Leu-enkephalin

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[ Other Name] Leucine Enkephalin; [Leu5]-Enkephalin
[ Sequence ] Tyr-Gly-Gly-Phe-Leu
[ CAS NO. ] 58822-25-6
[ Molecular Formula ] C28H37N5O7
[ Molecular Weight ] 555.62
[ Appearance ] White Powder
[ Purity ] ≥98%

[ Function ]
Its primary functions are pain relief and the modulation of pain sensitivity; it acts by binding to opioid receptors, producing effects similar to morphine but originating from within the body. Beyond pain relief, it is involved in regulating body temperature, cardiovascular function, and the release of endocrine hormones; some studies have also identified its expression in the pancreas, suggesting a potential role in processes such as insulin secretion.

About Leu-enkephalin
Leu-enkephalin is an endogenous neuropeptide with significant pharmacological activity in living organisms. Chemically, it consists of five amino acid residues with the sequence Tyr-Gly-Gly-Phe-Leu (abbreviated as YGGFL). As a pentapeptide, it exhibits pharmacological properties similar to morphine, acting notably as an agonist at opioid receptors. It is an endogenous opioid peptide produced in vertebrate species—including rodents, primates, and humans—through the cleavage of proenkephalin or prodynorphin.
As an endogenous opioid peptide, Leu-enkephalin primarily acts on opioid receptors in the central nervous system—such as the μ, δ, and κ receptors—showing a particularly high affinity for the δ receptor. Upon binding to the receptor, it activates G proteins coupled to the receptor, thereby inhibiting adenylate cyclase activity and reducing intracellular cAMP production. This cascade modulates ion channel activity—such as closing voltage-gated calcium channels and opening potassium channels—ultimately leading to neuronal hyperpolarization and the inhibition of neurotransmitter release, which produces physiological effects like analgesia. Recent research indicates that, beyond its classic analgesic role, Leu-enkephalin plays a significant part in regulating mood and immune function. Studies using animal models of depression suggest it participates in mood regulation by modulating neurotransmitter systems, while within the immune system, it regulates immune cell activity and cytokine secretion.
Mechanistically, Leu-enkephalin exerts its regulatory effects by binding to specific receptors in the brain. It not only alleviates pain but also influences mood and behavior, and in some instances, promotes feelings of pleasure. The release and action of this peptide are part of complex physiological processes involving neurotransmitter release and receptor activation.