A novel toxicity-based assay for the identification of modulators of voltage-gated Na+ channels

Journal of Neuroscience Methods

Volumn 137, Issue 1, 2004, Pages 79-85

  Weiser, Thomas ^a  

^a BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG   (Germany)

Author keywords

BIII 890; BIIR 561; Cytotoxicity; Na+ channel blocker; Na+ K+ATPase; Ouabain; Veratridine; Voltage gated Na+ channel

Indexed keywords

ADENOSINE TRIPHOSPHATASE (POTASSIUM SODIUM) INHIBITOR; AMBROXOL; BENZOMORPHAN DERIVATIVE; BIII 980; CROBENETINE; DIMETHYL[2 [2 (3 PHENYL 1,2,4 OXADIAZOL 5 YL)PHENOXY]ETHYL]AMINE; LAMOTRIGINE; MEXILETINE; NEUROPROTECTIVE AGENT; OUABAIN; PROPIDIUM IODIDE; PROTEIN SUBUNIT; RILUZOLE; SODIUM CHANNEL BLOCKING AGENT; SODIUM ION; TETRODOTOXIN; UNCLASSIFIED DRUG; VERATRIDINE; VOLTAGE GATED SODIUM CHANNEL;

ANIMAL CELL; ANIMAL MODEL; ARTICLE; BRAIN CELL; CELL DEATH; CELL SURVIVAL; CHO CELL; CONTROLLED STUDY; CORRELATION COEFFICIENT; DRUG ACTIVITY; DRUG EFFECT; DRUG POTENCY; DRUG SCREENING; EXPERIMENTAL MODEL; FLUORESCENCE; GENETIC RECOMBINATION; IC 50; INCUBATION TIME; INTRACELLULAR TRANSPORT; NEUROMODULATION; NEUROPROTECTION; NEUROTOXICITY; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; TOXICITY TESTING; VOLTAGE CLAMP;

ANIMALS; BIOLOGICAL ASSAY; CELL SURVIVAL; CHO CELLS; CRICETINAE; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; DRUG INTERACTIONS; MEMBRANE POTENTIALS; NA(+)-K(+)-EXCHANGING ATPASE; NERVE TISSUE PROTEINS; OUABAIN; PATCH-CLAMP TECHNIQUES; RATS; SODIUM CHANNEL BLOCKERS; SODIUM CHANNELS; TETRODOTOXIN; TOXICITY TESTS; TRIAZINES; VERATRIDINE;

EID: 2942633345     PISSN: 01650270     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.jneumeth.2004.02.004     Document Type: Article

References (33)

