Benzolamide (CL11366) 是一种有效的碳酸酐酶 (CA) 抑制剂，抑制hCA I，hCA II，EcoCAγ 和 VchCAγ 的 Ki 值分别为15 nM，9 nM，94 nM 和 78 nM。Benzolamide 还抑制 CAS3，Ki 值为 54 nM。Benzolamide 可用于青光眼和癫痫的研究。
Benzolamide (CL11366) is a potent carbonic anhydrase (CA) inhibitor, with Kis of 15 nM, 9 nM, 94 nM and 78 nM for hCA I, hCA II, EcoCAγ and VchCAγ, respectively. Benzolamide also inhibits CAS3, with a Ki of 54 nM. Benzolamide can be used for the research of glaucoma and seizures[1][2][3].
Benzolamide inhibits hCA I, hCA II, EcoCAγ and VchCAγ, with Kis of 15 nM, 9 nM, 94 nM and 78 nM, respectively[1].Benzolamide shows selectivity for CAS3 (Ki=54 nM) over CAS1 (Ki=2115 nM) and CAS2 (Ki=410 nM)[2].
Benzolamide (90 µmol/kg; i.p.) decreases brain pH and suppresses electrographic post-asphyxia seizures in rats[3].
[1]. Prete SD, et, al. Escherichia coli γ-carbonic anhydrase: characterisation and effects of simple aromatic/heterocyclic sulphonamide inhibitors. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1545-1554.
[2]. Vullo D, et, al. Sulfonamide Inhibition Studies of the β-Class Carbonic Anhydrase CAS3 from the Filamentous Ascomycete Sordaria macrospora. Molecules. 2020 Feb 25;25(5):1036.
[3]. Pospelov AS, et, al. Carbonic anhydrase inhibitors suppress seizures in a rat model of birth asphyxia. Epilepsia. 2021 Jun 27.
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