vkor

Phenindione (Rectadione) is an indandione that has been used as an anticoagulant. Phenindione has actions similar to WARFARIN, but it is now rarely employed because of its higher incidence of severe adverse effects.

An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.

Tecarfarin sodium is a novel orally active non-competitive vitamin K epoxide reductase antagonist. Tecarfarin sodium has the antithrombotic activity.

Tecarfarin (ATI-5923) is an orally active, potent vitamin K epoxide reductase (VKOR) antagonist and cannabinoid-1 receptor inverse agonist with antithrombotic activity, which attenuates abdominal pain and increases intestinal transit in mice.

10-hydroxy Warfarin is a metabolite of (R)-warfarin .1It is formed from (R)-warfarin by the cytochrome P450 (CYP) isoform CYP3A4. 10-hydroxy Warfarin is an inhibitor of CYP2C9 (IC50= 1.6 μM), the enzyme that converts (S)-warfarin to its 6-hydroxy warfarin and 7-hydroxy warfarin metabolites.2 1.Kaminsky, L.S., and Zhang, Z.-Y.Human P450 metabolism of warfarinPharmacol. Ther.73(1)67-74(1997) 2.Jones, D.R., Kim, S.-Y., Guderyon, M., et al.Hydroxywarfarin metabolites potently inhibit CYP2C9 metabolism of S-warfarinChem. Res. Toxicol.23(5)939-945(2010)