Discovery of (R)-N-Benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide [(R)-AS-1], a Novel Orally Bioavailable EAAT2 Modulator with Drug-like Properties and Potent Antiseizure Activity In Vivo

[Image: see text] (R)-7 [(R)-AS-1] showed broad-spectrum antiseizure activity across in vivo mouse seizure models: maximal electroshock (MES), 6 Hz (32/44 mA), acute pentylenetetrazol (PTZ), and PTZ-kindling. A remarkable separation between antiseizure activity and CNS-related adverse effects was al...

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Detalles Bibliográficos
Autores principales: Abram, Michał, Jakubiec, Marcin, Reeb, Katelyn, Cheng, Mary Hongying, Gedschold, Robin, Rapacz, Anna, Mogilski, Szczepan, Socała, Katarzyna, Nieoczym, Dorota, Szafarz, Małgorzata, Latacz, Gniewomir, Szulczyk, Bartłomiej, Kalinowska-Tłuścik, Justyna, Gawel, Kinga, Esguerra, Camila V., Wyska, Elżbieta, Müller, Christa E., Bahar, Ivet, Fontana, Andréia C. K., Wlaź, Piotr, Kamiński, Rafał M., Kamiński, Krzysztof
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9469208/
https://www.ncbi.nlm.nih.gov/pubmed/35984707
http://dx.doi.org/10.1021/acs.jmedchem.2c00534

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9469208/
https://www.ncbi.nlm.nih.gov/pubmed/35984707
http://dx.doi.org/10.1021/acs.jmedchem.2c00534

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