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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 (Kd or Ki value) or target modulation (IC50). However, these metrics are determined at equilibrium conditions, and consequently information regarding the onset and offset of target engagement and modul...

Ausführliche Beschreibung

Gespeichert in:
Hauptverfasser: Reggie Bosma, Gesa Witt, Lea A. I. Vaas, Ivana Josimovic, Philip Gribbon, Henry F. Vischer, Sheraz Gul, Rob Leurs
Format: Artigo
Sprache:Inglês
Veröffentlicht: Frontiers Media S.A. 2017-09-01
Schriftenreihe:Frontiers in Pharmacology
Schlagworte:
residence time
recovery time
GPCR
histamine H1 receptor
calcium mobilization
DMR
Online-Zugang:http://journal.frontiersin.org/article/10.3389/fphar.2017.00667/full
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