Dermorphin
Heptapeptide μ-Opioid Receptor AgonistFor research use only
Dermorphin is a natural heptapeptide (H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2) originally isolated from Phyllomedusa frog skin secretions. It is a highly potent and…
Half-life
Short and context-dependent; rapid plasma degradation typical of peptides (minutes to low hours in preclinical models). Central effects may outlast plasma exposure.
Delivery
Primarily central routes in animal research (e.g., intrathecal, intracerebroventricular). Peripheral or intranasal routes have limited CNS penetration due to peptide nature; carrier systems or analogs are often explored in preclinical work.
Suggested dosage
Not specified
Usage
Employed in pain and neuropharmacology research to study μ-receptor activation, G-protein/β-arrestin signaling, antinociception, tolerance development, and receptor selectivity versus δ/κ pathways.
Mechanism of action
Binds μ-opioid receptors (MOR) with high affinity; activates Gi/o proteins to inhibit adenylyl cyclase, reduce cAMP, open GIRK channels, and inhibit voltage-gated Ca2+ channels—dampening neurotransmitter release in pain pathways.
Benefits (3)
- Robust antinociceptive effects in animal models
- High μ-receptor selectivity versus other opioid receptors
- Tool compound for biased-agonism and tolerance studies
Side effects (6)
- Respiratory depression
- Sedation, dizziness, nausea
- Pruritus and constipation
- Bradycardia or hypotension (dose/context-dependent)
- Tolerance, dependence, and withdrawal with repeated exposure
- Risk of misuse/abuse; clinical use is generally not approved
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