Acetazolamide-d₃

Acetazolamide-d₃ is intended for use as an internal standard for the quantification of acetazolamide by GC- or LC-MS. Acetazolamide is an inhibitor of carbonic anhydrase I (CAI), CAII, CAIX, and CAXII (K_is = 310, 12, 25, and 5.7 nM, respectively, for the human enzymes).¹ It inhibits the migration and invasion of Caki-1, Caki-2, and ACHN renal carcinoma cells when used at a concentration of 10 µM.² Acetazolamide (5.6 mg/kg per day) increases currents in calcium-activated potassium channels in patch clamp assays using skeletal muscle tissues isolated from potassium-deficient rats.³ It induces vasodilation and increases cerebral, renal, and hepatic blood flow and blood oxygen levels in normotensive rabbits when administered at a dose of 12 mg/kg.⁴ Formulations containing acetazolamide have been used in the treatment of edema, open-angle glaucoma, epilepsy, and acute mountain sickness.

WARNING This product is not for human or veterinary use.

1. Brzozowski, Z., Slawiǹski, J., Innocenti, A., et al. Carbonic anhydrase inhibitors. Regioselective synthesis of novel 1-substituted 1,4-dihydro-4-oxo-3-pyridinesulfonamides and their inhibition of the human cytosolic isozymes I and II and transmembrane cancer-associated isozymes IX and XII. Eur. J. Med. Chem. 45(9), 3656-3661 (2010).

2. Parkkila, S., Rajaniemi, H., Parkkila, A.K., et al. Carbonic anhydrase inhibitor suppresses invasion of renal cancer cells in vitro. Proc. Natl. Acad. Sci. USA 97(5), 2220-2224 (2000).

3. Tricarico, D., Mele, A., and Conte Camerino, D. Carbonic anhydrase inhibitors ameliorate the symptoms of hypokalaemic periodic paralysis in rats by opening the muscular Ca²⁺-activated-K⁺ channels. Neuromuscul. Disord. 16(1), 39-45 (2006).

4. Taki, K., Oogushi, K., Hirahara, K., et al. Preferential acetazolamide-induced vasodilation based on vessel size and organ: Confirmation of peripheral vasodilation with use of colored microspheres. Angiology 52(7), 483-488 (2001).