COX
Cyclooxygenase (COX) is an enzyme (specifically, a family of isozymes) that is responsible for formation of prostanoids, including thromboxane and prostaglandins such as prostacyclin. Pharmaceutical inhibition of COX can provide relief from the symptoms of inflammation and pain. Nonsteroidal anti-inflammatory drugs (NSAIDs), such as aspirin and ibuprofen, exert their effects through inhibition of COX. The two isozymes found in human are called COX-1 and COX-2 in the medical literature.
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NS-398是一种COX-2抑制剂,抑制作用呈浓度依赖性。100μM NS-398不影响COX-1活性, 而抑制COX-2活性(IC50: 3.8 μM)。
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Bufexamac是COX环氧酶抑制剂,靶点是IFN-α, EC50 为8.9 μM, 具有抗炎活性。
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Nimesulide是COX-2选择性抑制剂和非甾体抗炎化合物。
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Rofecoxib是COX-2抑制剂,IC50为18nM。
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Niflumic acid是钙离子激活的氯离子通道阻断剂,可作用于风湿性关节炎。
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