Brinzolamide is a carbonic anhydrase inhibitor used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
CAT No: 10-101-134
CAS No:138890-62-7
Synonyms/Alias:AGN-190342; AL-4862; AL 4862; AL4862; UK-14304; (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide(R)-4-Ethylamino-2-(3-methoxypropyl)-1,1-dioxo-1,2,3,4-tetrahydro-1λ6-thieno[3,2-e][1,2]thiazine-6-sulfonic acid amide
Chemical Name:(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide
Brinzolamide is a synthetic sulfonamide derivative recognized for its role as a selective carbonic anhydrase II (CA-II) inhibitor. Structurally distinct from naturally occurring amino acids or peptides, it represents a small-molecule compound with significant relevance in enzymology and biochemical research. Its mechanistic specificity for CA-II has made it an essential tool in the study of carbonic anhydrase function, isoform selectivity, and inhibitor design. The compound's unique inhibitory profile allows researchers to explore fundamental aspects of enzyme regulation, acid-base homeostasis, and the physiological consequences of carbonic anhydrase modulation in various biological systems.
Enzyme inhibition studies: Brinzolamide is widely utilized in biochemical assays to investigate the kinetics and inhibition profiles of carbonic anhydrase isoforms, particularly CA-II. By providing a highly selective inhibitory effect, it enables researchers to dissect the catalytic mechanisms and substrate interactions of carbonic anhydrases in vitro. This application is pivotal for elucidating structure-activity relationships, validating inhibitory potency, and characterizing the molecular determinants of isoform selectivity, all of which inform the rational design of next-generation enzyme inhibitors.
Physiological pathway analysis: In experimental models, brinzolamide serves as a probe to modulate intracellular and extracellular pH regulation mediated by carbonic anhydrase activity. Its selective inhibition allows scientists to examine the consequences of altered bicarbonate production and CO2 transport in tissues such as the kidney, eye, and central nervous system. This approach is instrumental in unraveling the roles of carbonic anhydrases in fluid secretion, electrolyte balance, and cellular acid-base homeostasis, providing insight into both normal physiology and pathophysiological conditions.
Drug discovery and SAR research: As a reference compound, brinzolamide is frequently employed in structure-activity relationship (SAR) studies aimed at developing novel carbonic anhydrase inhibitors. Its well-characterized binding mode and inhibitory constants serve as benchmarks for the evaluation of new chemical entities. Researchers leverage this compound to assess the impact of chemical modifications on potency, selectivity, and pharmacodynamic properties, accelerating the optimization of lead compounds in early-stage drug discovery pipelines.
Analytical method development: The compound is also valuable in the development and validation of analytical methodologies, such as high-performance liquid chromatography (HPLC) and mass spectrometry, for the quantification of sulfonamide-type inhibitors in biological matrices. Its physicochemical properties and stability make it a suitable standard for calibrating detection systems, optimizing extraction protocols, and ensuring the accuracy and reproducibility of quantitative assays in laboratory settings.
Comparative enzymology: Brinzolamide's selective inhibition profile supports comparative studies across different carbonic anhydrase isoforms and species. By leveraging its differential activity, researchers can explore evolutionary conservation and divergence in enzyme structure and function, as well as investigate the molecular basis for species-specific inhibitor sensitivity. Such studies contribute to a deeper understanding of enzyme evolution, functional specialization, and the development of isoform-targeted research tools.
Brinzolamide is a novel carbonic anhydrase inhibitor that elicits an ocular hypotensive effect when instilled topically. A multicenter, double-masked, placebo-controlled, parallel trial was conducted to evaluate the optimal intraocular pressure (IOP)-lowering concentration and ocular tolerability of topically administered brinzolamide (0.3%, 1%, 2%, and 3%) in patients with primary, open-angle glaucoma or ocular hypertension.
Silver L H, Brinzolamide Dose-Response Study Group. Dose-response evaluation of the ocular hypotensive effect of brinzolamide ophthalmic suspension (Azopt®)[J]. Survey of ophthalmology, 2000, 44: S147-S153.
To assess the effects of brinzolamide and dorzolamide on ocular haemodynamics and retinal oxygen saturation in patients with primary open-angle glaucoma (OAG). This pilot study suggests that brinzolamide and dorzolamide may increase retinal oxygen saturation in patients with OAG.
Siesky B, Harris A, Cantor L B, et al. A comparative study of the effects of brinzolamide and dorzolamide on retinal oxygen saturation and ocular microcirculation in patients with primary open-angle glaucoma[J]. British journal of ophthalmology, 2008, 92(4): 500-504.
Brinzolamide 1.0% produced clinically relevant intraocular pressure reductions in substantial numbers of patients. Brinzolamide's effectiveness equaled that of dorzolamide 2.0% and it produced less ocular discomfort (burning and stinging) on instillation.
Silver L H, Group T B P T S. Clinical efficacy and safety of brinzolamide (AzoptTM), a new topical carbonic anhydrase inhibitor for primary open-angle glaucoma and ocular hypertension[J]. American journal of ophthalmology, 1998, 126(3): 400-408.
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