High‐expression β1 adrenergic receptor/cell membrane chromatography method based on a target receptor to screen active ingredients from traditional Chinese medicines

β-Adrenergic receptors are important targets for drug discovery. We have developed a new β1-adrenergic receptor cell membrane chromatography (β1AR-CMC) with offline ultra-performance LC (UPLC) and MS method for screening active ingredients from traditional Chinese medicines. In this study, Chinese hamster ovary-S cells with high β1AR expression levels were established and used to prepare a cell membrane stationary phase in a β1AR-CMC model. The retention fractions were separated and identified by the UPLC–MS system. The screening results found that isoimperatorin from Rhizoma et Radix Notopterygii was the targeted component that could act on β1AR 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 β1AR antagonist. It will be a useful method for drug discovery as a leading compound resource.