CAS:138890-62-7Brinzolamide

Synonyms: AL 4862

Brinzolamide is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

138890-62-7

储存条件

分子式

C12H21N3O5S3

运输

蓝冰

分子量

383.51

别名

AL 4862

溶解度

动物实验配方

生物活性

描述Brinzolamide, the newest topical CAI, exhibits selectivity, high affinity, and potent inhibitory activity for the carbonic anhydrase type II isozyme (CA-II), which is involved in aqueous humor secretion. Notable among its attributes as a safe and efficacious glaucoma drug is brinzolamide's superior ocular comfort profile because of its optimized suspension formulation at physiologic pH. Brinzolamide (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours. Brinzolamide dosages of 30 mg/kg, produces a 44% reduction in intestinal charcoal meal progression, but 1 and 10 mg/kg produced 8% and 18% decreases, respectively, in male CD-1 mice. Brinzolamide of 1 mg/kg, 10 mg/kg, and 30 mg/kg prolongs barbiturate sleep time by 57%, 15%, and 35%, respectively, in male CD-1 mice^[3]. The optimal intraocular pressure-lowering concentration of brinzolamide is 1%, brinzolamide 1% is well tolerated by patients with primary open-angle glaucoma or ocular hypertension when administered twice daily^[4].