Adenosine A2b receptor

Adenosine A2b receptor
Identifiers
ADORA2B Gene
RNA expression pattern

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]

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:[18] antagonist, high affinity and good subtype selectivity
  • ATL-801
  • CVT-6883
  • MRS-1706
  • MRS-1754
  • OSIP-339,391
  • PSB-603
  • PSB-0788
  • PSB-1115

References

External links

Further reading

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