Dynorphin
Also known as: Big Dynorphin, Dynorphin A, Dynorphin B, Leu-enkephalin-Arg, PDYN-derived peptide
Summary
Dynorphin is an endogenous opioid neuropeptide derived from the prodynorphin precursor. It exists in multiple forms (Dynorphin A, Dynorphin B, Big Dynorphin) and serves as the primary endogenous ligand for kappa-opioid receptors. It plays roles in pain modulation, stress, mood regulation, and neuroendocrine control. It is used as a research tool and is not approved as a therapeutic agent.
Mechanism of Action
Endogenous agonist at kappa-opioid receptors (KOR); also binds mu- and delta-opioid receptors with lower affinity. Activation of KOR modulates pain perception, stress response, mood, neuroendocrine function, and reward pathways. KOR activation generally produces dysphoria, sedation, and analgesia.
Routes of Administration
Goals & Uses
- Stress and mood researchPsychiatry / NeuroscienceHigh
- Pain modulation researchResearchHigh
- Addiction and reward pathway researchAddiction / NeuroscienceModerate
- Spinal cord injury / neuroprotection researchNeuropathologyLow
- Neuroendocrine regulation researchEndocrinology / NeuroscienceModerate
Contraindications
- Systemic administration in humans (therapeutic use)Clinical SafetyHigh
- Known hypersensitivity to dynorphin peptidesAllergy / ImmunologyHigh
Adverse Effects
- Cardiovascular depressionCardiovascularUncommon
- DysphoriaPsychiatricCommon
- DiuresisRenalCommon
- Neurotoxicity (high doses, spinal)NeurologicalRare
- SedationCNSCommon
Drug Interactions
- KOR antagonists (e.g., nor-BNI, JDTic)Low
- Naloxone / NaltrexoneModerate
- Mu-opioid agonists (e.g., morphine, fentanyl)Moderate
Population Constraints
- Pregnant or lactating individualsReproductiveAbsolute
- Individuals with psychiatric disordersPsychiatricRelative
- Human subjects (general)Clinical PopulationAbsolute
Regulatory Status
- European UnionUnapprovedNo EMA approval; used solely in preclinical and basic research.
- United StatesUnapprovedResearch compound only; not FDA-approved for any therapeutic indication.
- United KingdomUnapprovedNo MHRA approval; research use only.
Dynorphin itself is not an approved therapeutic drug in any major jurisdiction. It is used exclusively as a research compound to study opioid receptor pharmacology and related CNS pathways.
Evidence & Sources
No sources recorded yet.