Adenosine GPCR Family Subtypes and Products

What Are Adenosine Receptors?

Adenosine receptors are a family of G protein-coupled receptors (GPCRs) that consist of four known receptor subtypes in humans: A1, A2A, A2B and A3. Activation of adenosine receptors with ligand adenosine and agonists and blocking with antagonists enable researchers to study the effects of stimulating and impeding individual adenosine receptor subtypes. The study of adenosine receptors is producing a new generation of compounds that have greater subtype selectivity for a potentially broader field of medical applications.

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Adenosine Receptor Information

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A1

A2A

A2B

A3

Adenosine A1 receptor (ADORA1 or RDC7) is a G protein- coupled receptor for adenosine. RT-PCR detected A1 expression in the brain, colon, jejunum, ileum and kidney. A1 functions in sleep-wake regulation, the fertilization process, and modulates coronary blood flow.
Adenosine regulates the function of the innate and adaptive immune systems through targeting virtually every cell type that is involved in orchestrating an immune/inflammatory response. Of the four adenosine receptors (A1, A2A, A2B, A3), A2A receptor is the primary anti-inflammatory effectors of extracellular adenosine. A2A receptor predominant expresses in monocytes/macrophages, dendritic cells, mast cells, neutrophils, endothelial cells, eosinophils, epithelial cells, as well as lymphocytes, NK cells, and NKT cells. Its activation inhibits early and late events occurring during an immune response. A2A receptor also participates in tissue remodeling and reparation. A2A receptor has been shown to impact the course of a wide spectrum of ischemic, autoimmune, infectious, and allergic diseases, and has regulatory roles in immune/inflammatory diseases of various organs, including heart, lung, gut, liver, kidney, joints, and brain. Recently, A2A receptor has become a particularly attractive target to manage psychiatric disorders.

Adenosine A2B receptor is upregulated during intestinal inflammation and mediates key events such as chloride, IL-6 and fibronectin secretion in intestinal epithelial cells. A2B receptor antagonists may have important clinical value in the treatment of inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), as well as inflammatory bowel disease.

Adenosine A3 receptors are involved in a variety of intracellular signaling pathways and physiological functions. They are expressed in a wide range of human tissues, but most predominantly in the lung and liver. Recent animal model studies have shown that A3 receptors play important roles in brain ischemia, immunosuppresion, and bronchospasm. A3 receptor agonists and/or agonists may have important clinical value in the treatment of asthma and inflammation.

Adenosine Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
AdenosineA1humanHEK293TC1427BDC1427BMC1427B
A1humanCHO-K1C1427-1DC1427-1MC1427-1
A1ratHEK293TCr1427DCr1427MCr1427
A2AhumanHEK293TC1428DC1428MC1428
A2AhumanCHO-K1C1428-1DC1428-1MC1428-1
A2AmouseHEK293TCm1428ADCm1428AMCm1428A
A2AmouseHEK293TCm1428BDCm1428BMCm1428B
A2AmouseCHO-K1Cm1428-1DCm1428-1MCm1428-1
A2AratHEK293TCr1428DCr1428MCr1428
A2BhumanHEK293TC1429DC1429MC1429
A2BhumanCHO-K1C1429-1DC1429-1MC1429-1
A2BhumanHEK293TC1429aDC1429aMC1429a
A2BratHEK293TCr1429DCr1429MCr1429
A3humanHEK293TC1430DC1430MC1430
A3humanCHO-K1C1430-1DC1430-1MC1430-1
A3ratHEK293TCr1430DCr1430MCr1430

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