An active metabolite of diclofenac
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Diclofenac acyl-β-D-glucuronide is an active metabolite of diclofenac and the predominant metabolite in rat. Diclofenac acyl-β-D-glucuronide is acutely toxic in vitro, suggesting it may play a role in the hepatotoxicty of diclofenac in vivo. Diclofenac acyl-β-D-glucuronide binds to organic anion transporters (OATs; Km = 60.2, 8.6, 112, and 103.9 µM for OAT1-4, respectively) as well as multi-drug resistance proteins. High levels of diclofenac are found in waste water treatment plant samples, which may be due to the back-transformation of diclofenac acyl-β-D-glucuronide to diclofenac.
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