Diclofenac diethylamine抑制剂、激动剂(CAS号78213-16-8)Diclofenac二乙胺是非选择性COX抑制剂,为非甾体抗炎化合物。 Diclofenac Diethylamine is a non-selective COX inhibitor used as a nonsteroidal anti-inflammatory drug (NSAID).
Target: COX
Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) taken or applied to reduce inflammation and as an analgesic reducing pain in certain conditions. The exact mechanism of action is not entirely known, but the primary mechanism responsible for its anti-inflammatory, antipyretic, and analgesic action is thought to be inhibition of prostaglandin synthesis by inhibition of cyclooxygenase (COX). It also appears to exhibit bacteriostatic activity by inhibiting bacterial DNA synthesis [1]. Diclofenac was an equipotent inhibitor of COX-1 and COX-2. Diclofenac were the most potent inhibitors of COX-1 (IC50 = 0.611 microM) and COX-2 isoforms (IC50 = 0.63 microM) [2]. Inhibition of COX also decreases prostaglandins in the epithelium of the stomach, making it more sensitive to corrosion by gastric acid. The action of one single dose is much longer (6 to 8 hr) than the very short half-life of the drug indicates.[citation needed] This could be partly because it persists for over 11 hours in synovial fluids [3].