Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives |
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Authors: | Ryckmans Thomas Berton Olivier Grimée Renée Kogej Thierry Lamberty Yves Pasau Patrick Talaga Patrice Genicot Christophe |
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Institution: | Chemical Research, R&D, UCB Pharma SA, Chemin du Foriest, B-1420, Braine-l'Alleud, Belgium. thomas_ryckmans@sandwich.pfizer.com |
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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. |
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