CaV1.2 - "Stable Recordings and High Throughput Pharmacology of Assay Ready CaV1.2 Cells on the SyncroPatch 384"
SyncroPatch 384 application note: (1.6 MB)
Cells were kindly provided by NMI TT Pharmaservices, Steinbeis-Innovationszentrum Zellkulturtechnik and acCELLerate
The CaV1.2 channel is a voltage-gated calcium channel (VGCC) expressed in a variety of mammalian tissues and is essential for multiple processes including CNS function, cardiac and smooth muscle contraction and neuroendocrine regulation. VGCC are composed of 4 subunits, which include an alpha 1 subunit which forms the Ca2+-selective pore, contains the voltage sensor and many of the binding sites for regulatory modulators and drugs and accessory subunits α2δ, β and γ which are involved in anchorage, trafficking and regulatory functions. The CaV1.2 channel contains the alpha-1C subunit, encoded by the CACNA1C gene on the human chromosome 12p13. Mutations in the L-type Ca2+ channels have been associated with inherited arrhythmic disorders such as Timothy, Brugada and early repolarization syndromes. In addition, the L-type Ca2+ channel is an important target for cardiac safety testing, especially in the light of the CiPA initiative. Here we present high quality data with reliable pharmacology on Assay Ready CaV1.2 Cells at a high throughput collected on the SyncroPatch 384. Current-voltage plots and concentration response curves for the compounds nifedipine and verapamil are shown. The IC50 values for these compounds are within the expected range and success rates of >75% for completed experiments were recorded. Importantly, CaV1.2 recorded on the Syncro- Patch 384 exhibited stable peak amplitude during the course of the experiment and displayed low rundown.
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