Adenosine A2A receptor

Adenosine A2A receptor

The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, but also denotes the human gene encoding it.

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Biochemistry

The 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.cite web | title = Entrez Gene: ADORA2A adenosine A2A receptor| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=135| accessdate = ]

Function

As with the A1, the A2A receptors are believed to play a role in regulating myocardial oxygen consumption and coronary blood flow.

The A2A receptor is responsible for regulating myocardial blood flow by vasodilating the coronary arteries, which increases blood flow to the myocardium, but may lead to hypotension. Just as in A1 receptors, this normally serves as a protective mechanism, but may be destructive in altered cardiac function.

Recent research on adenosine receptor function, and adenosine receptor antagonists such as theophylline has led to several randomized controlled trials using these receptor antagonists to treat bradyasystolic arrest.cite journal | author = Burton JH, Mass M, Menegazzi JJ, Yealy DM | title = Aminophylline as an adjunct to standard advanced cardiac life support in prolonged cardiac arrest | journal = Annals of emergency medicine | volume = 30 | issue = 2 | pages = 154–8 | year = 1997 | pmid = 9250637 | doi = 10.1016/S0196-0644(97)70134-3 | issn = ] cite journal | author = Khoury MY, Moukarbel GV, Obeid MY, Alam SE | title = Effect of aminophylline on complete atrioventricular block with ventricular asystole following blunt chest trauma | journal = Injury | volume = 32 | issue = 4 | pages = 335–8 | year = 2001 | pmid = 11325371 | doi = 10.1016/S0020-1383(00)00222-9 | issn = ] cite journal | author = Mader TJ, Bertolet B, Ornato JP, Gutterman JM | title = Aminophylline in the treatment of atropine-resistant bradyasystole | journal = Resuscitation | volume = 47 | issue = 2 | pages = 105–12 | year = 2000 | pmid = 11008148 | doi = 10.1016/S0300-9572(00)00234-3 | issn = ] cite journal | author = Mader TJ, Smithline HA, Durkin L, Scriver G | title = A randomized controlled trial of intravenous aminophylline for atropine-resistant out-of-hospital asystolic cardiac arrest | journal = Academic emergency medicine : official journal of the Society for Academic Emergency Medicine | volume = 10 | issue = 3 | pages = 192–7 | year = 2003 | pmid = 12615581 | doi = 10.1197/aemj.10.3.192 | issn = ] cite journal | author = Mader TJ, Gibson P | title = Adenosine receptor antagonism in refractory asystolic cardiac arrest: results of a human pilot study | journal = Resuscitation | volume = 35 | issue = 1 | pages = 3–7 | year = 1997 | pmid = 9259053 | doi = 10.1016/S0300-9572(97)01097-6 | issn = ] cite journal | author = Perouansky M, Shamir M, Hershkowitz E, Donchin Y | title = Successful resuscitation using aminophylline in refractory cardiac arrest with asystole | journal = Resuscitation | volume = 38 | issue = 1 | pages = 39–41 | year = 1998 | pmid = 9783508 | doi = 10.1016/S0300-9572(98)00079-3 | issn = ] cite journal | author = Viskin S, Belhassen B, Roth A, Reicher M, Averbuch M, Sheps D, Shalabye E, Laniado S | title = Aminophylline for bradyasystolic cardiac arrest refractory to atropine and epinephrine | journal = Ann. Intern. Med. | volume = 118 | issue = 4 | pages = 279–81 | year = 1993 | pmid = 8420445 | doi = | issn = | url = http://www.annals.org/cgi/content/abstract/118/4/279 ]

Agonists and antagonists

Specific antagonists include "KW6002" and "SCH-58261", while specific agonists include CGS21680 and "ATL-146e".cite journal | author = Jacobson KA, Gao ZG | title = Adenosine receptors as therapeutic targets | journal = Nature reviews. Drug discovery | volume = 5 | issue = 3 | pages = 247–64 | year = 2006 | pmid = 16518376 | doi = 10.1038/nrd1983 | issn = ]

