Target intelligence / Profile preview

Adenosine Receptor A2 Subtype (A2AR)

Target
A2AR
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The adenosine receptor A2 subtype refers to two closely related G protein-coupled receptors (GPCRs): the A2A and A2B adenosine receptors. These are activated by the endogenous nucleoside adenosine and primarily couple to Gs proteins, leading to increased intracellular cAMP. They play roles in vasodilation, neurotransmission, immunomodulation, and regulation of myocardial oxygen demand. A2A is a key target for Parkinson's disease and cancer immunotherapy, while both subtypes are implicated in cardiovascular diseases and inflammation.

Other names
Adenosine receptor A2AAdenosine receptor A2BADORA2AADORA2BA2A adenosine receptorA2B adenosine receptor
02

Mechanism of action

Agonists stimulate adenylate cyclase via Gs protein, increasing intracellular cAMP. Antagonists block adenosine binding and downstream signaling.

03

Biological functions

Signal transductionVasodilationNeurotransmission modulationImmunoregulationRegulation of myocardial oxygen demand
04

Disease associations

Parkinson’s diseaseCancerCardiovascular diseaseInflammationDepression
05

Safety considerations

Potential for off-target effects due to widespread adenosine receptor expression.Cardiovascular side effects.Immunosuppression.
06

Interacting drugs

Caffeine

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