Hypocretin (orexin) receptor 1

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)
End	31,632,518 bp
Gene location (Mouse)
Chr.	Chromosome 4 (mouse)
End	130,033,152 bp
RNA expression pattern
	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
	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
	3061
	230777
	ENSG00000121764
	ENSMUSG00000028778
	O43613
	P58307
	NM_001525
	NM_001163027; NM_198959; NM_001305392; NM_001357258
	NP_001516
	NP_001156499; NP_001292321; NP_945197; NP_001344187
	Wikidata
View/Edit Human	View/Edit Mouse

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]

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

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

References

^ ^a ^b ^c GRCh38: Ensembl release 89: ENSG00000121764 – Ensembl, May 2017
^ ^a ^b ^c GRCm38: Ensembl release 89: ENSMUSG00000028778 – Ensembl, May 2017
^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^ ^a ^b "Entrez Gene: HCRTR1 hypocretin (orexin) receptor 1".
^ "Eisai Demonstrates Efficacy of Investigational Dual Orexin Receptor Antagonist E2006 in Sleep Initiation and Maintenance Data from Phase II Clinical Trial for Insomnia".

External links

"Orexin Receptors: OX₁". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2016-02-06. Retrieved 2008-12-09.

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