Meclofenamic acid and diclofenac, novel templates of KCNQ2/Q3 potassium channel openers, depress cortical neuron activity and exhibit anticonvulsant properties

Molecular Pharmacology

Volumn 67, Issue 4, 2005, Pages 1053-1066

  Peretz, Asher ^a   Degani, Nurit ^a   Nachman, Rachel ^a   Uziyel, Yael ^a   Gibor, Gilad ^a   Shabat, Doron ^a   Attali, Bernard ^a  

^a TEL AVIV UNIVERSITY   (Israel)

Author keywords

[No Author keywords available]

Indexed keywords

ANTICONVULSIVE AGENT; DICLOFENAC; MECLOFENAMIC ACID; POTASSIUM CHANNEL KCNQ2; POTASSIUM CHANNEL KCNQ3; POTASSIUM CHANNEL STIMULATING AGENT; RETIGABINE; VOLTAGE GATED POTASSIUM CHANNEL;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTICONVULSANT ACTIVITY; ARTICLE; BRAIN CELL; CELL MEMBRANE STEADY POTENTIAL; CHO CELL; CONTROLLED STUDY; CONVULSION; ELECTRIC SHOCK; EMBRYO; EVOKED RESPONSE; HYPERPOLARIZATION; IMMUNOCYTOCHEMISTRY; MIGRAINE; NERVE EXCITABILITY; NERVE POTENTIAL; NEUROPATHIC PAIN; NONHUMAN; OOCYTE; PATCH CLAMP; POTASSIUM CURRENT; PRIORITY JOURNAL; RAT; VOLTAGE CLAMP; XENOPUS LAEVIS;

ACTION POTENTIALS; ANIMALS; ANTICONVULSANTS; CARBAMATES; CEREBRAL CORTEX; CHO CELLS; CRICETINAE; DICLOFENAC; KCNQ2 POTASSIUM CHANNEL; KCNQ3 POTASSIUM CHANNEL; MECLOFENAMIC ACID; PHENYLENEDIAMINES; POTASSIUM CHANNELS, VOLTAGE-GATED; RATS; RATS, SPRAGUE-DAWLEY;

EID: 15744362456     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.104.007112     Document Type: Article

References (43)

