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
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
Assay: Cannabinoid Receptors, GPCR, Pain, Therapeutic area
Area: CNS, Inflammation, Pain, Parkinson's Disease