Novel benzimidazole-4-carboxylic acid derivatives as potent and selective 5-HT3 receptor ligands

Article abstract of DOI:10.1016/0960-894X(96)00200-4

A series of benzimidazole-4-carboxylic acid derivatives was synthesized and evaluated for affinity at 5-HT₃ and 5-HT₄ serotoninergic receptors. Compounds 1b, c and j exhibited high affinity for the 5-HT₃ receptors (K(i)=6.1, 3.7 and 4.9 nM, respectively) and no significant affinity for 5- HT₄ (K(i)>1000 nM) and 5-HT(1A) (K(i)>10 000 nM) sites. Preliminary studies showed that 1c displayed activity in the two-compartment behavioural model.