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Identification and pharmacological properties of binding sites for the atypical thiazide diuretic, indapamide.

Author: FrelinC, LazdunskiM, SchaefferP, VigneP

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

Indapamide, a drug used to treat high blood pressure, was found to bind to a membrane form of carbonic anhydrase in pig renal cortex membranes. This binding was inhibited by acetazolamide and thiazide diuretics, suggesting that indapamide's antihypertensive effect may be related to its inhibition of carbonic anhydrase.
Paper Details　
Original Abstract of the Article :
[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...See full text at original site
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引用元：
https://doi.org/10.1016/0014-2999(90)90048-b

データ提供：米国国立医学図書館（NLM）

Indapamide: A Unique Thiazide Diuretic with a Hidden Oasis

This research delves into the intriguing world of indapamide, an atypical thiazide diuretic, exploring its binding properties and potential mechanisms of action. The study investigates the binding sites of indapamide in pig renal cortex membranes, revealing a unique interaction with carbonic anhydrase. This is like discovering a hidden oasis in the desert of diuretic research, offering insights into the unique pharmacological properties of indapamide.

Carbonic Anhydrase: A Key Player in Indapamide's Mechanism of Action

The study's findings suggest that the major renal binding site of indapamide is a membrane form of carbonic anhydrase, a crucial enzyme involved in fluid balance. This is like finding a hidden spring in the desert, providing a source of water and potentially explaining the antihypertensive effects of indapamide. The research highlights the importance of understanding the intricate mechanisms of action of medications for optimal therapeutic outcomes.

Navigating the Desert of Diuretic Research

This research expands our understanding of indapamide, a unique thiazide diuretic, highlighting its interaction with carbonic anhydrase. This is like discovering a new route through the desert of diuretic research, potentially leading to more effective and targeted therapies for managing hypertension. By understanding the unique properties of medications, we can better navigate the challenging landscape of drug development and provide patients with the most effective and appropriate treatments.

Dr. Camel's Conclusion

This research explores the binding properties and potential mechanisms of action of indapamide, an atypical thiazide diuretic. The study reveals a unique interaction with carbonic anhydrase, suggesting a hidden oasis in the desert of diuretic research. By understanding the intricate mechanisms of action of medications, we can better navigate the challenging landscape of drug development and provide patients with the most effective and appropriate treatments.

Date :
  1. Date Completed 1990-12-12
  2. Date Revised 2019-06-24
Further Info :

Pubmed ID

2226620

DOI: Digital Object Identifier

10.1016/0014-2999(90)90048-b

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Languages

English

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