Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation

…, A Dumuis, L Pardo, ML López-Rodríguez

Index: De La Fuente, Tania; Martin-Fontecha, Mar; Sallander, Jessica; Benhamu, Bellinda; Campillo, Mercedes; Medina, Rocio A.; Pellissier, Lucie P.; Claeysen, Sylvie; Dumuis, Aline; Pardo, Leonardo; Lopez-Rodriguez, Maria L. Journal of Medicinal Chemistry, 2010 , vol. 53, # 3 p. 1357 - 1369

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Citation Number: 24

Abstract

On the basis of our previously described pharmacophore model for serotonin 5-HT6 receptor (5-HT6R) antagonists, we have designed, synthesized, and pharmacologically characterized a series of benzimidazole derivatives 1− 20 that represent a new family of potent antagonists at the human 5-HT6R. Site-directed mutagenesis and a β2-adrenoceptor- based homology model of the 5-HT6R were used to predict the mode of binding of ...