Nav1.1 Archives - Sophion

Two new posters by Charles River Laboratories on HTS ion channel screening

Using the stacked solution technology Charles River have developed and validated an assay suited for high through screening on both P2X- and GABA receptors. The short exposure of ligand of less than 1 second enables repetitive stimulation which is necessary for this assay. In another assay with voltage-gated target, the vast number of parameters that can be measured with high fidelity e-phys makes it important that the underlying software is powerful enough to cope. Read more here for ligand-gated and here for the NaV1.1 assay.

High throughput screening on Nav1.1 using Qube

The voltage-gated sodium channel NaV1.1 is highly expressed in fast spiking interneurons (FSIs), which are important for memory encoding and other cognitive functions. An impaired function of FSIs is associated with disorders like autism, schizophrenia, Alzheimer’s and others. Potentiators of NaV1.1 have been shown to minimize cognitive dysfunction in transgenic mice with decreased levels of NaV1.1 in parvalbumin-positive neurons and this target thus lend itself to therapeutic intervention. The challenge is to identify the molecule with the desired mode-of-action which inherently requires electrophysiology. In summary we show that Qube 384 provides:

  • Success rates up to 97%
  • Stable, unattended measurements over 7 hours
  • Consistent current voltage relationship
  • High reliability of detecting NaV1.1 activators

For the full application report please see here.