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Hypocretin (orexin) receptor 2

Orexin receptor type 2 (Ox2R or OX<sub>2</sub>), also known as hypocretin receptor type 2 (HcrtR2), is a protein that in humans is encoded by the HCRTR2 gene. It should not be confused for the protein CD200R1 which shares the alias OX2R but is a distinct, unrelated gene located on the human chromosome 3.

Structure

The structure of the receptor has been solved to 2.5 Å resolution as a fusion protein bound to suvorexant using lipid-mediated crystallization.

Function

OX<sub>2</sub> is a G-protein coupled receptor expressed exclusively in the brain. It has 64% identity with OX<sub>1</sub>. OX<sub>2</sub> binds both orexin A and orexin B neuropeptides. OX<sub>2</sub> is involved in the central feedback mechanism that regulates feeding behaviour. Mice with enhanced OX<sub>2</sub> signaling are resistant to high-fat diet-induced obesity.

This receptor is activated by orexin, which is a wake-promoting hypothalamic neuropeptide that acts as a critical regulator of sleep in animals as Zebrafish or Mammals. This protein has mutations in Astyanax mexicanus that reduces the sleep needs of the cavefish.

Ligands

Agonists

  • Danavorexton/TAK-925 – selective OX<sub>2</sub> receptor agonist
  • Firazorexton/TAK-994 – selective OX<sub>2</sub> receptor agonist
  • Orexins – dual OX<sub>1</sub> and OX<sub>2</sub> receptor agonists
  • Orexin-A – approximately equipotent at the OX<sub>1</sub> and OX<sub>2</sub> receptors
  • Orexin-B – approximately 5- to 10-fold selectivity for the OX<sub>2</sub> receptor over the OX<sub>1</sub> receptor
  • SB-668875 – selective OX<sub>2</sub> receptor agonist
  • Suntinorexton – selective OX<sub>2</sub> receptor agonist
  • Oveporexton/TAK-861 – selective OX<sub>2</sub> receptor agonist
  • Cleminorexton - selective OX<sub>2</sub> receptor agonist

Antagonists

See also

References

Further reading