| Assay Method Information | |
| | SAR Analysis for the identification of selective inhibits of the transient receptor potential cation channel C4 (TRPC4): Automated Electrophysiology_2 |
| Description: | The inhibitory effects of test compounds on TRPC4 channels were evaluated in electrophysiological assays using a QPatch16 automated electrophysiology instrument. Whole cell recordings were made from HEK293 cells stably expressing TRPC4 channels along with micro-opioid receptors (TRPC4 cells). TRPC4 channels were activated by depolarizing membrane potential ramps and stimulation of GPCR signaling pathways. In control experiments, a micro-opioid agonist, 50 nM DAMGO ([D-Ala2, N-Me-Phe4, Gly5-ol]-Enkephalin acetate) produced robust activation of TRPC4 channels in repeated applications. Following DAMGO application, the effects of test compounds were measured in the continued presence of DAMGO. |
| Affinity data for this assay | |
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