Endomorphin 1

Endomorphin 1, 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 has antinociceptive properties[1][2][4].

Product Specifications

CAS Number

[189388-22-5]

UNSPSC

12352209

Hazard Statement

H302, H315, H319, H335

Target

Opioid Receptor

Type

Peptides

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Endomorphin_1.html

Purity

99.92

Solubility

DMSO : ≥ 50 mg/mL

Smiles

O=C(N)[C@H](CC1=CC=CC=C1)NC([C@H](CC2=CNC3=CC=CC=C23)NC([C@H]4N(C([C@H](CC5=CC=C(C=C5)O)N)=O)CCC4)=O)=O

Molecular Formula

C34H38N6O5

Molecular Weight

610.70

Precautions

H302, H315, H319, H335

References & Citations

[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.