DADLE
Also known as: [D-Ala2, D-Leu5]-Enkephalin, 63631-40-3, D-Ala(2)-Leu(5)-Enkephalin, DADLE
Summary
DADLE ([D-Ala2, D-Leu5]-enkephalin) is a synthetic enkephalin analogue with preferential delta-opioid receptor agonist activity. It has been extensively used in preclinical research to study opioid receptor pharmacology. Notable areas of investigation include neuroprotection, cardioprotection, ischemia/reperfusion injury, and organ preservation. It has also been studied for its ability to induce hibernation-like states in non-hibernating animals.
Mechanism of Action
Selective agonist at delta-opioid receptors (DOR); also has affinity for mu-opioid receptors. Activates Gi/Go proteins, inhibits adenylyl cyclase, modulates ion channels, and reduces neuronal excitability and neurotransmitter release.
Routes of Administration
Goals & Uses
- NeuroprotectionNeurologyModerate
- Cardioprotection / ischemia-reperfusion injuryCardiovascularModerate
- AntinociceptionResearch / AnalgesiaModerate
- Organ preservationResearch / TransplantationLow
- Induction of hibernation-like stateResearch / Suspended AnimationLow
- Opioid receptor pharmacology toolResearch / Receptor CharacterizationHigh
Contraindications
- Human therapeutic useRegulatory/safetyHigh
- Respiratory compromiseClinical (preclinical Extrapolation)High
Adverse Effects
- Cardiovascular depressionCardiovascularUncommon
- Respiratory depressionRespiratoryUnknown
- Sedation / CNS depressionNeurologicalCommon
- Tolerance and dependencePharmacologicalUnknown
Drug Interactions
- CNS depressantsHigh
- Naloxone / NaltrexoneLow
Population Constraints
- Humans (general)Regulatory / SafetyAbsolute
- Pregnant animalsReproductiveRelative
Regulatory Status
- European UnionUnapprovedNo EMA approval; available only as research reagent.
- United StatesUnapprovedResearch use only; not FDA-approved for any indication. Not scheduled under the Controlled Substances Act but subject to institutional research oversight.
- United KingdomUnapprovedNo MHRA approval; research use only.
Not approved for human therapeutic use in any jurisdiction. Used exclusively as a research tool compound. Not scheduled as a controlled substance in most jurisdictions, but subject to general research regulations.
Evidence & Sources
No sources recorded yet.