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http://hdl.handle.net/10261/63297
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dc.contributor.author | Cumella Montánchez, José María | - |
dc.contributor.author | Hernández-Folgado, Laura | - |
dc.contributor.author | Gómez-Cañas, M. | - |
dc.contributor.author | Girón, Rocío | - |
dc.contributor.author | Sánchez, E. | - |
dc.contributor.author | Morales, Paula | - |
dc.contributor.author | Hurst, D. P. | - |
dc.contributor.author | Gómez-Cañas, María | - |
dc.contributor.author | Gómez-Ruiz, M. | - |
dc.contributor.author | Pinto, Diana C. G. A. | - |
dc.contributor.author | Goya, Pilar | - |
dc.contributor.author | Reggio, P. H. | - |
dc.contributor.author | Martín, M. Isabel | - |
dc.contributor.author | Fernández-Ruiz, Javier | - |
dc.contributor.author | Silva, Artur M. S. | - |
dc.contributor.author | Jagerovic, Nadine | - |
dc.date.accessioned | 2012-12-19T12:32:15Z | - |
dc.date.available | 2012-12-19T12:32:15Z | - |
dc.date.issued | 2012 | - |
dc.identifier | doi: 10.1002/cmdc.201100568 | - |
dc.identifier | issn: 1860-7179 | - |
dc.identifier | e-issn: 1860-7187 | - |
dc.identifier.citation | ChemMedChem 7: 452- 463 (2012) | - |
dc.identifier.uri | http://hdl.handle.net/10261/63297 | - |
dc.description.abstract | The unwanted psychoactive effects of cannabinoid receptor agonists have limited their development as medicines. These CB 1-mediated side effects are due to the fact that CB 1 receptors are largely expressed in the central nervous system (CNS). As it is known that CB 1 receptors are also located peripherally, there is growing interest in targeting cannabinoid receptors located outside the brain. A library of chromenopyrazoles designed analogously to the classical cannabinoid cannabinol were synthesized, characterized, and tested for cannabinoid activity. Radioligand binding assays were used to determine their affinities at CB 1 and CB 2 receptors. Structural features required for CB 1/CB 2 affinity and selectivity were explored by molecular modeling. Some compounds in the chromenopyrazole series were observed to be selective CB 1 ligands. These modeling studies suggest that full CB 1 selectivity over CB 2 can be explained by the presence of a pyrazole ring in the structure. The functional activities of selected chromenopyrazoles were evaluated in isolated tissues. Invivo behavioral tests were then carried out on the most effective CB 1 cannabinoid agonist, 13a. Chromenopyrazole 13a did not induce modifications in any of the tested parameters on the mouse cannabinoid tetrad, thus discounting CNS-mediated effects. This lack of agonistic activity in the CNS suggests that this compound does not readily cross the blood-brain barrier. Moreover, 13a can induce antinociception in a rat peripheral model of orofacial pain. Taking into account the negative results obtained with the hot-plate test, the antinociception induced by 13a in the orofacial test could be mediated through peripheral mechanisms. © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. | - |
dc.language.iso | eng | - |
dc.publisher | Wiley-VCH | - |
dc.rights | closedAccess | - |
dc.title | Chromenopyrazoles: Non-psychoactive and Selective CB 1 Cannabinoid Agonists with Peripheral Antinociceptive Properties | - |
dc.type | artículo | - |
dc.identifier.doi | 10.1002/cmdc.201100568 | - |
dc.date.updated | 2012-12-19T12:32:16Z | - |
dc.description.version | Peer Reviewed | - |
dc.identifier.pmid | 22302767 | - |
dc.type.coar | http://purl.org/coar/resource_type/c_6501 | es_ES |
item.openairetype | artículo | - |
item.grantfulltext | none | - |
item.cerifentitytype | Publications | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.fulltext | No Fulltext | - |
item.languageiso639-1 | en | - |
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