Dermorphin
A potent opioid heptapeptide originally isolated from the skin of South American Phyllomedusa frogs, containing an unusual D-alanine residue. It is a strong mu-opioid agonist most notorious as a doping agent in horse racing rather than a cosmetic or approved therapeutic.
01 Overview
Dermorphin is a naturally occurring opioid peptide roughly an order of magnitude more potent than morphine at the mu-opioid receptor, owing partly to its D-amino-acid content which resists peptidase breakdown. It produces analgesia and central opioid effects.
Its practical notoriety comes from horse-racing doping, where it was used as an undetectable painkiller/performance agent, prompting regulatory testing. It has no approved human therapeutic role, and as a potent opioid it carries the full opioid risk profile including respiratory depression and dependence.
02 Mechanism
High-affinity, highly selective mu-opioid receptor agonist; a D-alanine residue confers resistance to enzymatic degradation and prolongs activity.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Experimental (no human indication) | 1–10 mcg/kg | IV | No approved human dosing; figures reflect research/veterinary misuse contexts only. |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Potent analgesiaStrong opioid analgesia in animal studies; not developed for human therapeutic use. | >10x morphine potency (models) | Preclinical | |
| Central opioid effectsProduces typical mu-opioid CNS effects, the basis of both its misuse and its danger. | Sedation, euphoria | Preclinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Respiratory depressionAs a potent mu-agonist it can suppress breathing, the principal lethal opioid risk. | Life-threatening | Dose-dependent | Preclinical | |
| Dependence and toleranceRepeated opioid exposure produces tolerance and physical dependence. | Severe | With repeated use | Preclinical |