Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 ( COX-2 ) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibitsspiperone binding to cultured rat aortic myocytes ( IC 50 =3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A ( IC 50 =0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial , antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes.