Carbonic anhydrase activators. The selective serotonin reuptake inhibitors fluoxetine, sertraline and citalopram are strong activators of Isozymes I and II

Casini, Angela ORCID: https://orcid.org/0000-0003-1599-9542, Caccia, S, Scozzafava, A and Supuran, C. T. 2003. Carbonic anhydrase activators. The selective serotonin reuptake inhibitors fluoxetine, sertraline and citalopram are strong activators of Isozymes I and II. Biorganic and Medicinal Chemistry Letters 13 (16) , pp. 2765-2768. 10.1016/S0960-894X(03)00507-9

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Abstract

The selective serotonin reuptake inhibitors (SSRI) fluoxetine, sertraline and citalopram have been investigated for their ability to activate two carbonic anhydrase (CA) isozymes, hCA I and hCA II, in parallel with two standard activators for which the X-ray structure (in complex with isozyme II) has been resolved: histamine and phenylalanine. All three SSRI activated both isozymes with potencies comparable to that of the standards although the profile was different: for hCA I, best activators were fluoxetine and histamine, with citalopram and sertraline showing weaker activity. For hCA II, the best activators were phenylalanine and citalopram, and the weakest histamine and sertraline, whereas fluoxetine showed an intermediate behavior. These results suggest that SSRI efficacy in major depression complicating Alzheimer's disease may be partly due to their ability to activate CA isozymes and may lead to the development of potent activators for the therapy of diseases associated with significant decreases in brain CA activity.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Chemistry
Subjects:	Q Science > QD Chemistry
Uncontrolled Keywords:	Brain; Carbonic Anhydrase I; Carbonic Anhydrase II; Citalopram; Crystallography, X-Ray; Enzyme Activation; Enzyme Activators; Fluoxetine; Histamine; Phenylalanine; Serotonin Uptake Inhibitors; Sertraline; Structure-Activity Relationship
Publisher:	Elsevier
ISSN:	0960-894X
Last Modified:	31 Oct 2022 10:38
URI:	https://orca.cardiff.ac.uk/id/eprint/85546

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