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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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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: 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: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2019
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6750840/
https://ncbi.nlm.nih.gov/pubmed/31274307
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.9b00447
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