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布林佐胺

布林佐胺用途

Brinzolamide(AL 4862)是碳酸酐酶(carbonic anhydrase)II抑制剂,IC50为3.19 nM。

布林佐胺名称

[ CAS 号 ]:
138890-62-7

[ 中文名 ]:
布林佐胺

[ 英文名 ]:
Brinzolamide

[中文别名 ]:

[英文别名 ]:

MFCD08067749
Birnzolamide
Brinzolamide (BRZ)
3znc
Azopt (TN)
Azopt
Brinzolamide [USAN]
Brinzolamide

布林佐胺生物活性

[ 描述 ]:

Brinzolamide(AL 4862)是碳酸酐酶(carbonic anhydrase)II抑制剂,IC50为3.19 nM。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 碳酸酐酶

研究领域 >> 其他

[参考文献]

[1]. DeSantis, L., Preclinical overview of brinzolamide. Surv Ophthalmol, 2000. 44 Suppl 2: p. S119-29.

[2]. Silver, L.H., Dose-response evaluation of the ocular hypotensive effect of brinzolamide ophthalmic suspension (Azopt). Brinzolamide Dose-Response Study Group. Surv Ophthalmol, 2000. 44 Suppl 2: p. S147-53.

[相关活性小分子]

布林佐胺物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
586.0±60.0 °C at 760 mmHg

[ 分子式 ]:
C₁₂H₂₁N₃O₅S₃

[ 分子量 ]:
383.507

[ 闪点 ]:
308.2±32.9 °C

[ 精确质量 ]:
383.064331

[ PSA ]:
163.80000

[ LogP ]:
-0.65

[ 外观性状 ]:
结晶固体

[ 蒸汽压 ]:
0.0±1.6 mmHg at 25°C

[ 折射率 ]:
1.626

[ 储存条件 ]:
?20°C

布林佐胺MSDS

布林佐胺安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38:Irritating to eyes, respiratory system and skin .

[ 安全声明 (欧洲) ]:
S26-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
XJ9095055

[ 海关编码 ]:
2935009090

布林佐胺合成路线

布林佐胺上下游产品

布林佐胺上游产品

布林佐胺下游产品

布林佐胺制备

硫脲(1.287kg,16.93mol)、苄基氯(1.858L,2.044kg,16.14mol)、13.5L乙醇和4.5L水，一起回流2h。在20min中，冷却至74℃。依次加入3-乙酰基-2.5-二氯噻吩(3.0kg,15.38mol)和10L4mol/L氢氧化钠水溶液。回流3h至反应完全，冷至室温过夜。然后加入10L水，搅拌30min,再加入3L5.25％次氯酸钠溶液，再搅拌30min。过滤收集固体，用4×2.5L水和3×2L异丙醇洗，室温空气中干燥至恒重，得4.224kg化合物(Ⅰ)，收率97％，熔点86～88℃。

布林佐胺海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

布林佐胺文献

Optimization of methazolamide-loaded solid lipid nanoparticles for ophthalmic delivery using Box-Behnken design.

J. Liposome Res. 24(3) , 171-81, (2014)

The purpose of the present study was to optimize methazolamide (MTZ)-loaded solid lipid nanoparticles (SLNs) which were used as topical eye drops by evaluating the relationship between design factors ...

Soluble CD44 and vascular endothelial growth factor levels in patients with acute primary angle closure.

Acta Ophthalmol. 93 , e261-5, (2015)

Acute elevation of intraocular pressure (IOP) in acute primary angle closure (APAC) can cause huge damage to the variable cells in the eye; however, the mechanisms that connect the two processes still...

Meta-analysis of α2-adrenergic agonists versus carbonic anhydrase inhibitors as adjunctive therapy.

Curr. Med. Res. Opin. 28(4) , 543-50, (2012)

To evaluate the efficacy of α2-adrenergic agonist (AA) brimonidine and topical carbonic anhydrase inhibitors (CAIs) dorzolamide and brinzolamide in reducing intraocular pressure (IOP) when used as adj...

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