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...

Disgrifiad llawn

Wedi'i Gadw mewn:
Manylion Llyfryddiaeth
Cyhoeddwyd yn:J Med Chem
Prif Awduron: 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
Fformat: Artigo
Iaith:Inglês
Cyhoeddwyd: American Chemical Society 2019
Mynediad Ar-lein: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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