Target intelligence / Profile preview

Opioid Delta Receptor (DOR)

Target
DOR
Molecular classification
G protein-coupled receptor, GPCR, Class A GPCR, Receptor
01

Overview

The opioid delta receptor (DOR), encoded by the OPRD1 gene, is a member of the opioid receptor family and a G protein-coupled receptor (GPCR). It is primarily activated by enkephalins and is involved in analgesia, mood regulation, and the reduction of gastrointestinal motility. DOR activation leads to inhibition of neuronal excitability along pain pathways and modulates both acute and chronic pain responses. It couples primarily to Gi/o proteins, leading to inhibition of adenylyl cyclase and modulates ion channels. Unlike other opioid receptors, DOR exhibits sustained antinociceptive effects via prolonged ERK activation from endosomal compartments. Delta-selective agonists are being investigated as novel analgesics with fewer side effects compared to mu-opioid drugs, and for their potential roles in treating mood disorders.

Other names
δ-opioid receptorDOPOPRD1
02

Mechanism of action

Activation of Gi/o proteins, inhibition of adenylyl cyclase, modulation of ion channels, ERK/PKC activation via endosomal signaling.

03

Biological functions

AnalgesiaMood regulationModulation of gastrointestinal motilitySignal transduction
04

Disease associations

Pain (acute and chronic)Mood disorders (anxiety, depression)Neurological disordersPsychiatric disorders
05

Safety considerations

Potential for desensitization upon prolonged stimulationPossible altered pharmacological properties due to heterodimerization with other GPCRsSide effects may exist, although potentially fewer than mu-opioid receptor agonists
06

Interacting drugs

Enkephalins

4 more in the full profile.

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