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Dermorphin research

What published studies found for Dermorphin: 8 papers, 1 in humans, with sample sizes and key results.

B
Some human evidence
Why: One 1985 randomized trial (150 postoperative patients) of intrathecal dermorphin for pain; everything else is animal pharmacology and reviews.

Dermorphin is a frog-skin opioid peptide that acts as a highly potent, selective mu-opioid agonist (reported 30-40 times more potent than morphine); most of the evidence is animal pharmacology and reviews. It has no approved human use and is a banned doping agent that was misused in horse racing. One 1985 randomized double-blind trial (150 postoperative patients) found intrathecal dermorphin gave longer pain relief than intrathecal morphine or intramuscular pentazocine, but it has never been repeated.

✓ 2 positive~ 1 mixed? 5 inconclusive

Only one human trial (1985, intrathecal use) reports side effects: urinary retention, vomiting and headache, not significantly different from morphine or pentazocine groups; broader opioid-class risks are uncharacterized for dermorphin.

US compounding: Not compoundable. Not an FDA-approved drug and not nominated for FDA's 503A bulks list, so US pharmacies can't legally compound it. Status for every peptide.

Browse and filter these papersDermorphin prices and vendors

Reported side effects

Human studies

✓ Positivehuman RCTPeptides · 1985

Intrathecal dermorphine in postoperative analgesia.

n = 150 humansProspective randomized double-blind comparison of intrathecal dermorphine, intrathecal morphine and intramuscular pentazocine

150 postoperative patients: intrathecal dermorphin (20 micrograms) gave pain relief lasting about 43 h versus 34 h for intrathecal morphine and 11 h for intramuscular pentazocine, with similar side effects.

Key resultAnalgesia lasted 43.41 +/- 1.64 hr with dermorphine vs 34.45 +/- 2.35 hr with morphine and 10.79 +/- 2.23 hr with pentazocine.
Studied
Patients after elective surgery
Compared with
Intrathecal morphine (500 micrograms); intramuscular pentazocine (30 mg)
Main outcome
Duration of postoperative pain relief
Sample
150 consecutive patients after elective surgery
Authors' conclusion
Intrathecal dermorphine produced profound, longer-lasting analgesia; urinary retention, vomiting and headache were not significantly different between groups.
Limitations
1985 trial; abstract gives limited methods detail.

Reviews

? InconclusivereviewJ Pain Res · 2018

Rediscovery of old drugs: the forgotten case of dermorphin for postoperative pain and palliation.

No new dataNarrative review / drug-repurposing analysis

Review arguing for re-examining intrathecal dermorphin for postoperative and palliative pain; it notes a single 1985 randomized placebo-controlled trial reported superiority over placebo and morphine, after which the drug was never developed clinically.

Authors' conclusion
A 1985 randomized placebo-controlled trial reported intrathecal dermorphin impressively superior to placebo and morphine in postoperative pain, yet it was never developed clinically; the authors suggest new studies of safety and efficacy.
Limitations
Review resting largely on one 1985 trial and animal data; no new data.
? InconclusivereviewPeptides · 2000

Pharmacology of amphibian opiate peptides.

No new dataNarrative pharmacology review

Pharmacology review: dermorphins are selective mu-opioid agonists from Phyllomedusa frog skin whose D-amino acid at position 2 underlies their potency, offering models for novel analgesics.

Authors' conclusion
Dermorphins are selective mu-opioid agonists from frog skin containing a D-amino acid at position 2; they provided models for novel analgesics with enhanced benefits and reduced toxicity.
Limitations
Narrative review with no original data.
? InconclusivereviewPeptides · 2011

Dermorphin tetrapeptide analogs as potent and long-lasting analgesics with pharmacological profiles distinct from morphine.

No new dataNarrative review of dermorphin N-terminal tetrapeptide analogs

Review of dermorphin tetrapeptide analogs: in animals they produce antinociception stronger than morphine by various routes and some show pharmacological profiles distinct from morphine.

