Adenosine A2B receptor: Difference between revisions

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==Ligands==
==Ligands==
Research into selective A<sub>2B</sub> ligands has lagged somewhat behind the development of ligands for the other three adenosine receptor subtypes, but a number of A<sub>2B</sub>-selective compounds have now been developed,<ref name="pmid12109910">{{cite journal | vauthors = Volpini R, Costanzi S, Lambertucci C, Taffi S, Vittori S, Klotz KN, Cristalli G | title = N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands | journal = Journal of Medicinal Chemistry | volume = 45 | issue = 15 | pages = 3271–9 |date=July 2002| pmid = 12109910 | doi = 10.1021/jm0109762| issn = }}</ref><ref name="pmid12369946">{{cite journal | vauthors = Volpini R, Costanzi S, Lambertucci C, Vittori S, Cristalli G | title = Purine nucleosides bearing 1-alkynyl chains as adenosine receptor agonists | journal = Current Pharmaceutical Design | volume = 8 | issue = 26 | pages = 2285–98 | year = 2002 | pmid = 12369946 | doi = 10.2174/1381612023392856| url = http://www.bentham-direct.org/pages/content.php?CPD/2002/00000008/00000026/0002B.SGM | issn = }}</ref><ref name="pmid14998332">{{cite journal | vauthors = Baraldi PG, Tabrizi MA, Preti D, Bovero A, Romagnoli R, Fruttarolo F, Zaid NA, Moorman AR, Varani K, Gessi S, Merighi S, Borea PA | title = Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists | journal = Journal of Medicinal Chemistry | volume = 47 | issue = 6 | pages = 1434–47 |date=March 2004| pmid = 14998332 | doi = 10.1021/jm0309654 | url = | issn = }}</ref><ref name="pmid16375751">{{cite journal | vauthors = Cacciari B, Pastorin G, Bolcato C, Spalluto G, Bacilieri M, Moro S | title = A2B adenosine receptor antagonists: recent developments | journal = Mini Reviews in Medicinal Chemistry | volume = 5 | issue = 12 | pages = 1053–60 |date=December 2005| pmid = 16375751 | doi = 10.2174/138955705774933374| url = http://www.bentham-direct.org/pages/content.php?MRMC/2005/00000005/00000012/0001N.SGM | issn = }}</ref><ref name="pmid17168717">{{cite journal | vauthors = Baraldi PG, Romagnoli R, Preti D, Fruttarolo F, Carrion MD, Tabrizi MA | title = Ligands for A2B adenosine receptor subtype | journal = Current Medicinal Chemistry | volume = 13 | issue = 28 | pages = 3467–82 | year = 2006 | pmid = 17168717 | doi = 10.2174/092986706779010306| url = http://www.bentham-direct.org/pages/content.php?CMC/2006/00000013/00000028/0008C.SGM | issn = }}</ref><ref name="pmid16847822">{{cite journal | vauthors = Beukers MW, Meurs I, Ijzerman AP | title = Structure-affinity relationships of adenosine A2B receptor ligands | journal = Medicinal Research Reviews | volume = 26 | issue = 5 | pages = 667–98 |date=September 2006| pmid = 16847822 | doi = 10.1002/med.20069 | url = | issn = }}</ref><ref name="pmid16275090">{{cite journal | vauthors = Elzein E, Kalla R, Li X, Perry T, Parkhill E, Palle V, Varkhedkar V, Gimbel A, Zeng D, Lustig D, Leung K, Zablocki J | title = Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists | journal = Bioorganic & Medicinal Chemistry Letters | volume = 16 | issue = 2 | pages = 302–6 |date=January 2006| pmid = 16275090 | doi = 10.1016/j.bmcl.2005.10.002 | url = | issn = }}</ref><ref name="pmid16392813">{{cite journal | vauthors = Carotti A, Cadavid MI, Centeno NB, Esteve C, Loza MI, Martinez A, Nieto R, Raviña E, Sanz F, Segarra V, Sotelo E, Stefanachi A, Vidal B | title = Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor | journal = Journal of Medicinal Chemistry | volume = 49 | issue = 1 | pages = 282–99 |date=January 2006| pmid = 16392813 | doi = 10.1021/jm0506221 | url = | issn = }}</ref><ref name="pmid18077171">{{cite journal | vauthors = Tabrizi MA, Baraldi PG, Preti D, Romagnoli R, Saponaro G, Baraldi S, Moorman AR, Zaid AN, Varani K, Borea PA | title = 1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists | journal = Bioorganic & Medicinal Chemistry | volume = 16 | issue = 5 | pages = 2419–30 |date=March 2008| pmid = 18077171 | doi = 10.1016/j.bmc.2007.11.058 | url = | issn = }}</ref><ref name="pmid18226909">{{cite journal | vauthors = Stefanachi A, Brea JM, Cadavid MI, Centeno NB, Esteve C, Loza MI, Martinez A, Nieto R, Raviña E, Sanz F, Segarra V, Sotelo E, Vidal B, Carotti A | title = 1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A2B adenosine receptor | journal = Bioorganic & Medicinal Chemistry | volume = 16 | issue = 6 | pages = 2852–69 |date=March 2008| pmid = 18226909 | doi = 10.1016/j.bmc.2008.01.002 | url = | issn = }}</ref> and research into their potential therapeutic applications is ongoing.<ref name="pmid12570760">{{cite journal | vauthors = Volpini R, Costanzi S, Vittori S, Cristalli G, Klotz KN | title = Medicinal chemistry and pharmacology of A2B adenosine receptors | journal = Current Topics in Medicinal Chemistry | volume = 3 | issue = 4 | pages = 427–43 | year = 2003 | pmid = 12570760 | doi = 10.2174/1568026033392264| url = http://www.bentham-direct.org/pages/content.php?CTMC/2003/00000003/00000004/0007R.SGM | issn = }}</ref><ref name="pmid17874974">{{cite journal | vauthors = Gao ZG, Jacobson KA | title = Emerging adenosine receptor agonists | journal = Expert Opinion on Emerging Drugs | volume = 12 | issue = 3 | pages = 479–92 |date=September 2007| pmid = 17874974 | doi = 10.1517/14728214.12.3.479 | url = | issn = }}</ref><ref name="pmid18536750">{{cite journal | vauthors = Kolachala V, Ruble B, Vijay-Kumar M, Wang L, Mwangi S, Figler H, Figler R, Srinivasan S, Gewirtz A, Linden J, Merlin D, Sitaraman S | title = Blockade of adenosine A2B receptors ameliorates murine colitis | journal = British Journal of Pharmacology | volume = 155 | issue = 1 | pages = 127–37 |date=September 2008| pmid = 18536750 | pmc = 2440087 | doi = 10.1038/bjp.2008.227 | url = | issn = }}</ref><ref name="pmid18758473">{{cite journal | vauthors = Haskó G, Linden J, Cronstein B, Pacher P | title = Adenosine receptors: therapeutic aspects for inflammatory and immune diseases | journal = Nature Reviews Drug Discovery | volume = 7 | issue = 9 | pages = 759–70 |date=September 2008| pmid = 18758473 | pmc = 2568887 | doi = 10.1038/nrd2638 | url = | issn = }}</ref><ref name="pmid19075778">{{cite journal | vauthors = Ham J, Rees DA | title = The adenosine a2b receptor: its role in inflammation | journal = Endocrine, Metabolic & Immune Disorders Drug Targets | volume = 8 | issue = 4 | pages = 244–54 |date=December 2008| pmid = 19075778 | doi = 10.2174/187153008786848303| url = http://www.bentham-direct.org/pages/content.php?EMIDDT/2008/00000008/00000004/0003V.SGM | issn = }}</ref><ref name="pmid19194991">{{cite journal | vauthors = Kim MO, Kim MH, Lee SH, Suh HN, Lee YJ, Lee MY, Han HJ | title = 5'-N-ethylcarboxamide induces IL-6 expression via MAPKs and NF-kappaB activation through Akt, Ca(2+)/PKC, cAMP signaling pathways in mouse embryonic stem cells | journal = Journal of Cellular Physiology | volume = 219 | issue = 3 | pages = 752–9 |date=June 2009| pmid = 19194991 | doi = 10.1002/jcp.21721 | url = | issn = }}</ref>
