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10 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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HCRTR1
hypocretin receptor 1
Chromosome 1 · 1p35.2
NCBI Gene: 3061Ensembl: ENSG00000121764.12HGNC: HGNC:4848UniProt: A6NMV7
85PubMed Papers
20Diseases
8Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
neuropeptide signaling pathwayprotein bindingorexin receptor activityplasma membraneinsomniaintelligenceSleep Disordersleep
✦AI Summary

HCRTR1 (hypocretin receptor 1) is a G-protein coupled receptor that binds orexin-A with high affinity and orexin-B with lower affinity 1. The receptor mediates its activity through G(q)-protein-coupled signaling pathways, activating the phosphatidylinositol-calcium second messenger system and promoting beta-arrestin recruitment for receptor internalization 1. HCRTR1 is primarily associated with regulation of motivation, reward, and autonomic functions, while its counterpart HCRTR2 is more strongly linked to sleep-wake control 1. The receptor plays significant roles in various physiological processes including feeding behavior, cardiovascular regulation, and stress response 23. In disease contexts, HCRTR1 genetic variants are associated with reward sensitivity in a gender-dependent manner and have been linked to aggressive behavior 4. The receptor shows clinical relevance in multiple conditions: variants affect anesthesia response and hemodynamic stability 3, contribute to migraine susceptibility 5, and influence daytime napping patterns with potential cardiometabolic implications 6. Therapeutically, HCRTR1 represents an important drug target, with selective antagonists showing promise for treating obesity by modulating feeding behavior 2, and orexin-A demonstrating neuroprotective effects in cerebral ischemia through anti-inflammatory and anti-apoptotic mechanisms 7.

Sources cited
1
HCRTR1 binds orexin-A with high affinity, functions through G(q)-protein signaling, and is associated with motivation and reward regulation
PMID: 34052813
2
HCRTR1 genetic variants are associated with reward sensitivity in a gender-dependent manner and linked to aggressive behavior
PMID: 32652147
3
HCRTR1 variants affect anesthesia response and hemodynamic stability during propofol-based anesthesia
PMID: 40439868
4
HCRTR1 is enriched in brainstem glutamatergic neurons and represents a therapeutic target for obesity treatment
PMID: 36411386
5
HCRTR1 variants are associated with daytime napping patterns and cardiometabolic health
PMID: 33568662
6
HCRTR1 genetic variants contribute to migraine susceptibility
PMID: 27191890
7
Orexin-A provides neuroprotective effects through HCRTR1-mediated anti-inflammatory and anti-apoptotic mechanisms
PMID: 34358627
Disease Associationsⓘ20
insomniaOpen Targets
0.60Moderate
intelligenceOpen Targets
0.42Moderate
Sleep DisorderOpen Targets
0.36Weak
sleepOpen Targets
0.33Weak
Alzheimer diseaseOpen Targets
0.30Weak
abnormality of serum enzyme levelsOpen Targets
0.29Weak
alcohol dependenceOpen Targets
0.29Weak
nutritional deficiency diseaseOpen Targets
0.28Weak
deliriumOpen Targets
0.28Weak
epilepsyOpen Targets
0.26Weak
duodenal ulcerOpen Targets
0.25Weak
Abnormality of the skeletal systemOpen Targets
0.12Weak
post-traumatic stress disorderOpen Targets
0.11Weak
opioid use disorderOpen Targets
0.10Weak
diabetic neuropathyOpen Targets
0.09Suggestive
major depressive disorderOpen Targets
0.09Suggestive
ovarian neoplasmOpen Targets
0.09Suggestive
diabetes mellitusOpen Targets
0.08Suggestive
attention deficit hyperactivity disorderOpen Targets
0.08Suggestive
alcohol abuseOpen Targets
0.08Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets8
ALMOREXANTPhase III
Orexin receptor antagonist
insomnia
DARIDOREXANTApproved
Orexin receptor 2 antagonist
insomnia
DARIDOREXANT HYDROCHLORIDEApproved
Orexin receptor 2 antagonist
insomnia
FILOREXANTPhase II
Orexin receptor antagonist
diabetic neuropathy
LEMBOREXANTApproved
Orexin receptor 1 antagonist
insomnia
ORN-0829 HYDRATEPhase III
Orexin receptor antagonist
insomnia
SB-649868Phase II
Orexin receptor 1 antagonist
insomnia
SUVOREXANTApproved
Orexin receptor antagonist
insomnia
Related Genes
CRHR1Protein interaction100%LINC02210-CRHR1Protein interaction100%OXR1Protein interaction93%ATXN3LProtein interaction79%HCRTR2Protein interaction77%PDYNProtein interaction77%
Tissue Expression6 tissues
Bone Marrow
100%
Heart
95%
Lung
28%
Brain
23%
Liver
18%
Ovary
18%
Gene Interaction Network
Click a node to explore
HCRTR1CRHR1LINC02210-CRHR1OXR1ATXN3LHCRTR2PDYN
PROTEIN STRUCTURE
Preparing viewer…
PDB6TOD · 2.11 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.92LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.67 [0.50–0.92]
RankingsWhere HCRTR1 stands among ~20K protein-coding genes
  • #5,613of 20,598
    Most Researched85
  • #421of 1,025
    FDA-Approved Drug Targets4
  • #8,426of 17,882
    Most Constrained (LOEUF)0.92
Genes detectedHCRTR1
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
Hypocretin/Orexin Receptor Pharmacology and Sleep Phases.
PMID: 34052813
Front Neurol Neurosci · 2021
1.00
2
Orexin-A alleviates astrocytic apoptosis and inflammation via inhibiting OX1R-mediated NF-κB and MAPK signaling pathways in cerebral ischemia/reperfusion injury.
PMID: 34358627
Biochim Biophys Acta Mol Basis Dis · 2021
0.90
3
Association of orexin/hypocretin receptor gene (HCRTR1) with reward sensitivity, and interaction with gender.
PMID: 32652147
Brain Res · 2020
0.80
4
Combined effects of HCRTR1/2 gene variants and non-genetic factors on sleep-wake transition and hemodynamic stability during propofol, dexmedetomidine, and remifentanil anesthesia.
PMID: 40439868
Pharmacol Rep · 2025
0.70
5
Pharmacological targeting of glutamatergic neurons within the brainstem for weight reduction.
PMID: 36411386
Nat Metab · 2022
0.60