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Dermorphin

Research

Also known as: Frog Opioid Peptide, YAGFLM-NH2

Half-life: ~30-60 minutes

Last reviewed:  ·  Published:

Anti Inflammatory

Overview

Dermorphin is a seven-amino-acid peptide originally isolated from the skin of South American Phyllomedusa frogs (most notably Phyllomedusa sauvagei). It is one of the most potent endogenous opioid receptor agonists known, with selective activity at the μ-opioid receptor (MOR) and analgesic potency in animal models 30-40 times greater than morphine on a per-mole basis. The peptide contains an unusual D-alanine at position 2 — one of the few naturally occurring D-amino acids found in vertebrates — which is essential for its potency and stability against enzymatic degradation.

Dermorphin has been of substantial pharmacological research interest since its discovery, as a probe for μ-opioid receptor pharmacology and as a starting point for the design of synthetic opioid analgesics. It has also gained notoriety as a doping agent in horse racing, where it has been detected in multiple high-profile cases of horses found to have anomalous analgesia or performance enhancement. Several US racing jurisdictions have specific regulations against Dermorphin use.

This peptide is included on this site for completeness because it is sold by uk-peptides.com and other research-chemical vendors. It is not a wellness peptide. Dermorphin is a potent opioid with all the addiction, respiratory-depression, and overdose risks of other strong opioids — those risks are likely amplified rather than reduced by the higher receptor selectivity and potency. Use of Dermorphin outside of a properly designed and reviewed research protocol is unsafe, very likely illegal (as an unscheduled opioid in most jurisdictions), and almost always inappropriate.

History

Dermorphin was first isolated and characterized in 1980 by the Italian research group of Pietro Melchiorri and Vittorio Erspamer from the skin secretions of Phyllomedusa sauvagei. Erspamer's prior work had established the existence of biologically active peptides in amphibian skin (he had previously discovered bombesin and other peptides). The unusual D-amino acid content and high μ-opioid receptor selectivity of dermorphin opened new directions in opioid pharmacology. The peptide has remained a research tool and a recognized doping agent in equine sport, but has never been developed for legitimate human clinical use.

Effects

  • Potent selective μ-opioid receptor agonism
  • Analgesia 30-40× more potent than morphine
  • Sedation and respiratory depression
  • Euphoria (opioid effect)
  • Tolerance and physical dependence develop rapidly with repeated use

Side Effects

  • Respiratory depression (life-threatening at high doses)
  • Sedation, drowsiness
  • Nausea and vomiting
  • Severe constipation
  • Physical dependence and addiction
  • Overdose risk
  • Hyperalgesia with chronic use
  • Hormonal suppression (testosterone, cortisol)

Tolerability

Dermorphin is acutely tolerated as expected for a potent opioid — that is to say, it produces all the effects and risks of an opioid drug. Repeated use produces tolerance, physical dependence, and the full constellation of opioid use disorder risks. Overdose is a meaningful risk because of the high per-mole potency: errors in dosing are amplified relative to morphine. This is not a peptide suitable for self-experimentation or off-protocol use under any circumstances.

Dosing Ranges

Animal opioid pharmacology research

Dose Range

Per protocol (typically µg/kg)

Frequency

Per protocol

Duration

Per protocol

Human self-experimentation

Dose Range

Not appropriate under any circumstances

Frequency

Duration

Dosing information is for educational purposes only. Consult a healthcare professional before using any peptide.

Reconstitution

Preparation Details

Typical Vial Size

2 mg

Water Type

Bacteriostatic water (BAC water)

Mixing Volume

1-2 mL

Half-Life

~30-60 minutes

Molecular Weight

802.9 Da

Store reconstituted vial refrigerated at 2-8°C. Use within 14-21 days. Note: this is a research opioid with all the risks of high-potency opioid drugs. Self-administration carries serious risk of overdose and addiction.

Calculate Dermorphin dose

Where to buy Dermorphin

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Regulatory Status

FDA Status

Not FDA approved. Not scheduled in the US (research peptide status), but functionally an unregulated opioid.

Legal Status

Legal status varies by jurisdiction. Banned in equestrian sport. Recognized as a doping agent. Sale and use as a research chemical exists in a regulatory grey zone in most countries.

USA

Not approved

Research chemical; banned by major racing jurisdictions

EU

Not approved

Not authorized as medicinal product; banned in equestrian sport

UK

Not approved

Classified as research chemical; equestrian sport banned

Australia

Not approved

TGA has not authorized; equestrian sport banned

Canada

Not approved

Not authorized for human use

Cited Studies

Deltorphins: a family of naturally occurring peptides with high affinity and selectivity for delta opioid binding sites

Erspamer V, Melchiorri P, Falconieri-Erspamer G, Negri L, Corsi R, Severini C, Barra D, Simmaco M, Kreil G

Proceedings of the National Academy of Sciences (1989)

Comprehensive overview of the amphibian opioid peptide family discovered by the Erspamer group, including dermorphin and the related deltorphins, establishing the unusual D-amino acid pharmacology that defines this peptide class.

View Study →

Dermorphin: an opioid peptide from amphibian skin active on the mammalian central nervous system

Broccardo M, Erspamer V, Falconieri Erspamer G, Improta G, Linari G, Melchiorri P, Montecucchi PC

British Journal of Pharmacology (1981)

Original pharmacological characterization of dermorphin demonstrating its potent CNS opioid activity and establishing its position as one of the most potent natural μ-opioid agonists known.

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Detection of dermorphin in racing horse urine — a case study from the regulatory laboratory

Maylin GA, Carlson G

Journal of Analytical Toxicology (2013)

Forensic / regulatory analysis of dermorphin detection in racing horse samples, illustrating the doping context that drives much of the modern regulatory and analytical interest in this peptide.

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