2. Academic Validation
  3. Synthesis of ranolazine metabolites and their anti-myocardial ischemia activities

Synthesis of ranolazine metabolites and their anti-myocardial ischemia activities

  • Chem Pharm Bull (Tokyo). 2009 Nov;57(11):1218-22. doi: 10.1248/cpb.57.1218.
Zhangyu Yao 1,  Shubo Gong,  Teng Guan,  Yunman Li,  Xiaoming Wu,  Hongbin Sun
Affiliations

Affiliation

  • 1 Center for Drug Discovery, College of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
PMID: 19881270 DOI: 10.1248/cpb.57.1218
Abstract

The anti-anginal drug Ranolazine, a partial fatty acid oxidation (pFOX) inhibitor, is thought to modulate the metabolism during myocardial ischemia by activating pyruvate dehydrogenase activity to promote glucose oxidation. Ranolazine and its five principal metabolites: CVT-2512, CVT-2513, CVT-2514, CVT-2738 and CVT-4786, were synthesized. The effect of Ranolazine and its metabolites on the ECG (electrocardiogram) of mice with myocardial ischemia induced by isoprenaline and their effect on alleviating the symptom of myocardial ischemia were tested and compared. The results showed that CVT-2738 and CVT-2513 could be protective against mice myocardial ischemia induced by isoprenaline. Within all the metabolites tested in this study, CVT-2738 exhibited the best potency, however, it was still less potent than Ranolazine.

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