ArticleActa pharmacologica Sinica2016
Novel KCNQ2 channel activators discovered using fluorescence-based and automated patch-clamp-based high-throughput screening techniques.
Article in Acta pharmacologica Sinica, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 15 citations in OpenAlex.
- Targeting Kv7 Potassium Channels for Epilepsy.CNS drugs · 2025Review
- Novel KCNQ2 missense variant expands the genotype spectrum of DEE7.Neurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology · 2024Article
- Establishment of a CaCC-based Cell Model and Method for High-throughput Screening of M3 Receptor Drugs.Cell biochemistry and biophysics · 2023Article
- Chemical modulation of Kv7 potassium channels.RSC medicinal chemistry · 2021Review
- Rhodol-based thallium sensors for cellular imaging of potassium channel activity.Organic & biomolecular chemistry · 2018Article
- Ion channels research in the post-genomic era.Acta pharmacologica Sinica · 2016Article
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimTo establish an improved, high-throughput screening techniques for identifying novel KCNQ2 channel activators.
methodsKCNQ2 channels were stably expressed in CHO cells (KCNQ2 cells). Thallium flux assay was used for primary screening, and 384-well automated patch-clamp IonWorks Barracuda was used for hit validation. Two validated activators were characterized using a conventional patch-clamp recording technique.
resultsFrom a collection of 80 000 compounds, the primary screening revealed a total of 565 compounds that potentiated the fluorescence signals in thallium flux assay by more than 150%. When the 565 hits were examined in IonWorks Barracuda, 38 compounds significantly enhanced the outward currents recorded in KCNQ2 cells, and were confirmed as KCNQ2 activators. In the conventional patch-clamp recordings, two validated activators ZG1732 and ZG2083 enhanced KCNQ2 currents with EC50 values of 1.04±0.18 μmol/L and 1.37±0.06 μmol/L, respectively.
conclusionThe combination of thallium flux assay and IonWorks Barracuda assay is an efficient high-throughput screening (HTS) route for discovering KCNQ2 activators.
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