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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Bibliografski detalji
Izdano u:J Med Chem
Glavni autori: 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
Format: Artigo
Jezik:Inglês
Izdano: American Chemical Society 2019
Online pristup: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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