brinzolamide

Brinzolamide (AL-4862) 是一种碳酸酐酶(carbonic anhydrase)II 抑制剂(IC50:3.19 nM)。

N-desethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1It inhibits CAII and CAIV activities (IC50s = 1.28 and 128 nM, respectively). 1.Kim, C.-Y., Whittington, D.A., Chang, J.S., et al.Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IVJ. Med. Chem.45(4)888-893(2002)

O-desmethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1,2It inhibits CAII and CAIV (IC50s = 0.136 and 165 nM, respectively).1 1.Huang, Q., Rui, E.Y., Cobbs, M., et al.Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressureJ. Med. Chem.58(6)2821-2833(2015) 2.Lo Faro, A.F., Tini, A., Gottardi, M., et al.Development and validation of a fast ultra-high-performance liquid chromatography tandem mass spectrometry method for determining carbonic anhydrase inhibitors and their metabolites in urine and hairDrug Test Anal.13(8)1552-1560(2021)

Brinzolamide (AL-4862) hydrochloride 是一种碳酸酐酶 II（carbonic anhydrase II）的选择性抑制剂 (IC50: 3.2 nM)。Brinzolamide hydrochloride 能够抑制睫状体 CA-II，减少房水分泌，进而降低眼压 (IOP)。Brinzolamide hydrochloride 能够用于研究青光眼疾病。

N-Desethyl Brinzolamide oxalate为Carbonic anhydraseII与Carbonic anhydraseIV的双重抑制剂，其IC50值分别为1.28 nM与128 nM。

O-Desmethyl Brinzolamide hydrochloride (compound 6a) 作为Brinzolamide的主要活性代谢物，具有显著的碳酸酐酶 (carbonic anhydrase(CA)) 抑制活性，其 Kd 值为 0.136 nM，对 CA IV 的 IC50 值达到 165 nM。