This Article Full Text (PDF) References Alert me when this article is cited Alert me if a correction is posted Citation Map Services Email this article to a friend Similar articles in this journal Similar articles in ISI Web of Science Similar articles in PubMed Alert me to new issues of the journal Add to Saved Citations Download to citation manager Request Permissions Request Reprints Add to My Marked Citations Citing Articles Citing Articles via HighWire Citing Articles via ISI Web of Science (31) Citing Articles via Google Scholar Citing Articles via Scopus Google Scholar Articles by Tang, W. Articles by Garyantes, T. Search for Related Content PubMed PubMed Citation Articles by Tang, W. Articles by Garyantes, T. Social Bookmarking                   What's this?

Development and Evaluation of High Throughput Functional Assay Methods for hERG Potassium Channel

Department of Profiling and High Throughput Screening, Aventis Pharmaceuticals, Bridgewater, NJ

Jiesheng Kang

Department of Safety Pharmacology, Aventis Pharmaceuticals, Bridgewater, NJ

Xiaying Wu

Department of Profiling and High Throughput Screening, Aventis Pharmaceuticals, Bridgewater, NJ

David Rampe

Department of Safety Pharmacology, Aventis Pharmaceuticals, Bridgewater, NJ

Lin Wang

Department of Safety Pharmacology, Aventis Pharmaceuticals, Bridgewater, NJ

Hong Shen

Department of Analytical Chemistry, Aventis Pharmaceuticals, Bridgewater, NJ

Zhuyin Li

Department of Profiling and High Throughput Screening, Aventis Pharmaceuticals, Bridgewater, NJ

Damien Dunnington

Axiom Biotechnology, San Diego, CA

Tina Garyantes

Department of Profiling and High Throughput Screening, Aventis Pharmaceuticals, Bridgewater, NJ

Three functional hERG channel assay methods have been developed and evaluated. The methods were tested against five known hERG channel inhibitors: dofetilide, terfenadine (Seldane), sertindole (Serdolect), astemizole (Hismanal), and cisapride (Propulsid). The DiBAC₄(3)-based assays were found to be the most economical but had high false-hit rates as a result of the interaction of dye with the test compounds. The membrane potential dye assay had fewer color-quenching problems but was expensive and still gave false hits. The nonradioactive Rb+ efflux assay was the most sensitive of all the assays evaluated and had the lowest false-hit rate.

Journal of Biomolecular Screening, Vol. 6, No. 5, 325-331 (2001)
DOI: 10.1177/108705710100600506


CiteULike    Connotea    Del.icio.us    Digg    Reddit    Technorati    What's this?

This article has been cited by other articles:

				M. J. Perrin, P. W. Kuchel, T. J. Campbell, and J. I. Vandenberg Drug Binding to the Inactivated State Is Necessary but Not Sufficient for High-Affinity Binding to Human Ether-a-go-go-Related Gene Channels Mol. Pharmacol., November 1, 2008; 74(5): 1443 - 1452. [Abstract] [Full Text] [PDF]

				B. D. Guth Preclinical Cardiovascular Risk Assessment in Modern Drug Development Toxicol. Sci., May 1, 2007; 97(1): 4 - 20. [Full Text] [PDF]

				A. Dorn, F. Hermann, A. Ebneth, H. Bothmann, G. Trube, K. Christensen, and C. Apfel Evaluation of a High-Throughput Fluorescence Assay Method for hERG Potassium Channel Inhibition J Biomol Screen, June 1, 2005; 10(4): 339 - 347. [Abstract] [PDF]

				C. Wolff, B. Fuks, and P. Chatelain Comparative Study of Membrane Potential-Sensitive Fluorescent Probes and their Use in Ion Channel Screening Assays J Biomol Screen, October 1, 2003; 8(5): 533 - 543. [Abstract] [PDF]

				M. Falconer, F. Smith, S. Surah-Narwal, G. Congrave, Z. Liu, P. Hayter, G. Ciaramella, W. Keighley, P. Haddock, G. Waldron, et al. High-Throughput Screening for Ion Channel Modulators J Biomol Screen, October 1, 2002; 7(5): 460 - 465. [Abstract] [PDF]

				D. F. Baxter, M. Kirk, A. F. Garcia, A. Raimondi, M. H. Holmqvist, K. K. Flint, D. Bojanic, P. S. Distefano, R. Curtis, and Y. Xie A Novel Membrane Potential-Sensitive Fluorescent Dye Improves Cell-Based Assays for Ion Channels J Biomol Screen, February 1, 2002; 7(1): 79 - 85. [Abstract] [PDF]