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Related Concept Videos

Patch Clamp01:18

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Many fundamental cell functions such as muscle contraction and nerve transmission rely on the electrical signals produced by the movement of positively and negatively charged ions across the cell membrane. One competent method to record current flowing across the whole cell or single ion channel is the patch-clamp technique.
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Related Experiment Video

Updated: Jan 30, 2026

Application of Automated Image-guided Patch Clamp for the Study of Neurons in Brain Slices
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Optimization of Ca(v)1.2 screening with an automated planar patch clamp platform.

Bharathi Balasubramanian1, John P Imredy, David Kim

  • 1Safety and Exploratory Pharmacology, Safety Assessment, Merck Research Laboratories, West Point, PA 19486, USA. bharathi_balasubramanian@merck.com

Journal of Pharmacological and Toxicological Methods
|April 16, 2009
PubMed
Summary

A new assay for screening Ca(v)1.2 channel blockers was developed using PatchXpress. This method offers a robust, medium-throughput approach for assessing drug cardiac liability during lead optimization.

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Area of Science:

  • Cardiovascular Pharmacology
  • Ion Channel Physiology
  • Drug Discovery

Background:

  • Calcium voltage-gated channel subfamily 1.2 (Ca(v)1.2) channels are crucial for cardiac action potential.
  • Screening for Ca(v)1.2 blockers is vital for identifying drugs lacking cardiac liability.
  • Traditional fluorescence assays have limitations, and patch clamping is labor-intensive.

Purpose of the Study:

  • Develop a robust, medium-throughput Ca(v)1.2 screening assay using PatchXpress 7000A.
  • Optimize cell isolation, recording solutions, and experimental parameters for reliable screening.

Main Methods:

  • Utilized HEK-293 cells stably expressing human Ca(v)1.2 channels.
  • Optimized cell isolation by reducing trypsin exposure time and temperature.
  • Modified intracellular and extracellular solutions to minimize channel rundown and enhance sensitivity.

Main Results:

  • Shortened incubation and trypsin exposure improved Ca(v)1.2 current amplitudes.
  • Reduced intracellular Mg2+ and added Ca2+ significantly minimized current rundown.
  • The assay successfully identified and characterized structurally diverse Ca(v)1.2 antagonists and an agonist.

Conclusions:

  • The developed PatchXpress assay provides a reliable method for Ca(v)1.2 channel screening.
  • This assay is suitable for assessing compound cardiac liability during drug lead optimization.