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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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Detalles Bibliográficos
Autores principales:	Bosma, Reggie, Witt, Gesa, Vaas, Lea A. I., Josimovic, Ivana, Gribbon, Philip, Vischer, Henry F., Gul, Sheraz, Leurs, Rob
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Frontiers Media S.A. 2017
Materias:	Pharmacology
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5627017/ https://www.ncbi.nlm.nih.gov/pubmed/29033838 http://dx.doi.org/10.3389/fphar.2017.00667

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