Dermorphin 99% Purity White Powder

Name:  Lynn
Wechat：  15914422644

Tel：+86  15914422644

Whatsapp: +852 6252 8290

Email：    guangsheng 5   @zgguangsheng.com

1. Core Molecular & Physicochemical Specifications

2. Mechanism of Action

1. Enhanced Receptor Affinity: The D‑configuration optimizes interaction with the MOR binding pocket, increasing potency vs. L‑alanine analogs.
2. Enzymatic Stability: D‑Ala resists proteolytic degradation by peptidases, prolonging half‑life and duration of action.
3. Selectivity: The N‑terminal Tyr‑D‑Ala‑Phe motif ensures preferential binding to MOR over δ or κ opioid receptors.

3. Pharmacological Profile

3.1 Potency & Efficacy

• Analgesia: ED₅₀ of 13–23 pmol/rat (intracerebroventricular), 30–40× more potent than morphine; long‑lasting effects (2–4 hours in rodents).
• In Vitro Activity: 57× more potent than Met‑enkephalin, 39× more potent than morphine on guinea‑pig ileum MOR.
• Tolerance & Dependence: Chronic use induces tolerance and withdrawal (naloxone‑precipitated), similar to other MOR agonists, but lower incidence at equivalent analgesic doses.

3.2 Pharmacokinetics

• Absorption: Poor oral bioavailability (peptide degradation); effective via intrathecal, intracerebroventricular, or subcutaneous injection.
• Half‑Life: 30–60 minutes (systemic); extended to 2–4 hours with D‑Ala‑mediated stability.
• Metabolism: Cleaved by peptidases (e.g., aminopeptidases) at non‑D‑Ala sites; excreted in urine as metabolites.

4. Key Applications

4.1 Research & Preclinical

• Opioid Receptor Pharmacology: Tool to study MOR structure–function and signaling pathways.
• Analgesic Drug Development: Template for designing stable, selective MOR agonists with reduced side effects.
• Neuroscience: Model for pain modulation, reward, and addiction mechanisms.

4.2 Clinical (Historical/Investigational)

• Postoperative Pain: Intrathecal dermorphin showed superior analgesia vs. morphine in small clinical trials (1980s), but limited adoption due to regulatory and safety concerns.
• Palliative Care: Potential for severe pain management (preclinical stage).

4.3 Forensic & Sports

• Doping Agent: Illegally used in horse racing for pain masking; banned by WADA.

5. Quality Control & Production

5.1 Synthesis

• Solid‑Phase Peptide Synthesis (SPPS): Fmoc protection strategy, with D‑Ala incorporated at position 2.
• Purification: Reverse‑phase HPLC (C18 column) to ≥96% purity; lyophilization for stability.

5.2 Quality Testing

• Purity: HPLC (UV detection at 220 nm); mass spectrometry (MS) for molecular weight confirmation.
• Potency: Guinea‑pig ileum or mouse tail flick assay to quantify analgesic activity.
• Sterility: Aseptic filtration (0.22 μm) for injectable formulations.

6. Safety & Handling Guidelines

6.1 Hazards

• Toxicity: LD₅₀ (mouse, i.v.): ~10 μg/kg; high risk of respiratory depression, sedation, and hypotension at supratherapeutic doses.
• Contraindications: Hypersensitivity to opioids; respiratory insufficiency; pregnancy (fetotoxicity).
• Adverse Reactions: Sedation, nausea, vomiting, constipation, respiratory depression (reversible with naloxone).

6.2 Handling Precautions

• Personal Protective Equipment (PPE): Lab coat, gloves, safety goggles; use in fume hood for powder handling.
• Reconstitution: Dissolve in sterile water or 0.9% NaCl; avoid shaking to prevent denaturation.
• Disposal: Follow biomedical waste regulations; incinerate unused material.