Hypocretin (orexin) receptor 2

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Hypocretin (orexin) receptor 2
Available structures
PDB Ortholog search: PDBe, RCSB
Symbols HCRTR2 ; OX2R
External IDs OMIM602393 MGI2680765 HomoloGene1168 IUPHAR: 322 ChEMBL: 4792 GeneCards: HCRTR2 Gene
RNA expression pattern
PBB GE HCRTR2 207393 at tn.png
More reference expression data
Species Human Mouse
Entrez 3062 387285
Ensembl ENSG00000137252 ENSMUSG00000032360
UniProt O43614 P58308
RefSeq (mRNA) NM_001526 NM_198962
RefSeq (protein) NP_001517 NP_945200
Location (UCSC) Chr 6:
55.11 – 55.28 Mb
Chr 9:
76.23 – 76.32 Mb
PubMed search [1] [2]
Orexin receptor type 2
Symbol Orexin_rec2
Pfam PF03827
InterPro IPR004060

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]


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]




See also[edit]


  1. ^ a b "Entrez Gene: HCRTR2 hypocretin (orexin) receptor 2". 
  2. ^ McAtee LC, Sutton SW, Rudolph DA, Li X, Aluisio LE, Phuong VK et al. (Aug 2004). "Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists". Bioorganic & Medicinal Chemistry Letters 14 (16): 4225–9. doi:10.1016/j.bmcl.2004.06.032. PMID 15261275. 
  3. ^ Roecker AJ, Mercer SP, Schreier JD, Cox CD, Fraley ME, Steen JT et al. (Feb 2014). "Discovery of 5-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia". ChemMedChem 9 (2): 311–22. doi:10.1002/cmdc.201300447. PMID 24376006. 
  4. ^ Kuduk SD, Skudlarek JW, DiMarco CN, Bruno JG, Pausch MH, O'Brien JA et al. (Jun 2015). "Identification of MK-8133: An orexin-2 selective receptor antagonist with favorable development properties". Bioorganic & Medicinal Chemistry Letters 25 (12): 2488–92. doi:10.1016/j.bmcl.2015.04.066. PMID 25981685. 
  5. ^ Cole AG, Stroke IL, Qin LY, Hussain Z, Simhadri S, Brescia MR et al. (Oct 2008). "Synthesis of (3,4-dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists". Bioorganic & Medicinal Chemistry Letters 18 (20): 5420–3. doi:10.1016/j.bmcl.2008.09.038. PMID 18815029. 
  6. ^ Fujimoto T, Kunitomo J, Tomata Y, Nishiyama K, Nakashima M, Hirozane M et al. (Nov 2011). "Discovery of potent, selective, orally active benzoxazepine-based Orexin-2 receptor antagonists". Bioorganic & Medicinal Chemistry Letters 21 (21): 6414–6. doi:10.1016/j.bmcl.2011.08.093. PMID 21917455. 

Further reading[edit]

This article incorporates text from the United States National Library of Medicine, which is in the public domain.