Adenosine receptor A2a (ADORA2A) (ADORA2A)

The Adenosine receptor A2a is a high-affinity G protein-coupled receptor (GPCR) that primarily signals through the Gs protein to stimulate adenylate cyclase and increase intracellular cAMP levels [UniProt: P30542]. In the rat brain, it is highly concentrated in the striatum, where it plays a pivotal role in modulating motor activity by interacting with dopamine D2 receptors [PubMed: 21531020]. This receptor is a key therapeutic target for Parkinson's disease, where antagonists are used to enhance dopaminergic signaling and reduce motor fluctuations [PubMed: 31540421]. Additionally, its expression on immune cells and vascular smooth muscle makes it a target for anti-inflammatory, oncology, and cardiovascular applications [PubMed: 29053183]. The rat model is frequently used in preclinical research to study A2A-mediated neurotransmission and to test novel ligands like CGS-21680 and ZM-241385 [PubMed: 15148138]. Agonists of this receptor, such as regadenoson, are clinically utilized as coronary vasodilators during cardiac stress testing [PubChem: CID 119032].

Other names

Adenosine A2A receptorA2aRADORA2AAdenosine receptor subtype A2a

Adenosine receptor A2a antagonists, such as istradefylline, work by blocking the inhibitory effect of adenosine on dopamine D2 receptor-expressing neurons in the striatum, thereby enhancing motor control in Parkinson's disease [PubMed: 31540421]. Agonists like regadenoson activate the Gs-adenylate cyclase-cAMP pathway, leading to coronary vasodilation for diagnostic imaging [PubChem: CID 119032].