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10 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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OPRD1
opioid receptor delta 1
Chromosome 1 · 1p35.3
NCBI Gene: 4985Ensembl: ENSG00000116329.12HGNC: HGNC:8153UniProt: P41143
140PubMed Papers
20Diseases
25Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
regulation of mitochondrial membrane potentialnegative regulation of gene expressionnegative regulation of protein-containing complex assemblyG protein-coupled opioid receptor activityPainalcohol dependencemigraine disorderdrug dependence
✦AI Summary

OPRD1 encodes the delta-opioid receptor, a G-protein coupled receptor that binds endogenous enkephalins and other opioids 1. Ligand binding triggers conformational changes activating G-protein signaling, inhibiting adenylate cyclase activity and modulating neurotransmitter release through altered calcium and potassium currents [UniProt]. The receptor regulates pain perception and opiate-mediated analgesia, while also contributing to analgesic tolerance development [UniProt]. OPRD1 contains over 2,000 genetic variants with diverse functional consequences 1. The variants rs1042114 and rs569356 have characterized functions: rs1042114 disrupts receptor maturation and has been linked to Alzheimer's disease through reduced beta-amyloid production 1, while rs569356 affects OPRD1 expression and shows association with anorexia 1. Intronic variants (rs2236861, rs2236857, rs3766951) demonstrate reproducible associations with opioid addiction across populations 1. OPRD1 rs2234918 increases heroin dependence vulnerability 1.42-fold 2, while rs4654327 acts as both a methylation and expression quantitative trait locus associated with opioid use disorder 3. These addiction-linked variants function as cis-eQTLs for upstream PHACTR4, affecting cytoskeletal dynamics and synaptic plasticity 4. In males, OPRD1 polymorphisms influence morphine analgesia variability 5. Notably, OPRD1 expression is downregulated in psychopathy-associated neurons 6, suggesting broader neuropsychiatric relevance beyond pain and addiction.

Sources cited
1
OPRD1 contains >2,000 genetic variants; rs1042114 and rs569356 have characterized functions; three intronic variants show reproducible opioid addiction associations
PMID: 28035534
2
OPRD1 rs2234918 C allele increases heroin dependence risk 1.42-fold; rs2236857 variants affect stress response in heroin-dependent patients
PMID: 30171993
3
OPRD1 rs4654327 functions as both methylation and expression quantitative trait locus associated with opioid use disorder
PMID: 37660978
4
OPRD1 addiction-linked variants are cis-eQTLs for PHACTR4, a mediator of cytoskeletal dynamics and synaptic plasticity in drug addiction
PMID: 34031368
5
In males, OPRD1 polymorphisms rs2234918 and rs533123 associate with morphine analgesia variability to rectal thermal stimulation
PMID: 28084056
6
OPRD1 expression is downregulated in neurons from individuals with psychopathy, explaining 30-92% of psychopathic symptom variance
PMID: 31455857
Disease Associationsⓘ20
PainOpen Targets
0.61Moderate
alcohol dependenceOpen Targets
0.60Moderate
migraine disorderOpen Targets
0.60Moderate
drug dependenceOpen Targets
0.59Moderate
opioid dependenceOpen Targets
0.58Moderate
obesityOpen Targets
0.58Moderate
major depressive disorderOpen Targets
0.54Moderate
ConstipationOpen Targets
0.48Moderate
CoughOpen Targets
0.47Moderate
HeadacheOpen Targets
0.46Moderate
septic shockOpen Targets
0.46Moderate
schizophreniaOpen Targets
0.45Moderate
substance-related disorderOpen Targets
0.43Moderate
nicotine dependenceOpen Targets
0.41Moderate
Chronic painOpen Targets
0.40Moderate
opioid use disorderOpen Targets
