Route to Prolonged Residence Time at the Histamine H(1) Receptor: Growing from Desloratadine to Rupatadine

[Image: see text] Drug–target binding kinetics are an important predictor of in vivo drug efficacy, yet the relationship between ligand structures and their binding kinetics is often poorly understood. We show that both rupatadine (1) and desloratadine (2) have a long residence time at the histamine...

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Detalles Bibliográficos
Autores principales: Bosma, Reggie, Wang, Zhiyong, Kooistra, Albert J., Bushby, Nick, Kuhne, Sebastiaan, van den Bor, Jelle, Waring, Michael J., de Graaf, Chris, de Esch, Iwan J., Vischer, Henry F., Sheppard, Robert J., Wijtmans, Maikel, Leurs, Rob
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2019
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6750840/
https://www.ncbi.nlm.nih.gov/pubmed/31274307
http://dx.doi.org/10.1021/acs.jmedchem.9b00447

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