Target intelligence / Profile preview

Delta-type opioid receptor (OPRD1) (OPRD1)

Target
OPRD1
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The Delta-type opioid receptor (OPRD1) is a member of the G protein-coupled receptor family that plays a critical role in the modulation of pain, mood, and reward pathways [5, 11]. It is primarily activated by endogenous enkephalins and is widely distributed throughout the central nervous system, particularly in the cortex, striatum, and limbic system [2, 5]. OPRD1 is a significant therapeutic target for the treatment of chronic pain, emotional disorders like depression and anxiety, and substance use disorders, including alcoholism and opioid addiction [6, 9]. Unlike the Mu-opioid receptor, activation of the Delta receptor is less associated with respiratory depression and physical dependence, making it an attractive target for novel analgesics [4, 9]. Drugs like naltrexone act as non-selective antagonists at this receptor, blocking the reinforcing effects of exogenous opioids and alcohol by preventing the activation of downstream signaling pathways [10, 15]. Genetic variations in the OPRD1 gene, such as specific single nucleotide polymorphisms, are associated with individual differences in pain perception and susceptibility to drug dependence [1, 14]. Furthermore, the receptor is involved in neuroimmunomodulation, influencing the activity of immune cells and inflammatory responses [4, 16].

Other names
Delta opioid receptorDORDOR-1OPRDOpioid receptor delta 1
02

Mechanism of action

Naltrexone acts as a competitive antagonist at the Delta-type opioid receptor (OPRD1), as well as the Mu and Kappa opioid receptors, thereby blocking the binding of endogenous and exogenous opioids to prevent their rewarding and physiological effects [10, 15].

03

Biological functions

Signal transductionModulation of pain perceptionRegulation of emotional statesNeurotransmissionImmune response
04

Disease associations

Substance use disorderChronic painDepressionAnxietyAlcoholism
05

Safety considerations

Potential for seizures with agonistsMood alterationsOpioid withdrawal symptomsTolerance development
06

Interacting drugs

Naltrexone

5 more in the full profile.

07

Biomarkers

OPRD1 gene polymorphisms (e.g., rs678849, rs2236861)Receptor occupancy (PET imaging)

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