Ranolazine-d8 (CVT 303-d8) 是 Ranolazine 的氘代物。Ranolazine (CVT 303) 是一种抗心绞痛和抗缺血剂，可通过抑制内向钠电流的后期作用 (对 INa 和 IKr 的 IC50 值分别为 6 μM 和 12 μM) 来发挥功效，而不会影响心率或血压。Ranolazine 还是脂肪酸氧化 (FAO) 的部分抑制剂。具有抗心绞痛作用。
Ranolazine-d8 (CVT 303-d8) is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Keating GM. Ranolazine: a review of its use as add-on therapy in patients with chronic stable angina pectoris. Drugs. 2013 Jan;73(1):55-73.
[3]. Wang WQ, et al. Antitorsadogenic effects of ({+/-})-N-(2,6-dimethyl-phenyl)-(4[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazine (ranolazine) in anesthetized rabbits. J Pharmacol Exp Ther. 2008 Jun;325(3):875-81.
[4]. Zacharowski K, et al. Ranolazine, a partial fatty acid oxidation inhibitor, reduces myocardial infarct size and cardiac troponin T release in the rat. Eur J Pharmacol. 2001 Apr 20;418(1-2):105-10.
动态评分
0.0