Ontology highlight
ABSTRACT:
SUBMITTER: Shen A
PROVIDER: S-EPMC6813027 | biostudies-literature | 2019 Oct
REPOSITORIES: biostudies-literature
Shen Ao A Chen Dana D Kaur Manpreet M Bartels Peter P Xu Bing B Shi Qian Q Martinez Joseph M JM Man Kwun-Nok Mimi KM Nieves-Cintron Madeline M Hell Johannes W JW Navedo Manuel F MF Yu Xi-Yong XY Xiang Yang K YK
eLife 20191014
G protein-coupled receptors (GPCRs) transduce pleiotropic intracellular signals in mammalian cells. Here, we report neuronal excitability of β-blockers carvedilol and alprenolol at clinically relevant nanomolar concentrations. Carvedilol and alprenolol activate β<sub>2</sub>AR, which promote G protein signaling and cAMP/PKA activities without action of G protein receptor kinases (GRKs). The cAMP/PKA activities are restricted within the immediate vicinity of activated β<sub>2</sub>AR, leading to ...[more]