PARECOXIB SODIUM

Описание

Parecoxib is a prodrug form of the COX-2 inhibitor valdecoxib . It is converted to valdecoxib by human liver microsomes in vitro and in vivo in rats, dogs, and cynomolgous monkeys. Parecoxib is also a cannabinoid (CB) receptor 1 agonist with an EC₅₀ value of 2.4 μM in HEK293 cells. It reduces hyperalgesia in a rat model of carrageenan-induced foot pad edema (ED₅₀ = 5 mg/kg) and decreases inflammation in a rat model of M. butyricum-induced arthritis (ED₅₀ = 0.08 mg/kg).

Химические свойства

White Solid

Использование

Anti-inflammatory, analgesic.

прикладной

Parecoxib sodium is a water-soluble sodium salt of the amide prodrug of valdecoxib. Parecoxibundergoes enzymatic hydrolysis in vivo to the active moiety valdecoxib, and is formulated as apowder for solution for parenteral administration. Valdecoxib is a selective inhibitor of the enzymeCOX-2.

Биологические функции

A water-soluble, injectable sodium salt form of parecoxib, an amide prodrug of the cyclooxygenase II (COX-2) selective, non-steroidal anti-inflammatory drug (NSAID) valdecoxib, with anti-inflammatory, analgesic, and antipyretic activities. Valdecoxib selectively binds to and inhibits COX-2. This prevents the conversion of arachidonic acid into prostaglandins, which are involved in the regulation of pain, inflammation, and fever. This NSAID does not inhibit COX-1 at therapeutic concentrations and, therefore, does not interfere with blood coagulation.