Leuphasyl
Also known as: Acetyl Tyr-D-Ala-Gly-Phe-Leu-OH · Enkephalin analog · Argireline synergist
Leuphasyl is an analogue of Met-enkephalin (a natural opioid neuropeptide) that binds to opioid receptors (predominantly delta-opioid receptors) at the presynaptic membrane of motor neurons. Opioid receptor activation at the NMJ inhibits adenylyl cyclase, reduces cAMP, activates K+ channels (hyperpolarization),...
What It Is
Leuphasyl is an analogue of Met-enkephalin (a natural opioid neuropeptide) that binds to opioid receptors (predominantly delta-opioid receptors) at the presynaptic membrane of motor neurons. Opioid receptor activation at the NMJ inhibits adenylyl cyclase, reduces cAMP, activates K+ channels (hyperpolarization), and inhibits Ca²⁺ influx — thereby reducing neurotransmitter (acetylcholine) release. This is mechanistically upstream and complementary to Argireline/Snap-8's SNARE-inhibiting mechanism. Clinical studies combining Leuphasyl (5%) + Argireline (5%) demonstrated greater wrinkle reduction than either peptide alone, confirming the dual-pathway synergy.
Supplies Needed
Active ingredient
Topical delivery vehicle
Verify formulation pH 5u20137 for peptide stability
Storage
Store at -20°C in powder form; stable 2+ years
Finished formulation: room temperature 6–12 months with preservation
This information is provided for educational and research purposes only. Not approved for human consumption by the FDA or any regulatory body. Always consult a qualified medical professional.
Dosing Protocols
Timing: Evening. Often formulated together with Argireline in commercial anti-wrinkle products
↓ Apply these values to the reconstitution calculatorTiming: Morning and evening. This specific combination (5%+5%) was used in published efficacy studies showing synergistic wrinkle reduction
↓ Apply these values to the reconstitution calculatorTiming: Morning and evening. Triple peptide NMJ inhibitor cocktail for maximum expression wrinkle reduction
↓ Apply these values to the reconstitution calculatorWeekly Timeline
| Week | Expected Effects |
|---|---|
| Week 1 | Subtle skin smoothing; peptide accumulating at NMJ |
| Week 2 | Early reduction in expression line visibility with consistent twice-daily use |
| Week 4 | Synergistic wrinkle reduction when combined with Argireline; measurable depth reduction |
| Week 8 | Maximum anti-wrinkle effect; sustained improvement with continued use |
Reconstitution Calculator
1 unit on U-100 syringe = 0.01 mL · Always label your vial after reconstitution
Injection Technique & Reconstitution
- Leuphasyl is supplied as a white powder or in solution concentrate
- Dissolve in water phase at 0.5u20131% (for 5% final product, check supplier stock concentration)
- Add to serum or emulsion at room temperature
- Avoid temperatures above 40u00b0C
- Store in sealed, dark container at room temperature; refrigerate if formulating without preservatives
Use our free Leuphasyl calculator to get the exact syringe units for your vial size and dose.
Mechanism of Action
Leuphasyl is an analogue of Met-enkephalin (a natural opioid neuropeptide) that binds to opioid receptors (predominantly delta-opioid receptors) at the presynaptic membrane of motor neurons. Opioid receptor activation at the NMJ inhibits adenylyl cyclase, reduces cAMP, activates K+ channels (hyperpolarization), and inhibits Ca²⁺ influx — thereby reducing neurotransmitter (acetylcholine) release. This is mechanistically upstream and complementary to Argireline/Snap-8's SNARE-inhibiting mechanism. Clinical studies combining Leuphasyl (5%) + Argireline (5%) demonstrated greater wrinkle reduction than either peptide alone, confirming the dual-pathway synergy.
Key Research Papers
Clinical study demonstrating 5% Argireline + 5% Leuphasyl produced statistically significant synergistic reduction of periorbital wrinkle depth greater than either peptide alone after 28 days.
View on PubMed →Stacks Well With
The clinically validated combination u2014 Leuphasyl inhibits ACh release via opioid receptor/Cau00b2u207a inhibition while Argireline inhibits via SNARE disruption; dual pathway produces synergistic wrinkle reduction
Triple combination (Leuphasyl + Argireline + Snap-8) targets three points in the NMJ signaling cascade for maximum muscle relaxation
Leuphasyl prevents wrinkle deepening; Palmitoyl Tripeptide-1 rebuilds the structural collagen matrix u2014 muscle relaxation plus structural repair
Frequently Asked Questions
Leuphasyl and Argireline inhibit acetylcholine release via completely different mechanisms u2014 Leuphasyl via delta-opioid receptors (upstream Cau00b2u207a inhibition) and Argireline via SNARE complex disruption (downstream). Their combination is synergistic, not redundant.
No u2014 topical opioid receptor activation at superficial skin NMJ junctions does not produce systemic opioid effects (sedation, analgesia, or addiction potential). The concentrations and absorption are far too low.
The clinically studied ratio is 5% Leuphasyl + 5% Argireline. Some formulations use 3% Leuphasyl + 7% Argireline. Equal ratios appear optimal for synergy.
Legal Status by Region
This information is provided for educational and research purposes only. Not approved for human consumption by the FDA or any regulatory body. Always consult a qualified medical professional.