Research into selective A<sub>2B</sub> ligands has lagged somewhat behind the development of ligands for the other three adenosine receptor subtypes, but a number of A<sub>2B</sub>-selective compounds have now been developed,<ref name="pmid12109910">{{cite journal | vauthors = Volpini R, Costanzi S, Lambertucci C, Taffi S, Vittori S, Klotz KN, Cristalli G | title = N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands | journal = Journal of Medicinal Chemistry | volume = 45 | issue = 15 | pages = 3271–9 |date=July 2002| pmid = 12109910 | doi = 10.1021/jm0109762| issn = }}</ref><ref name="pmid12369946">{{cite journal | vauthors = Volpini R, Costanzi S, Lambertucci C, Vittori S, Cristalli G | title = Purine nucleosides bearing 1-alkynyl chains as adenosine receptor agonists | journal = Current Pharmaceutical Design | volume = 8 | issue = 26 | pages = 2285–98 | year = 2002 | pmid = 12369946 | doi = 10.2174/1381612023392856 | url = http://www.bentham-direct.org/pages/content.php?CPD/2002/00000008/00000026/0002B.SGM | archive-url = https://archive.is/20130414131152/http://www.bentham-direct.org/pages/content.php?CPD/2002/00000008/00000026/0002B.SGM | dead-url = yes | archive-date = 2013-04-14 | issn =  }}</ref><ref name="pmid14998332">{{cite journal | vauthors = Baraldi PG, Tabrizi MA, Preti D, Bovero A, Romagnoli R, Fruttarolo F, Zaid NA, Moorman AR, Varani K, Gessi S, Merighi S, Borea PA | title = Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists | journal = Journal of Medicinal Chemistry | volume = 47 | issue = 6 | pages = 1434–47 |date=March 2004| pmid = 14998332 | doi = 10.1021/jm0309654 | url = | issn = }}</ref><ref name="pmid16375751">{{cite journal | vauthors = Cacciari B, Pastorin G, Bolcato C, Spalluto G, Bacilieri M, Moro S | title = A2B adenosine receptor antagonists: recent developments | journal = Mini Reviews in Medicinal Chemistry | volume = 5 | issue = 12 | pages = 1053–60 | date = December 2005 | pmid = 16375751 | doi = 10.2174/138955705774933374 | url = http://www.bentham-direct.org/pages/content.php?MRMC/2005/00000005/00000012/0001N.SGM | archive-url = https://archive.is/20130414141112/http://www.bentham-direct.org/pages/content.php?MRMC/2005/00000005/00000012/0001N.SGM | dead-url = yes | archive-date = 2013-04-14 | issn = }}</ref><ref name="pmid17168717">{{cite journal | vauthors = Baraldi PG, Romagnoli R, Preti D, Fruttarolo F, Carrion MD, Tabrizi MA | title = Ligands for A2B adenosine receptor subtype | journal = Current Medicinal Chemistry | volume = 13 | issue = 28 | pages = 3467–82 | year = 2006 | pmid = 17168717 | doi = 10.2174/092986706779010306 | url = http://www.bentham-direct.org/pages/content.php?CMC/2006/00000013/00000028/0008C.SGM | archive-url = https://archive.is/20130414075418/http://www.bentham-direct.org/pages/content.php?CMC/2006/00000013/00000028/0008C.SGM | dead-url = yes | archive-date = 2013-04-14 | issn = }}</ref><ref name="pmid16847822">{{cite journal | vauthors = Beukers MW, Meurs I, Ijzerman AP | title = Structure-affinity relationships of adenosine A2B receptor ligands | journal = Medicinal Research Reviews | volume = 26 | issue = 5 | pages = 667–98 |date=September 2006| pmid = 16847822 | doi = 10.1002/med.20069 | url = | issn = }}</ref><ref name="pmid16275090">{{cite journal | vauthors = Elzein E, Kalla R, Li X, Perry T, Parkhill E, Palle V, Varkhedkar V, Gimbel A, Zeng D, Lustig D, Leung K, Zablocki J | title = Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists | journal = Bioorganic & Medicinal Chemistry Letters | volume = 16 | issue = 2 | pages = 302–6 |date=January 2006| pmid = 16275090 | doi = 10.1016/j.bmcl.2005.10.002 | url = | issn = }}</ref><ref name="pmid16392813">{{cite journal | vauthors = Carotti A, Cadavid MI, Centeno NB, Esteve C, Loza MI, Martinez A, Nieto R, Raviña E, Sanz F, Segarra V, Sotelo E, Stefanachi A, Vidal B | title = Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor | journal = Journal of Medicinal Chemistry | volume = 49 | issue = 1 | pages = 282–99 |date=January 2006| pmid = 16392813 | doi = 10.1021/jm0506221 | url = | issn = }}</ref><ref name="pmid18077171">{{cite