Abstract：
:[3H]Indapamide bound to a single class of binding sites in pig renal cortex membranes with a dissociation constant Kd = 35 +/- 13 nM and a binding site density Bmax = 40 +/- 9 pmol/mg of protein. [3H]Indapamide binding was inhibited by the carbonic anhydrase inhibitor, acetazolamide, and by thiazide diuretics with the following rank order of potency: chlorothiazide greater than hydrochlorothiazide approximately metolazone greater than hydroflumethiazide. The effect of the latter drugs to inhibit [3H]indapamide binding was not related to their activity as thiazide diuretics, but was significantly correlated with their inhibitory effect on carbonic anhydrase II. These results suggest that the major renal binding site of [3H]indapamide is a membrane form of carbonic anhydrase. Inhibition of carbonic anhydrase may play a role in the antihypertensive effect of indapamide.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Schaeffer P,Vigne P,Frelin C,Lazdunski Mdoi
10.1016/0014-2999(90)90048-bsubject
Has Abstractpub_date
1990-07-17 00:00:00pages
503-8issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(90)90048-Bjournal_volume
182pub_type
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