Optimization of Cav1.2 screening with an automated planar patch clamp platform

Journal of Pharmacological and Toxicological Methods

Volumn 59, Issue 2, 2009, Pages 62-72

  Balasubramanian, Bharathi ^a   Imredy, John P ^a   Kim, David ^a   Penniman, Jacob ^a   Lagrutta, Armando ^a   Salata, Joseph J ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

BayK 8644; Cav1.2 channel; Calcium agonist; Calcium antagonist; L type Ca channel; Methods; Nifedipine; PatchXpress; Pharmacology; Voltage clamp

Indexed keywords

1,4 DIHYDRO 2,6 DIMETHYL 5 NITRO 4 [2 (TRIFLUOROMETHYL)PHENYL] 3 PYRIDINECARBOXYLIC ACID METHYL ESTER; BARIUM; BEPRIDIL; CALCIUM CHANNEL L TYPE; CALCIUM ION; DILTIAZEM; GALLOPAMIL; ISRADIPINE; MAGNESIUM ION; NIFEDIPINE; NIMODIPINE; TRYPSIN; VERAPAMIL;

ANIMAL CELL; ARTICLE; CELL ISOLATION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFECT; DRUG SCREENING; EXPERIMENTAL GUINEA PIG; HEART MUSCLE CELL; HUMAN; HUMAN CELL; MALE; NONHUMAN; PATCH CLAMP;

3-PYRIDINECARBOXYLIC ACID, 1,4-DIHYDRO-2,6-DIMETHYL-5-NITRO-4-(2-(TRIFLUOROMETHYL)PHENYL)-, METHYL ESTER; ANIMALS; BARIUM; CALCIUM CHANNEL AGONISTS; CALCIUM CHANNEL BLOCKERS; CALCIUM CHANNELS, L-TYPE; CELL LINE; COLLAGENASES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; ELECTROPHYSIOLOGY; GUINEA PIGS; HEART VENTRICLES; HUMANS; INHIBITORY CONCENTRATION 50; KIDNEY; MALE; MYOCYTES, CARDIAC; NIFEDIPINE; PATCH-CLAMP TECHNIQUES; PEPTIDE HYDROLASES; TEMPERATURE; TIME FACTORS; TRANSFECTION; TRYPSIN;

EID: 63749092193     PISSN: 10568719     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.vascn.2009.02.002     Document Type: Article

References (39)

