Design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT 1A/5-HT 3 ligands

…, D Avila, I Marco, L Schiapparelli, D Frechilla…

Index: Lopez-Rodriguez, Maria L.; Benhamu, Bellinda; Morcillo, Ma. Jose; Tejada, Ignacio; Avila, David; Marco, Isabel; Schiapparelli, Lucio; Frechilla, Diana; Del Rio, Joaquin Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 19 p. 3177 - 3180

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Citation Number: 16

Abstract

A series of new benzimidazole-arylpiperazine derivatives III were designed, synthesized and evaluated for binding affinity at serotoninergic 5-HT1A and 5-HT3 receptors. Compound IIIc was identified as a novel mixed 5-HT1A/5-HT3 ligand with high affinity for both serotonin receptors and excellent selectivity over α1-adrenergic and dopamine D2 receptors. This compound was characterized as a partial agonist at 5-HT1ARs and a 5-HT3R antagonist, ...