Nabumetone

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Chemical Structure| 42924-53-8 同义名 : BRL14777
CAS号 : 42924-53-8
货号 : A307752
分子式 : C15H16O2
纯度 : 98%
分子量 : 228.29
MDL号 : MFCD00079518
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • COX

  • COX
描述 Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the prodrug of the active metabolite 6MNA. Nabumetone (50 μmol - 2 mmol) dose-dependently inhibits the proliferation of K-562 and Meg-01 cells, but shows no obvious apoptotic effect. Nabumetone potentiates the apoptotic effect of ADR (Adriamycin) in the K-562 cell line. Moreover, Nabumetone reduces Bcl-2 expression[3]. An oral dose of nabumetone (79 mg/kg) or intravenous 6MNA produced effective anti-inflammatory activity together with significant inhibition of paw exudate PGE2. An anti-inflammatory oral dose of nabumetone or intravenous 6MNA produced minimal effects on gastric 6-keto-PGF1 alpha production, with an absence of gastric damage, in contrast to indomethacin[4]. When compared with currently available NSAIDs, nabumetone may be associated with a significantly lower incidence of gastroduodenal ulcer, and that nabumetone also appears to be safer for use in elderly patients and in those with renal or hepatic impairment[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01638962 Osteoarthritis, Knee Not Applicable Completed - Denmark ... 展开 >> University of Southern Denmark Odense, Region Syddanmark, Denmark, 5230 收起 <<
NCT01761864 Study Focus: Prescribing of Dr... 展开 >>ugs 收起 << Not Applicable Unknown January 2016 Belgium ... 展开 >> University of Antwerp Wilrijk, Belgium, 2610 收起 <<
NCT00363532 Migraine Without Aura Not Applicable Completed - Denmark ... 展开 >> Danish Headache Center, Neurological Dep. Glostrup hospital Glostrup, Denmark, 2770 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.38mL

0.88mL

0.44mL

21.90mL

4.38mL

2.19mL

43.80mL

8.76mL

4.38mL
参考文献

[1]Hedner T, Samulesson O, et al. Nabumetone: therapeutic use and safety profile in the management of osteoarthritis and rheumatoid arthritis. Drugs. 2004;64(20):2315-43; discussion 2344-5.

[2]Boyle EA, Freeman PC, et al. Nabumetone (BRL 14777, 4-[6-methoxy-2-naphthyl] -butan-2-one): a new anti-inflammatory agent. J Pharm Pharmacol. 1982 Sep;34(9):562-9.

[3]Vural F, Ozcan MA, Ozsan GH, Ateş H, Demirkan F, Pişkin O, Undar B. Cyclo-oxygenase 2 inhibitor, nabumetone, inhibits proliferation in chronic myeloid leukemia cell lines. Leuk Lymphoma. 2005 May;46(5):753-6

[4]Melarange R, Gentry C, O'Connell C, Blower PR, Neil C, Kelvin AS, Toseland CD. Anti-inflammatory and gastrointestinal effects of nabumetone or its active metabolite, 6MNA (6-methoxy-2-naphthylacetic acid): comparison with indomethacin. Agents Actions. 1992;Spec No:C82-3

[5]Roth SH. Nabumetone: a new NSAID for rheumatoid arthritis and osteoarthritis. Orthop Rev. 1992 Feb;21(2):223-7