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| Título: | Synthesis, conformation, and biological characterization of a sugar derivative of morphine that is a potent, long-lasting, and nontolerant antinociceptive |
Autor: | Arsequell, Gemma CSIC ORCID; Salvatella, Mariona; Valencia Parera, Gregorio CSIC; Fernández-Mayoralas, Alfonso CSIC ORCID ; Fontanella, Marco CSIC; Venturi, Chiara CSIC; Jiménez-Barbero, Jesús CSIC ORCID; Marrón Fernández de Velasco, E.; Rodríguez, Raquel E. | Fecha de publicación: | 7-abr-2009 | Editor: | American Chemical Society | Citación: | Journal of Medicinal Chemistry 52(9): 2656-2666 (2009) | Resumen: | A synthetic mannoside derivative, namely, 6-morphinyl-α-d-mannopyranoside, shows a naloxone-reversible antinociception that is 100-fold more potent and twice as long lasting compared to morphine when administered intraperitoneally to rats in paw pressure and tail flick tests. The compound does not produce tolerance and binds to rat μ opioid receptors with twice the affinity of morphine. NMR studies suggest that differences of activity between the derivative and its parent compound M6G might be related to their differing molecular dynamic behavior. | Descripción: | 11 pages.-- PMID: 19351163 [PubMed].-- Printed version published May 14, 2009. Supporting information (10 pages) available at: http://pubs.acs.org/doi/suppl/10.1021/jm8011245/suppl_file/jm8011245_si_001.pdf |
Versión del editor: | http://dx.doi.org/10.1021/jm8011245 | URI: | http://hdl.handle.net/10261/13178 | DOI: | 10.1021/jm8011245 | ISSN: | 0022-2623 |
| Aparece en las colecciones: | (IQAC) Artículos (IQOG) Artículos (CIB) Artículos |
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| Fichero | Descripción | Tamaño | Formato | |
|---|---|---|---|---|
| Antinociceptive_Press_release.pdf | CSIC Press release (Spanish lang.) | 47,14 kB | Adobe PDF |  Visualizar/Abrir |
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