Dermorphin
aka DRM
Mechanism
Naturally occurring heptapeptide first isolated from the skin of South American Phyllomedusa frogs. It is a highly selective, potent agonist of the mu-opioid receptor (MOR), reported to be roughly 30-40 times more potent than morphine on a molar basis, with low affinity for delta-opioid receptors. Its activity depends on the unusual D-alanine residue at position 2 (one of the few vertebrate peptides containing a D-amino acid) and C-terminal amidation, which confer resistance to peptidases. Dermorphin is not an approved human drug and has no legitimate clinical or nootropic use; it is studied as a pharmacological probe of opioid signaling.
Studied uses
- research probe for mu-opioid receptor pharmacology
- analgesia studies (animal models)
- no approved or evidence-based human/nootropic use
Identification
| CAS number | 77614-16-5 |
|---|---|
| Molecular formula | C40H50N8O10 |
| Sequence | Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2 |
| Typical dose | No established or legitimate human dose; used only at experimental quantities in laboratory animal studies |
| Half-life | Not well characterized in humans; the D-Ala and C-terminal amide confer greater enzymatic stability than typical endogenous opioid peptides |
Safety
Not FDA-approved; a potent opioid agonist with the attendant risks of respiratory depression, sedation, dependence, and overdose. Dermorphin gained notoriety as an illicit performance-enhancing 'frog juice' doping agent in horse racing and is a Class 1 prohibited substance in equine competition; in human sport it falls under WADA narcotics. Possession/use outside controlled research is illegal in most jurisdictions.
Vendors selling Dermorphin
| Vendor | Size | Price | Listed purity | Trust |
|---|---|---|---|---|
| zztai Peptide Ltd | — | — | — | 43 |
Research
Background Sudden death induced by intravenous bolus (IVb) injection of overdose fentanyl is the major cause of overdose opioid-induced deaths; however, the relevant countermeasure is lacking.
source →The urgent need for sustainable peptide manufacturing has accelerated efforts to replace conventional N , N -dimethylformamide (DMF)-based solid-phase peptide synthesis (SPPS) with greener alternatives.
source →The opioid receptor family comprises classical; MOP (mu/µ), KOP (kappa/k), DOP(delta/δ) receptors along with non-classical Nociceptin/Orphanin FQ (N/OFQ) peptide receptor (NOP). Expression on glial cells is controversial where there is a role for glia and opioids in pain processing and immunomodulation.
source →The hybrid approach remains a compelling strategy for designing molecules that combine enhanced biological activity with a favorable safety profile. Marine peptides, in particular, have attracted significant attention due to their well-documented broad spectrum of biological activities.
source →The neuropeptide's multifaceted involvement in various components of neural homeostasis impacts pain and behavioral regulation. One of the highly potent neuropeptides is dermorphin, extracted from the skin of the Amazon frog ( Phyllomedusa sauvagei ).
source →Opioids are among the most effective drugs for treating moderate to severe pain. Unfortunately, opioid use, even short-term, can lead to addiction, tolerance, overdose, and respiratory depression.
source →Burn injury-induced chronic pain is a highly debilitating condition that profoundly impacts the well-being of military veterans and the general population. Current pain management for burn injured patients mainly relies on central opioids, often causing sedation, addiction, and physical dependence.
source →The analytical and technological approaches employed in doping analysis are constantly reviewed and updated to allow for keeping pace with progresses in pharmaceutical and medicinal research and the therein inherent options of misuse as performance enhancing drugs or methods.
source →Chronic continuous hypoxia (CCH) demonstrates a pronounced protective effect in cardiac ischemia-reperfusion (IR). Opioids and opioid receptors play a significant role in this process. It has been previously shown that metabolic syndrome (MS) impairs the development of adaptive myocardial resistance to IR.
source →Diverse chemical and pharmacological strategies are currently being explored to minimize the unwanted side effects of currently used opioid analgesics while achieving effective pain relief. The use of multitarget ligands with activity at more than one receptor represents a promising therapeutic approach.
source →Development of theranostic nanomedicines to tackle glioma remains to be challenging. Here, we present an advanced blood-brain barrier (BBB)-crossing nanovaccine based on cancer cell membrane-camouflaged poly( N -vinylcaprolactam) (PVCL) nanogels (NGs) incorporated with MnO 2 and doxorubicin (DOX).
source →Cold injury or frostbite is a common medical condition that causes serious clinical complications including sensory abnormalities and chronic pain ultimately affecting overall well-being.
source →