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Título: | Exploring the Benzimidazole Ring as a Substitution for Indole in Cannabinoid Allosteric Modulators |
Autor: | Hernández-Folgado, Laura CSIC; Stevenson, Lesley A.; Morales, Paula CSIC ORCID; Gómez-Cañas, María; Pazos, Ruth; Cascio, Grazia; Jagerovic, Nadine CSIC ORCID ; Elguero, José CSIC ORCID; Pertwee, Roger; Goya, Pilar CSIC ORCID | Palabras clave: | Allosteric modulators ORG27569 Benzimidazole CB1 receptors |
Fecha de publicación: | 2016 | Editor: | Mary Ann Liebert | Citación: | Cannabis and Cannabinoid Research 1: 196-200 (2016) | Resumen: | Introduction and Objectives: The traditional approach to target a particular receptor is to design compounds that bind to the same site as the endogenous ligand, the so-called ‘‘orthosteric site.’’ However, recently the search has shifted to ligands that can interact with a different region of the receptor protein, the ‘‘allosteric site,’’ since this approach offers potential pharmacological and therapeutic advantages. The aim of our work was to explore the benzimidazole heterocycle as a novel scaffold for cannabinoid allosterism. Materials and Methods: We synthesized a series of novel benzimidazole-2-carboxamides, analogues of ORG27569, and performed their pharmacological characterization as CB 1 R allosteric modulators using compe- titive [ 3 H]-CP55940 and [ 35 S]-GTP c S binding assays. Results: The benzimidazoles 3 and 4 produced significant negative allosteric modulation (NAM) of CP55940 agonism at the mouse CB 1 R, although are somewhat less potent than the CB 1 R allosteric cannabinoid ORG27569. Conclusions: Replacing the indole ring with a benzimidazole ring within the structure of ORG27569 abolished the binding of the resultant ligands to CB 1 R, but the modulation on the agonist-induced GTP c S binding was maintained | Versión del editor: | http://dx.doi.org/10.1089/can.2016.0003 | URI: | http://hdl.handle.net/10261/152765 | DOI: | 10.1089/can.2016.0003 | Identificadores: | doi: 10.1089/can.2016.0003 issn: 2378-8763 |
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