1. Almers W., Levinson S.R. Tetrodotoxin binding to normal depolarized frog muscle and the conductance of a single sodium channel. J. Physiol. 247:1975;483-509
2. Asmild M., Oswald N., Krzywkowski K.M., Friis S., Jacobsen R.B., Reuter D., Taboryski R., Kutchinsky J., Vestergaard R.K., Schroder R.L., Sorensen C.B., Bech M., Korsgaard M.P., Willumsen N.J. Upscaling and automation of electrophysiology: toward high throughput screening in ion channel drug discovery. Receptors Channels. 9:2003;49-58
3. Barnes S., Hille B. Veratridine modifies open sodium channels. J. Gen. Physiol. 91:1988;421-443
4. Blanco G., Mercer R.W. Isozymes of the Na-K-ATPase: heterogeneity in structure, diversity in function. Am. J. Physiol. 275:1998;F633-F650
5. Carter A.J., Grauert M., Pschorn U., Bechtel W.D., Bartmann-Lindholm C., Qu Y., Scheuer T., Catterall W.A., Weiser T. Potent blockade of sodium channels and protection of brain tissue from ischemia by BIII 890 CL. Proc. Natl. Acad. Sci. U. S. A. 97:2000;4944-4949
6. + channel alpha subunit expressed heterologously in CHO cells. Pflugers Arch. 438:1999;378-383
7. Gonzalez J.E., Maher M.P. Cellular fluorescent indicators and voltage/ion probe reader (VIPR) tools for ion channel and receptor drug discovery. Receptors Channels. 8:2002;283-295
8. Grauert M., Bechtel W.D., Weiser T., Stransky W., Nar H., Carter A.J. Synthesis and structure-activity relationships of 6, 7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke. J. Med. Chem. 45:2002;3755-3764
9. Krieger C., Puil E., Kim S.U. Development of resting membrane potentials of embryonic murine spinal cord cells evaluated by flow cytometric analysis. Dev. Neurosci. 13:1991;11-19
10. Lawrence J.C., Catterall W.A. Tetrodotoxin-insensitive sodium channels. Binding of polypeptide neurotoxins in primary cultures of rat muscle cells. J. Biol. Chem. 256:1981;6223-6229
11. Lichtshtein D., Dunlop K., Kaback H.R., Blume A.J. Mechanism of monensin-induced hyperpolarization of neuroblastoma-glioma hybrid NG108-15. Proc. Natl. Acad. Sci. U. S. A. 76:1979;2580-2584
12. Matthews J.C., Warnick J.E., Albuquerque E.X., Eldefrawi M.E. Characterization of the electrogenic sodium channel from rat brain membranes using neurotoxin-dependent 22Na uptake. Membr. Biochem. 4:1981;71-104
13. Oku N., Nojima S., Inoue K. Selective release of non-electrolytes from liposomes upon perturbation of bilayers by temperature change or polyene antibiotics. Biochim. Biophys. Acta. 595:1980;277-290
14. Palmer A.M., Carter N. The role of sodium channels in disease. Drug News Perspect. 14:2001;568-576
15. Postma S.W., Catterall W.A. Inhibition of binding of [3H]batrachotoxinin A 20-alpha-benzoate to sodium channels by local anesthetics. Mol. Pharmacol. 25:1984;219-227
16. + channels in spinal cord astrocytes. J. Neurophysiol. 78:1997;3249-3258
17. Schwartz G., Fehlings M.G. Evaluation of the neuroprotective effects of sodium channel blockers after spinal cord injury: improved behavioral and neuroanatomical recovery with riluzole. J. Neurosurg. 94:2001;245-256
18. Sigel E. Effects of veratridine on single neuronal sodium channels expressed in Xenopus oocytes. Pflugers Arch. 410:1987;112-120
19. Stett A., Burkhardt C., Weber U., van Stiphout P., Knott T. CYTOCENTERING: a novel technique enabling automated cell-by-cell patch clamping with the CYTOPATCH chip. Receptors Channels. 9:2003;59-66
20. Stratton S.C., Large C.H., Cox B., Davies G., Hagan R.M. Effects of lamotrigine and levetiracetam on seizure development in a rat amygdala kindling model. Epilepsy Res. 53:2003;95-106
21. Takahashi S., Shibata M., Gotoh J., Fukuuchi Y. Astroglial cell death induced by excessive influx of sodium ions. Eur. J. Pharmacol. 408:2000;127-135
22. Tas P.W., Kress H.G., Koschel K. Halothane inhibits the neurotoxin stimulated [14C]guanidinium influx through 'silent' sodium channels in rat glioma C6 cells. FEBS Lett. 182:1985;269-272
23. Tornquist K., Ekokoski E. Intracellular free sodium concentrations in GH4C1 cells. J. Cell Physiol. 154:1993;608-614
24. Urenjak J., Obrenovitch T.P. Neuroprotection-rationale for pharmacological modulation of Na(+)-channels. Amino Acids. 14:1998;151-158
25. Wagner M.L., Landis B.E. Riluzole: a new agent for amyotrophic lateral sclerosis. Ann. Pharmacother. 31:1997;738-744
26. Weigele J.B., Barchi R.L. Functional reconstitution of the purified sodium channel protein from rat sarcolemma. Proc. Natl. Acad. Sci. U. S. A. 79:1982;3651-3655
27. Weiser T. AMPA receptor antagonists with additional mechanisms of action: new opportunities for neuroprotective drugs? Curr. Pharm. Des. 8:2002;941-951
28. Weiser T., Wilson N. Inhibition of tetrodotoxin (TTX)-resistant and TTX-sensitive neuronal Na(+) channels by the secretolytic ambroxol. Mol. Pharmacol. 62:2002;433-438
29. Weiser T., Qu Y., Catterall W.A., Scheuer T. Differential interaction of R-mexiletine with the local anesthetic receptor site on brain and heart sodium channel alpha-subunits. Mol. Pharmacol. 56:1999a;1238-1244
30. Weiser T., Brenner M., Palluk R., Bechtel W.D., Ceci A., Brambilla A., Ensinger H.A., Sagrada A., Wienrich M. BIIR 561 CL: a novel combined antagonist of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors and voltage-dependent sodium channels with anticonvulsive and neuroprotective properties. J. Pharmacol. Exp. Ther. 289:1999b;1343-1349
31. + channel alpha subunits in a somatic cell line. Neuron. 8:1992;59-70
32. Wilder R.T., Berde C.B., Griggs C.T., Chickalingaiah R., Strichartz G. Chronic exposure to lidocaine does not alter flux through sodium channels in cultured neuronal cells. Reg. Anesth. 18:1993;283-289
33. Xiao A.Y., Wei L., Xia S., Rothman S., Yu S.P. Ionic mechanism of ouabain-induced concurrent apoptosis and necrosis in individual cultured cortical neurons. J. Neurosci. 22:2002;1350-1362