Higenamine (HG) is a well-known selective activator of beta2-adrenergic receptor (β2-AR) with a positive inotropic effect. HG exerts an antispasmodic effect on cold-induced vasoconstriction by regulating the PI3K/Akt, ROS/α2C-AR and PTK9 pathways independently of the AMPK/eNOS/NO axis, it reduces HMGB1 during hypoxia-induced brain injury by induction of heme oxygenase-1 through PI3K/Akt/Nrf-2 signal pathways. HG enhances the antitumor effects of cucurbitacin B in breast cancer by inhibiting the interaction of AKT and CDK2. It attenuated LPS-induced depression-like behavior by regulating BDNF-mediated ER stress and autophagy. Demethylcoclaurine hydrochloride is a member of isoquinolines.