138890-62-7 Brinzolamide CAS NO.138890-62-7

brinzolamide chemical properties

melting point 130.0 to 134.0 °c

storage temp. 20°c

solubility dmso: ≥10mg/ml

color white to beige

merck 14,1376

cas database reference 138890-62-7(cas database reference)

safety information

rtecs xj9095055

msds information

brinzolamide usage and synthesis

ophthalmic drugs brinzolamide is a kind of novel heterocyclic sulfa topical carbonic anhydrase inhibitor. it has a strong affinity and inhibition on the carbonic anhydrase isoenzyme ii (caii) in human ciliary body. it can selectively and significantly inhibit the activity of isozyme ii carbonic anhydrase with high-affinity. it can effectively reduce the intraocular pressure with high efficiency, low toxicity, and small side effects. its physiological ph and suspension design makes the drug able to ensure eye comfort and thus admired by patients of all ages. it can be as a single drug treatment way for patients to whom β-blockers is ineffective or is contraindicated or used as a co-cure treatment drug together with β-blocker. after being dropped into the eye it can quickly enter into tissue, and has a long half-life in the iris, ciliary body, choroid, retina, and lens as well as in the blood. treating rabbit eyes with brinzolamide can further increase blood flow to the optic nerve which helps patients of glaucoma optic neuropathy. it has become the primary way for treatment of open angle glaucoma line drugs.

carbonic anhydrase (ca) is one of the major protein components of red blood cells. its position is only second to hemoglobin in the blood cell, which is presented in many body tissues including the eye organizations. carbonic anhydrase catalyzed hydration reaction of carbon dioxide into carbonic acid, and the reversible dehydration reaction of carbonic acid. inhibition of carbonic anhydrase in the ocular ciliary body can reduce the water secretion of camera aquosa. it reduces the transport of sodium and water possibly by reducing the generation of bicarbonate ions, and ultimately reduces the intraocular pressure. iop is an important risk factor for glaucoma optic nerve damage and glaucomatous visual field defects. brinzolamide mainly inhibits the dominant carbonic anhydrase type 2 isoenzyme in the eye tissue. in vitro tests had shown that the ic50 was 3.2nm and the ki value to the carbonic anhydrase type-ii isoenzyme was 0.13 nm.