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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