Synthesis and structure-activity relationships of 1-aralkyl-4-benzylpiperidine and 1-aralkyl-4-benzylpiperazine derivatives as potent σ ligands

…, O Prezzavento, F Vittorio, G Ronsisvalle…

Index: Costantino, Luca; Gandolfi, Francesca; Sorbi, Claudia; Franchini, Silvia; Prezzavento, Orazio; Vittorio, Franco; Ronsisvalle, Giuseppe; Leonardi, Amedeo; Poggesi, Elena; Brasili, Livio Journal of Medicinal Chemistry, 2005 , vol. 48, # 1 p. 266 - 273

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Citation Number: 24

Abstract

In the attempt to define more accurately structure-affinity relationships for σ1 and σ2 ligands, we synthesized and tested on σ subtype receptors a series of aralkyl derivatives of 4- benzylpiperidine, in which the effect of modifications on the aralkyl moiety was studied in a systematic way. The affinity of the compounds here described varied to a great extent, with a σ2/σ1 selectivity ranging from 0.1 to 9. Thus, to confirm the ability of the piperazine ...