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Carbonic Anhydrase Inhibitors of Different Structures Dilate Pre-Contracted Porcine Retinal Arteries

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dc.contributor Háskóli Íslands
dc.contributor University of Iceland
dc.contributor.author Eysteinsson, Thor
dc.contributor.author Guðmundsdóttir, Hrönn
dc.contributor.author Harðarson, Arnar Össur
dc.contributor.author Berrino, Emanuela
dc.contributor.author Selleri, Silvia
dc.contributor.author Supuran, Claudiu
dc.contributor.author carta, fabrizio
dc.date.accessioned 2020-05-18T13:41:27Z
dc.date.available 2020-05-18T13:41:27Z
dc.date.issued 2019-01-22
dc.identifier.citation Eysteinsson, T.; Gudmundsdottir, H.; Hardarson, A.O.; Berrino, E.; Selleri, S.; Supuran, C.T.; Carta, F. Carbonic Anhydrase Inhibitors of Different Structures Dilate Pre-Contracted Porcine Retinal Arteries. International Journal of Molecular Sciences 2019, 20, 467.
dc.identifier.issn 1422-0067
dc.identifier.uri https://hdl.handle.net/20.500.11815/1814
dc.description Publisher's version (útgefin grein)
dc.description.abstract Carbonic anhydrase inhibitors (CAIs), such as dorzolamide (DZA), are used as anti-glaucoma drugs to lower intraocular pressure, but it has been found that some of these drugs act as vasodilators of retinal arteries. The exact mechanism behind the vasodilatory effect is not yet clear. Here we have addressed the issue by using small vessel myography to examine the effect of CAIs of the sulfonamide and coumarin type on the wall tension in isolated segments of porcine retinal arteries. Vessels were pre-contracted by the prostaglandin analog U-46619, and CAIs with varying affinity for five different carbonic anhydrase (CA) isoenzymes found in human tissue tested. We found that all compounds tested cause a vasodilation of pre-contracted retinal arteries, but with varying efficacy, as indicated by the calculated mean EC 50 of each compound, ranging from 4.12 µM to 0.86 mM. All compounds had a lower mean EC 50 compared to DZA. The dilation induced by benzolamide (BZA) and DZA was additive, suggesting that they may act on separate mechanisms. No clear pattern in efficacy and affinity for CA isoenzymes could be discerned from the results, although Compound 5, with a low affinity for all isoenzymes except the human (h) CA isoform IV, had the greatest potency, with the lowest EC 50 and inducing the most rapid and profound dilation of the vessels. The results suggest that more than one isozyme of CA is involved in mediating its role in controlling vascular tone in retinal arteries, with a probable crucial role played by the membrane-bound isoform CA IV.
dc.description.sponsorship This research was funded by grants from the Helga Jónsdottir and Sigurlidi Kristjansson Memorial Fund.
dc.format.extent 467
dc.language.iso en
dc.publisher MDPI AG
dc.relation.ispartofseries International Journal of Molecular Sciences;20(3)
dc.rights info:eu-repo/semantics/openAccess
dc.subject Carbonic anhydrase
dc.subject Vascular tone
dc.subject Vasodilation
dc.subject Æðar
dc.subject Ensím
dc.subject Lífefnafræði
dc.title Carbonic Anhydrase Inhibitors of Different Structures Dilate Pre-Contracted Porcine Retinal Arteries
dc.type info:eu-repo/semantics/article
dcterms.license This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited
dc.description.version Peer Reviewed
dc.identifier.journal International Journal of Molecular Sciences
dc.identifier.doi 10.3390/ijms20030467
dc.relation.url http://www.mdpi.com/1422-0067/20/3/467/pdf
dc.contributor.department Læknadeild (HÍ)
dc.contributor.department Faculty of Medicine (UI)
dc.contributor.department Lífvísindasetur (HÍ)
dc.contributor.department Biomedical Center (UI)
dc.contributor.school Heilbrigðisvísindasvið (HÍ)
dc.contributor.school School of Health Sciences (UI)

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