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 |
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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.