High‐expression β 1 adrenergic receptor/cell membrane chromatography method based on a target receptor to screen active ingredients from traditional C hinese medicines

β‐Adrenergic receptors are important targets for drug discovery. We have developed a new β 1 ‐adrenergic receptor cell membrane chromatography (β 1 AR ‐ CMC ) with offline ultra‐performance LC ( UPLC ) and MS method for screening active ingredients from traditional C hinese medicines. In this study, Chinese hamster ovary‐ S cells with high β 1 AR expression levels were established and used to prepare a cell membrane stationary phase in a β 1 AR ‐ CMC model. The retention fractions were separated and identified by the UPLC – MS system. The screening results found that isoimperatorin from R hizoma et R adix N otopterygii was the targeted component that could act on β 1 AR in similar manner of metoprolol as a control drug. In addition, the biological effects of active component were also investigated in order to search for a new type of β 1 AR antagonist. It will be a useful method for drug discovery as a leading compound resource.