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Nabumetone

萘丁美酮
Mechanism of action:
Nabumetone 是一種萘基烷酮類(naphthylalkanone)衍生物。Nabumetone 為前驅藥,在肝臟中被代謝成主要活性產物 6-methoxy-2-naphthylacetic acid(6-MNA)。6-MNA 為環氧化酶(cyclooxygenase)抑制劑,對 COX-2 的抑制作用稍強於 COX-1。6-MNA 能阻斷前列腺素(prostaglandin)的生成。
Reference(s):
1. Davies NM et al. (1997). Clinical pharmacokinetics of nabumetone. The dawn of selective cyclo-oxygenase-2 inhibition? Clin Pharmacokinet.
2. Matsumoto K et al. (2015). Reductive metabolism of nabumetone by human liver microsomal and cytosolic fractions: exploratory prediction using inhibitors and substrates as marker probes. Eur J Drug Metab Pharmacokinet.
3. Nobilis M et al. (2013). Analytical power of LLE-HPLC-PDA-MS/MS in drug metabolism studies: identification of new nabumetone metabolites. J Pharm Biomed Anal.
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