Adenosine A2B receptor

The adenosine A_2B receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human adenosine A_2b receptor gene which encodes it.^[5]

ADORA2B
Identifiers
Aliases	ADORA2B, ADORA2, adenosine A2b receptor
External IDs	OMIM: 600446; MGI: 99403; HomoloGene: 20167; GeneCards: ADORA2B; OMA:ADORA2B - orthologs
Gene location (Human) Chr. Chromosome 17 (human)[1] Band 17p12 Start 15,945,130 bp[1] End 15,975,746 bp[1]
Gene location (Mouse) Chr. Chromosome 11 (mouse)[2] Band 11|11 B2 Start 62,139,810 bp[2] End 62,157,279 bp[2]
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in mucosa of transverse colon bronchial epithelial cell retinal pigment epithelium mucosa of sigmoid colon gonad olfactory zone of nasal mucosa mucosa of paranasal sinus nasal epithelium skin of thigh testicle Top expressed in gastrula retinal pigment epithelium yolk sac corneal stroma Epithelium of choroid plexus decidua otic placode lumbar subsegment of spinal cord embryo primary oocyte More reference expression data BioGPS More reference expression data
Gene ontology Molecular function G protein-coupled adenosine receptor activity G protein-coupled receptor activity signal transducer activity Cellular component integral component of membrane membrane plasma membrane integral component of plasma membrane intracellular anatomical structure synapse Schaffer collateral - CA1 synapse glutamatergic synapse Biological process cellular response to extracellular stimulus positive regulation of chronic inflammatory response to non-antigenic stimulus G protein-coupled receptor signaling pathway G protein-coupled adenosine receptor signaling pathway excretion positive regulation of guanylate cyclase activity adenylate cyclase-activating G protein-coupled receptor signaling pathway positive regulation of mast cell degranulation activation of adenylate cyclase activity cellular defense response JNK cascade positive regulation of interleukin-6 production relaxation of vascular associated smooth muscle positive regulation of chemokine production positive regulation of vascular endothelial growth factor production signal transduction positive regulation of cGMP-mediated signaling regulation of synaptic vesicle exocytosis Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 136 11541 Ensembl ENSG00000170425 ENSMUSG00000018500 UniProt P29275 Q60614 RefSeq (mRNA) NM_000676 NM_007413 RefSeq (protein) NP_000667 NP_031439 Location (UCSC) Chr 17: 15.95 – 15.98 Mb Chr 11: 62.14 – 62.16 Mb PubMed search [3] [4]
Wikidata
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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.^[5]

Ligands

Research into selective A_2B ligands has lagged somewhat behind the development of ligands for the other three adenosine receptor subtypes, but a number of A_2B-selective compounds have now been developed,^{[6][7][8][9][10][11][12][13][14][15]} and research into their potential therapeutic applications is ongoing.^{[16][17][18][19][20][21][22]}

Agonists

• BAY 60-6583
• NECA (N-ethylcarboxamidoadenosine)
• (S)-PHPNECA - high affinity and efficacy at A_2B, but poor selectivity over other adenosine receptor subtypes
• LUF-5835
• LUF-5845 - partial agonist

Antagonists and inverse agonists

• Compound 38:^[23] antagonist, high affinity and good subtype selectivity
• ISAM-R56A:^[22] non-xanthinic high affinity selective antagonist (K_i: 1.50 nM)
• ISAM-140:^[24] non-xanthinic selective antagonist (K_i = 3.49 nM).
• ISAM-R324A:^[25] Soluble and metabolically stable non-xanthinic selective antagonist (K_i = 6.10 nM).
• ATL-801
• CVT-6883
• MRS-1706
• MRS-1754
• OSIP-339,391
• PSB-603: xanthinic antagonist
• PSB-0788: xanthinic antagonist
• PSB-1115: xanthinic antagonist
• PSB-1901:^[26] xanthinic antagonist with picomolar potency