Naftidrofuryl exerts antiserotonergic but no endothelin-receptor blocking effects in AS4.1 cells, juxtaglomerular cells and isolated perfused rat kidneys

Endemann, Dierk and Schweda, Frank and Stubanus, Mike and Ittner, Karl-Peter and Fischereder, Michael and Kammerl, Martin C. and Kraemer, Bernhard K. (2002) Naftidrofuryl exerts antiserotonergic but no endothelin-receptor blocking effects in AS4.1 cells, juxtaglomerular cells and isolated perfused rat kidneys. JOURNAL OF CARDIOVASCULAR PHARMACOLOGY, 39 (1). pp. 1-8. ISSN 0160-2446, 1533-4023

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Abstract

Naftidrofuryl, a 5-hydroxytryptamine 2 (5-HT2) serotonergic receptor antagonist with vasodilator effects, has successfully been used for intermittent claudication, some forms of dementia, and glaucoma. Recently, an additional mode of action of naftidrofuryl (i.e., mixed endothelin receptor antagonism) has been suggested. However, in the current study naftidrofuryl was unable to block endothelin-3-induced free intracellular calcium increases, in contrast to a mixed endothelin receptor antagonist, bosentan. The inhibition of forskolin-induced renin secretion by endothelin-3 in primary cultures of mouse juxtaglomerular cells and by endothelin-1 in the isolated perfused rat kidney could not be blocked by naftidrofuryl. Naftidrofuryl was unable to block marked endothelin-1-induced renal vasoconstriction in isolated perfused rat kidney. In contrast, naftidrofuryl markedly attenuated serotonin-induced renal vasoconstriction and nearly completely blocked serotonin's renin inhibitory properties in isolated perfused rat kidney. The present results suggest that naftidrofuryl is a potent antagonist of serotonin's renal effects, but has no endothelin receptor-blocking properties.

Item Type: Article
Uncontrolled Keywords: GLOMERULAR MESANGIAL CELLS; RENIN GENE-EXPRESSION; INTERMITTENT CLAUDICATION; BLOOD-PRESSURE; SECRETION; SEROTONIN; METAANALYSIS; VASOPRESSIN; ANTAGONIST; MECHANISMS; naftidrofuryl; serotonin; renin secretion; renal vasoconstriction; endothelin
Subjects: 500 Science > 570 Life sciences
600 Technology > 610 Medical sciences Medicine
Divisions: Medicine > Lehrstuhl für Anästhesiologie
Medicine > Lehrstuhl für Innere Medizin II
Biology, Preclinical Medicine > Institut für Physiologie > Prof. Dr. Frank Schweda
Depositing User: Dr. Gernot Deinzer
Date Deposited: 16 Nov 2021 10:51
Last Modified: 16 Nov 2021 10:51
URI: https://pred.uni-regensburg.de/id/eprint/40766

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