Ligustrazine — Tetramethylpyrazine (Pyrazine Alkaloid · Vasodilatory · Cerebrovascular · TCM)
| Compound | Ligustrazine (Tetramethylpyrazine, TMP) |
| Chemical class | Alkaloid — Pyrazine (2,3,5,6-Tetramethylpyrazine) |
| CAS | 1124-11-4 |
| Primary source | Ligusticum chuanxiong (Chuanxiong / Szechuan lovage rhizome), fermented foods |
| Key applications | Vasodilatory, antiplatelet, cerebrovascular, neuroprotective, TCM microcirculation-promoting |
| Claim strength | Moderate |
| Typical form | Chuanxiong (Ligusticum chuanxiong) extract; TMP isolate; IV pharmaceutical (China) |
| Buy from Herbuno | Request availability and bulk pricing → |
Name origin: From Ligusticum (the plant genus) + -azine (pyrazine ring class). Tetramethylpyrazine (TMP) describes the chemical structure: four methyl groups on a pyrazine (diazine) ring. Ligustrazine is the same compound as TMP, with the botanical name used in pharmacological contexts and the chemical name in chemistry contexts. It is also produced by fermentation — TMP is formed during the Maillard reaction in fermented foods (soy sauce, vinegar, cocoa, Pu-erh tea) alongside other pyrazines. Traditional use: Chuanxiong (Ligusticum chuanxiong, Sichuan lovage) is one of the most important TCM herbs for blood-moving (promoting circulation) applications — used for over 2,000 years for headache, menstrual irregularity, cardiovascular conditions, and cerebrovascular disease. Ligustrazine was first isolated from Chuanxiong in 1972 by Chinese researchers and identified as the primary vasoactive alkaloid, initiating extensive TCM-pharmaceutical research. Research trajectory: Ligustrazine has been extensively studied in Chinese clinical contexts. IV TMP injection is a recognised treatment modality in Chinese hospitals for ischaemic stroke, coronary artery disease, and diabetic microvascular complications — with hundreds of Chinese clinical trials and a substantial Chinese meta-analysis literature. Multiple systematic reviews of Chinese RCTs (acknowledging quality variation) support vasodilatory, antiplatelet, neuroprotective, and cardioprotective activity. Commercial source: Ligusticum Chuanxiong extract is not currently available at commercial supplement scale from Herbuno. Contact Herbuno for availability assessment.
Evidence for Ligustrazine Applications
Vasodilatory and antihypertensive: Ligustrazine inhibits calcium channel activity (L-type VDCC antagonism), phosphodiesterase inhibition (elevating cAMP/cGMP), and promotes NO release from vascular endothelium. This multi-mechanism vasodilation is the basis for its IV use in Chinese hospitals for coronary artery disease and cerebrovascular conditions. Human clinical data are primarily from IV administration in Chinese clinical contexts — oral bioavailability and equivalent oral dosing are less well-characterised. Claim strength: Moderate (Chinese clinical IV context; oral supplement data limited).
Antiplatelet and antithrombotic: Ligustrazine inhibits platelet aggregation (inhibiting TXA2 synthesis and cAMP-PDE) and reduces blood viscosity — mechanisms relevant to thromboembolic risk reduction. Meta-analyses of Chinese RCTs for unstable angina and ischaemic stroke show significant benefit in Chinese clinical contexts. Claim strength: Moderate.
Neuroprotective — ischaemia: Ligustrazine reduces cerebral infarct volume in MCAO (middle cerebral artery occlusion) animal models, reduces neuroinflammation, and promotes neuronal survival via multiple mechanisms (antioxidant, anti-apoptotic, BDNF upregulation). Multiple Chinese clinical trials for ischaemic stroke with IV TMP show improvements in neurological function scores. Claim strength: Moderate (Chinese RCT context; IV administration).
Diabetic microvascular complications: Chinese RCTs with ligustrazine in diabetic nephropathy, retinopathy, and peripheral neuropathy patients show improvements in microcirculatory parameters. Anti-endothelin and anti-PDGF mechanisms are proposed for anti-fibrotic renal protection. Claim strength: Moderate (Chinese RCTs; IV context).
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Dosage & Formulator Specification
Chinese pharmaceutical IV use: 40–160 mg TMP in 250 mL saline IV infusion, once or twice daily for 10–14 days. Oral supplement dose is not well-established from controlled RCTs — oral bioavailability of TMP is approximately 80–90% in animal studies (good for a small molecule alkaloid). Extrapolation from IV clinical doses: 100–300 mg/day oral TMP is used in some Chinese oral supplement formulations. Ligustrazine is also produced by fermentation — fermented Chuanxiong preparations provide TMP alongside other pyrazines and ligustilide. Contact Herbuno for Chuanxiong extract availability and TMP quantification.
Frequently Asked Questions — Ligustrazine
Why is ligustrazine mainly studied in Chinese clinical contexts?
Ligustrazine (TMP) is approved as an IV pharmaceutical in China for cardiovascular and cerebrovascular applications — a regulatory context that does not exist in Western markets. The extensive Chinese clinical literature reflects this pharmaceutical use, not Western dietary supplement research. Western supplement companies have adopted TMP as an oral supplement based on the Chinese evidence base, but the same IV-to-oral extrapolation issues apply as for glycyrrhizin. The quality of Chinese RCTs varies significantly — systematic reviews apply strict quality filters that reduce the effective evidence base.
Is ligustrazine the same as the pyrazines in chocolate or soy sauce?
Ligustrazine (2,3,5,6-tetramethylpyrazine) is one of hundreds of pyrazines formed in Maillard reactions during roasting, fermentation, and cooking. It is present in trace amounts in cocoa, soy sauce, roasted coffee, Pu-erh tea, and other fermented or heat-processed foods. The pharmacological concentrations studied (40–300 mg/day) are far above dietary exposure from food consumption, so the health-relevant exposure is from concentrated extract or supplement preparations rather than food.
Can ligustrazine be used for post-stroke recovery?
The Chinese clinical literature on TMP IV infusion for ischaemic stroke recovery is substantial (hundreds of RCTs, multiple systematic reviews). However, most Western neurological guidelines do not recommend TMP for stroke management, and the translation from IV to oral formulation for supplement marketing requires careful evidence-level communication. For supplement positioning, describe as “studied in traditional Chinese medicine for cerebrovascular support” rather than referencing stroke treatment claims that imply pharmaceutical-level efficacy from supplement doses.
Does ligustrazine interact with other cardiovascular medications?
Given its vasodilatory and antiplatelet mechanisms, ligustrazine has potential interactions with: calcium channel blockers (additive vasodilation), nitrates (additive hypotension), anticoagulants and antiplatelet agents (additive bleeding risk), and antihypertensives (additive blood pressure reduction). These interactions are mechanistically predicted from the pharmacology and are not all specifically documented in controlled drug interaction studies. Standard advisory language for cardiovascular medication combinations applies.
Related compounds: Vasicinone, Deoxyvasicinone, Andrographolide, Glycyrrhizin
Claim-strength scale – High = multiple human RCTs; Moderate = limited trials or strong preclinical convergence; Emerging = early-stage lab or animal data.
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