دورية أكاديمية

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

التفاصيل البيبلوغرافية
العنوان: Carbonic Anhydrase Inhibitors of Different Structures Dilate Pre-Contracted Porcine Retinal Arteries.
المؤلفون: Eysteinsson T; Department of Physiology, BioMedical Center, Faculty of Medicine, University of Iceland, Reykjavik, Iceland. thoreys@hi.is., Gudmundsdottir H; Department of Physiology, BioMedical Center, Faculty of Medicine, University of Iceland, Reykjavik, Iceland., Hardarson AO; Department of Physiology, BioMedical Center, Faculty of Medicine, University of Iceland, Reykjavik, Iceland., Berrino E; NEUROFARBA Department, University of Florence, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy., Selleri S; NEUROFARBA Department, University of Florence, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy., Supuran CT; NEUROFARBA Department, University of Florence, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy., Carta F; NEUROFARBA Department, University of Florence, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy.
المصدر: International journal of molecular sciences [Int J Mol Sci] 2019 Jan 22; Vol. 20 (3). Date of Electronic Publication: 2019 Jan 22.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: MDPI Country of Publication: Switzerland NLM ID: 101092791 Publication Model: Electronic Cited Medium: Internet ISSN: 1422-0067 (Electronic) Linking ISSN: 14220067 NLM ISO Abbreviation: Int J Mol Sci Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Basel, Switzerland : MDPI, [2000-
مواضيع طبية MeSH: Carbonic Anhydrase Inhibitors/*pharmacology , Carbonic Anhydrases/*metabolism , Muscle, Smooth, Vascular/*drug effects , Retinal Artery/*drug effects , Vasodilation/*drug effects, Acetazolamide/chemistry ; Acetazolamide/pharmacology ; Animals ; Benzolamide/chemistry ; Benzolamide/pharmacology ; Carbonic Anhydrase Inhibitors/chemistry ; Sulfonamides/chemistry ; Sulfonamides/pharmacology ; Swine ; Thiophenes/chemistry ; Thiophenes/pharmacology
مستخلص: 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.
Competing Interests: The authors declare no conflict of interest.
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فهرسة مساهمة: Keywords: carbonic anhydrase; vascular tone; vasodilation
المشرفين على المادة: 0 (Carbonic Anhydrase Inhibitors)
0 (Sulfonamides)
0 (Thiophenes)
9JDX055TW1 (dorzolamide)
EC 4.2.1.1 (Carbonic Anhydrases)
FC5AAH89R5 (Benzolamide)
O3FX965V0I (Acetazolamide)
تواريخ الأحداث: Date Created: 20190126 Date Completed: 20190513 Latest Revision: 20231006
رمز التحديث: 20240628
مُعرف محوري في PubMed: PMC6387369
DOI: 10.3390/ijms20030467
PMID: 30678227
قاعدة البيانات: MEDLINE
الوصف
تدمد:1422-0067
DOI:10.3390/ijms20030467