Brinzolamide-d5 is intended for use as an internal standard for the quantification of brinzolamide by GC- or LC-MS. Brinzolamide is a potent inhibitor of carbonic anhydrase II (CAII) and CAIV (IC50s = 3.19 and 45.3 nM, respectively).1 It is selective for CAII and CAIV over CAI (IC50 = ~1,365 nM). Brinzolamide (30 mg/kg) reduces intestinal charcoal meal progression by 44% and prolongs pentobarbital sodium-induced sleep time by 35% in mice. Topical administration of brinzolamide (0.25, 0.5, and 1 mg/eye) reduces intraocular pressure in a rabbit model of spontaneous ocular hypertension. It also reduces intraocular pressure in a cynomolgus monkey model of argon laser trabeculoplasty-induced ocular hypertension. Formulations containing brinzolamide have been used in the treatment of glaucoma and ocular hypertension.
|1. DeSantis, L. Preclinical overview of brinzolamide. Surv. Ophthalmol. 44(Suppl. 2), S119-S129 (2000).