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Leu-Enkephalin

Leu-enkephalin is an endogenous opioid peptide that acts as an agonist at μ-opioid receptors (μORs) and δ-opioid receptors (δORs). Met-enkephalin exhibits neuromodulatory, antinociceptive/analgesic, and gastrointestinal motility modulating activities. Like other endogenous opioids, leu-enkephalin modulates expression of opioid receptors and plays a role in reward/reinforcement signaling. Leu-enkephalin increases pain thresholds in vivo and inhibits gastrointestinal muscle contractility in other animal models, inhibiting motility and gastric emptying.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18938775

Cas No.

58822-25-6

Purity

≥95%

Formula

C28H37N5O7

Formula Wt.

555.62

IUPAC Name

2-[[2-[[2-[[2-[[2-amino-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoic acid

Synonym

1-5-b-Neoendorphin (human) (9CI)

Appearance

White to off white powder

Popov M, Abu Hammad I, Bachar T, et al. Delivery of analgesic peptides to the brain by nano-sized bolaamphiphilic vesicles made of monolayer membranes. Eur J Pharm Biopharm. 2013 Nov;85(3 Pt A):381-9. PMID: 23791683.

Crayton R, Soller W, Mattiasson A, et al. Exogenously administered opioids contract the female rat intrinsic urethral sphincter in vivo. Neurourol Urodyn. 2010 Jun;29(5):777-82. PMID: 19899147.

Holzer P. Opioid receptors in the gastrointestinal tract. Regul Pept. 2009 Jun 5;155(1-3):11-7. PMID: 19345246.

Del Borgo MP, Blanchfield JT, Toth I. Internalisation of the mu-opioid receptor by endomorphin-1 and leu-enkephalin is dependant on aromatic amino acid residues. Bioorg Med Chem. 2008 Apr 15;16(8):4341-6. PMID: 18329886.

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