Therapeutic potential of tetrahydrobiopterin for treating vascular and cardiac disease

An L. Moens, David A. Kass

Research output: Contribution to journalReview articlepeer-review

65 Scopus citations


Tetrahydrobiopterin is the reduced unconjugated pterin that serves as an essential cofactor for the normal enzymatic function of the aromatic amino acid hydroxylases and for the nitric oxide synthases (NOS). Its role in the latter biochemistry is being increasing appreciated, as depletion or oxidation of BH4 results in a condition of NOS uncoupling, resulting in a nitroso-oxidative imbalance. Recent experimental studies support an important pathophysiologic role of BH4 deficiency as well as the therapeutic potential of BH4 repletion for hypertension, endothelial dysfunction, atherosclerosis, diabetes, cardiac hypertrophic remodeling, and heart failure. In addition to BH4, studies are also examining the potential role of folic acid therapy, because folic acid can enhance BH4 levels and the NOS coupling state. This review summarizes these recent studies focusing on the biochemistry and pharmacology of BH4 and its potential role for treating cardiovascular disease.

Original languageEnglish (US)
Pages (from-to)238-246
Number of pages9
JournalJournal of cardiovascular pharmacology
Issue number3
StatePublished - Sep 2007


  • Superoxide
  • Tetrahydrobiopterin
  • eNOS uncoupling

ASJC Scopus subject areas

  • Pharmacology
  • Cardiology and Cardiovascular Medicine


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