Comparing CB1 receptor GIRK channel responses to receptor internalization using a kinetic imaging assay.

ABSTRACT: The type 1 cannabinoid receptor (CB1R) mediates neurotransmitter release and synaptic plasticity in the central nervous system. Endogenous, plant-derived, synthetic cannabinoids bind to CB1R, initiating the inhibitory G-protein (G_i) and the β-arrestin signaling pathways. Within the G_i signaling pathway, CB1R activates G protein-gated, inwardly-rectifying potassium (GIRK) channels. The β-arrestin pathway reduces CB1R expression on the cell surface through receptor internalization. Because of their association with analgesia and drug tolerance, GIRK channels and receptor internalization are of interest to the development of pharmaceuticals. This research used immortalized mouse pituitary gland cells transduced with a pH-sensitive, fluorescently-tagged human CB1R (AtT20-

SUBMITTER: Andersen HK 

PROVIDER: S-EPMC11306342 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature