Adenozinski A2A receptor

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Adenozinski A2A receptor

Kristalografska struktura adenozinskog A2A receptora (N-terminus = plavo, C-terminus = crveno) u kompleksu sa ZM-241,385 (štapićasti dijagram), bazirana na 3EML koordinatama.
Dostupne strukture
3EML
Identifikatori
Simboli ADORA2A; ADORA2; RDC8; hA2AR
Vanjski ID OMIM102776 MGI99402 HomoloGene20166 IUPHAR: A2A GeneCards: ADORA2A Gene
Pregled RNK izražavanja
PBB GE ADORA2A 205013 s at tn.png
podaci
Ortolozi
Vrsta Čovek Miš
Entrez 135 11540
Ensembl ENSG00000128271 ENSMUSG00000020178
UniProt P29274 Q2NLC1
RefSeq (mRNA) NM_000675 NM_009630
RefSeq (protein) NP_000666 NP_033760
Lokacija (UCSC) Chr 22:
23.15 - 23.17 Mb
Chr 10:
74.77 - 74.78 Mb
PubMed pretraga [1] [2]

Adenozinski A2A receptor (ADORA2A) je adenozinski receptor. On je kodiran humanim ADORA2A genom.[1][2]

Struktura[уреди]

Ovaj protein je član familije G protein-spregnutih receptora koji imaju sedam transmembranskih alfa heliksa. Kristalografska struktura adenozinskog A2A receptora (3EML) pokazuje da je mesto vezivanja liganda distinktno u odnosu na druge GPCR proteine sa određenom strukturom (npr., beta-2 adrenergički receptor i rodopsin).[3]

Heteromeri[уреди]

Dejstva A2A receptora su komplikovana činjenicom da je mnoštvo funkcionalnih heteromera, koji su kombinacije A2A podjedinica i drugih nesrodnih G-protein spregnutih receptora, nađeno u mozgu. To uvećava kompleksnost uloge adenozina u modulaciji neuronske aktivnosti. Heteromeri koji sadrže adenozinski A1/A2A,[4][5] dopaminski D2/A2A[6] iD3/A2A,[7] glutamatni mGluR5/A2A[8] i kanabinoidni CB1/A2A[9] su zapaženi, kao i CB1/A2A/D2 heterotrimeri.[10] Istraživanje funkcionalnog značaja i endogene uloge tih hibridnih receptora je u toku.[11][12][13]

Funkcija[уреди]

Ovaj protein je jedan od nekoliko podtipova adenozinskih receptora. Njegova aktivnost je posredovana G proteinima koji aktiviraju adenilat ciklazu. Ovog proteina ima u izobilju u bazalnoj gangliji, vaskulaturi i krvnim pločicama. On je jedan od glavnih meta kofeina.[14]

Fiziološka uloga[уреди]

Poput A1, A2A receptori učestvuju u regulaciji potrošnje miokardijalnog kiseonika i koronarnog krvnog protoka.

A2A receptor je odgovoran za regulaciju miokardijalnog protoka krvi putem vazodilatacije koronarnih arterija, čime se povećava krvni protok do miokardijuma, mada to može da dovede do hipotenzije. Kao i A1 receptori, ovo dejstvo normalno služi kao zaštitni mehanizam.

A2A receptori su izraženi u mozgu, gde regulišu glutamatno i dopaminsko oslogađanje. On je potencijalna terapeutska meta za lečenje insomnije, bola, depresije, zavisnosti od droge i Parkinsonove bolesti.[15][16][17][18][19][20][21]

Ligandi[уреди]

Brojni selektivni A2A ligandi su razvijeni,[22][23][24][25][26][27][28][29][30][31][32][33] sa nekoliko mogućih terapeutskih primena.[34][35][36][37][38][39] Starija ispitivanja funkcije adenozinskog receptora, i neselektivni antagonisti adenozinskog receptora kao što je aminofilin, su bili usredsređeni na ulogu adenozinskih receptora u funkciji srca. To je rezultovalo u nekoliko kliničkih ispitivanja tih antagonista za lečenje bradikardijskog srčanog zastoja.[40][41][42][43][44][45][46]

Međutim razvoj selektivnijih A2A liganda je doveo do drugih primena. Najznačajniji fokus istraživanja je potencijalna terapeutska uloga A2A antagonista u lečenju Parkinsonove bolesti.[47][48][49][50]

Agonisti

Antagonisti

Interakcije[уреди]

Za adenozinski A2A receptor je pokazano da interaguje sa dopaminskim receptorom D2.[58]

Reference[уреди]

  1. ^ Libert F, Parmentier M, Lefort A, Dinsart C, Van Sande J, Maenhaut C, Simons MJ, Dumont JE, Vassart G (May 1989). „Selective amplification and cloning of four new members of the G protein-coupled receptor family“. Science 244 (4904): 569–72. DOI:10.1126/science.2541503. PMID 2541503. 
  2. ^ Libert F, Passage E, Parmentier M, Simons MJ, Vassart G, Mattei MG (September 1991). „Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor“. Genomics 11 (1): 225–7. DOI:10.1016/0888-7543(91)90125-X. PMID 1662665. 
  3. ^ Jaakola VP, Griffith MT, Hanson MA, Cherezov V, Chien EY, Lane JR, IJzerman AP, Stevens RC (October 2008). „The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist“. Science 322 (5905): 1211–7. DOI:10.1126/science.1164772. PMC 2586971. PMID 18832607. 
  4. ^ Ciruela F, Casadó V, Rodrigues RJ, Luján R, Burgueño J, Canals M, Borycz J, Rebola N, Goldberg SR, Mallol J, Cortés A, Canela EI, López-Giménez JF, Milligan G, Lluis C, Cunha RA, Ferré S, Franco R (February 2006). „Presynaptic control of striatal glutamatergic neurotransmission by adenosine A1-A2A receptor heteromers“. The Journal of Neuroscience : the Official Journal of the Society for Neuroscience 26 (7): 2080–7. DOI:10.1523/JNEUROSCI.3574-05.2006. PMID 16481441. 
  5. ^ Ferre S, Ciruela F, Borycz J, Solinas M, Quarta D, Antoniou K, Quiroz C, Justinova Z, Lluis C, Franco R, Goldberg SR (2008). „Adenosine A1-A2A receptor heteromers: new targets for caffeine in the brain“. Frontiers in Bioscience : a Journal and Virtual Library 13 (13): 2391–9. DOI:10.2741/2852. PMID 17981720. 
  6. ^ Fuxe K, Ferré S, Canals M, Torvinen M, Terasmaa A, Marcellino D, Goldberg SR, Staines W, Jacobsen KX, Lluis C, Woods AS, Agnati LF, Franco R (2005). „Adenosine A2A and dopamine D2 heteromeric receptor complexes and their function“. Journal of Molecular Neuroscience : MN 26 (2-3): 209–20. DOI:10.1385/JMN:26:2-3:209. PMID 16012194. 
  7. ^ Torvinen M, Marcellino D, Canals M, Agnati LF, Lluis C, Franco R, Fuxe K (February 2005). „Adenosine A2A receptor and dopamine D3 receptor interactions: evidence of functional A2A/D3 heteromeric complexes“. Molecular Pharmacology 67 (2): 400–7. DOI:10.1124/mol.104.003376. PMID 15539641. 
  8. ^ Zezula J, Freissmuth M (March 2008). „The A(2A)-adenosine receptor: a GPCR with unique features?“. British Journal of Pharmacology. 153 Suppl 1 (S1): S184–90. DOI:10.1038/sj.bjp.0707674. PMC 2268059. PMID 18246094. 
  9. ^ Ferré S, Goldberg SR, Lluis C, Franco R (2009). „Looking for the role of cannabinoid receptor heteromers in striatal function“. Neuropharmacology. 56 Suppl 1: 226–34. DOI:10.1016/j.neuropharm.2008.06.076. PMC 2635338. PMID 18691604. 
  10. ^ Marcellino D, Carriba P, Filip M, Borgkvist A, Frankowska M, Bellido I, Tanganelli S, Müller CE, Fisone G, Lluis C, Agnati LF, Franco R, Fuxe K (April 2008). „Antagonistic cannabinoid CB1/dopamine D2 receptor interactions in striatal CB1/D2 heteromers. A combined neurochemical and behavioral analysis“. Neuropharmacology 54 (5): 815–23. DOI:10.1016/j.neuropharm.2007.12.011. PMID 18262573. 
  11. ^ Ferré S, Ciruela F, Quiroz C, Luján R, Popoli P, Cunha RA, Agnati LF, Fuxe K, Woods AS, Lluis C, Franco R (2007). „Adenosine receptor heteromers and their integrative role in striatal function“. TheScientificWorldJournal 7: 74–85. DOI:10.1100/tsw.2007.211. PMID 17982579. 
  12. ^ Wardas J (2008). „Potential role of adenosine A2A receptors in the treatment of schizophrenia“. Frontiers in Bioscience : a Journal and Virtual Library 13 (13): 4071–96. DOI:10.2741/2995. PMID 18508501. 
  13. ^ Simola N, Morelli M, Pinna A (2008). „Adenosine A2A receptor antagonists and Parkinson's disease: state of the art and future directions“. Current Pharmaceutical Design 14 (15): 1475–89. DOI:10.2174/138161208784480072. PMID 18537671. 
  14. ^ „Entrez Gene: ADORA2A adenosine A2A receptor“. 
  15. ^ Hack SP, Christie MJ (2003). „Adaptations in adenosine signaling in drug dependence: therapeutic implications“. Critical Reviews in Neurobiology 15 (3-4): 235–74. DOI:10.1615/CritRevNeurobiol.v15.i34.30. PMID 15248812. 
  16. ^ Morelli M, Di Paolo T, Wardas J, Calon F, Xiao D, Schwarzschild MA (December 2007). „Role of adenosine A2A receptors in parkinsonian motor impairment and l-DOPA-induced motor complications“. Progress in Neurobiology 83 (5): 293–309. DOI:10.1016/j.pneurobio.2007.07.001. PMID 17826884. 
  17. ^ 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. DOI:10.1016/j.pneurobio.2007.05.001. PMC 2148496. PMID 17646043. 
  18. ^ Ferré S, Diamond I, Goldberg SR, Yao L, Hourani SM, Huang ZL, Urade Y, Kitchen I (December 2007). „Adenosine A2A receptors in ventral striatum, hypothalamus and nociceptive circuitry implications for drug addiction, sleep and pain“. Progress in Neurobiology 83 (5): 332–47. DOI:10.1016/j.pneurobio.2007.04.002. PMC 2141681. PMID 17532111. 
  19. ^ Brown RM, Short JL (November 2008). „Adenosine A(2A) receptors and their role in drug addiction“. The Journal of Pharmacy and Pharmacology 60 (11): 1409–30. DOI:10.1211/jpp/60.11.0001. PMID 18957161. 
  20. ^ 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. DOI:10.2174/138161208784480090. PMC 2423946. PMID 18537674. 
  21. ^ Mingote S, Font L, Farrar AM, Vontell R, Worden LT, Stopper CM, Port RG, Sink KS, Bunce JG, Chrobak JJ, Salamone JD (September 2008). „Nucleus accumbens adenosine A2A receptors regulate exertion of effort by acting on the ventral striatopallidal pathway“. The Journal of Neuroscience : the Official Journal of the Society for Neuroscience 28 (36): 9037–46. DOI:10.1523/JNEUROSCI.1525-08.2008. PMC 2806668. PMID 18768698. 
  22. ^ Ongini E, Monopoli A, Cacciari B, Baraldi PG (2001). „Selective adenosine A2A receptor antagonists“. Farmaco (Società Chimica Italiana : 1989) 56 (1-2): 87–90. PMID 11347973. 
  23. ^ Baraldi PG, Cacciari B, Romagnoli R, Spalluto G, Monopoli A, Ongini E, Varani K, Borea PA (January 2002). „7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility“. Journal of Medicinal Chemistry 45 (1): 115–26. DOI:10.1021/jm010924c. PMID 11754583. 
  24. ^ Baraldi PG, Fruttarolo F, Tabrizi MA, Preti D, Romagnoli R, El-Kashef H, Moorman A, Varani K, Gessi S, Merighi S, Borea PA (March 2003). „Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists“. Journal of Medicinal Chemistry 46 (7): 1229–41. DOI:10.1021/jm021023m. PMID 12646033. 
  25. ^ Weiss SM, Benwell K, Cliffe IA, Gillespie RJ, Knight AR, Lerpiniere J, Misra A, Pratt RM, Revell D, Upton R, Dourish CT (December 2003). „Discovery of nonxanthine adenosine A2A receptor antagonists for the treatment of Parkinson's disease“. Neurology 61 (11 Suppl 6): S101–6. PMID 14663021. 
  26. ^ Cristalli G, Lambertucci C, Taffi S, Vittori S, Volpini R (2003). „Medicinal chemistry of adenosine A2A receptor agonists“. Current Topics in Medicinal Chemistry 3 (4): 387–401. DOI:10.2174/1568026033392282. PMID 12570757. 
  27. ^ Cacciari B, Pastorin G, Spalluto G (2003). „Medicinal chemistry of A2A adenosine receptor antagonists“. Current Topics in Medicinal Chemistry 3 (4): 403–11. DOI:10.2174/1568026033392183. PMID 12570758. 
  28. ^ Cristalli G, Cacciari B, Dal Ben D, Lambertucci C, Moro S, Spalluto G, Volpini R (March 2007). „Highlights on the development of A(2A) adenosine receptor agonists and antagonists“. ChemMedChem 2 (3): 260–81. DOI:10.1002/cmdc.200600193. PMID 17177231. 
  29. ^ Diniz C, Borges F, Santana L, Uriarte E, Oliveira JM, Gonçalves J, Fresco P (2008). „Ligands and therapeutic perspectives of adenosine A(2A) receptors“. Current Pharmaceutical Design 14 (17): 1698–722. DOI:10.2174/138161208784746842. PMID 18673194. 
  30. ^ 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. DOI:10.2174/138161208784480081. PMID 18537675. 
  31. ^ Gillespie RJ, Adams DR, Bebbington D, Benwell K, Cliffe IA, Dawson CE, Dourish CT, Fletcher A, Gaur S, Giles PR, Jordan AM, Knight AR, Knutsen LJ, Lawrence A, Lerpiniere J, Misra A, Porter RH, Pratt RM, Shepherd R, Upton R, Ward SE, Weiss SM, Williamson DS (May 2008). „Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives“. Bioorganic & Medicinal Chemistry Letters 18 (9): 2916–9. DOI:10.1016/j.bmcl.2008.03.075. PMID 18406614. 
  32. ^ Gillespie RJ, Cliffe IA, Dawson CE, Dourish CT, Gaur S, Giles PR, Jordan AM, Knight AR, Lawrence A, Lerpiniere J, Misra A, Pratt RM, Todd RS, Upton R, Weiss SM, Williamson DS (May 2008). „Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives“. Bioorganic & Medicinal Chemistry Letters 18 (9): 2920–3. DOI:10.1016/j.bmcl.2008.03.076. PMID 18407496. 
  33. ^ Gillespie RJ, Cliffe IA, Dawson CE, Dourish CT, Gaur S, Jordan AM, Knight AR, Lerpiniere J, Misra A, Pratt RM, Roffey J, Stratton GC, Upton R, Weiss SM, Williamson DS (May 2008). „Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines“. Bioorganic & Medicinal Chemistry Letters 18 (9): 2924–9. DOI:10.1016/j.bmcl.2008.03.072. PMID 18411049. 
  34. ^ Sullivan GW (November 2003). „Adenosine A2A receptor agonists as anti-inflammatory agents“. Current Opinion in Investigational Drugs (London, England : 2000) 4 (11): 1313–9. PMID 14758770. 
  35. ^ Lappas CM, Sullivan GW, Linden J (July 2005). „Adenosine A2A agonists in development for the treatment of inflammation“. Expert Opinion on Investigational Drugs 14 (7): 797–806. DOI:10.1517/13543784.14.7.797. PMID 16022569. 
  36. ^ El Yacoubi M, Costentin J, Vaugeois JM (December 2003). „Adenosine A2A receptors and depression“. Neurology 61 (11 Suppl 6): S82–7. PMID 14663017. 
  37. ^ Kaster MP, Rosa AO, Rosso MM, Goulart EC, Santos AR, Rodrigues AL (January 2004). „Adenosine administration produces an antidepressant-like effect in mice: evidence for the involvement of A1 and A2A receptors“. Neuroscience Letters 355 (1-2): 21–4. DOI:10.1016/j.neulet.2003.10.040. PMID 14729225. 
  38. ^ Takahashi RN, Pamplona FA, Prediger RD (2008). „Adenosine receptor antagonists for cognitive dysfunction: a review of animal studies“. Frontiers in Bioscience : a Journal and Virtual Library 13 (13): 2614–32. DOI:10.2741/2870. PMID 17981738. 
  39. ^ Lobato KR, Binfaré RW, Budni J, Rosa AO, Santos AR, Rodrigues AL (May 2008). „Involvement of the adenosine A1 and A2A receptors in the antidepressant-like effect of zinc in the forced swimming test“. Progress in Neuro-psychopharmacology & Biological Psychiatry 32 (4): 994–9. DOI:10.1016/j.pnpbp.2008.01.012. PMID 18289757. 
  40. ^ Burton JH, Mass M, Menegazzi JJ, Yealy DM (1997). „Aminophylline as an adjunct to standard advanced cardiac life support in prolonged cardiac arrest“. Annals of emergency medicine 30 (2): 154–8. DOI:10.1016/S0196-0644(97)70134-3. PMID 9250637. 
  41. ^ Khoury MY, Moukarbel GV, Obeid MY, Alam SE (2001). „Effect of aminophylline on complete atrioventricular block with ventricular asystole following blunt chest trauma“. Injury 32 (4): 335–8. DOI:10.1016/S0020-1383(00)00222-9. PMID 11325371. 
  42. ^ Mader TJ, Bertolet B, Ornato JP, Gutterman JM (2000). „Aminophylline in the treatment of atropine-resistant bradyasystole“. Resuscitation 47 (2): 105–12. DOI:10.1016/S0300-9572(00)00234-3. PMID 11008148. 
  43. ^ Mader TJ, Smithline HA, Durkin L, Scriver G (2003). „A randomized controlled trial of intravenous aminophylline for atropine-resistant out-of-hospital asystolic cardiac arrest“. Academic emergency medicine : official journal of the Society for Academic Emergency Medicine 10 (3): 192–7. DOI:10.1197/aemj.10.3.192. PMID 12615581. 
  44. ^ Mader TJ, Gibson P (1997). „Adenosine receptor antagonism in refractory asystolic cardiac arrest: results of a human pilot study“. Resuscitation 35 (1): 3–7. DOI:10.1016/S0300-9572(97)01097-6. PMID 9259053. 
  45. ^ Perouansky M, Shamir M, Hershkowitz E, Donchin Y (1998). „Successful resuscitation using aminophylline in refractory cardiac arrest with asystole“. Resuscitation 38 (1): 39–41. DOI:10.1016/S0300-9572(98)00079-3. PMID 9783508. 
  46. ^ Viskin S, Belhassen B, Roth A, Reicher M, Averbuch M, Sheps D, Shalabye E, Laniado S (1993). „Aminophylline for bradyasystolic cardiac arrest refractory to atropine and epinephrine“. Ann. Intern. Med. 118 (4): 279–81. PMID 8420445. 
  47. ^ Jenner P (December 2003). „A2A antagonists as novel non-dopaminergic therapy for motor dysfunction in PD“. Neurology 61 (11 Suppl 6): S32–8. PMID 14663007. 
  48. ^ Mori A, Shindou T (December 2003). „Modulation of GABAergic transmission in the striatopallidal system by adenosine A2A receptors: a potential mechanism for the antiparkinsonian effects of A2A antagonists“. Neurology 61 (11 Suppl 6): S44–8. PMID 14663009. 
  49. ^ Pinna A, Wardas J, Simola N, Morelli M (November 2005). „New therapies for the treatment of Parkinson's disease: adenosine A2A receptor antagonists“. Life Sciences 77 (26): 3259–67. DOI:10.1016/j.lfs.2005.04.029. PMID 15979104. 
  50. ^ Kelsey JE, Langelier NA, Oriel BS, Reedy C (January 2009). „The effects of systemic, intrastriatal, and intrapallidal injections of caffeine and systemic injections of A2A and A1 antagonists on forepaw stepping in the unilateral 6-OHDA-lesioned rat“. Psychopharmacology 201 (4): 529–39. DOI:10.1007/s00213-008-1319-0. PMID 18791705. 
  51. ^ Jacobson KA, Gao ZG (2006). „Adenosine receptors as therapeutic targets“. Nature reviews. Drug discovery 5 (3): 247–64. DOI:10.1038/nrd1983. PMID 16518376. 
  52. ^ Yoneyama F, Yamada H, Satoh K, Taira N (March 1992). „Vasodepressor mechanisms of 2-(1-octynyl)-adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels“. Eur. J. Pharmacol. 213 (2): 199–204. DOI:10.1016/0014-2999(92)90682-T. PMID 1521559. 
  53. ^ Kase H, Aoyama S, Ichimura M, Ikeda K, Ishii A, Kanda T, Koga K, Koike N, Kurokawa M, Kuwana Y, Mori A, Nakamura J, Nonaka H, Ochi M, Saki M, Shimada J, Shindou T, Shiozaki S, Suzuki F, Takeda M, Yanagawa K, Richardson PJ, Jenner P, Bedard P, Borrelli E, Hauser RA, Chase TN (December 2003). „Progress in pursuit of therapeutic A2A antagonists: the adenosine A2A receptor selective antagonist KW6002: research and development toward a novel nondopaminergic therapy for Parkinson's disease“. Neurology 61 (11 Suppl 6): S97–100. PMID 14663020. 
  54. ^ Mott AM, Nunes EJ, Collins LE, Port RG, Sink KS, Hockemeyer J, Müller CE, Salamone JD (January 2009). „The adenosine A(2A) antagonist MSX-3 reverses the effects of the dopamine antagonist haloperidol on effort-related decision making in a T-maze cost/benefit procedure“. Psychopharmacology 204 (1): 103–12. DOI:10.1007/s00213-008-1441-z. PMC 2875244. PMID 19132351. 
  55. ^ Hodgson RA, Bertorelli R, Varty GB, Lachowicz JE, Forlani A, Fredduzzi S, Cohen-Williams ME, Higgins GA, Impagnatiello F, Nicolussi E, Parra LE, Foster C, Zhai Y, Neustadt BR, Stamford AW, Parker EM, Reggiani A, Hunter JC (March 2009). „Characterization of the Potent and Highly Selective A2A Receptor Antagonists Preladenant and SCH 412348 in Rodent Models of Movement Disorders and Depression“. The Journal of Pharmacology and Experimental Therapeutics 330 (1): 294–303. DOI:10.1124/jpet.108.149617. PMID 19332567. 
  56. ^ Pinna A, Fenu S, Morelli M (March 2001). „Motor stimulant effects of the adenosine A2A receptor antagonist SCH 58261 do not develop tolerance after repeated treatments in 6-hydroxydopamine-lesioned rats“. Synapse 39 (3): 233–8. DOI:10.1002/1098-2396(20010301)39:3<233::AID-SYN1004>3.0.CO;2-K. PMID 11284438. 
  57. ^ Rose S, Jackson MJ, Smith LA, Stockwell K, Johnson L, Carminati P, Jenner P (September 2006). „The novel adenosine A2a receptor antagonist ST1535 potentiates the effects of a threshold dose of L-DOPA in MPTP treated common marmosets“. European Journal of Pharmacology 546 (1-3): 82–7. DOI:10.1016/j.ejphar.2006.07.017. PMID 16925991. 
  58. ^ Kamiya, Toshio; Saitoh Osamu, Yoshioka Kazuaki, Nakata Hiroyasu (Jun. 2003). „Oligomerization of adenosine A2A and dopamine D2 receptors in living cells“. Biochem. Biophys. Res. Commun. (United States) 306 (2): 544–9. DOI:10.1016/S0006-291X(03)00991-4. ISSN 0006-291X. PMID 12804599. 