Authors' conclusion
D-Arg2 tetrapeptide analogs show antinociceptive activity greater than morphine by various routes, and some stimulate dynorphin release, which may reduce side effects; they may be targets for novel analgesics with fewer side effects.
Limitations
Narrative review; only a handful of analogs developed.
? InconclusivereviewGen Pharmacol · 1996

The dermorphin peptide family.

No new dataNarrative review

Review of the dermorphin peptide family: potent mu-opioid analgesics in rodents and primates including man, with less tolerance and dependence than morphine in rodents; evidence cited is largely preclinical.

Authors' conclusion
Dermorphins are potent analgesics with higher efficacy and potency than morphine in rodents and less tolerance, dependence and opiate side effects in chronically exposed rats and mice.
Limitations
Narrative review; mostly animal data.

Animal & lab studies

? InconclusiveanimalJ Vet Pharmacol Ther · 2015

Pharmacokinetics and pharmacodynamics of dermorphin in the horse.

n = 10 animalsPharmacokinetic and pharmacodynamic studyPlasma detection to 12 h; urine 48-72 h

In 10 horses given dermorphin IV or IM, the half-life was under an hour; IV dosing caused excitation and increased heart rate, and the drug was detectable in urine for 48-72 hours.

Key resultIV elimination half-life 0.76 +/- 0.22 h; IM terminal half-life 0.68 +/- 0.24 h; IM bioavailability 47-100% (n=3); heart-rate EC50 21.1 +/- 8.8 ng/mL; detected in plasma 12 h and urine 48 or 72 h
Studied
Horses given dermorphin (9.3 +/- 1.0 ug/kg) intravenously and/or intramuscularly
Main outcome
Plasma concentration-time profile, heart rate and behavior, urinary excretion
Sample
10 horses
Authors' conclusion
Dermorphin has a short half-life in horses, with excitation and increased heart rate after IV dosing only, and remains detectable in urine for 48-72 h.
Limitations
Small number of horses; IM bioavailability in only 3 horses.
✓ PositiveanimalToxicol Appl Pharmacol · 2026

Dermorphin blocks apneic response to intravenous bolus injection of fentanyl.

AnimalsAnimal study of intravenous bolus dermorphin and fentanyl, with naloxonazine

Anaesthetized rats: dermorphin pretreatment blocked the apnoea caused by an intravenous bolus of fentanyl, though dermorphin itself caused a brief apnoea on first injection.

Key resultRespiratory recovery after dermorphin took 0.5 min vs 30 min after fentanyl.
Studied
Anesthetized, spontaneously breathing rats
Main outcome
Cardiorespiratory responses; fentanyl-induced apnea
Authors' conclusion
Dermorphin pretreatment prevented fentanyl-induced apnea in rats, suggesting a possible countermeasure, though dermorphin itself triggered a brief apnea acting on mu1 opioid receptors.
Limitations
Rat study, acute respiratory model only.
~ Mixedin vitroEur J Pharmacol · 1994

Dermorphin-induced hyperexcitability in hippocampal CA3 and CA1 in vitro.

AnimalsIn vitro electrophysiology of dermorphin, an inactive analogue and naloxone

Rat hippocampal slices: dermorphin (50-100 nM) enhanced CA3 responses and at 500 nM caused epileptiform bursting, an effect blocked by naloxone, supporting a pro-convulsant risk from excess mu-opioid activation.

Key resultThreshold CA3 responses were markedly enhanced at 50-100 nM; at 500 nM all responses became epileptiform.
Studied
Rat hippocampal slices
Main outcome
Population responses in CA3 and CA1
Authors' conclusion
Excessive mu-opioid receptor activation can be proconvulsant in hippocampus, though at normal levels receptors may act as facilitatory modulators.
Limitations
Brain slice study.

Verdicts are judged on each paper's own main outcome; grades run from A (strong human evidence) to D (little or none). Details are read from the abstracts, and figures are reproduced only from openly licensed full texts. Not medical advice.