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...

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Detaylı Bibliyografya
Yayımlandı:Front Pharmacol
Asıl Yazarlar: Bosma, Reggie, Witt, Gesa, Vaas, Lea A. I., Josimovic, Ivana, Gribbon, Philip, Vischer, Henry F., Gul, Sheraz, Leurs, Rob
Materyal Türü: Artigo
Dil:Inglês
Baskı/Yayın Bilgisi: Frontiers Media S.A. 2017
Konular:
Pharmacology
Online Erişim: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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