Dorzolamide-d5 is intended for use as an internal standard for the quantification of dorzolamide by GC- or LC-MS. Dorzolamide is an inhibitor of carbonic anhydrase (CA), inhibiting CAII, CAV, CAVI, CAIX, CAXII, CAXIII, and CAXIV with Ki values ranging from 3.5 to 52 nM.1,2,3 It is selective for these isoforms over CAI, CAIII, and CAIV (Kis = 50, 8, and 8.5 μM, respectively).1 Dorzolamide inhibits carbonic anhydrase in isolated rabbit iris-ciliary body by 87% when used at a concentration of 0.02%.3 It also reduces intraocular pressure in an α-chymotrypsin-treated rabbit model of ocular hypertension and in normotensive rabbits when applied topically at a concentration of 0.5%.3 Formulations containing dorzolamide have been used in the treatment of glaucoma.4,5
1.Supuran, C.T., and Scozzafava, A.Carbonic anhydrases as targets for medicinal chemistryBioorganic & Medicinal Chemistry15(13)4336-4350(2007) 2.Greer, J., Erickson, J.W., Baldwin, J.J., et al.Application of the three-dimensional structures of protein target molecules in structure-based drug designJournal of Medicinal Chemistry37(8)1035-1054(1994) 3.Hunt, C.A., Mallorga, P.J., Michelson, S.R., et al.3-Substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitorsJournal of Medicinal Chemistry37(2)240-247(1994) 4.Loftsson, T., Jansook, P., and StefÁnsson, E.Topical drug delivery to the eye: DorzolamideActa. Ophthalmol.90(7)603-608(2012) 5.Cheng, J.W., Cheng, S.W., Gao, L.D., et al.Intraocular pressure-lowering effects of commonly used fixed-combination drugs with Timolol: A systematic review and meta-analysisPLoS One7(9)45079(2012)