Adenosine GPCR Assays

Background of Adenosine Receptors

Adenosine receptors (AR) are a family of G-protein coupled receptor that has adenosine as its endogenous ligand and can be found in nearly all human tissues and organs. They are known to play a role in a wide range of physiopathological responses, including vasodilation, pain, and inflammation. In particular, adenosine acts as a neuromodulator in the central nervous system (CNS), with varied actions depending on the type of AR and subsequent cellular signaling involved.

Fig. 1 Structure of the human adenosine A1 receptor.¹ (PDB: 5UEN)

Distribution and Function of Adenosine Receptors

AR are found in nearly every organ and tissue, including the brain, heart, lungs, liver, kidney, bone, eye, skin, joints, and blood cells, implying that these proteins have the capacity to affect nearly every physiological function. This wide range of locations reflects the multitude of physiological effects orchestrated by it, including neurotransmitter inhibition, sedation, anticonvulsant, anxiolytic, analgesia, and regulation of sleep.

Subtypes and Mechanism of Adenosine Receptors

The A1, A2A, A2B, and A3 receptors are the four members of the AR family. A1 and A3 receptors inhibit adenylyl cyclase (AC) through G_i/G_o proteins, while A2A and A2B receptors stimulate it through G_s proteins.

Assay List of Adenosine Receptors

Creative Biolabs can provide a range of assays of adenosine receptors. You can choose the assay in the list or contact us for more information:

Published Data

References

1. Glukhova, A.; et al. Structure of the adenosine A1 receptor reveals the basis for subtype selectivity. Cell. 2017, 168(5): 867-877. e13.
2. Wall, M.J.; et al. Selective activation of Gαob by an adenosine A1 receptor agonist elicits analgesia without cardiorespiratory depression. Nature communications. 2022, 13(1): 1-22.