journal | vauthors = Tabrizi MA, Baraldi PG, Preti D, Romagnoli R, Saponaro G, Baraldi S, Moorman AR, Zaid AN, Varani K, Borea PA | title = 1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists | journal = Bioorganic & Medicinal Chemistry | volume = 16 | issue = 5 | pages = 2419–30 |date=March 2008| pmid = 18077171 | doi = 10.1016/j.bmc.2007.11.058 | url = | issn = }}</ref><ref name="pmid18226909">{{cite journal | vauthors = Stefanachi A, Brea JM, Cadavid MI, Centeno NB, Esteve C, Loza MI, Martinez A, Nieto R, Raviña E, Sanz F, Segarra V, Sotelo E, Vidal B, Carotti A | title = 1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A2B adenosine receptor | journal = Bioorganic & Medicinal Chemistry | volume = 16 | issue = 6 | pages = 2852–69 |date=March 2008| pmid = 18226909 | doi = 10.1016/j.bmc.2008.01.002 | url = | issn = }}</ref> and research into their potential therapeutic applications is ongoing.<ref name="pmid12570760">{{cite journal | vauthors = Volpini R, Costanzi S, Vittori S, Cristalli G, Klotz KN | title = Medicinal chemistry and pharmacology of A2B adenosine receptors | journal = Current Topics in Medicinal Chemistry | volume = 3 | issue = 4 | pages = 427–43 | year = 2003 | pmid = 12570760 | doi = 10.2174/1568026033392264 | url = http://www.bentham-direct.org/pages/content.php?CTMC/2003/00000003/00000004/0007R.SGM | archive-url = https://archive.is/20130414065741/http://www.bentham-direct.org/pages/content.php?CTMC/2003/00000003/00000004/0007R.SGM | dead-url = yes | archive-date = 2013-04-14 | issn = }}</ref><ref name="pmid17874974">{{cite journal | vauthors = Gao ZG, Jacobson KA | title = Emerging adenosine receptor agonists | journal = Expert Opinion on Emerging Drugs | volume = 12 | issue = 3 | pages = 479–92 |date=September 2007| pmid = 17874974 | doi = 10.1517/14728214.12.3.479 | url = | issn = }}</ref><ref name="pmid18536750">{{cite journal | vauthors = Kolachala V, Ruble B, Vijay-Kumar M, Wang L, Mwangi S, Figler H, Figler R, Srinivasan S, Gewirtz A, Linden J, Merlin D, Sitaraman S | title = Blockade of adenosine A2B receptors ameliorates murine colitis | journal = British Journal of Pharmacology | volume = 155 | issue = 1 | pages = 127–37 |date=September 2008| pmid = 18536750 | pmc = 2440087 | doi = 10.1038/bjp.2008.227 | url = | issn = }}</ref><ref name="pmid18758473">{{cite journal | vauthors = Haskó G, Linden J, Cronstein B, Pacher P | title = Adenosine receptors: therapeutic aspects for inflammatory and immune diseases | journal = Nature Reviews Drug Discovery | volume = 7 | issue = 9 | pages = 759–70 |date=September 2008| pmid = 18758473 | pmc = 2568887 | doi = 10.1038/nrd2638 | url = | issn = }}</ref><ref name="pmid19075778">{{cite journal | vauthors = Ham J, Rees DA | title = The adenosine a2b receptor: its role in inflammation | journal = Endocrine, Metabolic & Immune Disorders Drug Targets | volume = 8 | issue = 4 | pages = 244–54 | date = December 2008 | pmid = 19075778 | doi = 10.2174/187153008786848303 | url = http://www.bentham-direct.org/pages/content.php?EMIDDT/2008/00000008/00000004/0003V.SGM | archive-url = https://archive.is/20130414105722/http://www.bentham-direct.org/pages/content.php?EMIDDT/2008/00000008/00000004/0003V.SGM | dead-url = yes | archive-date = 2013-04-14 | issn = }}</ref><ref name="pmid19194991">{{cite journal | vauthors = Kim MO, Kim MH, Lee SH, Suh HN, Lee YJ, Lee MY, Han HJ | title = 5'-N-ethylcarboxamide induces IL-6 expression via MAPKs and NF-kappaB activation through Akt, Ca(2+)/PKC, cAMP signaling pathways in mouse embryonic stem cells | journal = Journal of Cellular Physiology | volume = 219 | issue = 3 | pages = 752–9 |date=June 2009| pmid = 19194991 | doi = 10.1002/jcp.21721 | url = | issn = }}</ref>


