Here, we discuss the biological activity of synephrine, its source, chemical and pharmacological features, target receptors, anti-inflammatory, anti-cancer, and other effects, as well as its possible derivatives as potential clinical benefits in comparison with the effects of GR ligands, selective glucocorticoid receptors agonist CpdA, which are structurally similar to synephrine. The gene discussed is NR3C1; the disease is cancer.