2749856-75-3

Dorzolamide-d5 is intended for use as an internal standard for the quantification of dorzolamide (Item No. 14616) 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.4,5WARNING This product is not for human or veterinary use.

[1] CLAUDIU T. SUPURAN  Andrea S. Carbonic anhydrases as targets for medicinal chemistry[J]. Bioorganic & Medicinal Chemistry, 2007, 15 13: Pages 4336-4350. DOI: 10.1016/j.bmc.2007.04.020
[2] JONATHAN GREER. Application of the Three-Dimensional Structures of Protein Target Molecules in Structure-Based Drug Design[J]. Journal of Medicinal Chemistry, 1994, 37 8: 1035-1054. DOI: 10.1021/jm00034a001
[3] CECILIA A. HUNT. 3-Substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors[J]. Journal of Medicinal Chemistry, 1994, 37 2: 240-247. DOI: 10.1021/jm00028a006
[4] THORSTEINN LOFTSSON  Einar S  Phatsawee Jansook. Topical drug delivery to the eye: dorzolamide[J]. Acta Ophthalmologica, 2012, 90 7: 603-608. DOI: 10.1111/j.1755-3768.2011.02299.x
[5] JIN-WEI CHENG. Intraocular pressure-lowering effects of commonly used fixed-combination drugs with timolol: a systematic review and meta-analysis.[J]. PLoS ONE, 2012: e45079. DOI: 10.1371/journal.pone.0045079