Niflumic acid alters gating of HCN2 pacemaker channels by interaction with the outer region of S4 voltage sensing domains

Molecular Pharmacology

Volumn 75, Issue 5, 2009, Pages 1210-1221

  Cheng, Lan ^a   Sanguinetti, Michael C ^a  

^a UNIVERSITY OF UTAH SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLIC NUCLEOTIDE GATED CHANNEL; NIFLUMIC ACID;

ANIMAL CELL; ARTICLE; CHANNEL GATING; CONCENTRATION RESPONSE; CONDUCTANCE; CONTROLLED STUDY; DRUG MECHANISM; DRUG PROTEIN BINDING; EXTRACELLULAR SPACE; HYPERPOLARIZATION; ION CURRENT; MEMBRANE CURRENT; NONHUMAN; OOCYTE; PACEMAKER ELECTRODE; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN EXPRESSION; SITE DIRECTED MUTAGENESIS; VOLTAGE CLAMP; XENOPUS LAEVIS;

ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; DOSE-RESPONSE RELATIONSHIP, DRUG; ION CHANNEL GATING; ION CHANNELS; MICE; NIFLUMIC ACID; PROTEIN STRUCTURE, TERTIARY; XENOPUS LAEVIS;

EID: 66049153849     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.108.054437     Document Type: Article

References (30)

1. f) of rabbit SA node myocytes by niflumic acid. Pflugers Arch 431:757-762.
2. Bell DC, Yao H, Saenger RC, Riley JH, and Siegelbaum SA (2004) Changes in local S4 environment provide a voltage-sensing mechanism for mammalian hyperpolarization-activated HCN channels. J Gen Physiol 123:5-19. (Pubitemid 38082783)
3. Bucchi A, Baruscotti M, and DiFrancesco D (2002) Current-dependent block of rabbit sino-atrial node If channels by ivabradine. J Gen Physiol 120:1-13. (Pubitemid 34755772)
4. Busch AE, Herzer T, Wagner CA, Schmidt F, Raber G, Waldegger S, and Lang F (1994) Positive regulation by chloride channel blockers of IsK channels expressed in Xenopus oocytes. Mol Pharmacol 46:750-753. (Pubitemid 24984457)
5. Chen J, Mitcheson JS, Tristani-Firouzi M, Lin M, and Sanguinetti MC (2001) The S4-S5 linker couples voltage sensing and activation of pacemaker channels. Proc Natl Acad Sci U S A 98:11277-11282. (Pubitemid 32928719)
6. Chen J, Mitcheson JS, Lin M, and Sanguinetti MC (2000) Functional roles of charged residues in the putative voltage sensor of the HCN2 pacemaker channel. J Biol Chem 275:36465-36471.
7. Eskandari S, Zampighi GA, Leung DW, Wright EM, and Loo DD (2002) Inhibition of gap junction hemichannels by chloride channel blockers. J Membr Biol 185:93-102. (Pubitemid 34095240)
8. Goldin AL (1991) Expression of ion channels by injection of mRNA into Xenopus oocytes. Methods Cell Biol 36:487-509.
9. Jabeen T, Singh N, Singh RK, Sharma S, Somvanshi RK, Dey S, and Singh TP (2005) Non-steroidal anti-inflammatory drugs as potent inhibitors of phospholipase A2: structure of the complex of phospholipase A2 with niflumic acid at 2.5 Angstroms resolution. Acta Crystallogr D Biol Crystallogr 61:1579-1586. (Pubitemid 43943115)
10. + channel, by meclofenamic acid. Eur J Pharmacol 378:349-356.
11. Liantonio A, Picollo A, Babini E, Carbonara G, Fracchiolla G, Loiodice F, Tortorella V, Pusch M, and Camerino DC (2006) Activation and inhibition of kidney CLC-K chloride channels by fenamates. Mol Pharmacol 69:165-173. (Pubitemid 43048903)
12. - channel block/activation: optimal pharmacophoric requirements towards high-affinity ligands. Proc Natl Acad Sci U S A 105:1369-1373.
13. Malykhina AP, Shoeb F, and Akbarali HI (2002) Fenamate-induced enhancement of heterologously expressed HERG currents in Xenopus oocytes. Eur J Pharmacol 452:269-277. (Pubitemid 35279429)
14. Männikkö R, Elinder F, and Larsson HP (2002) Voltage-sensing mechanism is conserved among ion channels gated by opposite voltages. Nature 419:837-841. (Pubitemid 35238569)
15. Monnet X, Ghaleh B, Colin P, de Curzon OP, Giudicelli JF, and Berdeaux A (2001) Effects of heart rate reduction with ivabradine on exercise-induced myocardial ischemia and stunning. J Pharmacol Exp Ther 299:1133-1139. (Pubitemid 33104986)
16. Ca channels by niflumic, flufenamic, and mefenamic acids. Biophys J 67:2272-2279.
17. Peretz A, Degani N, Nachman R, Uziyel Y, Gibor G, Shabat D, and Attali B (2005) Meclofenamic acid and diclofenac, novel templates of KCNQ2/Q3 potassium channel openers, depress cortical neuron activity, and exhibit anticonvulsant properties. Mol Pharmacol 67:1053-1066. (Pubitemid 40410406)
18. Picollo A, Liantonio A, Babini E, Camerino DC, and Pusch M (2007) Mechanism of interaction of niflumic acid with heterologously expressed kidney CLC-K chloride channels. J Membr Biol 216:73-82. (Pubitemid 47479551)
19. h) in rod photoreceptor cells. Neurosci Res 40:375-381.
20. - channel by niflumic acid. Mol Membr Biol 21:27-38.
21. Sesti F, Rajan S, Gonzalez-Colaso R, Nikolaeva N, and Goldstein SA (2003) Hyperpolarization moves S4 sensors inward to open MVP, a methanococcal voltage-gated potassium channel. Nat Neurosci 6:353-361. (Pubitemid 36373980)
22. Shin KS, Rothberg BS, and Yellen G (2001) Blocker state dependence and trapping in hyperpolarization-activated cation channels: evidence for an intracellular activation gate. J Gen Physiol 117:91-101. (Pubitemid 32423749)
23. Sinkkonen ST, Mansikkamäki S, Möykkynen T, Lüddens H, Uusi-Oukari M, and Korpi ER (2003) Receptor subtype-dependent positive and negative modulation of GABA(A) receptor function by niflumic acid, a nonsteroidal anti-inflammatory drug. Mol Pharmacol 64:753-763. (Pubitemid 37048580)
24. Stühmer W (1992) Electrophysiological recording from Xenopus oocytes. Methods Enzymol 207:319-339.
25. Vaca L, Stieber J, Zong X, Ludwig A, Hofmann F, and Biel M (2000) Mutations in the S4 domain of a pacemaker channel alter its voltage dependence. FEBS Lett 479:35-40. (Pubitemid 30625254)
26. Vemana S, Pandey S, and Larsson HP (2004) S4 movement in a mammalian HCN channel. J Gen Physiol 123:21-32. (Pubitemid 38082784)
27. f current inhibitor ivabradine A new therapeutic approach to ischemic heart disease. Pharmacol Res 53:424-434.
28. Vilaine JP, Bidouard JP, Lesage L, Reure H, and Péglion JL (2003) Anti-ischemic effects of ivabradine, a selective heart rate-reducing agent, in exercise-induced myocardial ischemia in pigs. J Cardiovasc Pharmacol 42:688-696. (Pubitemid 37305989)
29. to2 current. Circ Res 81:711-718.
30. - channels in Xenopus oocytes. Mol Pharmacol 37: 720-724.