Hypocretin (orexin) receptor 2
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| Orexin receptor type 2 | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Identifiers | |||||||||
| Symbol | Orexin_rec2 | ||||||||
| Pfam | PF03827 | ||||||||
| InterPro | IPR004060 | ||||||||
|
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Orexin receptor type 2 (Ox2R or OX2), also known as hypocretin receptor type 2, is a protein that in humans is encoded by the HCRTR2 gene.[1]
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.[2]
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.[1]
Ligands
Agonists
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)[3]
- Lemborexant - Dual OX1 and OX2 antagonist
- MIN-202 - Selective OX2 antagonist
- MK-1064 - Selective OX2 antagonist[4]
- MK-8133 - Selective OX2 antagonist[5]
- 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[6]
- Compound 1m - Selective OX2 antagonist [7]
See also
References
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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.
