دورية أكاديمية
Benzolamide is not a membrane-impermeant carbonic anhydrase inhibitor.
| العنوان: | Benzolamide is not a membrane-impermeant carbonic anhydrase inhibitor. |
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| المؤلفون: | Supuran CT; Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Italy. claudiu.supuran@unifi.it, Scozzafava A |
| المصدر: | Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2004 Jun; Vol. 19 (3), pp. 269-73. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Taylor & Francis Country of Publication: England NLM ID: 101150203 Publication Model: Print Cited Medium: Print ISSN: 1475-6366 (Print) Linking ISSN: 14756366 NLM ISO Abbreviation: J Enzyme Inhib Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Basingstoke, UK : Taylor & Francis, c2002- |
| مواضيع طبية MeSH: | Cell Membrane Permeability*, Benzolamide/*metabolism , Benzolamide/*pharmacology , Carbonic Anhydrase Inhibitors/*metabolism, Benzolamide/chemistry ; Carbonic Anhydrase Inhibitors/chemistry ; Carbonic Anhydrase Inhibitors/pharmacology ; Carbonic Anhydrases/metabolism ; Erythrocyte Membrane/chemistry ; Erythrocyte Membrane/drug effects ; Erythrocyte Membrane/enzymology ; Humans ; Isoenzymes/antagonists & inhibitors ; Isoenzymes/metabolism ; Molecular Structure ; Structure-Activity Relationship ; Sulfonamides/chemistry ; Sulfonamides/pharmacology |
| مستخلص: | Benzolamide, an orphan drug belonging to the pharmacological class of sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) is widely used in many physiological and pharmacological studies, together with the clinically employed classical drugs, acetazolamide, methazolamide, ethoxzolamide or dichlorophenamide, it being frequently stated that benzolamide is a membrane-impermeant inhibitor. We prove here that this is false: in fact benzolamide is rather similar to acetazolamide from the point of view of penetrability through blood red cell membranes. Unlike these neutral drugs, the cationic, positively-charged CAIs incorporating either tetraalkyl ammonium or pyridinium moieties, due to their salt-like character are indeed membrane-impermeant, being the only type of low molecular weight compound possessing such properties. Selective inhibition of membrane-associated CA isozymes is relevant indeed in many physiological studies and also pharmacologically, since the tumor-associated isozymes (CA IX and XII) are both membrane-bound. |
| المشرفين على المادة: | 0 (Carbonic Anhydrase Inhibitors) 0 (Isoenzymes) 0 (Sulfonamides) EC 4.2.1.1 (Carbonic Anhydrases) FC5AAH89R5 (Benzolamide) |
| تواريخ الأحداث: | Date Created: 20041027 Date Completed: 20041124 Latest Revision: 20190516 |
| رمز التحديث: | 20240628 |
| DOI: | 10.1080/14756360410001689559 |
| PMID: | 15499999 |
| قاعدة البيانات: | MEDLINE |
PDF full text from Publisher | تدمد: | 1475-6366 |
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| DOI: | 10.1080/14756360410001689559 |