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A medicinal-chemistry-guided approach to selective and druglike sigma 1 ligands.
Corbera J, Vaño D, Martínez D, Vela JM, Zamanillo D, Dordal A, Andreu F, Hernandez E, Perez R, Escriche M, Salgado L, Yeste S, Serafini MT, Pascual R, Alegre J, Calvet MC, Cano N, Carro M, Buschmann H, Holenz J. Corbera J, et al. Among authors: serafini mt. ChemMedChem. 2006 Jan;1(1):140-54. doi: 10.1002/cmdc.200500034. ChemMedChem. 2006. PMID: 16892345
Bispecific sigma-1 receptor antagonism and mu-opioid receptor partial agonism: WLB-73502, an analgesic with improved efficacy and safety profile compared to strong opioids.
Vidal-Torres A, Fernández-Pastor B, García M, Ayet E, Cabot A, Burgueño J, Monroy X, Aubel B, Codony X, Romero L, Pascual R, Serafini MT, Encina G, Almansa C, Zamanillo D, Merlos M, Vela JM. Vidal-Torres A, et al. Among authors: serafini mt. Acta Pharm Sin B. 2023 Jan;13(1):82-99. doi: 10.1016/j.apsb.2022.09.018. Epub 2022 Sep 25. Acta Pharm Sin B. 2023. PMID: 36815042 Free PMC article.
Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).
Díaz JL, Cuberes R, Berrocal J, Contijoch M, Christmann U, Fernández A, Port A, Holenz J, Buschmann H, Laggner C, Serafini MT, Burgueño J, Zamanillo D, Merlos M, Vela JM, Almansa C. Díaz JL, et al. Among authors: serafini mt. J Med Chem. 2012 Oct 11;55(19):8211-24. doi: 10.1021/jm3007323. Epub 2012 Jul 27. J Med Chem. 2012. PMID: 22784008
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual μ-Opioid Receptor Agonists and σ1 Receptor Antagonists for the Treatment of Pain.
García M, Virgili M, Alonso M, Alegret C, Fernández B, Port A, Pascual R, Monroy X, Vidal-Torres A, Serafini MT, Vela JM, Almansa C. García M, et al. Among authors: serafini mt. J Med Chem. 2020 Mar 12;63(5):2434-2454. doi: 10.1021/acs.jmedchem.9b01256. Epub 2019 Dec 5. J Med Chem. 2020. PMID: 31743642 Free article.
21 results