产品说明书

Methazolamide

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Chemical Structure| 554-57-4 同义名 : L584601;CL 8490;N Methylacetazolamide;Naptazane;Neptazaneat;Methenamide;Neptazane
CAS号 : 554-57-4
货号 : A120295
分子式 : C5H8N4O3S2
纯度 : 98%
分子量 : 236.272
MDL号 : MFCD00083416
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(211.62 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+water 8 mg/mL clear

PO 0.5% CMC-Na 32 mg/mL suspension

生物活性
靶点

  • Carbonic Anhydrase IV

    bCAIV, Ki:36 nM

  • Carbonic Anhydrase I

    hCAI, Ki:50 nM

  • Carbonic Anhydrase II

    hCAII, Ki:14 nM
描述 Methazolamide (L584601) is a sulfonamide derivative used as a carbonic anhydrase inhibitor with a Ki of 14 nM for human carbonic anhydrase II[3]. Methazolamide is an intraocular pressure-lowering drug that is used in the treatment of glaucoma and other ophthalmologic abnormalities[4]. Methazolamide can increase systemic metabolic acidosis and sequentially improve ventilation and oxygenation level. In addition to the effect as a carbonic anhydrase inhibitor, methazolamide directly activates the transcription factor anti-oxidative nuclear factor-related factor 2 (Nrf2) and inhibits interleukin-1β (IL-1β) release. Methazolamide may thus represent an alternative for acetazolamide when taken for high-altitude illnesses prophylaxis and treatment[5]. Methazolamide exhibits dose-dependent efficacy for the treatment of excessive erythrocytosis induced by long-term hypoxia[6].
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
NCT03165045 - Active, not recruiting January 31, 2019 -
NCT03362021 - Recruiting March 2019 Greece ... 展开 >> Attikon University Hospital Recruiting Athens, Attiki, Greece, 12462 Contact: Paraskevi MATSOTA, MD, PhD    00302105832374    matsota@yahoo.gr    Principal Investigator: PARASKEVI MATSOTA, MD, PHD 收起 <<
NCT02390284 Glaucoma Phase 3 Recruiting July 2019 United States, Florida ... 展开 >> Bascom Palmer Eye Institute - University of Miami Recruiting Miami, Florida, United States, 33136 Contact: Marlene Perez, RC    305-482-4309    marlene.perez@med.miami.edu    Contact: Shiva Roghaee, RA    305 482 4309    sxr935@med.miami.edu    Principal Investigator: Vittorio Porciatti, DSc          Sub-Investigator: John J McSoley, OD          Sub-Investigator: Luis E Vazquez, MD,PhD          Sub-Investigator: Steven J Gedde, MD          Sub-Investigator: Pedro F Monsalve, RA          Sub-Investigator: Maja Kostic, PhD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.23mL

0.85mL

0.42mL

21.16mL

4.23mL

2.12mL

42.32mL

8.46mL

4.23mL
参考文献

[1]Casini A, Antel J, et al. Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IV. Bioorg Med Chem Lett. 2003 Mar 10;13(5):841-5.

[2]Kiwull-Schone HF, Li Y, et al. Methazolamide does not impair respiratory work performance in anesthetized rabbits. Am J Physiol Regul Integr Comp Physiol. 2009 Sep;297(3):R648-54.

[3]Abbate F, Casini A, Scozzafava A, Supuran CT. Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the perfluorobenzoyl analogue of methazolamide. Implications for the drug design of fluorinated inhibitors. J Enzyme Inhib Med Chem. 2003 Aug;18(4):303-8

[4]Yang F, Xuan J, Chen J, Zhong H, Luo H, Zhou P, Sun X, He L, Chen S, Cao Z, Luo X, Xing Q. HLA-B*59:01: a marker for Stevens-Johnson syndrome/toxic epidermal necrolysis caused by methazolamide in Han Chinese. Pharmacogenomics J. 2016 Feb;16(1):83-7

[5]Lu H, Zhang H, Jiang Y. Methazolamide in high-altitude illnesses. Eur J Pharm Sci. 2020 May 30;148:105326

[6]Zhang Z, Xiao Z, Deng B, Liu X, Liu W, Nie H, Li X, Chen Z, Yang D, Duan R. Therapeutic Efficacy of Methazolamide Against Intermittent Hypoxia-Induced Excessive Erythrocytosis in Rats. High Alt Med Biol. 2018 Mar;19(1):69-80