| CAS | 189388-22-5 |
| Sequence | H-Tyr-Pro-Trp-Phe-NH2 |
| Sequence Single | YPWF-NH2 |
| Molecular Formula | C34H38N6O5 |
| Molecular Weight | 610.71 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Application | Alzheimer’s Disease|Opioid Research |
| Description | Endomorphin-1 (YPWF-amide) is the most potent and selective endogenous agonist for the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties. It may be a natural ligand for this receptor. Endomorphin-1 has been shown to inhibit the aggregation of Aβ in vitro and is effective in vivo. |
| References | 1. Interleukin-4 and -13 promote basolateral secretion of H(+) and cathepsin L by glomerular epithelial cells. J.G.van den Berg et al., Am. J. Physiol. Renal Physiol., 282, F26 (2002) 2. Endomorphin 1 and 2, endogenous ligands for the mu-opioid receptor, decrease cardiac output, and total peripheral resistance in the rat. R.-s.Zhang et al., Brain Res., 1629, 210 (2015) 3. A potent and selective endogenous agonist for the mu-opiate receptor. H.C.Champion et al., Peptides, 18, 1393 (1997) 4. Structural basis for inhibiting beta-amyloid oligomerization by a non-coded beta-breaker-substituted endomorphin analogue. J.E.Zadina et al., Nature, 386, 499 (1997) 5. Morphine protects against intracellular amyloid toxicity by inducing estradiol release and upregulation of Hsp70. A.Frydman-Marom et al., ACS Chem. Biol., 6, 1265 (2011) 6. The effects of endomorphins on striatal [3H]GABA release induced by electrical stimulation: an in vitro superfusion study in rats. J.Cui et al., J. Neurosci., 31, 16227 (2011) 7. Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain. Goldberg IE, et al. J Pharmacol Exp Ther. 1998 Aug;286(2):1007-13. 8. The antinociceptive properties of endomorphin-1 and endomorphin-2 in the mouse. Tseng LF. Jpn J Pharmacol. 2002 Jul;89(3):216-20. 9. Effects of endomorphin-1 postconditioning on myocardial ischemia/reperfusion injury and myocardial cell apoptosis in a rat model. Zhang WP, et al. Mol Med Rep. 2016 Oct;14(4):3992-8. 10. Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. Koda Y, et al. Bioorg Med Chem. 2008 Jun 1;16(11):6286-96. 11. The effects of endomorphin-1 and endomorphin-2 in CHO cells expressing recombinant mu-opioid receptors and SH-SY5Y cells. Harrison C, et al. Br J Pharmacol. 1999 Sep;128(2):472-8. 12. Endomorphin-1 alters interleukin-8 secretion in Caco-2 cells via a receptor mediated process. Neudeck BL, et al. Immunol Lett. 2002 Dec 3;84(3):217-21. |