Gα_s signalling of the CB₁ receptor and the influence of receptor number.

ABSTRACT:

Background and purpose

CB₁ receptor signalling is canonically mediated through inhibitory Gα_i proteins, but occurs through other G proteins under some circumstances, Gα_s being the most characterized secondary pathway. Determinants of this signalling switch identified to date include Gα_i blockade, CB₁ /D₂ receptor co-stimulation, CB₁ agonist class and cell background. Hence, we examined the effects of receptor number and different ligands on CB₁ receptor signalling.

Experimental approach

CB₁ receptors were expressed in HEK cells at different levels, and signalling characterized for cAMP by real-time BRET biosensor -CAMYEL - and for phospho-ERK by AlphaScreen. Homogenate and whol

SUBMITTER: Finlay DB 

PROVIDER: S-EPMC5513864 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature