Ranolazine-d₈ dihydrochloride  (Synonyms: CVT 303-dd₈ dihydrochloride; RS 43285-d₈)

Ranolazine-d₈ (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent 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 dihydrochloride is also a partial fatty acid oxidation inhibitor[3].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

508.51

C₂₄H₂₇D₈Cl₂N₃O₄

1219802-60-4

固体

White to off-white

盐酸雷诺嗪 d₈ (双盐酸盐)

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [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.  [Content Brief]

  [3]. Wang WQ, Robertson C, Dhalla AK, Belardinelli L. 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. doi: 10.1124/jpet.108.137729. Epub 2008 Mar 5.  [Content Brief]

  [4]. Zacharowski K, Blackburn B, Thiemermann C. 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.  [Content Brief]