Adenosine A3 receptor

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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 potencial in bronchial asthma (17,18).

Gene

Multiple transcript variants encoding different isoforms have been found for this gene.[1]

Therapeutic implications

An adenosine A3 receptor agonist (CF-101) is in clinical trials for the treatment of rheumatoid arthritis.[2] In a mouse model of infarction the A3 selective agonist CP-532,903 protected against myocardial ischemia and reperfusion injury.[3]

Selective Ligands

A number of selective A3 ligands are available.[4][5][6][7][8][9][10][11][12][13][14][15]

Agonists/Positive Allosteric Modulators

  • 2-(1-Hexynyl)-N-methyladenosine
  • CF-101 (IB-MECA)
  • CF-102
  • 2-Cl-IB-MECA
  • CP-532,903
  • Inosine[16]
  • LUF-6000
  • MRS-3558

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[17][18]

Inverse Agonists

References

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  16. Xiaowei Jin, Rebecca K. Shepherd, Brian R. Duling, and Joel Linden. "Inosine Binds to A3 Adenosine Receptors and Stimulates Mast Cell Degranulation"
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Further reading

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External links

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