パレコキシブナトリウム 化學(xué)特性,用途語(yǔ),生産方法
効能
鎮(zhèn)痛薬, 抗炎癥薬, シクロオキシゲナーゼ2阻害薬
説明
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 EC
50 value of 2.4 μM in HEK293 cells. It reduces hyperalgesia in a rat model of carrageenan-induced foot pad edema (ED
50 = 5 mg/kg) and decreases inflammation in a rat model of
M. butyricum-induced arthritis (ED
50 = 0.08 mg/kg).
化學(xué)的特性
White Solid
使用
Anti-inflammatory, analgesic.
主な応用
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.
生物學(xué)の機(jī)能
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.
パレコキシブナトリウム 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品