The adenosine A
2B receptor, also known as ADORA2B, is a
G-protein coupled
G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily-related p ...
adenosine receptor
The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the endogenous ligand. There are four known types of adenosine receptors in humans: A1, A2A, A2B and A3; each is encoded by a dif ...
, and also denotes the human adenosine A
2b receptor
gene
In biology, the word gene (from , ; "... Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth'' or ''gender'') can have several different meanings. The Mendelian gene is a b ...
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-1706 is a selective inverse agonist for the adenosine
Adenosine ( symbol A) is an organic compound that occurs widely in nature in the form of diverse derivatives. The molecule consists of an adenine attached to a ribose via a β-N9-glycos ...
* 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