0.40Weak
Low back painOpen Targets
0.39Weak
heroin dependenceOpen Targets
0.38Weak
bipolar I disorderOpen Targets
0.37Weak
Muscle spasmOpen Targets
0.37Weak
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets25
ADL-5747Phase II
Delta opioid receptor agonist
Pain
ADL-5859Phase II
Delta opioid receptor agonist
rheumatoid arthritis
AXOMADOLPhase II
Delta opioid receptor agonist
Back pain
AZD-7268Phase II
Delta opioid receptor agonist
anxiety disorder
BENZHYDROCODONE HYDROCHLORIDEApproved
Opioid receptors; mu/kappa/delta agonist
Pain
CEBRANOPADOLPhase III
Nociceptin receptor agonist
diabetic neuropathy
CODEINEApproved
Opioid receptors; mu/kappa/delta agonist
Pain
CODEINE PHOSPHATEApproved
Opioid receptors; mu/kappa/delta agonist
Pain
CODEINE SULFATEApproved
Opioid receptors; mu/kappa/delta agonist
drug dependence
DEXTROMORAMIDEApproved
Opioid receptors; mu/kappa/delta agonist
Pain
HYDROCODONEApproved
Opioid receptors; mu/kappa/delta agonist
Pain
HYDROCODONE BITARTRATEApproved
Opioid receptors; mu/kappa/delta agonist
Pain
NALBUPHINEApproved
Opioid receptors; mu/kappa/delta agonist
Pain
NALBUPHINE HYDROCHLORIDEApproved
Opioid receptors; mu/kappa/delta agonist
NALMEFENEApproved
Delta opioid receptor antagonist
opioid dependence
NALMEFENE HYDROCHLORIDE DIHYDRATEApproved
Delta opioid receptor antagonist
alcohol dependence
NALOXONEApproved
Opioid receptors; mu/kappa/delta antagonist
Constipation
NALOXONE HYDROCHLORIDEApproved
Opioid receptors; mu/kappa/delta antagonist
Pain
NALTREXONEApproved
Opioid receptors; mu/kappa/delta antagonist
alcohol dependence
NALTREXONE HYDROCHLORIDEApproved
Opioid receptors; mu/kappa/delta antagonist
ONDELOPRANApproved
Opioid receptors; mu/kappa/delta antagonist
alcohol dependence
OXYMORPHONEApproved
Opioid receptors; mu/kappa/delta agonist
Pain
OXYMORPHONE HYDROCHLORIDEApproved
Opioid receptors; mu/kappa/delta agonist
Pain
SAMIDORPHANPhase III
Delta opioid receptor partial agonist
schizophrenia
SAMIDORPHAN L-MALATEApproved
Delta opioid receptor partial agonist
bipolar I disorder
Related Genes
GNAI1Protein interaction99%PDYNProtein interaction98%POMCProtein interaction97%KNG1Protein interaction94%GNAI2Protein interaction92%GNAI3Protein interaction91%
Tissue Expression6 tissues
Brain
100%
Liver
6%
Bone Marrow
6%
Lung
4%
Ovary
4%
Heart
0%
Gene Interaction Network
Click a node to explore
OPRD1GNAI1PDYNPOMCKNG1GNAI2GNAI3
PROTEIN STRUCTURE
Preparing viewer…
PDB4N6H · 1.80 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
1.45LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.96 [0.66–1.45]
RankingsWhere OPRD1 stands among ~20K protein-coding genes
  • #3,285of 20,598
    Most Researched140 · top quartile
  • #82of 1,025
    FDA-Approved Drug Targets19 · top 10%
  • #14,815of 17,882
    Most Constrained (LOEUF)1.45
Genes detectedOPRD1
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
OPRD1 Genetic Variation and Human Disease.
PMID: 28035534
Handb Exp Pharmacol · 2018
1.00
2
OPRD1 gene affects disease vulnerability and environmental stress in patients with heroin dependence in Han Chinese.
PMID: 30171993
Prog Neuropsychopharmacol Biol Psychiatry · 2019
0.90
3
Methylation and expression quantitative trait loci rs1799971 in the OPRM1 gene and rs4654327 in the OPRD1 gene are associated with opioid use disorder.
PMID: 37660978
Neurosci Lett · 2023
0.80
4
OPRD1 SNPs associated with opioid addiction are cis-eQTLs for the phosphatase and actin regulator 4 gene, PHACTR4, a mediator of cytoskeletal dynamics.
PMID: 34031368
Transl Psychiatry · 2021
0.70
5
Genetic Influences of OPRM1, OPRD1 and COMT on Morphine Analgesia in a Multi-Modal, Multi-Tissue Human Experimental Pain Model.
PMID: 28084056
Basic Clin Pharmacol Toxicol · 2017
0.60