Author/Authors :
Andrés A. Trabanco، نويسنده , , Shirley Pullan، نويسنده , , José M. Alonso-Meijide، نويسنده , , Rosa M. Alvarez، نويسنده , , José I. Andrés، نويسنده , , Inge Boeckx، نويسنده , , Javier Fernandez-Suarez، نويسنده , , Antonio G?mez، نويسنده , , Laura Iturrino، نويسنده , , Frans E. Janssens، نويسنده , , Joseph E. Leenaerts، نويسنده , , Ana I. De Lucas، نويسنده , , Encarna Matesanz، نويسنده , , Theo Meert، نويسنده , , Thomas Steckler، نويسنده ,
Abstract :
A novel series of 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives has been prepared and their synthesis described herein. In vitro affinities for δ-, μ-, and κ-opioid receptors, as well as the functional activity in the [35S]GTPγS assay are reported. The most potent and selective δ-opioid agonist 18a exhibited a Ki of 18 nM, and was >258-fold and 28-fold selective over μ- and κ-receptors, respectively; the compound is a full agonist with an EC50 value of 14 nM.