===Agonists===
===Agonists===
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*{{cite journal  | author=Stiles GL |title=Adenosine receptors. |journal=J. Biol. Chem. |volume=267 |issue= 10 |pages= 6451–4 |year= 1992 |pmid= 1551861 |doi=  }}
*{{cite journal  | author=Stiles GL |title=Adenosine receptors. |journal=J. Biol. Chem. |volume=267 |issue= 10 |pages= 6451–4 |year= 1992 |pmid= 1551861 |doi=  }}
*{{cite journal  | vauthors=Pierce KD, Furlong TJ, Selbie LA, Shine J |title=Molecular cloning and expression of an adenosine A2b receptor from human brain. |journal=Biochem. Biophys. Res. Commun. |volume=187 |issue= 1 |pages= 86–93 |year= 1992 |pmid= 1325798 |doi=10.1016/S0006-291X(05)81462-7  }}
*{{cite journal  | vauthors=Pierce KD, Furlong TJ, Selbie LA, Shine J |title=Molecular cloning and expression of an adenosine A2b receptor from human brain. |journal=Biochem. Biophys. Res. Commun. |volume=187 |issue= 1 |pages= 86–93 |year= 1992 |pmid= 1325798 |doi=10.1016/S0006-291X(05)81462-7  }}
*{{cite journal  | vauthors=Li Q, Han X, Lan X, Hong X, Li Q, Gao Y, Luo T, Yang Q, Koehler RC, Zhai Y, Zhou J, Wang J |title=Inhibition of tPA-induced hemorrhagic transformation involves adenosine A2b receptor activation after cerebral ischemia. |journal=Neurobiology of disease |volume=108 |pages= 173–182 |year= 2017 |pmid= 28830843 |doi= 10.1016/j.nbd.2017.08.011 }}
*{{cite journal  | vauthors=Li Q, Han X, Lan X, Hong X, Li Q, Gao Y, Luo T, Yang Q, Koehler RC, Zhai Y, Zhou J, Wang J |title=Inhibition of tPA-induced hemorrhagic transformation involves adenosine A2b receptor activation after cerebral ischemia. |journal=Neurobiology of Disease |volume=108 |pages= 173–182 |year= 2017 |pmid= 28830843 |doi= 10.1016/j.nbd.2017.08.011 |pmc=5675803}}
*{{cite journal  | vauthors=Jacobson MA, Johnson RG, Luneau CJ, Salvatore CA |title=Cloning and chromosomal localization of the human A2b adenosine receptor gene (ADORA2B) and its pseudogene. |journal=Genomics |volume=27 |issue= 2 |pages= 374–6 |year= 1995 |pmid= 7558011 |doi= 10.1006/geno.1995.1061 }}
*{{cite journal  | vauthors=Jacobson MA, Johnson RG, Luneau CJ, Salvatore CA |title=Cloning and chromosomal localization of the human A2b adenosine receptor gene (ADORA2B) and its pseudogene. |journal=Genomics |volume=27 |issue= 2 |pages= 374–6 |year= 1995 |pmid= 7558011 |doi= 10.1006/geno.1995.1061 }}
*{{cite journal  | vauthors=Townsend-Nicholson A, Baker E, Sutherland GR, Schofield PR |title=Localization of the adenosine A2b receptor subtype gene (ADORA2B) to chromosome 17p11.2-p12 by FISH and PCR screening of somatic cell hybrids. |journal=Genomics |volume=25 |issue= 2 |pages= 605–7 |year= 1995 |pmid= 7790006 |doi=10.1016/0888-7543(95)80074-V  }}
*{{cite journal  | vauthors=Townsend-Nicholson A, Baker E, Sutherland GR, Schofield PR |title=Localization of the adenosine A2b receptor subtype gene (ADORA2B) to chromosome 17p11.2-p12 by FISH and PCR screening of somatic cell hybrids. |journal=Genomics |volume=25 |issue= 2 |pages= 605–7 |year= 1995 |pmid= 7790006 |doi=10.1016/0888-7543(95)80074-V  }}
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==External links==
==External links==
* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2170 | title = Adenosine Receptors: A<sub>2B</sub>  | accessdate = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }}
* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2170 | title = Adenosine Receptors: A<sub>2B</sub>  | accessdate = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | quote = }}
* {{UCSC gene info|ADORA2B}}
* {{UCSC gene info|ADORA2B}}
{{G protein-coupled receptors}}
{{G protein-coupled receptors}}

