Opioid ligands related to tifluadom

Article abstract of DOI:10.1016/0223-5234(89)90022-6

In an effort to prepare ligands with kappa selective affintity suitable for use in affinity chromatography, we synthesized the haloacetamido derivatives 17 and 18 of tifluadom.These compounds showed modest opioid binding affinity but were more active at the mu than at the kappa site.The nitro compounds 7 and 16 were prepared as potential intermediates.The former, a weak mu agonist, was devoid of kappa affinity (IC₅₀ > 1E-6 M), whereas the latter was a mu selective agonist.Keywords: tifluadom/ benzodiazepines/ affinity chromathography/ opioid binding activity