Endomorphin 1 acetate, a high affinity, highly selective agonist of 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 acetate has antinociceptive properties[1][2][4].
Endomorphin 1 acetate inhibits Forskolin (1 μM) stimulated cyclic AMP formation with a pIC50 value of 8.03 in In CHOμ cells[5].
Endomorphin 1 (1-10 μM) acetate increases interleukin-8 secretion in Caco-2 cells[6].
Endomorphin 1 (1 μM) acetate inhibits excitatory transmission in adult rat substantia gelatinosa neurons[7].
Endomorphin 1 (i.c.v.) acetate shows antinociceptive properties in mice, with an ED50 value of 6.16 nM[2].
Endomorphin 1 (50 μg/kg, i.v., rats) acetate alleviates myocardial ischemia/reperfusion injury (MIRI) by inhibiting the inflammatory response[3].
| Animal Model: | ICR mice[2]. |
| Dosage: | 6.16 nM (ED50) |
| Administration: | Intracerebroventricularly (i.c.v.) injection |
| Result: | Inhibited dose-dependently the tail-flick response. |
| Animal Model: | Rats[3]. |
| Dosage: | 50 μg/kg |
| Administration: | Intravenously following LAD ligation for 25 min, subsequently the LAD was reperfused for 120 min. |
| Result: | Alleviated MIRI by reducing the production of free radicals. Dncreased LDH and CK-MB activities. Increased SOD activity and decreased MDA content. Decreased IL-6 and TNF-α plasma content. |
[1]. Goldberg IE, et al. Pharmacological characterization of endomorphin-1 and endomorphin-2 in mouse brain. J Pharmacol Exp Ther. 1998 Aug;286(2):1007-13.
[2]. Tseng LF. The antinociceptive properties of endomorphin-1 and endomorphin-2 in the mouse. Jpn J Pharmacol. 2002 Jul;89(3):216-20.
[3]. Zhang WP, et al. Effects of endomorphin-1 postconditioning on myocardial ischemia/reperfusion injury and myocardial cell apoptosis in a rat model. Mol Med Rep. 2016 Oct;14(4):3992-8.
[4]. Koda Y, et al. Synthesis and in vitro evaluation of a library of modified endomorphin 1 peptides. Bioorg Med Chem. 2008 Jun 1;16(11):6286-96.
[5]. Harrison C, et al. The effects of endomorphin-1 and endomorphin-2 in CHO cells expressing recombinant mu-opioid receptors and SH-SY5Y cells. Br J Pharmacol. 1999 Sep;128(2):472-8.
[6]. Neudeck BL, et al. Endomorphin-1 alters interleukin-8 secretion in Caco-2 cells via a receptor mediated process. Immunol Lett. 2002 Dec 3;84(3):217-21.
[7]. Fujita T, et al. Inhibition by endomorphin-1 and endomorphin-2 of excitatory transmission in adult rat substantia gelatinosa neurons. Neuroscience. 2006;139(3):1095-105.