191034-03-4Relevant academic research and scientific papers
Dual NK1 antagonists - Serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives
Ryckmans, Thomas,Berton, Olivier,Grimee, Renee,Kogej, Thierry,Lamberty, Yves,Pasau, Patrick,Talaga, Patrice,Genicot, Christophe
, p. 3195 - 3198 (2007/10/03)
The synthesis, structure-affinity relationship and activity of benzyloxyphenethyl piperazine derivatives combining NK1 antagonism and serotonin reuptake inhibition is described. Compound 7u was shown to be active in animal models of 5-HT reuptake inhibition and central NK1 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.
SUBSTITUTED 1-INDOLYLPROPYL-4-BENZYLPIPERAZINE DERIVATIVES
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, (2008/06/13)
A class of 1-[3-(1H-indol-3-yl)propyl]-4-benzylpiperazine derivatives of formula I, substituted at the 5-position of the indole nucleus by a 1, 2,4-triazol-4-yl moiety, and on the methylene linkage of the benzyl moiety by a range of substituted alkyl groups, are selective agonists of 5-HT 1-like receptors, being potent agonists of the human 5-HT 1Dα receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT 1Dα receptor subtype relative to the 5-HT. sub.1Dβ subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT 1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT 1D receptor agonists. STR1
