Adenosine_A2B_receptor

Adenosine A<sub>2B</sub> receptor

Adenosine A2B receptor

Cell surface receptor found in humans

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.[5]

Quick Facts ADORA2B, Identifiers ...

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.[5]

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,[6][7][8][9][10][11][12][13][14][15] and research into their potential therapeutic applications is ongoing.[16][17][18][19][20][21][22]

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:[23] antagonist, high affinity and good subtype selectivity
  • ISAM-R56A:[22] non-xanthinic high affinity selective antagonist (Ki: 1.50 nM)
  • ISAM-140:[24] non-xanthinic selective antagonist (Ki = 3.49 nM).
  • ISAM-R324A:[25] Soluble and metabolically stable non-xanthinic selective antagonist (Ki = 6.10 nM).
  • ATL-801
  • CVT-6883
  • MRS-1706
  • MRS-1754
  • OSIP-339,391
  • PSB-603: xanthinic antagonist
  • PSB-0788: xanthinic antagonist
  • PSB-1115: xanthinic antagonist
  • PSB-1901:[26] xanthinic antagonist with picomolar potency


References

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    GRCh38: Ensembl release 89: ENSG00000170425 – Ensembl, May 2017
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    GRCm38: Ensembl release 89: ENSMUSG00000018500 – Ensembl, May 2017
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    "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
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    "Entrez Gene: ADORA2B adenosine A2b receptor".
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