Abstract
Ion channels play essential roles in nervous system signaling, electrolyte transport, and muscle contraction. As such, ion channels are important therapeutic targets, and the search for compounds that modulate ion channels is accelerating. In order to identify and optimize ion channel modulators, assays are needed that are reliable and provide sufficient throughput for all stages of the drug discovery process. Electrophysiological assays offer the most direct and accurate characterization of channel activity and, by controlling membrane potential, can provide information about drug interactions with different conformational states. However, these assays are technically challenging and notoriously low-throughput. The recent development of several automated electrophysiology platforms has greatly increased the throughput of whole cell electrophysiological recordings, allowing them to play a more central role in ion channel drug discovery. While challenges remain, this new technology will facilitate the pharmaceutical development of ion channel modulators.
Keywords: Automated electrophysiology, ion channel modulators, drug discovery, assay development, patch clamp
Current Pharmaceutical Design
Title: Automated Electrophysiology in Drug Discovery
Volume: 13 Issue: 23
Author(s): B.T. Priest, A.M. Swensen and O.B. McManus
Affiliation:
Keywords: Automated electrophysiology, ion channel modulators, drug discovery, assay development, patch clamp
Abstract: Ion channels play essential roles in nervous system signaling, electrolyte transport, and muscle contraction. As such, ion channels are important therapeutic targets, and the search for compounds that modulate ion channels is accelerating. In order to identify and optimize ion channel modulators, assays are needed that are reliable and provide sufficient throughput for all stages of the drug discovery process. Electrophysiological assays offer the most direct and accurate characterization of channel activity and, by controlling membrane potential, can provide information about drug interactions with different conformational states. However, these assays are technically challenging and notoriously low-throughput. The recent development of several automated electrophysiology platforms has greatly increased the throughput of whole cell electrophysiological recordings, allowing them to play a more central role in ion channel drug discovery. While challenges remain, this new technology will facilitate the pharmaceutical development of ion channel modulators.
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Cite this article as:
B.T. Priest , A.M. Swensen and O.B. McManus , Automated Electrophysiology in Drug Discovery, Current Pharmaceutical Design 2007; 13 (23) . https://dx.doi.org/10.2174/138161207781368701
DOI https://dx.doi.org/10.2174/138161207781368701 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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