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  • Title: Design and synthesis of new benzimidazole-arylpiperazine derivatives acting as mixed 5-HT1A/5-HT3 ligands.
    Author: López-Rodríguez ML, Benhamú B, Morcillo MJ, Tejada I, Avila D, Marco I, Schiapparelli L, Frechilla D, Del Río J.
    Journal: Bioorg Med Chem Lett; 2003 Oct 06; 13(19):3177-80. PubMed ID: 12951088.
    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.
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