Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2550344 | Journal of Pharmacological and Toxicological Methods | 2008 | 12 Pages |
Abstract
The assay described combines a functional assessment of hNav1.5 with medium-throughput. Furthermore the assay was able to reveal information on the use-dependency of compound block, as well as predicting Na+ channel effects in more integrated systems such as the cardiac Purkinje fibre action potential. This makes it possible to determine quantitative potency data, and mechanistic information about use-dependence, in a timeframe short enough to influence medicinal chemistry.
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Authors
A.R. Harmer, N. Abi-Gerges, A. Easter, A. Woods, C.L. Lawrence, B.G. Small, J.-P. Valentin, C.E. Pollard,