Hypocretin (orexin) receptor 2
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| Orexin receptor type 2 | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Identifiers | |||||||||
| Symbol | Orexin_rec2 | ||||||||
| Pfam | PF03827 | ||||||||
| InterPro | IPR004060 | ||||||||
| |||||||||
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.[1] 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.[2]
Structure
[edit | edit source]The structure of the receptor has been solved to 2.5 Å resolution as a fusion protein bound to suvorexant using lipid-mediated crystallization.[3]
Function
[edit | edit source]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.[1] Mice with enhanced OX2 signaling are resistant to high-fat diet-induced obesity.[4]
This receptor is activated by Hipocretin, 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.[5]
Ligands
[edit | edit source]Agonists
[edit | edit source]- Danavorexton/TAK-925 – selective OX2 receptor agonist
- Firazorexton/TAK-994 – selective OX2 receptor agonist[6][7]
- Orexins – dual OX1 and OX2 receptor agonists
- SB-668875 – selective OX2 receptor agonist
- Suntinorexton – selective OX2 receptor agonist[6][7]
- Oveporexton/TAK-861 – selective OX2 receptor agonist[10]
Antagonists
[edit | edit source]- Almorexant - Dual OX1 and OX2 antagonist
- Daridorexant (nemorexant) - Dual OX1 and OX2 antagonist
- EMPA - Selective OX2 antagonist
- Filorexant - Dual OX1 and OX2 antagonist
- JNJ-10397049 (600x selective for OX2 over OX1)[11]
- Lemborexant - Dual OX1 and OX2 antagonist
- MK-1064 - Selective OX2 antagonist[12]
- MK-8133 - Selective OX2 antagonist[13]
- SB-649,868 - Dual OX1 and OX2 antagonist
- Seltorexant - Selective OX2 antagonist
- Suvorexant - Dual OX1 and OX2 antagonist
- TCS-OX2-29 - Selective OX2 antagonist
- (3,4-dimethoxyphenoxy)alkylamino acetamides[14]
- Compound 1m - Selective OX2 antagonist[15]
See also
[edit | edit source]References
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- ^ a b WO application 2019027058, Kajita, Yuichi; Mikami, Satoshi & Miyanohana, Yuhei et al., "Heterocyclic compound and use therof", published Lua error in Module:Citation/CS1/Configuration at line 2172: attempt to index field '?' (a nil value)., assigned to Takeda Pharmaceutical Company
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Further reading
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This article incorporates text from the United States National Library of Medicine, which is in the public domain.