journal cover

BRET-based β-arrestin2 recruitment to the histamine H1 receptor for investigating antihistamine binding kinetics

Pharmacological Research : the Official Journal of the Italian Pharmacological Society

Jul 30, 2016

Reggie BosmaHenry F Vischer

Abstract

Ligand residence time is thought to be a critical parameter for optimizing the in vivo efficacy of drug candidates. For the histamine H1 receptor (H1R) and other G protein-coupled receptors, the kinetics of ligand binding are typically measured by low throughput radioligand binding expe...read more

Mentioned in this Paper

Histamine
Histamine Antagonists
Histamine H1 Antagonists
HRH1 gene
Ceplene
Histamine Measurement
Assay
NFAT Transcription Factor 3
In Vivo
Ligand Binding
Paper Details
References
  • References32
  • Citations2
1234

BRET-based β-arrestin2 recruitment to the histamine H1 receptor for investigating antihistamine binding kinetics

Pharmacological Research : the Official Journal of the Italian Pharmacological Society

Jul 30, 2016

Reggie BosmaHenry F Vischer

PMID: 27468652

DOI: 10.1016/j.phrs.2016.07.034

Abstract

Ligand residence time is thought to be a critical parameter for optimizing the in vivo efficacy of drug candidates. For the histamine H1 receptor (H1R) and other G protein-coupled receptors, the kinetics of ligand binding are typically measured by low throughput radioligand binding expe...read more

Mentioned in this Paper

Histamine
Histamine Antagonists
Histamine H1 Antagonists
HRH1 gene
Ceplene
Histamine Measurement
Assay
NFAT Transcription Factor 3
In Vivo
Ligand Binding

Related Papers

Paper Details
References
  • References32
  • Citations2
1234
/papers/bret-based--arrestin2-recruitment-to-the/27468652