1. What is Dermorphin?
Dermorphin is a naturally occurring opioid peptide originally isolated from the skin of the South American frog Phyllomedusa sauvagii. It has attracted significant research interest due to its high affinity for μ-opioid receptors (MORs) and unique structural properties that distinguish it from classical opioid compounds. Dermorphin continues to serve as a valuable tool in neuropharmacology and receptor biology research 【1】.
2. Dermorphin Structure
Molecular Formula:C₄₀H₅₀N₈O₁₀
6Molecular Weight:802.9g/mol
CAS Number:77614-16-5
3. Dermorphin Research
Research Overview
Dermorphin is studied as a selective μ-opioid receptor agonist with distinctive binding characteristics. In preclinical models, it has been shown to interact with MORs in ways that provide insights into pain modulation, receptor signaling, and opioid pharmacology 【2】.
【1】 Mechanism of Action
Dermorphin binds selectively to μ-opioid receptors and triggers G-protein coupled signaling cascades. In laboratory models, this has been associated with:
l Reduced neuronal excitability and nociceptive signaling
l Modulation of endorphin-related pathways
l Extended receptor activation due to resistance to enzymatic degradation
Because of its unique structure, dermorphin demonstrates greater receptor affinity compared to morphine in comparative assays.
【2】 Research Applications
Dermorphin has been investigated in several research contexts, including:
l 🧬 Pain pathway studies, to understand central opioid receptor function
l 🧪 Comparative pharmacology, assessing potency and receptor selectivity relative to other opioids
l 🧠 Neuropharmacology, focusing on peptide-receptor interactions in the CNS
l 🧩 Addiction and tolerance research, as a model for studying receptor desensitization and dependence mechanisms
【3】 Tool in Experimental Biology
Dermorphin and its analogs have also been adapted as biotechnological tools:
l Fluorescent dermorphin analogs enable visualization of μ-opioid receptor trafficking 【3】
l Synthetic derivatives such as DALDA (Dermorphin [D-Arg², Lys⁴] amide) are studied in peripheral opioid receptor research 【4】
✅ Why Consider Dermorphin (Research Context)?
l High μ-opioid receptor selectivity and binding affinity
l Structural resistance to enzymatic degradation, enabling extended receptor interaction
l Serves as a research model for pain modulation and neuropharmacology
l Provides insights into opioid tolerance and receptor desensitization
l Basis for development of dermorphin analogs in receptor-targeted studies
4. Future Dermorphin Research
Future directions include:
l Peripheral-selective analogs: Compounds such as DALDA and glycodermorphins are being evaluated in preclinical models as μ-opioid receptor agonists with potentially reduced CNS involvement 【5】.
l Neuropharmacology tools: Labeled dermorphin analogs are applied in receptor imaging to study opioid signaling dynamics.
l Analogue-based drug discovery: Tetrapeptide derivatives are of interest for developing novel μ₁-biased ligands with improved selectivity.
5. Application Area
Dermorphin is primarily studied in the following research fields:
l 🧪 Laboratory research on pain signaling and opioid receptor selectivity
l 🧬 Neuropharmacology studies involving central nervous system peptide signaling
l 🔬 Analgesic peptide development and analog screening in experimental pharmacology
l 🧠 Receptor desensitization and tolerance mechanisms
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