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Adenosine receptors

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The adenosine receptors (or P1 receptors[1]) are a class of purinergic receptors, G-protein coupled receptors with adenosine as endogenous ligand.[2]


In humans, there are four adenosine receptors. Each is encoded by a separate gene and has different functions, although with some overlapping.[3] For instance, both A1 receptors and A2A play roles in the heart, regulating myocardial oxygen consumption and coronary blood flow, while the A2A receptor also has broader antiinflammatory effects throughout the body.[4] These two receptors also have important roles in the brain,[5] regulating the release of other neurotransmitters such as dopamine and glutamate,[6][7][8] while the A2B and A3 receptors are located mainly peripherally and are involved in processes such as inflammation and immune responses.



Comparison of subtypesEdit

Adenosine receptors
Receptor Gene Mechanism [15] Effects Agonists Antagonists
A1 ADORA1 Gi/ocAMP↑/↓
  • Inhibition
    • ↓ vesicle release
  • bronchospasm
A3 ADORA3 Gi/o
  • 2-(1-Hexynyl)-N-methyladenosine
  • CF-101 (IB-MECA)
  • 2-Cl-IB-MECA
  • CP-532,903
  • MRS-3558
  • theophylline
  • MRS-1191
  • MRS-1220
  • MRS-1334
  • MRS-1523
  • MRS-3777
  • MRE3008F20
  • PSB-10
  • PSB-11
  • VUF-5574

A1 adenosine receptorEdit

Main article: Adenosine A1 receptor



This receptor has an inhibitory function on most of the tissues in which it rests. In the brain, it slows metabolic activity by a combination of actions. Presynaptically, it reduces synaptic vesicle release while post synaptically it has been found to stabilize the magnesium on the NMDA receptor.

Antagonism and agonismEdit

Specific A1 antagonists include 8-Cyclopentyl-1,3-dipropylxanthine (DPCPX), and Cyclopentyltheophylline‎ (CPT) or 8-cyclopentyl-1,3-dipropylxanthine‎ (CPX), while specific agonists include 2-chloro-N(6)-cyclopentyladenosine (CCPA).

In the heartEdit



In neonatal medicineEdit

Adenosine antagonists are widely used in neonatal medicine;



A2A adenosine receptorEdit

Main article: Adenosine A2A receptor



The activity of A2A adenosine receptor, a G-protein coupled receptor family member, is mediated by G proteins which activate adenylyl cyclase. It is abundant in basal ganglia, vasculature and platelets and it is a major target of caffeine.[16]



Agonists and antagonistsEdit


A2B adenosine receptorEdit

Main article: Adenosine A2B receptor


A3 adenosine receptorEdit

Main article: Adenosine A3 receptor


References Edit

  1. Fredholm BB, Abbracchio MP, Burnstock G, Dubyak GR, Harden TK, Jacobson KA, Schwabe U, Williams M (1997). Towards a revised nomenclature for P1 and P2 receptors. Trends Pharmacol. Sci. 18 (3): 79–82.
  2. Fredholm BB, IJzerman AP, Jacobson KA, Klotz KN, Linden J (2001). International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors. Pharmacol. Rev. 53 (4): 527–52.
  3. Gao ZG, Jacobson KA (September 2007). Emerging adenosine receptor agonists. Expert Opinion on Emerging Drugs 12 (3): 479–92.
  4. Haskó G, Pacher P (March 2008). A2A receptors in inflammation and injury: lessons learned from transgenic animals. Journal of Leukocyte Biology 83 (3): 447–55.
  5. Kalda A, Yu L, Oztas E, Chen JF (October 2006). Novel neuroprotection by caffeine and adenosine A(2A) receptor antagonists in animal models of Parkinson's disease. Journal of the Neurological Sciences 248 (1-2): 9–15.
  6. Fuxe K, Ferré S, Genedani S, Franco R, Agnati LF (September 2007). Adenosine receptor-dopamine receptor interactions in the basal ganglia and their relevance for brain function. Physiology & Behavior 92 (1-2): 210–7.
  7. Schiffmann SN, Fisone G, Moresco R, Cunha RA, Ferré S (December 2007). Adenosine A2A receptors and basal ganglia physiology. Progress in Neurobiology 83 (5): 277–92.
  8. Cunha RA, Ferré S, Vaugeois JM, Chen JF (2008). Potential therapeutic interest of adenosine A2A receptors in psychiatric disorders. Current Pharmaceutical Design 14 (15): 1512–24.
  9. Peart JN, Headrick JP (May 2007). Adenosinergic cardioprotection: multiple receptors, multiple pathways. Pharmacology & Therapeutics 114 (2): 208–21.
  10. Cohen MV, Downey JM (May 2008). Adenosine: trigger and mediator of cardioprotection. Basic Research in Cardiology 103 (3): 203–15.
  11. Ferré S (May 2008). An update on the mechanisms of the psychostimulant effects of caffeine. Journal of Neurochemistry 105 (4): 1067–79.
  12. Osadchii OE (June 2007). Myocardial phosphodiesterases and regulation of cardiac contractility in health and cardiac disease. Cardiovascular Drugs and Therapy / Sponsored by the International Society of Cardiovascular Pharmacotherapy 21 (3): 171–94.
  13. Baraldi PG, Tabrizi MA, Gessi S, Borea PA (January 2008). Adenosine receptor antagonists: translating medicinal chemistry and pharmacology into clinical utility. Chemical Reviews 108 (1): 238–63.
  14. Cristalli G, Lambertucci C, Marucci G, Volpini R, Dal Ben D (2008). A2A adenosine receptor and its modulators: overview on a druggable GPCR and on structure-activity relationship analysis and binding requirements of agonists and antagonists. Current Pharmaceutical Design 14 (15): 1525–52.
  15. Unless else specified in boxes, then ref is:senselab
  16. Entrez Gene: ADORA2A adenosine A2A receptor.
  17. 17.0 17.1 Jacobson KA, Gao ZG (2006). Adenosine receptors as therapeutic targets. Nature reviews. Drug discovery 5 (3): 247–64.

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