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The Target Residence Time of Antihistamines Determines Their Antagonism of the G Protein-Coupled Histamine H1 Receptor

The pharmacodynamics of drug-candidates is often optimized by metrics that describe target binding (K(d) or K(i) value) or target modulation (IC(50)). However, these metrics are determined at equilibrium conditions, and consequently information regarding the onset and offset of target engagement and...

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Publicat a:Front Pharmacol
Autors principals: Bosma, Reggie, Witt, Gesa, Vaas, Lea A. I., Josimovic, Ivana, Gribbon, Philip, Vischer, Henry F., Gul, Sheraz, Leurs, Rob
Format: Artigo
Idioma:Inglês
Publicat: Frontiers Media S.A. 2017
Matèries:
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC5627017/
https://ncbi.nlm.nih.gov/pubmed/29033838
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.3389/fphar.2017.00667
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