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ADORA2A - ADORA2A

Target Class GPCR FamilyAdenosine
SpeciesHuman   
Background
This gene encodes a protein which is one of several receptor subtypes for adenosine. The activity of the encoded protein, a G-protein coupled receptor family member, is mediated by G proteins which activate adenylyl cyclase. The encoded protein is abundant in basal ganglia, vasculature and platelets and it is a major target of caffeine. [provided by RefSeq, Jul 2008]

Cell Background
RBL-2H3
Readout
Calcium
Method
Detect calcium mobilization using DiscoverX Calcium No WashPLUS
Agonist/Ligand
NECA
Agonist/Ligand EC50
27
Agonist Effect (Activation)
coronary vasodilation; decrease BP and reflex; increase HR; decrease platelet aggregation and leukocyte activation; decrease in locomotor activity; sleep
Antagonist Effect (Inhibition)
potential for stimulation of platelet aggregation; increase BP; nervousness; arousal; insomnia
Ref.
Bowes et. al. 2012
AgonistEC50(nM)
NECA27
2-CADO19
CGS-2168030
AntagonistIC50(nM)
SCH-44241611
Alloxazine18
DPCPX2
Cells are plated in a 384-well plate and incubated overnight at 37°C/5% CO2 to allow the cells to attach and grow. Culture media is removed and replaced with dye loading buffer from the Calcium No WashPLUS detection kit according to the recommended protocol. Target cells and native parental cells are stimulated with a control agonist and calcium mobilization is detected using a FLIPR® Tetra (Molecular Devices, Inc.).
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