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

• Κύριοι συγγραφείς: Reggie Bosma (Συγγραφέας), Gesa Witt (Συγγραφέας), Lea A. I. Vaas (Συγγραφέας), Ivana Josimovic (Συγγραφέας), Philip Gribbon (Συγγραφέας), Henry F. Vischer (Συγγραφέας), Sheraz Gul (Συγγραφέας), Rob Leurs (Συγγραφέας)
• Μορφή: Βιβλίο
• Έκδοση: Frontiers Media S.A., 2017-09-01T00:00:00Z.
• Θέματα: article
• Διαθέσιμο Online: 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...