Methazolamide-d6 is intended for use as an internal standard for the quantification of methazolamide by GC- or LC-MS. Methazolamide is a carbonic anhydrase inhibitor (IC50 = 130 nM).1 It reduces intraocular pressure and cerebrospinal fluid flow in a rat model of glaucoma. Methazolamide reduces electroshock-induced seizures in rats with an ED50 value of 19.2 mg/kg.2 It also inhibits production of reactive oxygen species (ROS) in a primary cortical neuron (PCN) cellular model of subarachnoid hemorrhage (SAH) and reduces cerebral edema in a mouse model of SAH.3 Methazolamide is larvicidal, with a 50% larvicidal concentration (LC50) value of 724 ppm, but has no activity when administered in the diet to adult A. aegypti.4 Formulations containing methazolamide have been used in the treatment of glaucoma.
1.Maren, T.H.Carbonic anhydrase: Chemistry, physiology, and inhibitionPhysiol. Rev.47(4)595-781(1967) 2.Gray, W.D., and Rauh, C.E.The anticonvulsant action of the carbonic anhydrase inhibitor methazolamide: Possible involvement of a noradrenergic mechanismEur. J. Pharmacol.28(1)42-54(1974) 3.Li, M., Wang, W., Mai, H., et al.Methazolamide improves neurological behavior by inhibition of neuron apoptosis in subarachnoid hemorrhage miceSci. Rep.635055(2016) 4.Francis, S.A., Taylor-Wells, J., Gross, A.D., et al.Toxicity and physiological actions of carbonic anhydrase inhibitors to Aedes aegypti and Drosophila melanogasterInsects8(1)2(2016)