Evaluation of the Rubidium Efflux Assay for Preclinical Identification of hERG Blockade

2006 ◽  
Vol 4 (1) ◽  
pp. 73-82 ◽  
Author(s):  
Khuram W. Chaudhary ◽  
Janet M. O'Neal ◽  
Zun-Li Mo ◽  
Bernard Fermini ◽  
Robert H. Gallavan ◽  
...  
Keyword(s):  
Rubidium Efflux

Characterization of a hERG Screen Using the IonWorks HT: Comparison to a hERG Rubidium Efflux Screen

2005 ◽  
Vol 3 (1) ◽  
pp. 47-57 ◽  
Author(s):  
Steve Sorota ◽  
Xue-Song Zhang ◽  
Michael Margulis ◽  
Kristal Tucker ◽  
Tony Priestley
Keyword(s):  
Rubidium Efflux

Measurements of mitochondrial K+ fluxes in whole rat hearts using 87Rb-NMR

1999 ◽  
Vol 276 (1) ◽  
pp. C193-C200 ◽  
Author(s):  
Marco L. H. Gruwel ◽  
Bozena Kuzio ◽  
Roxanne Deslauriers ◽  
Valerie V. Kupriyanov
Keyword(s):  
Rat Heart ◽  
Efflux Rate ◽  
Energy Depletion ◽  
Cellular Energy ◽  
Rat Hearts ◽  
Efflux Rate Constant ◽  
Rubidium Efflux ◽  
Rat Heart Mitochondria ◽  
Energy Deprivation ◽  
Mitochondrial Uncoupler

The rubidium efflux from hypothermic rat hearts perfused by the Langendorff method at 20°C was studied. At this temperature 87Rb-NMR efflux experiments showed the existence of two 87Rb pools: cytoplasmic and mitochondrial. Rat heart mitochondria showed a very slow exchange of mitochondrial Rb+ for cytoplasmic K+. After washout of cytosolic Rb+, mitochondria kept a stable Rb+level for >30 min. Rb+ efflux from mitochondria was stimulated with 0.1 mM 2,4-dinitrophenol (DNP), by sarcolemmal permeabilization and concomitant cellular energy depletion by saponin (0.01 mg/ml for 4 min) in the presence of a perfusate mimicking intracellular conditions, or by ATP-sensitive K (KATP) channel openers. DNP, a mitochondrial uncoupler, caused the onset of mitochondrial Rb+ exchange; however, the washout was not complete (80 vs. 56% in control). Energy deprivation by saponin, which permeabilizes the sarcolemma, resulted in a rapid and complete Rb+ efflux. The mitochondrial Rb+ efflux rate constant ( k) decreased in the presence of glibenclamide, a KATP channel inhibitor (5 μM; k = 0.204 ± 0.065 min−1; n = 8), or in the presence of ATP plus phosphocreatine (1.0 and 5.0 mM, respectively; k = 0.134 ± 0.021 min−1; n = 4) in the saponin experiments (saponin only; k = 0.321 ± 0.079 min−1; n = 3), indicating the inhibition of mitochondrial KATP channels. Thus hypothermia in combination with 87Rb-NMR allowed the probing of the mitochondrial K+ pool in whole hearts without mitochondrial isolation.

scholarly journals Scorpion venom inhibits carbamylcholine-induced 86 rubidium efflux from rat parotid acini

FEBS Letters ◽  
1987 ◽  
Vol 219 (2) ◽  
pp. 451-454 ◽  
Author(s):  
Jean-Paul Dehaye ◽  
Jacques Winand ◽  
Jean Christophe
Keyword(s):  
Scorpion Venom ◽  
Rubidium Efflux ◽  
Rat Parotid

Distinct effects of acetylcholine and glucose on 45 calcium and 86 rubidium efflux from mouse pancreatic islets

FEBS Letters ◽  
1984 ◽  
Vol 176 (2) ◽  
pp. 457-461 ◽  
Author(s):  
M. Nenquin ◽  
P. Awouters ◽  
F. Mathot ◽  
J.C. Henquin
Keyword(s):  
Pancreatic Islets ◽  
Mouse Pancreatic Islets ◽  
Rubidium Efflux
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