Gαi/o GPCR assays

Gi/o-coupled G protein-coupled receptors (GPCRs) are a subset of GPCRs that couple with the Gαi/o protein subunit.

GPCR-GIRK Thalliun Flux Assay Principle -1-1
GPCR-GIRK Thalliun Flux Assay Principle -2-1
GPCR-GIRK Thalliun Flux Assay Principle -3-1
GPCR-GIRK Thalliun Flux Assay Principle -4-3

Gαi/o GPCRs are involved in physiological processes ranging from pain sensing, to neurotransmission, to autoimmune responses. Gi/o-coupled receptors include many neurotransmitter receptors such as serotonin, GABA, and dopamine receptors, some opioid receptors, and many more pharmacologically relevant targets for treating an array of medical conditions.

A key signaling pathway for Gi/o-coupled GPCRs, is through activation of G protein-gated Inward Rectifying Potassium (K⁺) channels, better known as GIRK channels. Not only is the GPCR-mediated modulation of GIRK channels of great physiological importance, it also provides a convenient means of measuring Gαi/o GPCR activity using fluorescence-based thallium flux assays.

A GIRK-based thallium flux assay approach offers some key advantages compared to other approaches that are used to measure the activity of Gαi/o GPCRs. Unlike the most common approach which utilizes fixed-endpoint measures of cAMP, the GIRK assay is a real-time measure of GPCR activation and does not require non-physiological elevations of intracellular cAMP. Another popular approach is the expression of chimeric Gα subunits (e.g. Gα16) to induce Gi/o GPCRs to promote intracellular calcium release through non-native coupling. However, GIRK-based thallium flux enables the measurement of Gαi/o GPCR activity through their native Gβ/γ coupling mechanism.

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Thallium flux assays for GPCRs

Examples of Gi/o GPCR assays using our kit
Gi GPCR assay data for Dopamine D2 receptor, including a kinetic trace and dose response curve
Gi GPCR high throughput screening data for Dopamine D2 receptor, including a kinetic trace and Z’ analysis for hit discovery.
Gi GPCR 96-well dose response curves for Dopamine D2 receptor, Serotonin receptor (5HT1A), muscarinic receptor (M2), and delta opioid receptor.
Gi GPCR 384-well dose response curves for Serotonin receptor (5HT1A), muscarinic receptor (M2), and delta opioid receptor.
Searching for thallium indicators instead?

Is your GPCR already GFP-tagged? Talk to us about using our red-shifted thallium indicator, Thallos Gold, for your assay.

Cell lines for Gi/o GPCR assays

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Image Products Excitation Emission Kd Price Quantity Action
Gio GPCR-GIRK Thallium Flux Assay
Gi/o GPCR-GIRK Thallium Flux Assay
A complete Gi/o GPCR assay for discovering modulators through direct coupling to GIRK channels. Cell lines and thallium flux reagents are included.
$695.00 – $11,690.00
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