Pharmacological characterization of new β-agonists using Huβ1- and Huβ2-adrenergic receptor binding assay in transfected HEK-293 cells
- 作者：Civitareale ; Cinzia ; Ambrosio ; Caterina ; Sbraccia ; Maria ; Fiori ; Maurizio ; Brambilla ; Gianfranco ; et. al.
- 关键词：β ; -Adrenoceptor agonists ; β ; -Adrenergic receptors ; Receptor binding assay ; Human embryonic kidney cells
- 刊名：Analytica Chimica Acta
- 出版年：2005
- 期刊代码：2_00032670
- 类别：ch
- 出版时间：January 24, 2005
- 卷：529
- 期：1-2
- 页码：53-56
- 文件大小：110 K
摘要
The continuous turn over of β-agonists molecules, may affect the reliability of screening tests. To overcome possible false negative results, a bioassay is under development to detect the presence of new β-agonists in feeds and biological matrices and so to provide a valid tool for a multi-analyte screening method. Preliminary study were focused on the pharmacological characterisation of new β-agonists, with the aim to combine both the screening results with a toxicological evaluation about the potential health risk for consumers. The interaction of G4, G5, G6, G8 adrenergic drugs with human β1- and β2-adrenergic receptors expressed separately in membranes of human embryonic kidney cells in culture (HEK-293-Huβ1 and HEK-293-Huβ2), were studied by a receptor binding assay and results compared with those from a well-known β-adrenergic agonist (clenbuterol). The specificity of the test was assured by the use of a specific radiolabel tracer ligand ([125I]iodopindolol) as competitor.