The adenosine A<sub>2B</sub> receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human adenosine A<sub>2b</sub> 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<sub>2B</sub> ligands has lagged somewhat behind the development of ligands for the other three adenosine receptor subtypes, but a number of A<sub>2B</sub>-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<sub>2B</sub>, 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<sub>i</sub>: 1.50 nM)
- ISAM-140: non-xanthinic selective antagonist (K<sub>i</sub> = 3.49 nM).
- ISAM-R324A: Soluble and metabolically stable non-xanthinic selective antagonist (K<sub>i</sub> = 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
External links