DPDPE

Summary

DPDPE ([D-Pen2,D-Pen5]-enkephalin) is a synthetic, conformationally constrained cyclic enkephalin analogue developed as a highly selective delta-opioid receptor agonist. It is a critical pharmacological tool compound used in research to characterize delta-opioid receptor subtypes, study opioid analgesia, and explore delta-receptor-mediated effects on mood, neuroprotection, and cardioprotection. It is not approved for clinical use.

Mechanism of Action

Selective delta-opioid receptor (DOR) agonist; cyclic disulfide-bridged enkephalin analogue that binds with high selectivity to delta-opioid receptors, activating Gi/Go signaling to inhibit adenylyl cyclase, reduce cAMP, modulate ion channels, and decrease neuronal excitability and nociceptive transmission.

Routes of Administration

Goals & Uses

• Analgesia (preclinical)Pain / NociceptionHigh
• Cardioprotection (preclinical)Cardiovascular ResearchModerate
• Mood and antidepressant effects (preclinical)Neuropsychiatry ResearchModerate
• Neuroprotection (preclinical)Neuroscience ResearchModerate
• Delta-opioid receptor characterizationResearch / PharmacologyHigh

Contraindications

• Known hypersensitivity to enkephalin analoguesAllergy/ImmunologyHigh
• Human therapeutic useRegulatory/safetyHigh

Adverse Effects

• Convulsions/SeizuresNeurologicalUncommon
• Cardiovascular effectsCardiovascularUnknown
• Tolerance developmentPharmacologicalCommon
• Respiratory depressionRespiratoryUncommon
• SedationCNSCommon

Drug Interactions

• CNS depressantsModerate
• Mu-opioid receptor agonists (e.g., morphine)Moderate
• Naltrindole (delta-opioid antagonist)High

Population Constraints

• Pregnant or lactating animalsReproductiveRelative
• Human subjectsRegulatory/SafetyAbsolute

Regulatory Status

• European UnionUnapprovedNot approved by EMA; research use only under appropriate institutional and national regulatory oversight.
• United StatesUnapprovedNot FDA-approved; used as a research tool compound only. May be subject to DEA scheduling as opioid analogue.
• United KingdomUnapprovedNot approved by MHRA; controlled under UK drug regulations as an opioid analogue for research purposes only.

DPDPE is not approved by any regulatory agency (FDA, EMA, MHRA) for human therapeutic use. It is classified as a Schedule I controlled substance analogue in some jurisdictions due to its opioid activity. Used exclusively as a research tool compound in preclinical and basic science studies.

Evidence & Sources

No sources recorded yet.