CB1 Cannabinoid Receptor Assay

Human CB1 cannabinoid receptor assay (CNR1) from Innoprot provides the analysis of both signalling pathways involving GPCR activation; G Protein by the analysis of Gi/Go activation and β-arrestin recruitment using Nomad multiplex technology. When an agonist binds to CNR1, it activates Gi/Go, which in turn, triggers a cellular response involving PKA activation. In this assay we measure Gi/Go activation in combination with β-arrestin recruitment.

CB1 cannabinoid receptor belongs to the large superfamily of GPCRs located in the central and peripheral nervous system. The expression of CNR1 modulates neurotransmitter release in a manner that prevents the development of excessive neuronal activity. It reduces pain and other inflammatory symptoms.

The CB1 receptor appears pre-synaptically in both glutaminergic and GABAergic interneurons and, in effect, acts as a neuromodulator to inhibit release of glutamate and GABA. Repeated administration of receptor agonists may result in receptor internalization and/ or a reduction in receptor protein signalling.

Cell line used: CB1 Nomad Cell Line

Readout: Gi/Go Activation & β-arrestin recruitment

Agonist: CP55940

EC50 Agonist: 2.25 x 10-7 M for Gi/Go Assay & 1.40 x 10-7 for β-arrestin recruitment

Type of Assay: Cell-based / Functional

Detection Method: Fluorimetry

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