Leu-Enkephalin

Pain / Immune

Also known as: Leucine-Enkephalin, LENK, Tyr-Gly-Gly-Phe-Leu

Endogenous Opioid PeptidesResearch phase: Endogenous peptide (well characterized)Regulatory: Endogenous peptide. Not used clinically as a drug.

Mechanism

Leu-enkephalin is the sister peptide to met-enkephalin, differing by just one amino acid (leucine instead of methionine at position 5). It is derived from both proenkephalin and prodynorphin precursors. Like met-enkephalin, it primarily activates delta-opioid receptors to modulate pain, but it also has affinity for kappa-opioid receptors.

Technical detail

Leu-enkephalin (Tyr-Gly-Gly-Phe-Leu) is a pentapeptide derived from both proenkephalin (PENK) and prodynorphin (PDYN) processing. It has high affinity for delta-opioid receptors (DOR) and moderate affinity for kappa-opioid receptors (KOR). DOR activation produces Gi/Go-mediated inhibition of adenylyl cyclase and voltage-gated Ca2+ channels, modulating nociception in the spinal dorsal horn and periaqueductal gray. Leu-enkephalin is more resistant to aminopeptidase degradation than met-enkephalin due to the Leu5 substitution. Also modulates immune function via opioid receptors on lymphocytes and NK cells.

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