Literatura[уреди]

  • Ongini E, Adami M, Ferri C, Bertorelli R (1997). „Adenosine A2A receptors and neuroprotection.“. Ann. N. Y. Acad. Sci. 825 (1 Neuroprotecti): 30–48. DOI:10.1111/j.1749-6632.1997.tb48412.x. PMID 9369973. 
  • Furlong TJ, Pierce KD, Selbie LA, Shine J (1992). „Molecular characterization of a human brain adenosine A2 receptor.“. Brain Res. Mol. Brain Res. 15 (1-2): 62–6. DOI:10.1016/0169-328X(92)90152-2. PMID 1331670. 
  • Makujina SR, Sabouni MH, Bhatia S, et al. (1992). „Vasodilatory effects of adenosine A2 receptor agonists CGS 21680 and CGS 22492 in human vasculature.“. Eur. J. Pharmacol. 221 (2-3): 243–7. DOI:10.1016/0014-2999(92)90708-C. PMID 1426003. 
  • Karlsten R, Gordh T, Post C (1992). „Local antinociceptive and hyperalgesic effects in the formalin test after peripheral administration of adenosine analogues in mice.“. Pharmacol. Toxicol. 70 (6 Pt 1): 434–8. DOI:10.1111/j.1600-0773.1992.tb00503.x. PMID 1438021. 
  • Libert F, Passage E, Parmentier M, et al. (1992). „Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.“. Genomics 11 (1): 225–7. DOI:10.1016/0888-7543(91)90125-X. PMID 1662665. 
  • Martinez-Mir MI, Probst A, Palacios JM (1992). „Adenosine A2 receptors: selective localization in the human basal ganglia and alterations with disease.“. Neuroscience 42 (3): 697–706. DOI:10.1016/0306-4522(91)90038-P. PMID 1835521. 
  • Libert F, Parmentier M, Lefort A, et al. (1989). „Selective amplification and cloning of four new members of the G protein-coupled receptor family.“. Science 244 (4904): 569–72. DOI:10.1126/science.2541503. PMID 2541503. 
  • Kim J, Wess J, van Rhee AM, et al. (1995). „Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2A adenosine receptor.“. J. Biol. Chem. 270 (23): 13987–97. DOI:10.1074/jbc.270.23.13987. PMID 7775460. 
  • Szondy Z (1995). „Adenosine stimulates DNA fragmentation in human thymocytes by Ca(2+)-mediated mechanisms.“. Biochem. J.. 304 ( Pt 3): 877–85. PMC 1137415. PMID 7818494. 
  • MacCollin M, Peterfreund R, MacDonald M, et al. (1994). „Mapping of a human A2A adenosine receptor (ADORA2) to chromosome 22.“. Genomics 20 (2): 332–3. DOI:10.1006/geno.1994.1181. PMID 8020991. 
  • Nonaka H, Ichimura M, Takeda M, et al. (1994). „KF17837 ((E)-8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-methylxanthine), a potent and selective adenosine A2 receptor antagonist.“. Eur. J. Pharmacol. 267 (3): 335–41. DOI:10.1016/0922-4106(94)90159-7. PMID 8088373. 
  • Iwamoto T, Umemura S, Toya Y, et al. (1994). „Identification of adenosine A2 receptor-cAMP system in human aortic endothelial cells.“. Biochem. Biophys. Res. Commun. 199 (2): 905–10. DOI:10.1006/bbrc.1994.1314. PMID 8135838. 
  • Salmon JE, Brogle N, Brownlie C, et al. (1993). „Human mononuclear phagocytes express adenosine A1 receptors. A novel mechanism for differential regulation of Fc gamma receptor function.“. J. Immunol. 151 (5): 2775–85. PMID 8360491. 
  • Peterfreund RA, MacCollin M, Gusella J, Fink JS (1996). „Characterization and expression of the human A2A adenosine receptor gene.“. J. Neurochem. 66 (1): 362–8. DOI:10.1046/j.1471-4159.1996.66010362.x. PMID 8522976. 
  • Le F, Townsend-Nicholson A, Baker E, et al. (1996). „Characterization and chromosomal localization of the human A2A adenosine receptor gene: ADORA2A.“. Biochem. Biophys. Res. Commun. 223 (2): 461–7. DOI:10.1006/bbrc.1996.0916. PMID 8670304. 
  • Jiang Q, Van Rhee AM, Kim J, et al. (1996). „Hydrophilic side chains in the third and seventh transmembrane helical domains of human A2A adenosine receptors are required for ligand recognition.“. Mol. Pharmacol. 50 (3): 512–21. PMID 8794889. 
  • Ledent C, Vaugeois JM, Schiffmann SN, et al. (1997). „Aggressiveness, hypoalgesia and high blood pressure in mice lacking the adenosine A2A receptor.“. Nature 388 (6643): 674–8. DOI:10.1038/41771. PMID 9262401. 
  • Koshiba M, Rosin DL, Hayashi N, et al. (1999). „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.“. Mol. Pharmacol. 55 (3): 614–24. PMID 10051547. 
  • Borgland SL, Castañón M, Spevak W, Parkinson FE (1999). „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.“. Can. J. Physiol. Pharmacol. 76 (12): 1132–8. DOI:10.1139/cjpp-76-12-1132. PMID 10326835.