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Updated: Jun 12, 2026

Cell-based Calcium Assay for Medium to High Throughput Screening of TRP Channel Functions using FlexStation 3
Published on: August 17, 2011
The alpha2-delta protein: an auxiliary subunit of voltage-dependent calcium channels as a recognized drug target
Andrew J Thorpe1, James Offord
1Pfizer Inc, US Medical Affairs, New York, NY 10017, USA. andrew.thorpe@pfizer.com
Abstract:
Currently, there are two drugs on the market, gabapentin (Neurontin) and pregabalin (Lyrica), that are proposed to exert their therapeutic effect through binding to the alpha2-delta subunit of voltage-sensitive calcium channels. This activity was unexpected, as the alpha2-delta subunit had previously been considered not to be a pharmacological target. In this review, the role of the alpha2-delta subunits is discussed and the mechanism of action of the alpha2-delta ligands in vitro and in vivo is summarized. Finally, new insights into the mechanism of drugs that bind to this protein are discussed.
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