Harman Patil (Editor)

Hypocretin (orexin) receptor 2

Updated on
Edit
Like
Comment
Share on FacebookTweet on TwitterShare on LinkedInShare on Reddit
Species
  
Human

Entrez
  
3062

Human
  
Mouse

Ensembl
  
ENSG00000137252

Hypocretin (orexin) receptor 2

Aliases
  
HCRTR2, OX2R, Hypocretin (orexin) receptor 2, hypocretin receptor 2

External IDs
  
MGI: 2680765 HomoloGene: 1168 GeneCards: HCRTR2

Orexin receptor type 2 (Ox2R or OX2), also known as hypocretin receptor type 2 (HcrtR2), is a protein that in humans is encoded by the HCRTR2 gene.

Contents

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

OX2 is a G-protein coupled receptor expressed exclusively in the brain. It has 64% identity with OX1. OX2 binds both orexin A and orexin B neuropeptides. OX2 is involved in the central feedback mechanism that regulates feeding behaviour.

Agonists

  • Orexin-A
  • Orexin-B
  • SB-668,875

    • Antagonists

  • Almorexant - Dual OX1 and OX2 antagonist
  • EMPA - Selective OX2 antagonist
  • Filorexant - Dual OX1 and OX2 antagonist
  • JNJ-10397049 (600x selective for OX2 over OX1)
  • Lemborexant - Dual OX1 and OX2 antagonist
  • MIN-202 - Selective OX2 antagonist
  • MK-1064 - Selective OX2 antagonist
  • MK-8133 - Selective OX2 antagonist
  • SB-649,868 - Dual OX1 and OX2 antagonist
  • Suvorexant - Dual OX1 and OX2 antagonist
  • TCS-OX2-29 - Selective OX2 antagonist
  • (3,4-dimethoxyphenoxy)alkylamino acetamides
  • Compound 1m - Selective OX2 antagonist

    • References

    Hypocretin (orexin) receptor 2 Wikipedia
    (Text) CC BY-SA