Synthesis and molecular modeling of new 1-aryl-3-[4-arylpiperazin-1-yl]-1-propane derivatives with high affinity at the serotonin transporter and at 5-HT1A receptors

L Orús, S Pérez-Silanes, AM Oficialdegui…

Index: Orus, Lara; Perez-Silanes, Silvia; Oficialdegui, Ana-M.; Martinez-Esparza, Javier; Del Castillo, Juan-C; Mourelle, Marisa; Langer, Thierry; Guccione, Salvatore; Donzella, Giuseppina; Krovat, Eva M.; Poptodorov, Konstantin; Lasheras, Berta; Ballaz, Santiago; Hervias, Isabel; Tordera, Rosa; Del Rio, Joaquin; Monge, Antonio Journal of Medicinal Chemistry, 2002 , vol. 45, # 19 p. 4128 - 4139

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Citation Number: 56

Abstract

It has been proposed that 5-HT1A receptor antagonists augment the antidepressant efficacy of selective serotonin (5-HT) reuptake inhibitors. In a search toward new and efficient antidepressants, 1-(aryl)-3-[4-arylpiperazin-1-yl]-1-propane molecular hybrids were designed, synthesized, and evaluated for 5-HT reuptake inhibition and 5-HT1A receptor affinity. The design was based in coupling structural moieties related to inhibition of ...