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

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Ryckmans T, Berton O, Grimee R, Kogej T, Lamberty Y, Pasau P, Talaga P, Genicot C

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

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3195-8.

PubMed ID
12372532 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
AprepitantNeurokinin 1 receptorIC 50 (nM)0.1N/AN/ADetails