M. Higginbottom et al., THE DESIGN AND SYNTHESIS OF KAPPA-OPIOID LIGANDS BASED ON A BINDING MODEL FOR KAPPA AGONISTS, Bioorganic & medicinal chemistry letters, 3(5), 1993, pp. 841-846
The chemical structures of known kappa opioid receptor agonists are us
ed in a modelling study to propose a binding model for kappa ligands.
Based on this model three novel non-peptide structures are synthesised
and one compound (8) has kappa receptor K(i) = 160 nM, mu K(i) > 1000
0 nM.