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10 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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OPRL1
opioid related nociceptin receptor 1
Chromosome 20 · 20q13.33
NCBI Gene: 4987Ensembl: ENSG00000125510.18HGNC: HGNC:8155UniProt: A0A5F9ZI64
77PubMed Papers
20Diseases
4Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
CLINICAL
Clinical Trials
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
phospholipase C-activating G protein-coupled receptor signaling pathwayadenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayG protein-coupled receptor activityplasma membraneneurodegenerative diseasediabetic neuropathycoronary artery diseaseAbnormality of the skeletal system
✦AI Summary

OPRL1 encodes the nociceptin receptor (NOP), a G protein-coupled receptor that binds the endogenous neuropeptide nociceptin to modulate pain perception and locomotor activity [UniProt]. The receptor signals through inhibition of adenylate cyclase and calcium channels, with alternative arrestin-mediated pathways activating MAP kinases [UniProt]. OPRL1 dysfunction associates with multiple neuropsychiatric and neurodegenerative conditions. Genetic polymorphisms in OPRL1 are linked to alcohol dependence, with SNP rs6010718 showing significant association in Scandinavian populations 1. OPRL1 methylation emerges as a critical epigenetic regulator: low intron 1 methylation mediates psychosocial stress-induced binge drinking through altered ventral striatum reward processing 2, while elevated promoter methylation is associated with Alzheimer's disease and serves as a potential diagnostic biomarker 3. Environmental stressors during early life increase hippocampal Oprl1 expression through histone modifications, potentially contributing to cognitive impairment in male offspring 4. Functionally, OPRL1 demonstrates anti-inflammatory properties, with NFκB signaling regulating NOP transcription during inflammatory responses 5. In PTSD, OPRL1 variants associate with amygdala-dependent fear processing and trauma susceptibility; NOP receptor agonists impair fear memory consolidation 6. These findings establish OPRL1 as a convergent hub linking stress, reward processing, inflammation, and fear circuitry.

Sources cited
1
OPRL1 genetic polymorphisms, particularly SNP rs6010718, are significantly associated with alcohol dependence in Scandinavian populations
PMID: 18269382
2
Low OPRL1 methylation in intron 1 mediates the effect of psychosocial stress on binge drinking through altered reward anticipation in the ventral striatum
PMID: 29197086
3
Elevated OPRL1 promoter methylation is significantly associated with Alzheimer's disease and serves as a potential methylation biomarker for AD diagnosis
PMID: 30152845
4
Adverse maternal environment and Western diet increase hippocampal Oprl1 expression and variant V4 through epigenetic modifications, potentially contributing to cognitive impairment in male offspring
PMID: 35983908
5
NFκB signaling regulates NOP/OPRL1 transcription during inflammatory responses, suggesting an anti-inflammatory role for the nociceptin system
PMID: 39768201
6
OPRL1 variants associate with amygdala-dependent fear processing and PTSD symptoms; NOP receptor agonists impair fear memory consolidation
PMID: 23740899
Disease Associationsⓘ20
neurodegenerative diseaseOpen Targets
0.40Moderate
diabetic neuropathyOpen Targets
0.26Weak
coronary artery diseaseOpen Targets
0.21Weak
Abnormality of the skeletal systemOpen Targets
0.20Weak
cardiovascular diseaseOpen Targets
0.20Weak
response to statinOpen Targets
0.18Weak
breast cancerOpen Targets
0.17Weak
metabolic diseaseOpen Targets
0.17Weak
hypertensionOpen Targets
0.13Weak
nephrolithiasisOpen Targets
0.12Weak
bladder calculusOpen Targets
0.12Weak
metabolic syndromeOpen Targets
0.11Weak
major depressive disorderOpen Targets
0.11Weak
osteoarthritis, kneeOpen Targets
0.10Weak
HypercholesterolemiaOpen Targets
0.10Suggestive
CoughOpen Targets
0.09Suggestive
ulcerative colitisOpen Targets
0.08Suggestive
alcohol dependenceOpen Targets
0.08Suggestive
neoplasmOpen Targets
0.08Suggestive
Parkinson diseaseOpen Targets
0.08Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets4
CEBRANOPADOLPhase III
Nociceptin receptor agonist
diabetic neuropathy
LY-2940094Phase II
Nociceptin receptor antagonist
major depressive disorder
LY2940094Phase II
Nociceptin receptor antagonist
major depressive disorder
SCH-486757Phase II
Nociceptin receptor agonist
Cough
Related Genes
GNAI1Protein interaction99%NPYProtein interaction98%POMCProtein interaction97%SSTProtein interaction95%TAC1Protein interaction95%GNB1Protein interaction83%
Tissue Expression6 tissues
Bone Marrow
100%
Brain
82%
Lung
22%
Heart
10%
Liver
6%
Ovary
6%
Gene Interaction Network
Click a node to explore
OPRL1GNAI1NPYPOMCSSTTAC1GNB1
PROTEIN STRUCTURE
Preparing viewer…
PDB5DHG · 3.00 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.72LoF Tolerant
pLIⓘ
0.31Tolerant
Observed/Expected LoF0.41 [0.25–0.72]
RankingsWhere OPRL1 stands among ~20K protein-coding genes
  • #6,190of 20,598
    Most Researched77
  • #5,524of 17,882
    Most Constrained (LOEUF)0.72
Genes detectedOPRL1
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
Adverse maternal environment alters Oprl1 variant expression in mouse hippocampus.
PMID: 35983908
Anat Rec (Hoboken) · 2023
1.00
2
Association between the nociceptin receptor gene (OPRL1) single nucleotide polymorphisms and alcohol dependence.
PMID: 18269382
Addict Biol · 2008
0.90
3
Elevated methylation of OPRM1 and OPRL1 genes in Alzheimer's disease.
PMID: 30152845
Mol Med Rep · 2018
0.80
4
Methylation of OPRL1 mediates the effect of psychosocial stress on binge drinking in adolescents.
PMID: 29197086
J Child Psychol Psychiatry · 2018
0.70
5
Endogenous opiates and behavior: 2017.
PMID: 31805297
Peptides · 2020
0.60