Next Article in Journal
Exosomal Expression of CXCR4 Targets Cardioprotective Vesicles to Myocardial Infarction and Improves Outcome after Systemic Administration
Next Article in Special Issue
NF-κB-Associated Pain-Related Neuropeptide Expression in Patients with Degenerative Disc Disease
Previous Article in Journal
One New Phenolic Compound from Castanea mollissima Shells and its Suppression of HepatomaCell Proliferation and Inflammation by Inhibiting NF-κB Pathway
Previous Article in Special Issue
Discovery of Food-Derived Dipeptidyl Peptidase IV Inhibitory Peptides: A Review
Open AccessArticle

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

Department of Physiology, BioMedical Center, Faculty of Medicine, University of Iceland, 107 Reykjavik, Iceland
NEUROFARBA Department, University of Florence, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(3), 467;
Received: 12 December 2018 / Revised: 13 January 2019 / Accepted: 17 January 2019 / Published: 22 January 2019
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 EC50 of each compound, ranging from 4.12 µM to 0.86 mM. All compounds had a lower mean EC50 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 EC50 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. View Full-Text
Keywords: carbonic anhydrase; vasodilation; vascular tone carbonic anhydrase; vasodilation; vascular tone
Show Figures

Figure 1

MDPI and ACS Style

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. Int. J. Mol. Sci. 2019, 20, 467.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map

Back to TopTop