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...

Deskribapen osoa

Gorde:
Xehetasun bibliografikoak
Argitaratua izan da:Front Pharmacol
Egile Nagusiak: Bosma, Reggie, Witt, Gesa, Vaas, Lea A. I., Josimovic, Ivana, Gribbon, Philip, Vischer, Henry F., Gul, Sheraz, Leurs, Rob
Formatua: Artigo
Hizkuntza:Inglês
Argitaratua: Frontiers Media S.A. 2017
Gaiak:
Pharmacology
Sarrera elektronikoa:https://ncbi.nlm.nih.gov/pmc/articles/PMC5627017/
https://ncbi.nlm.nih.gov/pubmed/29033838
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.3389/fphar.2017.00667
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