Diuretic and Saluretic Activity
In Vitro Methods
Carbonic Anhydrase Inhibition In Vitro
Purpose and Rationale
Acetazolamide (Diamox) was one of the first synthetic non‐mercurial diuretics. The mode of action was found to be inhibition of carbonic anhydrase. Carbonic anhydrase is a zinc‐containing enzyme that catalyzes the reversible hydration (or hydroxylation) of CO2 to form H2CO3 which dissociates non‐enzymatically into HCO3 − and H+. The enzyme is located within the cytoplasm and at the apical and basolateral membranes of proximal tubules as well as on the apical (lumenal) surface of distal tubules and in the thick ascending limb of the loop of Henle. Its primary function is to enhance H+ secretion into the urine. At least three isoenzymes, designated as I, II and II or A, B and C, are known to exist..
Carbonic anhydrase inhibitors were originally used as diuretics but are no longer used for this purpose except in limited circumstances (metabolic alkalosis accompanied by edema)....
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Notes
- 1.
Contribution by H. Gögelein.
- 2.
Contribution by R. Greger (first edition) and M. Bleich (second edition).
- 3.
Contribution by M. Hropot.
- 4.
Contribution by M. Hropot.
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Vogel, H. (2007). Activity on Urinary Tract. In: Vogel, H.G. (eds) Drug Discovery and Evaluation. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-540-70995-4_4
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