Design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT1A/5-HT3 ligands.
Basic Information
ID: ALA1136226
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT1A/5-HT3 ligands.
Authors: López-Rodríguez ML, Benhamú B, Morcillo MJ, Tejada I, Avila D, Marco I, Schiapparelli L, Frechilla D, Del Río J.
Abstract: A series of new benzimidazole-arylpiperazine derivatives III were designed, synthesized and evaluated for binding affinity at serotoninergic 5-HT(1A) and 5-HT(3) receptors. Compound IIIc was identified as a novel mixed 5-HT(1A)/5-HT(3) ligand with high affinity for both serotonin receptors and excellent selectivity over alpha(1)-adrenergic and dopamine D(2) receptors. This compound was characterized as a partial agonist at 5-HT(1A)Rs and a 5-HT(3)R antagonist, and was effective in preventing the cognitive deficits induced by muscarinic receptor blockade in a passive avoidance learning test.
CiteXplore: 12951088
DOI: 10.1016/s0960-894x(03)00706-6
Patent ID: ┄