KOR agonist 1

KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC50s of 3.4, 701.2 and 1649 nM, for KOR, MOR and DOR, respectively. KOR agonist 1 binds KOR, MOR and DOR, with Kis of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED50 in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg) [1].

Product Specifications

UNSPSC

12352005

Target

Opioid Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/kor-agonist-1.html

Smiles

COC1=C(O2)C([C@]([C@@H]2[C@]3(OC)[C@@H](C4=CC=CC=C4NCC5=CC=CC=C5)C6)(CCN7CC8CC8)[C@@]6(CC3)C7C9)=C9C=C1

Molecular Formula

C37H42N2O3

Molecular Weight

562.74

References & Citations

[1]Li Z, et al., Discovery of an Ortho-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydronorthebaine Derivative as a Selective and Potent Kappa Opioid Receptor Agonist with Subsided Sedative Effect. J Med Chem. 2024 May 9;67 (9) :7112-7129.