The adenosine A
2B receptor, also known as ADORA2B, is a
G-protein coupled 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 di ...
, 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 ba ...
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
A bay is a recessed, coastal body of water that directly connects to a larger main body of water, such as an ocean, a lake, or another bay. A large bay is usually called a gulf, sea, sound, or bight. A cove is a small, circular bay with a narr ...
* 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
ISAM-140 is a selective non- xanthinic adenosine A2B receptor atagonist. Discovered in 2016, has a K''i'' of 3.49 nM in A2B receptor and >1000-fold selectivity with respect to the other three adenosine receptor subtypes. It has been shown to ...
: 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 A2B receptor. It inhibits release of interleukin
Interleukins (ILs) are a group of cytokines (secreted proteins and signal molecules) that are expressed and secreted by white blood cel ...
* 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