Target intelligence / Profile preview

Opioid Receptor Delta (DOR)

Target
DOR
Molecular classification
GPCR, 7-transmembrane domain receptor, Receptor
01

Overview

The delta opioid receptor (DOR) is a member of the opioid receptor family and a G protein-coupled receptor that primarily couples to inhibitory G proteins. Its endogenous ligands are enkephalins. It is widely distributed throughout the central nervous system and involved in analgesia (particularly chronic pain), mood regulation, and gastrointestinal motility. Selective delta agonists are being developed as potential analgesics with reduced side effects compared to mu-opioid agonists. Recent research highlights compartmentalized signaling from endosomes, contributing to prolonged analgesic effects during inflammatory states.

Other names
δ-Opioid ReceptorDelta Opioid ReceptorDelta ReceptorOPRD1
02

Mechanism of action

Gi/Go protein activation leading to inhibition of adenylyl cyclase, modulation of ion channels (K+ channel activation, Ca2+ channel inhibition), and activation of kinase cascades (ERK, Akt, JNKs, STAT3, p38 MAPK)

03

Biological functions

Signal transductionAnalgesiaMood regulationRegulation of gastrointestinal motilityNeuronal excitability modulationNeurotransmitter release modulation
04

Disease associations

Pain (chronic/persistent)Mood disorders (anxiety, depression)Inflammatory diseases (e.g., colitis)
05

Safety considerations

Respiratory depression (less than mu-opioid agonists)Seizures (at high doses with some delta agonists)Desensitization upon sustained stimulation
06

Interacting drugs

Enkephalins

3 more in the full profile.

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