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Leucine-enkephalin | CAS 64963-01-5 | Delta Opioid Receptor Agonist for Neuroscience

Product Description

Leucine-enkephalin is a synthetic pentapeptide and a stable analog of the endogenous opioid peptide Leu-enkephalin. By substituting the second amino acid residue with D-alanine, this analog resists enzymatic degradation, leading to prolonged biological activity and greater selectivity toward the delta opioid receptor (DOR). The compound has become a cornerstone in neuropharmacological research, particularly in the study of pain modulation, receptor binding, and neuronal signaling pathways.

Leu-enkephalin, one of the two major enkephalins found in the mammalian central nervous system, plays an essential role in modulating nociceptive transmission, stress response, and emotional regulation. However, native enkephalins are rapidly degraded by peptidases such as enkephalinase and aminopeptidase, which severely limits their in vivo utility. Leucine-enkephalin overcomes this limitation by incorporating a D-alanine residue that resists enzymatic cleavage, resulting in a long-acting delta-selective opioid peptide.

This peptide’s structure enables it to bind efficiently to delta receptors while minimizing interaction with mu and kappa opioid receptors. Such receptor specificity allows researchers to dissect the complex signaling mechanisms of endogenous opioid systems without confounding cross-reactivity. Studies employing Leucine-enkephalin have helped elucidate the delta receptor’s role in neuroprotection, mood regulation, and immune modulation.

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Uploaded on October 28, 2025