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http://hdl.handle.net/2445/194101
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DC Field | Value | Language |
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dc.contributor.author | Codony Gisbert, Sandra | - |
dc.contributor.author | Entrena, José M. | - |
dc.contributor.author | Calvó-Tusell, Carla | - |
dc.contributor.author | Jora, Beatrice Elena | - |
dc.contributor.author | González Cano, Rafael C. | - |
dc.contributor.author | Osuna, Sílvia | - |
dc.contributor.author | Corpas Expósito, Rubén | - |
dc.contributor.author | Morisseau, Christophe | - |
dc.contributor.author | Pérez, Belén | - |
dc.contributor.author | Barniol-Xicota, Marta | - |
dc.contributor.author | Griñán Ferré, Christian | - |
dc.contributor.author | Pérez, Concepción | - |
dc.contributor.author | Rodríguez-Franco, María Isabel | - |
dc.contributor.author | Martínez, Antón L. | - |
dc.contributor.author | Loza, María Isabel | - |
dc.contributor.author | Pallàs i Llibería, Mercè, 1964- | - |
dc.contributor.author | Verhelst, Steven H. L. | - |
dc.contributor.author | Sanfeliu i Pujol, Coral | - |
dc.contributor.author | Feixas, Ferran | - |
dc.contributor.author | Hammock, Bruce D. | - |
dc.contributor.author | Brea, José | - |
dc.contributor.author | Cobos, Enrique J. | - |
dc.contributor.author | Vázquez Cruz, Santiago | - |
dc.date.accessioned | 2023-02-24T08:11:24Z | - |
dc.date.available | 2023-02-24T08:11:24Z | - |
dc.date.issued | 2022-10-27 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | http://hdl.handle.net/2445/194101 | - |
dc.description.abstract | The soluble epoxide hydrolase (sEH) has been suggested as a pharmacological target for the treatment of several diseases, including pain-related disorders. Herein, we report further medicinal chemistry around new benzohomoadamantane-based sEH inhibitors (sEHI) in order to improve the drug metabolism and pharmacokinetics properties of a previous hit. After an extensive in vitro screening cascade, molecular modeling, and in vivo pharmacokinetics studies, two candidates were evaluated in vivo in a murine model of capsaicin-induced allodynia. The two compounds showed an anti-allodynic effect in a dose-dependent manner. Moreover, the most potent compound presented robust analgesic efficacy in the cyclophosphamide-induced murine model of cystitis, a well-established model of visceral pain. Overall, these results suggest painful bladder syndrome as a new possible indication for sEHI, opening a new range of applications for them in the visceral pain field. | - |
dc.format.extent | 21 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | American Chemical Society | - |
dc.relation.isformatof | Reproducció del document publicat a: https://doi.org/10.1021/acs.jmedchem.2c00515 | - |
dc.relation.ispartof | Journal of Medicinal Chemistry, 2022, vol. 65, num. 20, p. 13660-13680 | - |
dc.relation.uri | https://doi.org/10.1021/acs.jmedchem.2c00515 | - |
dc.rights | (c) Sandra Codony Gisbert, et al., 2022 | - |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/3.0/es/ | * |
dc.source | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) | - |
dc.subject.classification | Urea | - |
dc.subject.classification | Inflamació | - |
dc.subject.classification | Química clínica | - |
dc.subject.other | Urea | - |
dc.subject.other | Inflammation | - |
dc.subject.other | Clinical chemistry | - |
dc.title | Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/publishedVersion | - |
dc.identifier.idgrec | 726508 | - |
dc.date.updated | 2023-02-24T08:11:24Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
Appears in Collections: | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) |
Files in This Item:
File | Description | Size | Format | |
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726508.pdf | 5.64 MB | Adobe PDF | View/Open |
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