New — Free Peptide Starter Guide (2026): 13 chapters, 34 cited studies

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Pentapeptide-18

Also known as: Leuphasyl, YAGFL, enkephalin analog pentapeptide

Pentapeptide-18 (Leuphasyl) is a synthetic pentapeptide that mimics the sequence of enkephalin, an endogenous neuropeptide. It acts on neuronal pain receptors in facial muscles to reduce muscle contraction intensity and depth of expression lines, functioning similarly to Argireline (Acetyl Hexapeptide-3) but via a different receptor mechanism.

Half-Life

Not applicable (topical)

Route

Topical

Category

Skin & Cosmetic, Anti-Aging & Longevity

Studies

4 references

Key Benefits

  • Reduces depth of expression lines (forehead, crow's feet, glabellar)
  • Inhibits acetylcholine release for muscle-relaxing effect
  • Complementary mechanism to Argireline for enhanced anti-wrinkle activity
  • Reversible and well-tolerated
  • No risk of systemic paralysis at cosmetic concentrations
  • Suitable for daily use in serums and creams

Mechanism of Action

Pentapeptide-18 binds to delta-opioid receptors on nerve terminals, mimicking enkephalin signaling to reduce the release of acetylcholine at the neuromuscular junction. This reduces the amplitude of muscle contractions in facial expression muscles, decreasing the formation of dynamic wrinkles. Unlike botulinum toxin, the effect is reversible and dose-dependent without complete paralysis. When combined with Argireline (which acts on SNAP-25), the two peptides provide complementary inhibition of neurotransmitter release.

Dosing Protocols

Expression Line Reduction (Standard)

Dose
0.005–0.05% in formulation
Frequency
Twice daily
Timing
AM and PM after cleansing, target expression-prone areas
Cycle
8–12 weeks, ongoing

Best combined with Argireline (0.5–1%) for synergistic dual-mechanism anti-wrinkle effect. Apply to forehead, periorbital area, and nasolabial folds. Some formulations combine all three: Pentapeptide-18, Argireline, and SNAP-8.

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Side Effects

  • Generally very well-tolerated topically
  • Rare skin sensitivity or mild irritation
  • Theoretical opioid receptor desensitization with very prolonged high-dose use (not documented cosmetically)

Contraindications

Known opioid peptide sensitivityCaution in pregnancy (insufficient data)

Storage

Store at room temperature in a sealed container away from light. Stable in slightly acidic to neutral pH formulations. Avoid excessive heat.

  1. 1.
    Pentapeptide-18 as an anti-aging candidate: Spectroscopic characterization and molecular interaction analysis

    Akhan D, Bicak B, Akalin E, Gunduz SK · Computational biology and chemistry · 2026PubMed Verified

  2. 2.
    Retinol and Oligopeptide-Loaded Lipid Nanocarriers as Effective Raw Material in Anti-Acne and Anti-Aging Therapies

    Pawłowska M, Marzec M, Jankowiak W, Nowak I · Life (Basel, Switzerland) · 2024PubMed Verified

  3. 3.
    Solid Lipid Nanoparticles Incorporated with Retinol and Pentapeptide-18-Optimization, Characterization, and Cosmetic Application

    Pawłowska M, Marzec M, Jankowiak W, Nowak I · International journal of molecular sciences · 2024PubMed Verified

  4. 4.
    D-tyrosine adds an anti-melanogenic effect to cosmetic peptides

    Park J, Jung H, Jang B, Song HK, Han IO, Oh ES · Scientific reports · 2020PubMed Verified

Medical disclaimer: This information is for educational purposes only and does not constitute medical advice. Many compounds listed are research chemicals not approved for human use. Always consult a qualified healthcare professional before starting any protocol.

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