ARYLACETAMIDE KAPPA-SELECTIVE OPIOID LIGANDS
Citation
Ad. Pechulis et al., ARYLACETAMIDE KAPPA-SELECTIVE OPIOID LIGANDS, Bioorganic & medicinal chemistry letters, 7(17), 1997, pp. 2271-2276
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
SICI code
0960-894X(1997)7:17<2271:AKOL>2.0.ZU;2-8
Abstract
A family of arylacetamide opioid ligands was prepared. Competition bin
ding studies indicate that in each case the (S)-(+) series was two ord
ers of magnitude more potent than the corresponding (R)-(-) series and
that the amine (S)-(+)-3 and the acetamide (S)-(+)-4 were selective f
or the kappa opioid binding site. Binding and flow cytometry experimen
ts demonstrated that (S)-(+)-FITC-AA 5 was the enantiomer that bound t
o the re opioid receptor. (C) 1997 Elsevier Science Ltd.
