scholarly journals Novel KCNQ2 channel activators discovered using fluorescence-based and automated patch-clamp-based high-throughput screening techniques

2016 ◽  
Vol 37 (1) ◽  
pp. 105-110 ◽  
Author(s):  
Jin-feng Yue ◽  
Guan-hua Qiao ◽  
Ni Liu ◽  
Fa-jun Nan ◽  
Zhao-bing Gao
Keyword(s):  
Patch Clamp ◽  
High Throughput ◽  
High Throughput Screening ◽  
Screening Techniques ◽  
Automated Patch Clamp

High-Throughput Screening of NaV1.7 Modulators Using a Giga-Seal Automated Patch Clamp Instrument

2016 ◽  
Vol 14 (2) ◽  
pp. 93-108 ◽  
Author(s):  
Chris Chambers ◽  
Ian Witton ◽  
Cathryn Adams ◽  
Luke Marrington ◽  
Juha Kammonen
Keyword(s):  
Patch Clamp ◽  
High Throughput ◽  
High Throughput Screening ◽  
Automated Patch Clamp

An update on the advancing high-throughput screening techniques for patch clamp-based ion channel screens: implications for drug discovery

2018 ◽  
Vol 13 (3) ◽  
pp. 269-277 ◽  
Author(s):  
Alison Obergrussberger ◽  
Tom A. Goetze ◽  
Nina Brinkwirth ◽  
Nadine Becker ◽  
Søren Friis ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Patch Clamp ◽  
Ion Channel ◽  
High Throughput ◽  
High Throughput Screening ◽  
Screening Techniques

scholarly journals Automated Patch Clamp Meets High-Throughput Screening: 384 Cells Recorded in Parallel on a Planar Patch Clamp Module

2015 ◽  
Vol 21 (6) ◽  
pp. 779-793 ◽  
Author(s):  
A. Obergrussberger ◽  
A. Bru ggemann ◽  
T. A. Goetze ◽  
M. Rapedius ◽  
C. Haarmann ◽  
...  
Keyword(s):  
Patch Clamp ◽  
High Throughput ◽  
High Throughput Screening ◽  
Automated Patch Clamp

scholarly journals An advanced automated patch clamp protocol design to investigate drug - ion channel binding dynamics.

2021 ◽  
Author(s):  
Peter Lukacs ◽  
Krisztina Pesti ◽  
Matyas C Foldi ◽  
Katalin Zboray ◽  
Adam V Toth ◽  
...  
Keyword(s):  
Patch Clamp ◽  
Mechanism Of Action ◽  
Time Scale ◽  
High Throughput Screening ◽  
Therapeutic Potential ◽  
Neuromuscular Disorders ◽  
Rapid Assessment ◽  
Drug Effects ◽  
Dissociation Kinetics ◽  
Automated Patch Clamp

Standard high throughput screening projects using automated patch-clamp instruments often fail to grasp essential details of the mechanism of action, such as binding/unbinding dynamics and modulation of gating. In this study, we aim to demonstrate that depth of analysis can be combined with acceptable throughput on such instruments. Using the microfluidics-based automated patch clamp, IonFlux Mercury, we developed a method for a rapid assessment of the mechanism of action of sodium channel inhibitors, including their state-dependent association and dissociation kinetics. The method is based on a complex voltage protocol, which is repeated at 1 Hz. Using this time resolution we could monitor the onset and offset of both channel block and modulation of gating upon drug perfusion and washout. Our results show that the onset and the offset of drug effects are complex processes, involving several steps, which may occur on different time scales. We could identify distinct sub-processes on the millisecond time scale, as well as on the second time scale. Automated analysis of the results allows collection of detailed information regarding the mechanism of action of individual compounds, which may help the assessment of therapeutic potential for hyperexcitability-related disorders, such as epilepsies, pain syndromes, neuromuscular disorders, or neurodegenerative diseases.

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