References

Further reading

PBB_Further_reading
citations =
*cite journal | author=Ongini E, Adami M, Ferri C, Bertorelli R |title=Adenosine A2A receptors and neuroprotection. |journal=Ann. N. Y. Acad. Sci. |volume=825 |issue= |pages= 30-48 |year= 1997 |pmid= 9369973 |doi=
*cite journal | author=Furlong TJ, Pierce KD, Selbie LA, Shine J |title=Molecular characterization of a human brain adenosine A2 receptor. |journal=Brain Res. Mol. Brain Res. |volume=15 |issue= 1-2 |pages= 62-6 |year= 1992 |pmid= 1331670 |doi=
*cite journal | author=Makujina SR, Sabouni MH, Bhatia S, "et al." |title=Vasodilatory effects of adenosine A2 receptor agonists CGS 21680 and CGS 22492 in human vasculature. |journal=Eur. J. Pharmacol. |volume=221 |issue= 2-3 |pages= 243-7 |year= 1992 |pmid= 1426003 |doi=
*cite journal | author=Karlsten R, Gordh T, Post C |title=Local antinociceptive and hyperalgesic effects in the formalin test after peripheral administration of adenosine analogues in mice. |journal=Pharmacol. Toxicol. |volume=70 |issue= 6 Pt 1 |pages= 434-8 |year= 1992 |pmid= 1438021 |doi=
*cite journal | author=Libert F, Passage E, Parmentier M, "et al." |title=Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor. |journal=Genomics |volume=11 |issue= 1 |pages= 225-7 |year= 1992 |pmid= 1662665 |doi=
*cite journal | author=Martinez-Mir MI, Probst A, Palacios JM |title=Adenosine A2 receptors: selective localization in the human basal ganglia and alterations with disease. |journal=Neuroscience |volume=42 |issue= 3 |pages= 697-706 |year= 1992 |pmid= 1835521 |doi=
*cite journal | author=Libert F, Parmentier M, Lefort A, "et al." |title=Selective amplification and cloning of four new members of the G protein-coupled receptor family. |journal=Science |volume=244 |issue= 4904 |pages= 569-72 |year= 1989 |pmid= 2541503 |doi=
*cite journal | author=Kim J, Wess J, van Rhee AM, "et al." |title=Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2A adenosine receptor. |journal=J. Biol. Chem. |volume=270 |issue= 23 |pages= 13987-97 |year= 1995 |pmid= 7775460 |doi=
*cite journal | author=Szondy Z |title=Adenosine stimulates DNA fragmentation in human thymocytes by Ca(2+)-mediated mechanisms. |journal=Biochem. J. |volume=304 ( Pt 3) |issue= |pages= 877-85 |year= 1995 |pmid= 7818494 |doi=
*cite journal | author=MacCollin M, Peterfreund R, MacDonald M, "et al." |title=Mapping of a human A2A adenosine receptor (ADORA2) to chromosome 22. |journal=Genomics |volume=20 |issue= 2 |pages= 332-3 |year= 1994 |pmid= 8020991 |doi= 10.1006/geno.1994.1181
*cite journal | author=Nonaka H, Ichimura M, Takeda M, "et al." |title=KF17837 ((E)-8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-methylxanthine), a potent and selective adenosine A2 receptor antagonist. |journal=Eur. J. Pharmacol. |volume=267 |issue= 3 |pages= 335-41 |year= 1994 |pmid= 8088373 |doi=
*cite journal | author=Iwamoto T, Umemura S, Toya Y, "et al." |title=Identification of adenosine A2 receptor-cAMP system in human aortic endothelial cells. |journal=Biochem. Biophys. Res. Commun. |volume=199 |issue= 2 |pages= 905-10 |year= 1994 |pmid= 8135838 |doi= 10.1006/bbrc.1994.1314
*cite journal | author=Salmon JE, Brogle N, Brownlie C, "et al." |title=Human mononuclear phagocytes express adenosine A1 receptors. A novel mechanism for differential regulation of Fc gamma receptor function. |journal=J. Immunol. |volume=151 |issue= 5 |pages= 2775-85 |year= 1993 |pmid= 8360491 |doi=
*cite journal | author=Peterfreund RA, MacCollin M, Gusella J, Fink JS |title=Characterization and expression of the human A2A adenosine receptor gene. |journal=J. Neurochem. |volume=66 |issue= 1 |pages= 362-8 |year= 1996 |pmid= 8522976 |doi=
*cite journal | author=Le F, Townsend-Nicholson A, Baker E, "et al." |title=Characterization and chromosomal localization of the human A2A adenosine receptor gene: ADORA2A. |journal=Biochem. Biophys. Res. Commun. |volume=223 |issue= 2 |pages= 461-7 |year= 1996 |pmid= 8670304 |doi= 10.1006/bbrc.1996.0916
*cite journal | author=Jiang Q, Van Rhee AM, Kim J, "et al." |title=Hydrophilic side chains in the third and seventh transmembrane helical domains of human A2A adenosine receptors are required for ligand recognition. |journal=Mol. Pharmacol. |volume=50 |issue= 3 |pages= 512-21 |year= 1996 |pmid= 8794889 |doi=
*cite journal | author=Ledent C, Vaugeois JM, Schiffmann SN, "et al." |title=Aggressiveness, hypoalgesia and high blood pressure in mice lacking the adenosine A2A receptor. |journal=Nature |volume=388 |issue= 6643 |pages= 674-8 |year= 1997 |pmid= 9262401 |doi= 10.1038/41771
*cite journal | author=Koshiba M, Rosin DL, Hayashi N, "et al." |title=Patterns of A2A extracellular adenosine receptor expression in different functional subsets of human peripheral T cells. Flow cytometry studies with anti-A2A receptor monoclonal antibodies. |journal=Mol. Pharmacol. |volume=55 |issue= 3 |pages= 614-24 |year= 1999 |pmid= 10051547 |doi=
*cite journal | author=Borgland SL, Castañón M, Spevak W, Parkinson FE |title=Effects of propentofylline on adenosine receptor activity in Chinese hamster ovary cell lines transfected with human A1, A2A, or A2B receptors and a luciferase reporter gene. |journal=Can. J. Physiol. Pharmacol. |volume=76 |issue= 12 |pages= 1132-8 |year= 1999 |pmid= 10326835 |doi=

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