GIRK1/2 Assay(s)

Background Information

Inwardly rectifying K⁺ channels (Kir3.1/3.2) are the primary downstream effectors of Gi-coupled receptors including opioid (μ, δ), dopamine D2, 5-HT1A, GABA-B, A1 adenosine, and muscarinic M2 receptors. GIRK mediates vagal heart rate slowing in the sinoatrial node. In DRG neurons, GIRK channels mediate the hyperpolarizing component of opioid analgesia.

Family: Ion Channel
Protein Name: Kir3.1/3.2 (GIRK1/2)
Gene Name: KCNJ3/6

Organism : Human
Therapeutic Area: Pain, Cardiovascular, Neuropsychiatry

Assay Information

Validated Assay(s): Thallium-free Potassium Channel Assay, Thallium Assay, APC
Assay type: Cell-based
Method: Fluorescence

Instrumentation: Panoptic
Plate Format: 384-well
Expression: Stable
Cell type: HEK293

Testing Information

Functional Mode(s): Activator, Inhibitor
Reference compound(s): ML297, SCH-23390

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