci. 18:2003;2133-2145
28. Wilson H.L., Dipp M., Thomas J.M., Lad C., Galione A., Evans A.M. ADP-ribosyl cyclase and cyclic ADP-ribose hydrolase act as a redox sensor. J. Biol. Chem. 276:2001;11180-11188
29. + channel gene expression. Circulation. 107:2003;1917-1922
30. Zhang W., Chu X., Tong Q., Cheung J.Y., Conrad K., Masker K., Miller B.A. A novel TRPM2 isoform inhibits calcium influx and susceptibility to cell death. J. Biol. Chem. 278:2003;16222-16229