Hypocretin (orexin) receptor 1

Orexin receptor type 1 (Ox1R or OX₁), also known as hypocretin receptor type 1 (HcrtR1), is a protein that in humans is encoded by the HCRTR1 gene.^[5]

HCRTR1
Available structures PDB Ortholog search: PDBe RCSB List of PDB id codes 4ZJ8, 4ZJC
Identifiers
Aliases	HCRTR1, OX1R, Hypocretin (orexin) receptor 1, hypocretin receptor 1, ORXR1, OXR1
External IDs	OMIM: 602392; MGI: 2385650; HomoloGene: 37492; GeneCards: HCRTR1; OMA:HCRTR1 - orthologs
Gene location (Human) Chr. Chromosome 1 (human)[1] Band 1p35.2 Start 31,617,686 bp[1] End 31,632,518 bp[1]
Gene location (Mouse) Chr. Chromosome 4 (mouse)[2] Band 4|4 D2.2 Start 130,024,010 bp[2] End 130,033,152 bp[2]
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in apex of heart primary visual cortex superior frontal gyrus right lobe of thyroid gland placenta prefrontal cortex left lobe of thyroid gland left ventricle skeletal muscle tissue Hypothalamus Top expressed in substantia nigra spinal ganglia embryo blastocyst central gray substance of midbrain dentate gyrus of hippocampal formation granule cell granulocyte visual cortex primary visual cortex dorsal tegmental nucleus More reference expression data BioGPS More reference expression data
Gene ontology Molecular function peptide hormone binding peptide binding G protein-coupled receptor activity signal transducer activity orexin receptor activity Cellular component integral component of membrane plasma membrane membrane integral component of plasma membrane Biological process cellular response to hormone stimulus regulation of circadian sleep/wake cycle, sleep signal transduction response to peptide chemical synaptic transmission regulation of cytosolic calcium ion concentration positive regulation of ERK1 and ERK2 cascade neuropeptide signaling pathway feeding behavior G protein-coupled receptor signaling pathway Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 3061 230777 Ensembl ENSG00000121764 ENSMUSG00000028778 UniProt O43613 P58307 RefSeq (mRNA) NM_001525 NM_001163027 NM_198959 NM_001305392 NM_001357258 RefSeq (protein) NP_001516 NP_001156499 NP_001292321 NP_945197 NP_001344187 Location (UCSC) Chr 1: 31.62 – 31.63 Mb Chr 4: 130.02 – 130.03 Mb PubMed search [3] [4]
Wikidata
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Function

The orexin 1 receptor (OX₁), is a G-protein coupled receptor that is heavily expressed in projections from the lateral hypothalamus and is involved in the regulation of feeding behaviour. OX₁ selectively binds the orexin-A neuropeptide. It shares 64% identity with OX₂.^[5]

Ligands

Agonists

• Orexin-A

Antagonists

Further information: Orexin antagonist

• RTIOX-276 - Selective OX₁ antagonist
• ACT-335827 - Selective OX₁ antagonist
• Almorexant - Dual OX₁ and OX₂ antagonist
• Lemborexant - Dual OX₁ and OX₂ antagonist^[6]
• Nemorexant - Dual OX₁ and OX₂ antagonist
• SB-334,867 - Selective OX₁ antagonist
• SB-408,124 - Selective OX₁ antagonist
• SB-649,868 - Dual OX₁ and OX₂ antagonist
• Suvorexant - Dual OX₁ and OX₂ antagonist

See also

• Orexin receptor