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http://hdl.handle.net/10261/152765
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dc.contributor.author | Hernández-Folgado, Laura | - |
dc.contributor.author | Stevenson, Lesley A. | - |
dc.contributor.author | Morales, Paula | - |
dc.contributor.author | Gómez-Cañas, María | - |
dc.contributor.author | Pazos, Ruth | - |
dc.contributor.author | Cascio, Grazia | - |
dc.contributor.author | Jagerovic, Nadine | - |
dc.contributor.author | Elguero, José | - |
dc.contributor.author | Pertwee, Roger | - |
dc.contributor.author | Goya, Pilar | - |
dc.date.accessioned | 2017-07-14T09:09:03Z | - |
dc.date.available | 2017-07-14T09:09:03Z | - |
dc.date.issued | 2016 | - |
dc.identifier | doi: 10.1089/can.2016.0003 | - |
dc.identifier | issn: 2378-8763 | - |
dc.identifier.citation | Cannabis and Cannabinoid Research 1: 196-200 (2016) | - |
dc.identifier.uri | http://hdl.handle.net/10261/152765 | - |
dc.description.abstract | 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 | - |
dc.description.sponsorship | The authors gratefully acknowledge research support from Spanish Grant SAF2012-400075-C02-02 and CAM S2010/BMD-2308. P.M. is recipient of a fellowship JAE-Pre-2010-01119 from ‘‘Junta para la Ampliación de Estudios’’ that is co-financed by FSE. | - |
dc.publisher | Mary Ann Liebert | - |
dc.relation.isversionof | Publisher's version | - |
dc.rights | openAccess | - |
dc.subject | Allosteric modulators | - |
dc.subject | ORG27569 | - |
dc.subject | Benzimidazole | - |
dc.subject | CB1 receptors | - |
dc.title | Exploring the Benzimidazole Ring as a Substitution for Indole in Cannabinoid Allosteric Modulators | - |
dc.type | artículo | - |
dc.identifier.doi | 10.1089/can.2016.0003 | - |
dc.relation.publisherversion | http://dx.doi.org/10.1089/can.2016.0003 | - |
dc.date.updated | 2017-07-14T09:09:03Z | - |
dc.description.version | Peer Reviewed | - |
dc.language.rfc3066 | eng | - |
dc.contributor.funder | European Commission | - |
dc.contributor.funder | Comunidad de Madrid | - |
dc.contributor.funder | Ministerio de Economía y Competitividad (España) | - |
dc.relation.csic | Sí | - |
dc.identifier.funder | http://dx.doi.org/10.13039/501100000780 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/501100003329 | es_ES |
dc.identifier.funder | http://dx.doi.org/10.13039/100012818 | es_ES |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.openairetype | artículo | - |
item.grantfulltext | open | - |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | With Fulltext | - |
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