Stimulation of Gi-coupled receptors in heart and brain activates G-protein-gated inward rectifier K+ channels (GIRK) via Gβɣ (Dascal, N. 2001). This activity can be detected using a GIRK-mediated thallium flux assay described by Niswender et al., 2008. This assay is compatible with HTS and represents a novel and a sensitive assay for detecting Gi/o-coupled GPCRs.
Human M4 Muscarinic Receptor GIRK1 and GIRK4 Cell Line
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