Arylacetamide kappa-selective opioid ligands

[摘要] A family of arylacetamide opioid ligands was prepared. Competition binding studies indicate that in each case the (S)-(+) series was two orders of magnitude more potent than the corresponding (R)-(-) series and that the amine (S)-(+)-3 and the acetamide (S)-(+)-4 were selective for the kappa opioid binding site. Binding and flow cytometry experiments demonstrated that (S)-(+)-FITC-AA 5 was the enantiomer that bound to the re opioid receptor. (C) 1997 Elsevier Science Ltd.

[发布日期] 1997-09-09