Document Detail

Tetramethylpyrazine, a Chinese drug, blocks coronary vasoconstriction by endothelin-1 and decreases plasma endothelin-1 levels in experimental animals.
MedLine Citation:
PMID:  9595468     Owner:  NLM     Status:  MEDLINE    
The purpose of this study was to investigate effects of tetramethylpyrazine (TMP), a Chinese plant-derived medicine, on coronary vasoconstriction and related electrocardiographic and histologic changes caused by endothelin-1 (ET-1), and on plasma ET-1 levels. ET-1 (75 pmol) was administered into the left coronary artery (LCA) in anesthetized closed-chest dogs with and without prior infusion of TMP (80 mg/kg). Coronary arterial diameter (CAD) was determined by coronary arteriography (CAG). Blood pressure and electrocardiogram (ECG) were monitored continuously. Histologic damage in tissues was ascertained microscopically. Plasma ET-1 and 6-keto-PGF1 levels were determined by RIA 90 min after i.v. injection of TMP (25 mg/kg; n = 5) in rabbits. Intracoronary injection of ET-1 resulted in a significant vasoconstriction of the entire vascular bed of the LCA, with a decrease in CAD of 35.9 +/- 5.7% (n = 5; p < 0.01) and ischemic changes on ECG and in tissues of endocardium, myocardium, coronary endothelial cells, and capillary vessels. Pretreatment with TMP produced a significant increase in CAD by 38.5 +/- 7.8% (n = 5; p < 0.01) and greatly suppressed the vasoconstriction produced by ET-1. The myocardial tissue damage estimated from the ratio of ischemic area for the entire area after ET-1 injection (35.6%) was completely abolished by TMP (0.6%). In addition, TMP injection induced a significant decrease in plasma ET-1 levels and an increase in 6-keto-PGF1 levels in rabbits. The Chinese medicine TMP could be a useful therapeutic agent in ischemic heart disease by suppressing coronary vasoconstriction and ischemic changes in the tissues produced by ET-1.
Z Zeng; W Zhu; X Zhou; Z Jin; H Liu; X Chen; J Pan; H Demura; M Naruse; Y Shi
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of cardiovascular pharmacology     Volume:  31 Suppl 1     ISSN:  0160-2446     ISO Abbreviation:  J. Cardiovasc. Pharmacol.     Publication Date:  1998  
Date Detail:
Created Date:  1998-07-17     Completed Date:  1998-07-17     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7902492     Medline TA:  J Cardiovasc Pharmacol     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  S313-6     Citation Subset:  IM    
Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Beijing, China.
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MeSH Terms
6-Ketoprostaglandin F1 alpha / blood
Coronary Vessels / anatomy & histology,  drug effects*
Drugs, Chinese Herbal / pharmacology*
Endothelin-1 / antagonists & inhibitors*,  blood*,  pharmacology
Pyrazines / pharmacology*
Vasoconstriction / drug effects*
Vasodilator Agents / pharmacology*
Reg. No./Substance:
0/Drugs, Chinese Herbal; 0/Endothelin-1; 0/Pyrazines; 0/Vasodilator Agents; 1124-11-4/tetramethylpyrazine; 58962-34-8/6-Ketoprostaglandin F1 alpha

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