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 compound widely recognized for its role as a carbonic anhydrase inhibitor. Its unique chemical structure allows it to selectively target and inhibit the activity of carbonic anhydrase II, making it a valuable tool in various biochemical and pharmaceutical research contexts. The compound's solubility and stability under standard laboratory conditions further enhance its versatility, enabling researchers to integrate it into diverse experimental protocols. Due to its well-characterized mechanism of action, Brinzolamide has become a staple in the study of enzyme inhibition, ocular pharmacology, and the exploration of metabolic processes influenced by carbonic anhydrase activity. Its compatibility with in vitro assays and cell-based studies ensures that it remains relevant across multiple scientific disciplines, supporting the advancement of both fundamental and applied research.
Ophthalmic Research: In the field of ophthalmic research, Brinzolamide is extensively utilized to investigate the modulation of intraocular pressure and aqueous humor dynamics. By inhibiting carbonic anhydrase in ciliary body tissues, the compound reduces bicarbonate ion formation, subsequently decreasing fluid transport and secretion. This mechanism allows scientists to elucidate the physiological pathways regulating eye pressure, providing critical insights into the development of novel interventions for ocular disorders. Utilizing Brinzolamide in experimental models helps researchers dissect the contribution of carbonic anhydrase to eye health and disease, paving the way for the discovery of innovative therapeutic targets.
Enzyme Inhibition Studies: As a prototypical carbonic anhydrase inhibitor, Brinzolamide serves as a reference compound in enzyme inhibition assays. Its selective action against the enzyme allows for the precise characterization of inhibitory activity, supporting the validation of new inhibitors and the assessment of structure-activity relationships. Researchers frequently employ it as a positive control in high-throughput screening platforms, ensuring the reliability and reproducibility of experimental outcomes. This application is critical for advancing the understanding of enzyme kinetics and for the rational design of next-generation carbonic anhydrase modulators.
Metabolic Pathway Analysis: Brinzolamide's influence on carbonic anhydrase activity extends to the study of metabolic pathways involving acid-base balance and ion transport. By modulating the enzyme's function, researchers can investigate the downstream effects on cellular pH regulation, CO2 transport, and electrolyte homeostasis. This approach is instrumental in unraveling the complex interplay between carbonic anhydrase and various physiological processes, offering new perspectives on cellular metabolism and its dysregulation in pathological states. The compound's utility in both isolated cell systems and tissue preparations broadens its applicability in metabolic research.
Pharmacological Profiling: In drug discovery and development, Brinzolamide is frequently employed to profile the pharmacological properties of candidate molecules targeting carbonic anhydrase. Its well-documented activity provides a benchmark for evaluating the potency, selectivity, and off-target effects of novel compounds. Comparative studies using Brinzolamide help delineate the molecular determinants of inhibitor efficacy and inform the optimization of lead compounds. This application is essential for guiding medicinal chemistry efforts and for bridging the gap between early-stage research and preclinical evaluation.
Toxicological Assessment: Toxicology studies often incorporate Brinzolamide to assess the safety and cellular response to carbonic anhydrase inhibition. By monitoring cellular viability, stress markers, and compensatory mechanisms following exposure to the compound, researchers gain valuable information about the potential risks associated with enzyme modulation. These investigations contribute to the broader understanding of sulfonamide compound safety profiles and support the identification of adverse effects that may arise from prolonged or high-dose exposure. The insights gained from such studies are instrumental in shaping future research directions and ensuring the responsible use of carbonic anhydrase inhibitors in scientific and industrial settings.
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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