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

• Main Authors: Reggie Bosma (Author), Gesa Witt (Author), Lea A. I. Vaas (Author), Ivana Josimovic (Author), Philip Gribbon (Author), Henry F. Vischer (Author), Sheraz Gul (Author), Rob Leurs (Author)
• Format: Book
• Published: Frontiers Media S.A., 2017-09-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...