Tetramethylpyrazine

Tetramethylpyrazine (TMP), also known as ligustrazine, is an alkylpyrazine compound and the principal active ingredient of the traditional Chinese medicinal herb Ligusticum wallichii (Chuan Xiong). It is also found in fermented foods such as nattō and cocoa beans. TMP exhibits a range of pharmacological effects including antioxidant, anti-inflammatory, vasodilative, antiplatelet aggregation, anticoagulant, and positive inotropic activities. Its mechanisms include inhibition of platelet aggregation, reduction of blood viscosity, increase in coronary flow, scavenging free radicals, protection of cerebral vessels and expansion of renal vessels. Clinically and preclinically it has been used for cardiovascular diseases (such as atherosclerosis), pulmonary arterial hypertension (PAH), chronic thromboembolic pulmonary hypertension (CTEPH), acute kidney injury (AKI), chronic kidney disease (CKD), renal fibrosis and central nervous system disorders. The drug acts through multiple pathways including modulation of calcium homeostasis in vascular smooth muscle cells; regulation of PI3K/Akt/mTORC1 signaling; antioxidant activity via Nrf2 pathway; anti-inflammatory effects by downregulating TLR4; endothelial protection via VEGF signaling; inhibition of smooth muscle proliferation via PDGF downregulation; antiplatelet activity through VCAM-1 suppression; among others[1][2][3][5][6]. TMP is rapidly absorbed after oral or intravenous administration with wide tissue distribution but has a short half-life due to rapid metabolism primarily by CYP3A4/2C9/1A2 enzymes[5]. It is widely used in China for cardiovascular indications but not approved as a pharmaceutical outside Asia.

Brand names

川青

Other names

tetramethylpyrazineligustrazineTMP