Document Report Card

Basic Information

ID: ALA1134952

Journal: Bioorg Med Chem Lett

Title: Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives.

Authors: Ryckmans T, Berton O, Grimée R, Kogej T, Lamberty Y, Pasau P, Talaga P, Genicot C.

Abstract: The synthesis, structure-affinity relationship and activity of benzyloxyphenethyl piperazine derivatives combining NK(1) antagonism and serotonin reuptake inhibition is described. Compound 7u was shown to be active in animal models of 5-HT reuptake inhibition and central NK(1) receptor blockade, and was demonstrated to be orally active in an integrated model sensitive to both mechanisms. This class of compounds potentially represents a new generation of antidepressants.

CiteXplore: 12372532

DOI: 10.1016/s0960-894x(02)00563-2