Rb+ efflux through functional activation of cardiac KCNQ1/minK channels by the benzodiazepine R-L3 (L-364,373)

Assay and Drug Development Technologies

Volumn 4, Issue 4, 2006, Pages 443-450

  Jow, Flora ^a   Tseng, Eugene ^a   Maddox, Taneya ^a   Shen, Ru ^a   Kowal, Dianne ^a   Dunlop, John ^a   Mekonnen, Belew ^a   Wang, KeWei ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1,3 DIHYDRO 5 (2 FLUOROPHENYL) 3 (1H INDOL 3 YLMETHYL) 1 METHYL 2H 1,4 BENZODIAZEPIN 2 ONE; BENZODIAZEPINE DERIVATIVE; COMPLEMENTARY DNA; POTASSIUM CHANNEL; POTASSIUM CHANNEL BLOCKING AGENT; POTASSIUM CHANNEL KCNQ1; RUBIDIUM ION; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; ATOMIC ABSORPTION SPECTROMETRY; CHO CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DNA SEQUENCE; DRUG INDICATION; DRUG MECHANISM; DRUG SCREENING; ION TRANSPORT; LONG QT SYNDROME; MEMBRANE ELECTROPHYSIOLOGY; NONHUMAN; NUCLEOTIDE SEQUENCE; PROTEIN ANALYSIS; PROTEIN EXPRESSION; PROTEIN FUNCTION; TRANSPORT KINETICS;

ANIMALS; ANTHRACENES; BENZODIAZEPINES; CHO CELLS; CHROMANS; CRICETINAE; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; GENE EXPRESSION; ION CHANNELS; KCNQ1 POTASSIUM CHANNEL; LONG QT SYNDROME; MEMBRANE POTENTIALS; MYOCARDIUM; POTASSIUM CHANNEL BLOCKERS; POTASSIUM CHANNELS, VOLTAGE-GATED; POTASSIUM CHLORIDE; RATS; REPRODUCIBILITY OF RESULTS; RISK FACTORS; RUBIDIUM; SPECTROPHOTOMETRY, ATOMIC; TETRAETHYLAMMONIUM;

EID: 33751224747     PISSN: 1540658X     EISSN: None     Source Type: Journal    
DOI: 10.1089/adt.2006.4.443     Document Type: Article

References (16)

1. Sanguinetti MC, Curran ME, Zou A, Shen J, Spector PS, Atkinson DL, Keating MF: Coassembly of K(V)LQT1 and minK (IsK) proteins to form cardiac I(Ks) potassium channel. Nature 1996;384:80-83.
2. Barhanin J, Lesage F, Guillemare E, Fink M, Lazdunski M, Romey G: K(V)LQT1 and 1sK (minK) proteins associate to form the I(Ks) cardiac potassium current. Nature 1996;384:78-80.
3. van den Berg MH, Wilde AA, Robles de Medina EO, Meyer H, Geelen JL, Jongbloed RJ, Wellens HJ, Geraedts JP: The long QT syndrome: a novel missense mutation in the S6 region of the KVLQT1 gene. Hum Genet 1997;100: 356-361.
4. de Jager T, Corbett CH, Badenhorst JC, Brink PA, Corfield VA: Evidence of a long QT founder gene with varying phenotypic expression in South African families. J Med Genet 1996;33:567-573.
5. Abitbol I, Peretz A, Lerche C, Busch AE, Attali B: Stilbenes and fenamates rescue the loss of I(KS) channel function induced by an LQT5 mutation and other IsK mutants. EMBO J 1999; 18:4137-4148.
6. + currents. Mol Pharmacol 1998;54:220-230.
7. Xu Y, Salata JJ, Wang J, Wu Y, Yan GY, Liu T, Marinchak RA, Kowey PR: Increasing I(Ks) corrects abnormal repolarization in rabbit models of acquired LQT2 and ventricular hypertrophy. Am J Physiol Heart Circ Physiol 2002;283:H664-H670.
8. Terstappen GC: Functional analysis of native and recombinant ion channels using a high-capacity nonradioactive rubidium efflux assay. Anal Biochem 1999;272:149-155.
9. Scott CW, Wilkins DE, Trivedi S, Crankshaw DJ: A medium-throughput functional assay of KCNQ2 potassium channels using rubidium efflux and atomic absorption spectrometry. Anal Biochem 2003;319:251-257.
10. Wang K, McIlvain B, Tseng E, Kowal D, Jow F, Shen R, Zhang H, Shan QJ, He L, Chen D, Lu Q, Dunlop J: Validation of an atomic absorption rubidium ion efflux assay for KCNQ/M-channels using the ion Channel Reader 8000. Assay Drug Dev Technol 2004;2:525-534.
11. Zhang JH, Chung TD, Oldenburg KR: A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 1999;4: 67-73.
12. Wang HS, Brown BS, McKinnon D, Cohen IS: Molecular basis for differential sensitivity of KCNQ and I(Ks) channels to the cognitive enhancer XE991. Mol Pharmacol 2000;57:1218-1223.
13. Seebohm G, Pusch M, Chen J, Sanguinetti MC: Pharmacological activation of normal and arrhythmia-associated mutant KCNQ1 potassium channels. Circ Res 2003;93: 941-947.
14. Wang HS, Pan Z, Shi W, Brown BS, Wymore RS, Cohen IS, Dixon JE, McKinnon D: KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 1998;282:1890-1893.
15. Hadley JK, Noda M, Selyanko AA, Wood IC, Abogadie FC, Brown DA: Differential tetraethylammonium sensitivity of KCNQ1-4 potassium channels. Br J Pharmacol 2000;129:413-415.
16. Wang KW, Goldstein SA: Subunit composition of minK potassium channels. Neuron 1995;14:1303-1309.