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- W2056521778 endingPage "58" @default.
- W2056521778 startingPage "33" @default.
- W2056521778 abstract "The human histamine receptors hH(1)R and hH(2)R constitute important drug targets, and hH(3)R and hH(4)R have substantial potential in this area. Considering the species-specificity of pharmacology of H(x)R orthologs, it is important to analyze hH(x)Rs. Here, we summarize current knowledge of hH(x)Rs endogenously expressed in human cells and hH(x)Rs recombinantly expressed in mammalian and insect cells. We present the advantages and disadvantages of the various systems. We also discuss problems associated with the use of hH(x)R antibodies, an issue of general relevance for G-protein-coupled receptors (GPCRs). There is much greater overlap in activity of 'selective' ligands for other hH(x)Rs than the cognate receptor subtype than generally appreciated. Studies with native and recombinant systems support the concept of ligand-specific receptor conformations, encompassing agonists and antagonists. It is emerging that for characterization of hH(x)R ligands, one cannot rely on a single test system and a single parameter. Rather, multiple systems and parameters have to be studied. Although such studies are time-consuming and expensive, ultimately, they will increase drug safety and efficacy." @default.
- W2056521778 created "2016-06-24" @default.
- W2056521778 creator A5007797524 @default.
- W2056521778 creator A5026325920 @default.
- W2056521778 creator A5040439170 @default.
- W2056521778 creator A5044768118 @default.
- W2056521778 creator A5082356190 @default.
- W2056521778 creator A5088719485 @default.
- W2056521778 date "2013-01-01" @default.
- W2056521778 modified "2023-10-01" @default.
- W2056521778 title "Molecular and cellular analysis of human histamine receptor subtypes" @default.
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