Dermorphin 5mg: Research Peptide Profile

Dermorphin is a naturally occurring heptapeptide known for its exceptional potency and selectivity as a µ-opioid receptor (MOR) agonist. This profile provides essential information for researchers working with this compound.

What is Dermorphin?

Dermorphin is a natural heptapeptide with the sequence H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2 . It is a µ-opioid receptor (MOR) agonist originally isolated from the skin of the South American frog Phyllomedusa sauvagei .

Key Identifiers:

• CAS Number: 77614-16-5 

• Molecular Formula: C₄₀H₅₀N₈O₁₀ 

• Molecular Weight: 802.87 g/mol 

• Purity: Typically ≥98% for research-grade material 

Physical Properties:

• Soluble in water (up to 120 mg/mL) 

• Store at -20°C for long-term stability 

Mechanism of Action: µ-Opioid Receptor Agonist

Dermorphin functions primarily as a potent and selective agonist at the µ-opioid receptor (MOR) . It demonstrates high affinity for MOR (Ki = 0.54 nM) and significant selectivity over δ-opioid receptors (Ki = 929 nM) .

The peptide also shows interaction with ε-opioid receptors, while having questionable interaction with δ receptors and no effect on κ receptors .

Unique Structural Feature

A defining characteristic of dermorphin is its D-Alanine residue at the second position, a post-translational modification that is essential for its biological activity. The synthetic L-form (with L-Ala²) is almost completely devoid of opioid receptor affinity and pharmacological activity . This D-amino acid incorporation contributes to dermorphin’s high potency and enzymatic stability .

Receptor Internalization

Research indicates that dermorphin’s analgesic effects are linked to its ability to induce µ-opioid receptor internalization. Blocking this internalization process attenuates antinociception, suggesting that internalization is an integral part of the signaling pathway .

Research Applications

1. Analgesic Research

Dermorphin is primarily studied as a powerful tool for investigating opioid analgesia. Preclinical data demonstrates potent antinociceptive effects in models such as the hot-plate and tail-flick tests . Initial clinical assessment indicated it was superior to morphine in several respects, though toxicity reactions have restricted full clinical trials .

2. Neuropathic Pain Models

Dermorphin analogs, particularly the peripherally restricted [D-Arg², Lys⁴] (1–4) amide (DALDA), are being investigated in rat models of chemotherapy-induced neuropathic pain (CINP) . These studies aim to explore the therapeutic potential of peripheral µ-opioid receptor activation while minimizing central side effects like sedation and addiction .

3. Gastrointestinal Motility

Dermorphin has been shown to delay gastric emptying, inhibit gastric acid secretion, and slow colonic motility in pylorus-ligated rats .

4. Anti-Doping Research

Dermorphin has emerged as a substance of concern in equine sports, leading to the development of specific detection methods (LC-MS/MS) following positive tests in racehorses between 2012-2013 .

Safety & Regulatory Status

FDA Status

Dermorphin is not FDA-approved for any human therapeutic indication. It has no Investigational New Drug (IND) application or New Drug Application (NDA) on file, and there is no legal pathway for human use or compounding in the United States .

Prohibited Status

• Horse Racing: The Association of Racing Commissioners International (ARCI) classifies dermorphin as a Class 1 prohibited substance (Penalty Class A), the highest severity tier .

• Human Sport: It would fall under the WADA S0 (non-approved substances) category, making it prohibited in human sports as well .

Key Safety Considerations

• Potency: Dermorphin is estimated to be 30 to 40 times more potent than morphine, meaning dose estimation errors carry severe consequences .

• Respiratory Depression: As a full µ-opioid agonist, it carries a high risk of respiratory depression .

• Unregulated Products: Research-chemical grade material is unregulated and carries unknown contamination and dosing risks .

Reconstitution & Handling for Research

Solubility & Storage

• Solubility: Soluble in water; prepare stock solution at concentrations up to 120 mg/mL .

• Stock Solution Storage: Store at -80°C for up to 6 months or at -20°C for up to 1 month. Avoid repeated freeze-thaw cycles by storing in separate aliquots .

General Handling

• Dermorphin is for in vitro research use only.

• Work in a controlled laboratory environment with appropriate safety protocols.

• Do not use in humans or animals outside approved research protocols.

Frequently Asked Questions

What is the primary mechanism of Dermorphin?

Dermorphin acts as a potent and selective agonist at the µ-opioid receptor (MOR). Its unique D-Ala² residue is essential for high-affinity receptor binding and pharmacological activity .

Is Dermorphin FDA-approved?

No. It is not FDA-approved for any indication and there is no legal pathway for human use in the United States .

How potent is Dermorphin compared to morphine?

Dermorphin is estimated to be 30 to 40 times more potent than morphine at the µ-opioid receptor .

Why is the D-Ala residue important?

The D-Ala at position 2 is a post-translational modification essential for opioid receptor binding and activity. The synthetic L-form is almost completely inactive .

What are the research applications of Dermorphin?

Dermorphin is studied as a research tool in analgesia, neuropathic pain models, and gastrointestinal motility. It has also been a subject of anti-doping research in equine sports .