1. 2+ channel inactivation in controlling heart excitation. Proceedings of the National Academy of Sciences 99 (2002) 17185-17190
2. Bean B.P. Nitrendipine block of cardiac calcium channels: High-affinity binding to the inactivated state. Proceedings of the National Academy of Sciences 81 (1984) 6388-6392
3. 2+ channels. Annual Review of Cell and Developmental Biology 16 (2000) 521-555
4. v1.2. Molecular Pharmacology 64 (2003) 491-501
5. v1.2. Molecular Pharmacology 66 (2004) 1236-1247
6. Dubin A.E., Nasser N., Rohrbacher J., Hermans A.N., Marrannes R., Grantham C., Van Rossem K., Cik M., Chaplan S.R., Gallacher D., Xu J., Guia A., Byrne N.G., and Mathes C. Identifying modulators of hERG channel activity using the PatchXpress((R)) planar patch clamp. Journal of Biomolecular Screening 10 (2005) 168-181
7. Ellis, S.B., Williams, M.E., Harpold, M.M., Schwartz, A., and Brenner, R. (1997) Cells expressing calcium channel alpha 2 subunit-encoding DNA. SIBIA Neurosciences, Inc., La Jolla, CA. United States Patent No. 5618720.
8. Fermini B., Jurkiewicz N.K., Jow B., Guinosso Jr. P.J., Baskin E.P., Lynch Jr. J.J., and Salata J.J. Use-dependent effects of the class III antiarrhythmic agent NE-10064 (azimilide) on cardiac repolarization: Block of delayed rectifier potassium and L-type calcium currents. Journal of Cardiovascular Pharmacology 26 (1995) 259-271
9. 2+ channels requires membrane targeting of PKA and phosphorylation of channel subunits. Neuron 19 (1997) 185-196
10. Godfraind T. Calcium antagonists and vasodilation. Pharmacology & Therapeutics 64 (1994) 37-75
11. Guo L., and Guthrie H. Automated electrophysiology in the preclinical evaluation of drugs for potential QT prolongation. Journal of Pharmacological and Toxicological Methods 52 (2005) 123-135
12. Hamilton S.L., Yatani A., Brush K., Schwartz A., and Brown A.M. A comparison between the binding and electrophysiological effects of dihydropyridines on cardiac membranes. Molecular Pharmacology 31 (1987) 221-231
13. Harpold, M.M., Ellis, S.B., Williams, M.E., Feldman, D.H., McCue, A.F., and Brenner, R. (1998) Human calcium channel alpha-1C/alpha-1D, alpha-2, beta-1, and gamma subunits and cells expressing the DNA. SIBIA Neurosciences, Inc., La Jolla, CA. United States Patent No. 5851824.
14. Harpold, M.M., Ellis, S.B., Williams, M.E., Feldman, D.H., McCue, A.F., and Brenner, R. (1999) DNA encoding human calcium channel alpha-1A, beta 1, beta-2, and beta-4 subunits, and assays using cells that express the subunits SIBIA Neurosciences, Inc., La Jolla, CA. United States Patent No. 5874236.
15. Herzig S., and Neumann J. Effects of serine/threonine protein phosphatases on ion channels in excitable membranes. Physiological Reviews 80 (2000) 173-210
16. Hosey M.M., Chien A.J., and Puri T.S. Structure and regulation of L-type calcium channels - A current assessment of the properties and roles of channel subunits. Trends in Cardiovascular Medicine 6 (1996) 265-273
17. Katz A.M. Calcium channel diversity in the cardiovascular system. Journal of the American College of Cardiology 28 (1996) 522-529
18. Katz A.M. Molecular biology of calcium channels in the cardiovascular system. The American Journal of Cardiology 80 (1997) 17I-22I
19. v1.2a,b) by protein kinases. American Journal of Physiology. Cell Physiology 281 (2001) C1743-C1756
20. Kiss L., Bennett P.B., Uebele V.N., Koblan K.S., Kane S.A., Neagle B., and Schroeder K. High throughput ion-channel pharmacology: Planar-array-based voltage clamp. Assay and Drug Development Technologies 1 (2003) 127-135
21. 2+ channel antagonist, DTZ323, on guinea-pig ventricular myocytes. European Journal of Pharmacology 325 (1997) 229-236
22. Lee K.S., and Tsien R.W. Mechanism of calcium channel blockade by verapamil, D600, diltiazem and nitrendipine in single dialysed heart cells. Nature 302 (1983) 790-794
23. 2+ channel α1 subunit as expressed in mouse L cells. FEBS Letters 315 (1993) 167-172
24. Nishimura S., Takeshima H., Hofmann F., Flockerzi V., and Imoto K. Requirement of the calcium channel β subunit for functional conformation. FEBS Letters 324 (1993) 283-286
25. Patton C., Thompson S., and Epel D. Some precautions in using chelators to buffer metals in biological solutions. Cell Calcium 35 (2004) 427-431
26. Perez-Garcia M.T., Kamp T.J., and Marban E. Functional properties of cardiac L-type calcium channels transiently expressed in HEK293 cells. Roles of α1 and β subunits. Journal of General Physiology 105 (1995) 289-305
27. Perez-Reyes E., Yuan W., Wei X., and Bers D.M. Regulation of the cloned L-type cardiac calcium channel by cyclic-AMP-dependent protein kinase. FEBS Letters 342 (1994) 119-123
28. Perier F., Radeke C.M., and Vandenberg C.A. Primary structure and characterization of a small-conductance inwardly rectifying potassium channel from human hippocampus. Proceedings of the National Academy of Sciences 91 (1994) 6240-6244
29. Kr. American Journal of Physiology. Heart and Circulatory Physiology 290 (2006) H1278-H1288
30. Sanguinetti M.C., Krafte D.S., and Kass R.S. Voltage-dependent modulation of Ca channel current in heart cells by Bay K8644. Journal of General Physiology 88 (1986) 369-392
31. Shen J.B., Jiang B., and Pappano A.J. Comparison of L-type calcium channel blockade by nifedipine and/or cadmium in guinea pig ventricular myocytes. Journal of Pharmacology and Experimental Therapeutics 294 (2000) 562-570
32. 2+ channel transcripts in human fibroblasts. Proceedings of the National Academy of Sciences 89 (1992) 4628-4632
33. Stauderman K.A., Mahaffy L.S., Akong M., Velicelebi G., Chavez-Noriega L.E., Crona J.H., Johnson E.C., Elliott K.J., Gillespie A., Reid R.T., Adams P., Harpold M.M., and Corey-Naeve J. Characterization of human recombinant neuronal nicotinic acetylcholine receptor subunit combinations α2β4, α3β4 and α4β4 stably expressed in HEK293 cells. Journal of Pharmacology and Experimental Therapeutics 284 (1998) 777-789
34. Ks) activity. Assay and Drug Development Technologies 5 (2007) 617-628
35. Uehara A., and Hume J.R. Interactions of organic calcium channel antagonists with calcium channels in single frog atrial cells. Journal of General Physiology 85 (1985) 621-647
36. 2+ concentration. American Journal of Physiology. Cell Physiology 291 (2006) C83-C92
37. Xia M., Imredy J.P., Koblan K.S., Bennett P., and Connolly T.M. State-dependent inhibition of L-type calcium channels: Cell-based assay in high-throughput format. Analytical Biochemistry 327 (2004) 74-81
38. Yatani A., Brown A.M., and Schwartz A. Bepridil block of cardiac calcium and sodium channels. Journal of Pharmacology and Experimental Therapeutics 237 (1986) 9-17
39. Zheng W., Spencer R.H., and Kiss L. High throughput assay technologies for ion channel drug discovery. Assay and Drug Development Technologies 2 (2004) 543-552