Adenosine A3 receptor
The adenosine A3 receptor, also known as ADORA3, is an adenosine receptor, but also denotes the human gene encoding it.
Function
Adenosine A3 receptors are G protein-coupled receptors that couple to Gi/Gq and are involved in a variety of intracellular signaling pathways and physiological functions. It mediates a sustained cardioprotective function during cardiac ischemia, it is involved in the inhibition of neutrophil degranulation in neutrophil-mediated tissue injury, it has been implicated in both neuroprotective and neurodegenerative effects, and it may also mediate both cell proliferation and cell death[citation needed]. Recent publications demonstrate that adenosine A3 receptor antagonists (SSR161421) could have therapeutic potential in bronchial asthma (17,18).
Gene
Multiple transcript variants encoding different isoforms have been found for this gene.[5]
Therapeutic implications
An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthritis.[6] In a mouse model of infarction the A3 selective agonist CP-532,903 protected against myocardial ischemia and reperfusion injury.[7]
Selective Ligands
A number of selective A3 ligands are available.[8][9][10][11][12][13][14][15][16][17][18][19][20]
Agonists/Positive Allosteric Modulators
- 2-(1-Hexynyl)-N-methyladenosine
- CF-101 (IB-MECA)
- CF-102
- 2-Cl-IB-MECA
- CP-532,903
- Inosine[21]
- LUF-6000[22]
- MRS-3558
- AST-004
Antagonists/Negative Allosteric Modulators
- KF-26777
- MRS-545
- MRS-1191
- MRS-1220
- MRS-1334
- MRS-1523
- MRS-3777
- MRE-3005-F20
- MRE-3008-F20
- PSB-11
- OT-7999
- VUF-5574
- SSR161421[23][24]
- ISAM-DM10
Inverse Agonists
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