Arylacetamide kappa-selective opioid ligands

Autor: Anthony D. Pechulis, Jean M. Bidlack, Sydney Archer, Mark P. Wentland, Ann M. Colasurdo
Rok vydání: 1997
Předmět:
Zdroj: Bioorganic & Medicinal Chemistry Letters. 7:2271-2276
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(97)00406-x
Popis: 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 κ opioid binding site. Binding and flow cytometry experiments demonstrated that (S)-(+)-FITC-AA 5 was the enantiomer that bound to the κ opioid receptor.
Databáze: OpenAIRE