Adenosine A2B receptor
Template:Cs1 config Template:Short description
Template:Infobox gene The adenosine A2B receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human adenosine A2b receptor gene which encodes it.[1]
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.[1]
Ligands
Research into selective A2B ligands has lagged somewhat behind the development of ligands for the other three adenosine receptor subtypes, but a number of A2B-selective compounds have now been developed,[2][3][4][5][6][7][8][9][10][11] and research into their potential therapeutic applications is ongoing.[12][13][14][15][16][17][18]
Agonists
- BAY 60-6583
- NECA (N-ethylcarboxamidoadenosine)
- (S)-PHPNECA - high affinity and efficacy at A2B, but poor selectivity over other adenosine receptor subtypes
- LUF-5835
- LUF-5845 - partial agonist
Antagonists and inverse agonists
- Compound 38:[19] antagonist, high affinity and good subtype selectivity
- ISAM-R56A:[18] non-xanthinic high affinity selective antagonist (Ki: 1.50 nM)
- ISAM-140:[20] non-xanthinic selective antagonist (Ki = 3.49 nM).
- ISAM-R324A:[21] Soluble and metabolically stable non-xanthinic selective antagonist (Ki = 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:[22] xanthinic antagonist with picomolar potency
References
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Further reading
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External links
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