1. KS channel function induced by an LQT5 mutation and other IsK mutants. EMBO (Eur Mol Biol Organ) J 18:4137-4148.
2. Baranauskas G, Tkatch T, Nagata K, Yeh J, and Surmeier DJ (2003) Kv3.4 subunits enhance the repolarizing efficiency of Kv3.1 channels in fast-spiking neurons. Nat Neurosci 6:258-266.
3. Biervert C, Schroeder BC, Kubisch C, Berkovic SF, Propping P, Jentsch TJ, and Steinlein OK (1998) A potassium channel mutation in neonatal human epilepsy. Science (Wash DC) 279:403-406.
4. Blackburn-Munro G and Jensen BS (2003) The anticonvulsant retigabine attenuates nociceptive behaviours in rat models of persistent and neuropathic pain. Eur J Pharmacol 460:109-116.
5. Brown DA (1988) M-currents, in In Ion channels, pp 55-99, Plenum, New York.
6. Brown DA and Adams PR (1980) Muscarinic suppression of a novel voltage-sensitive K+ current in a vertebrate neurone. Nature (Lond) 283:673-676.
7. Castaldo P, Miraglia del Giudice E, Coppola G, Pascotto A, Annunziato L, and Taglialatela M (2002) Benign familial neonatal convulsions caused by altered gating of KCNQ@/KCNQ3 potassium channels. J Neurosci 22:RC199.
8. Charlier C, Singh NA, Ryan SG, Lewis TB, Reus BE, Leach RJ, and Leppert M (1998) A pore mutation in a novel KQT-like potassium channel gene in an idiopathic epilepsy family. Nat Genet 18:53-55.
9. Cooper EC and Jan LY (2003) M-channels. Arch Neurol 60:496-499.
10. + channel. Proc Natl Acad Sci USA 98:12272-12277.
11. Dost R, Rostock A, and Rundfeldt C (2004) The anti-hyperalgesic activity of retigabine is mediated by KCNQ potassium channel activation. Naunyn-Schmiedeberg's Arch Pharmacol 369:382-390.
12. Du J, Zhang L, Weiser M, Rudy B, and McBain CJ (1996) Developmental expression and functional characterization of the potassium-channel subunit Kv3.1b in parvalbumin-containing interneurons of the rat hippocampus. J Neurosci 16:506-518.
13. Furst DE and Munster T (2001) Nonsteroidal ant-inflammatory drugs, disease-modifying antirheumatic drugs, nonopioid analgesics and drugs used in gout (Katzung BG ed) pp 596-623, McGraw-Hill Book Company, New York.
14. Grover GJ, D'Alonzo AJ, Sleph PG, Dzwonczyk S, Hess TA, and Darbendio RB (1994) The cardioprotective and electrophysiological effects of cromakalin are attenuated by meclofenamate through a cyclooxygenase-independent mechanism. J Pharmacol Exp Ther 269:536-540.
15. Hamill OP, Marty A, Neher E, Sakmann B, and Sigworth FJ (1981) Improved patch-clamp techniques for high resolution current recording from cells and cell-free membrane patches. Pflueg Arch Eur J Physiol 391:85-100.
16. Jentsch TJ (2000) Neuronal KCNQ potassium channels: physiology and role in diseases. Nat Neurosci 1:21-30.
17. Jurman ME, Boland LM, Liu Y, and Yellen G (1994) Visual identification of individual transfected cells for electrophysiology using antibody-coated beads. Biotechniques 17:876-881.
18. Lee YT and Wang Q (1999) Inhibition of hKv2.1, a major human neuronal voltage-gated K+ channel by meclofenamic acid. Eur J Pharmacol 378:349-356.
19. Lerche C, Scherer CR, Seebohm G, Derst C, Wei AD, Busch AE, and Steinmeyer K (2000) Molecular cloning and functional expression of KCNQ5, a potassium channel subunit that may contribute to neuronal M-current diversity. J Biol Chem 275:22395-22400.
20. Macdonald RL and Kelly KM (1995) Antiepileptic drug mechanisms of action, epilepsia 36 (Suppl 2):S2-S12.
21. Main MJ, Cryan JE, Dupere JRB, Cox B, Clare JJ, and Burbidge SA (2000) Modulation of KCNQ2/3 potassium channels by the novel anticonvulsant retigabine. Mol Pharmacol 58:253-262.
22. Marrion NV (1997) Control of M-current. Annu Rev Physiol 59:483-504.
23. Otto JF, Kimball MM, and Wilcox KS (2002) Effects of the anticonvulsant retigabine on cultured cortical neurons: changes in electroresponsive properties and synaptic transmission. Mol Pharmacol 61:921-927.
24. Ottolia M and Toro L (1994) Potentiation of large conductance KCa channels by niflumic, flufenamic and mefenamic acids. Biophys J 67:2272-2279.
25. Passmore GM, Selyanko AA, Mistry M, Al-Qatari M, Marsh SJ, Matthews EA, Dickenson AH, Brown TA, Burbidge SA, Main M, et al. (2003) KCNQ/M currents in sensory neurons: significance for pain therapy. J Neurosci 23:7227-7236.
26. Peretz A, Schottelndreier H, Ben Aharon-Shamgar L, and Attali B (2002) Modulation of homomeric and heteromeric KCNQ1 channels by external acidification. J Physiol (Lond) 545:751-766.
27. Rivera-Arconada I, Martinez-Gomez J, and Lopez-Garcia JA (2004) M-current modulators alter rat spinal nociceptive transmission: an electrophysiological study in vitro. Neuropharmacology 46:598-606.
28. Rogawski MA (2000) KCNQ2/KCNQ3 K+ channels and the molecular pathogenesis of epilepsy: implications for therapy. Trends Neurosci 23:393-398.
29. Schroder RL, Jespersen T, Christophersen P, Strobaek D, Jensen BS, and Olesen SP (2001) KCNQ4 channel activation by BMS-204352 and retigabine. Neuropharmacology 40:888-898.
30. Schroeder BC, Hechenberger M, Weinreich F, Kubisch C, and Jentsch TJ (2000) KCNQ5, a novel potassium channel broadly expressed in brain, mediates M-type currents. J Biol Chem 275:24089-24095.
31. Shah MM, Mistry M, Marsh SJ, Brown DA, and Delmas P (2002) Molecular correlates of the M-current in cultured rat hippocampal neurons. J Physiol (Lond) 544:29-37.
32. Singh NA, Charlier C, Stauffer D, DuPont BR, Leach RJ, Melis R, Ronen GM, Bjerre I, Quattlebaum T, Murphy JV, et al. (1998) A novel potassium channel gene, KCNQ2, is mutated in an inherited epilepsy of newborns. Nat Genet 8:25-29.
33. Tatulian L and Brown DA (2003) Effect of the KCNQ potassium channel opener retigabine on single KCNQ2/3 channels expressed in CHO cells. J Physiol (Lond) 549:57-63.
34. Tatulian L, Delmas P, Abogadie FC, and Brown DA (2001) Activation of expressed KCNQ potassium currents and native neuronal M-type potassium currents by the anti-convulsant drug retigabine. J Neurosci 21:5535-5545.
35. Voilley N, de Weille J, Mamet J, and Lazdunski M (2001) Nonsteroid antiinflammatory drugs inhibit both the activity and the inflammation-induced expression of acid-sensing ion channels in nociceptors. J Neurosci 21:8026-8033.
36. Wang H-S, Pan Z, Shi W, Brown BS, Wymore RS, Cohen IS, Dixon JE, and McKinnon D (1998) KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science (Wash DC) 282:1890-1893.
37. Wen H and Levitan IB (2002) Calmodulin is an auxiliary subunit of KCNQ2/3 potassium channels. J Neurosci 22:7991-8001.
38. Wickenden AD, Yu W, Zou A, Jegla T, and Wagoner PK (2000) Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels. Mol Pharmacol 58:591-600.
39. Wickenden AD, Zou A, Wagoner PK, and Jegla T (2001) Characterization of KCNQ5/Q3 potassium channels expressed in mammalian cells. Br J Pharmacol 132:381-384.
40. A receptors expressed in Xenopus oocytes. J Pharmacol Exp Ther 268:806-817.
41. Wu YJ, Boissard CG, Greco C, Gribkoff VK, Harden DG, He H, L'Heureux A, Kang SH, Kinney GG, Knox RJ, et al. (2003) (S)-N-[1-(3-Morpholin-4-ylphenyl) ethyl]-3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine. J Med Chem 46:3197-3200.
42. Wu YJ, He H, Sun LQ, L'Heureux A, Chen J, Dextraze P, Starrett JE Jr, Boissard CG, Gribkoff VK, Natale J, et al. (2004) Synthesis and structure-activity relationship of acrylamides as KCNQ2 potassium channel openers. J Med Chem 47:2887-2896.
43. Yus-Najera E, Santana-Castro I, and Villaroel A (2002) The identification and characterization of a noncontinuous calmodulin-binding site in noninactivating voltage-dependent KCNQ potassium channels. J Biol Chem 277:28545-28553.