1816990-29-0

K-Opioid receptor agonist-1 (Compound 5a) is an agonist for κ-Opioid receptor with Ki of 0.25 nM and EC50 of 2 nM. K-Opioid receptor agonist-1 is blood brain barrier (BBB) penetrate (brain/plasma ratios of 0.50 to 0.65). K-Opioid receptor agonist-1 exhibits anti-inflammatory activity in dermatitis models induced by Arachidonic acid (HY-109590) or oxazolidinone[1].

κ Opioid Receptor/KOR: 0.25 nM (Ki); μ Opioid Receptor/MOR: 43 nM (Ki); δ Opioid Receptor/DOR: 58 nM (Ki)

[1] Soeberdt M, et al., Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo. J Med Chem. 2017 Mar 23;60(6):2526-2551. DOI:10.1021/acs.jmedchem.6b01868