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Effect of avosentan (SPP-301) in porcine ciliary arteries

Konieczka, Katarzyna and Meyer, Peter and Schoetzau, Andreas and Neutzner, Albert and Mozaffarieh, Maneli and Flammer, Josef. (2011) Effect of avosentan (SPP-301) in porcine ciliary arteries. Current eye research, Vol. 36, H. 2. pp. 118-124.

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Official URL: http://edoc.unibas.ch/dok/A6004099

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Abstract

PURPOSE: To investigate the vasoactive effect of ET(A)-endothelin receptor antagonists avosentan (SPP-301) and BQ-123 in isolated porcine ciliary arteries with and without endothelium. To investigate the effect of avosentan on the endothelin-1 induced contractions in comparison with BQ-123 and BQ-788 (ET(B)-endothelin receptor antagonist) in isolated porcine ciliary arteries with and without endothelium. METHODS: Vessels were placed in a myograph system to measure isometric forces. In a first set of experiments, quiescent vessels were exposed, cumulatively, to increasing concentrations of avosentan and BQ-123 (10(-9) M-3 x 10(-6) M). In a second set of experiments, quiescent vessels were first incubated with avosentan (10(-6) M and 10(-8) M), BQ-123 (10(-6) M), and BQ-788 (10(-6) M), respectively. Then the vessels were exposed, cumulatively, to increasing concentrations of endothelin-1 (10(-12) M-3 x 10(-8) M). Each set of experiments was conducted in the vessels with and without endothelium. RESULTS: Cumulative concentrations of avosentan and BQ-123 had no vasoactive effect in quiescent vessels. Avosentan had a strong inhibitory effect on the endothelin-1-induced contractions. The inhibitory effect of 10(-6) M avosentan was significantly stronger than the effect of 10(-8) M avosentan. The effect of avosentan (10(-6) M) tended to be stronger than the effect of BQ-123 (10(-6) M). To a lesser extent, BQ-788 also had an inhibitory effect on the endothelin-1-induced contractions. CONCLUSIONS: Avosentan has a strong inhibitory effect on the endothelin-1-induced contractions. Blockade of ET receptors is potentially an attractive target in many eye diseases including glaucoma. Further studies are needed to evaluate the usefulness of endothelin blockers in ophthalmology.
Faculties and Departments:03 Faculty of Medicine > Bereich Spezialfächer (Klinik) > Ehemalige Einheiten Spezialfächer (Klinik) > Ophthalmologie (Flammer)
03 Faculty of Medicine > Departement Klinische Forschung > Bereich Spezialfächer (Klinik) > Ehemalige Einheiten Spezialfächer (Klinik) > Ophthalmologie (Flammer)
03 Faculty of Medicine > Departement Biomedizin > Department of Biomedicine, University Hospital Basel > Ocular Pharmacology and Physiology (Neutzner/Meyer)
UniBasel Contributors:Flammer, Josef and Neutzner, Albert and Meyer, Peter
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:IRL Press
ISSN:0271-3683
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:08 May 2015 08:45
Deposited On:25 Oct 2013 08:32

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