Opioid ligands related to tifluadom

…, A Seyed-Mozaffari, EJ Simon, TL Gioannini

Index: Archer, Sydney; Seyed-Mozaffari, Ahmad; Simon, Eric J.; Gioannini, Theresa L. European Journal of Medicinal Chemistry, 1989 , vol. 24, p. 569 - 572

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Abstract

Abstract In an effort to prepare ligands with kappa selective affinity 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 (IC 50> 10− 6 ...