Leuphasyl® is a pentapeptide (also known as Pentapeptide-18 with sequence Tyr-D-Ala-Gly-Phe-Leu) that modulates Ca2+ channels in vitro. It is an enkephalin-like peptide that has proven effective in reducing expression wrinkles with an alternative mechanism to Botulinum toxin-like molecules. It is a shorter analog of the opioid hexapeptide Dalargin (sequence Tyr-D-Ala-Gly-Phe-Leu-Arg), used to control gastric acidity and regulate gastrointestinal motility.
Endogenous enkephalins are endogenous opioids that inhibit neuronal activity. Their receptors are located on the outside of neurons, coupled to G proteins of the inhibitory type (Gi). The docking of enkephalin molecules in these receptors results in the release of the G protein subunits (alpha, beta, gamma) within the cell.
These subunits close Ca2+ channels and open K+ channels. Preventing the entry of Ca2+ into the neuron avoids vesicle fusion and consequently inhibits acetylcholine release across the synapse to the muscle.
Pentapeptide-18 acts similarly to natural enkephalins (as shown in an in vitro study): it binds to the enkephalin receptor on the surface of nerve cells. When Leuphasyl® couples to the receptor, a conformational change initiates a cascade inside the neuron that decreases its excitability: nerve cell activity is "turned down," and the release of acetylcholine is modulated. As a result, muscle contraction will be relaxed, and therefore, expression wrinkles will be diminished.Ingredients
Efficiency tests of Pentapeptide-18 showed that it is less effective than Botox injections, but it is safe, has no adverse effects, and preserves facial expressivity. Combined with other synaptic blockers, such as Argireline, it showed a potentiating effect, yielding more noticeable results.