Latest revision as of 02:59, 16 November 2018

VALUE_ERROR (nil)
Identifiers
Aliases
External IDsGeneCards: [1]
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

n/a

n/a

RefSeq (protein)

n/a

n/a

Location (UCSC)n/an/a
PubMed searchn/an/a
Wikidata
View/Edit Human

The adenosine A2B receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human adenosine A2b receptor gene which encodes it.[1]

Mechanism

This integral membrane protein stimulates adenylate cyclase activity in the presence of adenosine. This protein also interacts with netrin-1, which is involved in axon elongation.

Gene

The gene is located near the Smith-Magenis syndrome region on chromosome 17.[1]

Ligands

Research into selective A2B ligands has lagged somewhat behind the development of ligands for the other three adenosine receptor subtypes, but a number of A2B-selective compounds have now been developed,[2][3][4][5][6][7][8][9][10][11] and research into their potential therapeutic applications is ongoing.[12][13][14][15][16][17]

Agonists

  • BAY 60-6583
  • NECA (N-ethylcarboxamidoadenosine)
  • (S)-PHPNECA - high affinity and efficacy at A2B, but poor selectivity over other adenosine receptor subtypes
  • LUF-5835
  • LUF-5845 - partial agonist

Antagonists and inverse agonists

  • Compound 38:[18] antagonist, high affinity and good subtype selectivity
  • ATL-801
  • CVT-6883
  • MRS-1706
  • MRS-1754
  • OSIP-339,391
  • PSB-603
  • PSB-0788
  • PSB-1115

References

  1. 1.0 1.1 "Entrez Gene: ADORA2B adenosine A2b receptor".
  2. Volpini R, Costanzi S, Lambertucci C, Taffi S, Vittori S, Klotz KN, Cristalli G (July 2002). "N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands". Journal of Medicinal Chemistry. 45 (15): 3271–9. doi:10.1021/jm0109762. PMID 12109910.
  3. Volpini R, Costanzi S, Lambertucci C, Vittori S, Cristalli G (2002). "Purine nucleosides bearing 1-alkynyl chains as adenosine receptor agonists". Current Pharmaceutical Design. 8 (26): 2285–98. doi:10.2174/1381612023392856. PMID 12369946. Archived from the original on 2013-04-14.
  4. Baraldi PG, Tabrizi MA, Preti D, Bovero A, Romagnoli R, Fruttarolo F, Zaid NA, Moorman AR, Varani K, Gessi S, Merighi S, Borea PA (March 2004). "Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists". Journal of Medicinal Chemistry. 47 (6): 1434–47. doi:10.1021/jm0309654. PMID 14998332.
  5. Cacciari B, Pastorin G, Bolcato C, Spalluto G, Bacilieri M, Moro S (December 2005). "A2B adenosine receptor antagonists: recent developments". Mini Reviews in Medicinal Chemistry. 5 (12): 1053–60. doi:10.2174/138955705774933374. PMID 16375751. Archived from the original on 2013-04-14.
  6. Baraldi PG, Romagnoli R, Preti D, Fruttarolo F, Carrion MD, Tabrizi MA (2006). "Ligands for A2B adenosine receptor subtype". Current Medicinal Chemistry. 13 (28): 3467–82. doi:10.2174/092986706779010306. PMID 17168717. Archived from the original on 2013-04-14.
  7. Beukers MW, Meurs I, Ijzerman AP (September 2006). "Structure-affinity relationships of adenosine A2B receptor ligands". Medicinal Research Reviews. 26 (5): 667–98. doi:10.1002/med.20069. PMID 16847822.
  8. Elzein E, Kalla R, Li X, Perry T, Parkhill E, Palle V, Varkhedkar V, Gimbel A, Zeng D, Lustig D, Leung K, Zablocki J (January 2006). "Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists". Bioorganic & Medicinal Chemistry Letters. 16 (2): 302–6. doi:10.1016/j.bmcl.2005.10.002. PMID 16275090.
  9. Carotti A, Cadavid MI, Centeno NB, Esteve C, Loza MI, Martinez A, Nieto R, Raviña E, Sanz F, Segarra V, Sotelo E, Stefanachi A, Vidal B (January 2006). "Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor". Journal of Medicinal Chemistry. 49 (1): 282–99. doi:10.1021/jm0506221. PMID 16392813.
  10. Tabrizi MA, Baraldi PG, Preti D, Romagnoli R, Saponaro G, Baraldi S, Moorman AR, Zaid AN, Varani K, Borea PA (March 2008). "1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists". Bioorganic & Medicinal Chemistry. 16 (5): 2419–30. doi:10.1016/j.bmc.2007.11.058. PMID 18077171.
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Further reading

External links