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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A2A

A2B

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 Family	Receptor	Species	Parental	Stable Cell Lines	Division-Arrested Cells	Membranes
Adenosine	A1	human	HEK293T	C1427B	DC1427B	MC1427B
	A1	human	CHO-K1	C1427-1	DC1427-1	MC1427-1
	A1	rat	HEK293T	Cr1427	DCr1427	MCr1427
	A2A	human	HEK293T	C1428	DC1428	MC1428
	A2A	human	CHO-K1	C1428-1	DC1428-1	MC1428-1
	A2A	mouse	HEK293T	Cm1428A	DCm1428A	MCm1428A
	A2A	mouse	HEK293T	Cm1428B	DCm1428B	MCm1428B
	A2A	mouse	CHO-K1	Cm1428-1	DCm1428-1	MCm1428-1
	A2A	rat	HEK293T	Cr1428	DCr1428	MCr1428
	A2B	human	HEK293T	C1429	DC1429	MC1429
	A2B	human	CHO-K1	C1429-1	DC1429-1	MC1429-1
	A2B	human	HEK293T	C1429a	DC1429a	MC1429a
	A2B	rat	HEK293T	Cr1429	DCr1429	MCr1429
	A3	human	HEK293T	C1430	DC1430	MC1430
	A3	human	CHO-K1	C1430-1	DC1430-1	MC1430-1
	A3	rat	HEK293T	Cr1430	DCr1430	MCr1430