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.

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.

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, and research into their potential therapeutic applications is ongoing.

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: antagonist, high affinity and good subtype selectivity
* ISAM-R56A: non-xanthinic high affinity selective antagonist (K_''i'': 1.50 nM)
* ISAM-140: non-xanthinic selective antagonist (K_''i'' = 3.49 nM).
* ISAM-R324A: 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: xanthinic antagonist with picomolar potency

References

Further reading

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External links

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{{Adenosinergics

Adenosine receptors