Adenosine A2A Receptors

Adenosine A2A receptors are members of the adenosine receptor group of G-protein-coupled receptors that also includes A1, A2B and A3. A2A receptors display high expression levels in the spleen, thymus, leukocytes, blood platelets and the olfactory bulb.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
1063 CGS 21680 hydrochloride
A2A agonist
1710 CV 1808
Non-selective adenosine A2 receptor agonist
4603 LUF 5834
Potent adenosine A2A and A2B receptor partial agonist
4334 PSB 0777 ammonium salt
Potent adenosine A2A agonist

Antagonists

Cat No Product Name / Activity
3306 8-(3-Chlorostyryl)caffeine
Selective A2A antagonist. Also MAO-B inhibitor
3937 ANR 94
Adenosine A2A antagonist
5901 c-Di-AMP sodium salt
A2A inverse agonist; also endogenous STING and DDX41 agonist
5147 Istradefylline
Potent and selective adenosine A2A receptor antagonist
4783 Lu AA 47070
Prodrug of a potent and selective adenosine A2A receptor antagonist
2463 SCH 442416
Very selective, high affinity A2A antagonist
2270 SCH 58261
Potent, highly selective A2A antagonist
4407 TC-G 1004
Potent and selective A2A antagonist
1036 ZM 241385
Potent, highly selective A2A antagonist

Adenosine A2A receptors are members of the adenosine receptor group of G-protein-coupled receptors that also includes A1, A2B and A3. A2A receptors display high expression levels in the spleen, thymus, leukocytes, blood platelets, striatopallidal GABAergic neurons and the olfactory bulb. Lower expression levels are also found in the heart, lungs and blood vessels. A2A receptors mediate a sustained cardioprotective function during cardiac ischemia, inhibit neutrophil degranulation in neutrophil-mediated tissue injury and have been implicated in both neuroprotective and neurodegenerative effects. The human A2A receptor gene is localized on chromosome 22 (22q11.23).

Both A2A and A2B receptors are important in cancer immunology. The tumor microenvironment is hypoxic, which promotes the expression of CD39 and CD73 by immune cells. CD39 and CD73 are ectonucleotidases that convert ATP to adenosine, elevating concentrations of adenosine locally. Adenosine is a crucial mediator of altered immune function in cancer as it binds A2A and A2B receptors on lymphocytes silencing the antitumor immune response.

External sources of pharmacological information for Adenosine A2A Receptors :

Literature for Adenosine A2A Receptors

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Adenosine A2A Receptor Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human ADORA2A NM_000675 P29274
Mouse Adora2a NM_009630 Q60613
Rat Adora2a NM_053294 P30543