Synthesis of Ranolazine Metabolites and Their Anti-myocardial Ischemia Activities
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- Yao Zhangyu
- Center for Drug Discovery, College of Pharmacy, China Pharmaceutical University
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- Gong Shubo
- Department of Physiology, College of Pharmacy, China Pharmaceutical University
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- Guan Teng
- Department of Physiology, College of Pharmacy, China Pharmaceutical University
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- Li Yunman
- Department of Physiology, College of Pharmacy, China Pharmaceutical University
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- Wu Xiaoming
- Center for Drug Discovery, College of Pharmacy, China Pharmaceutical University
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- Sun Hongbin
- Center for Drug Discovery, College of Pharmacy, China Pharmaceutical University
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抄録
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.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 57 (11), 1218-1222, 2009
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390001204169411328
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- NII論文ID
- 130000124811
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 10412438
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可