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

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...

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Bibliographic Details
Main Authors: Reggie Bosma, Gesa Witt, Lea A. I. Vaas, Ivana Josimovic, Philip Gribbon, Henry F. Vischer, Sheraz Gul, Rob Leurs
Format: Article
Language:English
Published: Frontiers Media S.A. 2017-09-01
Series:Frontiers in Pharmacology
Subjects:
residence time
recovery time
GPCR
histamine H1 receptor
calcium mobilization
DMR
Online Access:http://journal.frontiersin.org/article/10.3389/fphar.2017.00667/full

Internet

http://journal.frontiersin.org/article/10.3389/fphar.2017.00667/full

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