THE DESIGN AND SYNTHESIS OF KAPPA-OPIOID LIGANDS BASED ON A BINDING MODEL FOR KAPPA AGONISTS

Authors
HIGGINBOTTOM M NOLAN W OTOOLE J RATCLIFFE GS REES DC ROBERTS E
Citation
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
Citations number
10
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
5
Year of publication
1993
Pages
841 - 846
Database
ISI
SICI code
0960-894X(1993)3:5<841:TDASOK>2.0.ZU;2-T
Abstract
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.