Summary: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.
Publications139 found, 100 shown here
- Non-catalytic role of carbonic anhydrase in rat intestinal absorptionAlan N Charney
Nephrology Section, VA Medical Center, New York University School of Medicine, 423 East 23rd Street, New York, NY 10010, USA
Biochim Biophys Acta 1573:141-8. 2002..Measurements were made in the presence and absence of 0.1 mM methazolamide, a membrane-permeant CA inhibitor. Ringer pH reduction from 7.6 to 7...
- Methazolamide and melatonin inhibit mitochondrial cytochrome C release and are neuroprotective in experimental models of ischemic injuryXin Wang
Department of Neurosurgery, Neuroapoptosis Laboratory, Brigham and Women s Hospital, Harvard Medical School, Boston, Massachusetts 02115, USA
Stroke 40:1877-85. 2009..We demonstrate that methazolamide and melatonin are protective in cellular and in vivo models of neuronal hypoxia.
- Design of cationic nanostructured heterolipid matrices for ocular delivery of methazolamideJohn Youshia
Pharmaceutics and Industrial Pharmacy Department, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt
Int J Nanomedicine 7:2483-96. 2012..This study assessed the feasibility of using nanostructured lipid matrices (NLMs) for ocular delivery of methazolamide-(MZA) adopting heterolipids composed of novel mixtures of Compritol (®) and cetostearyl alcohol (CSA), and ..
- Methazolamide is a new hepatic insulin sensitizer that lowers blood glucose in vivoNicky Konstantopoulos
Metabolic Research Unit, School of Medicine, Deakin University, Geelong, Victoria, Australia
Diabetes 61:2146-54. 2012We previously used Gene Expression Signature technology to identify methazolamide (MTZ) and related compounds with insulin sensitizing activity in vitro...
- Bilateral transient myopia, angle-closure glaucoma, and choroidal detachment induced by methazolamideSoon Jae Kwon
Department of Ophthalmology, School of Medicine, Kyungpook National University, 50 Samduk dong 2 ga, Jung Gu, Daegu 700721, Korea
Jpn J Ophthalmol 56:515-7. 2012We report the case of a patient with acute bilateral transient myopia, secondary angle-closure glaucoma, and choroidal detachment associated with oral administration of methazolamide.
- Stevens-Johnson syndrome induced by methazolamide treatmentS Shirato
Department of Ophthalmology, University of Tokyo School of Medicine, Japan
Arch Ophthalmol 115:550-3. 1997Four cases of Stevens-Johnson syndrome considered to be induced by methazolamide were reported. In all of the cases, the first signs of Stevens-Johnson syndrome (i.e...
- A potential new therapeutic system for glaucoma: solid lipid nanoparticles containing methazolamideRui Li
School of Pharmacy, Nanjing Medical University, 140 Hanzhong Road, Nanjing 210029, People s Republic of China
J Microencapsul 28:134-41. 2011b>Methazolamide (MTA) is an antiglaucoma drug; however, there are many side effects of its systemic administration with insufficient ocular therapeutic concentrations...
- Preparation and evaluation of in situ gelling ophthalmic drug delivery system for methazolamideYong Qian
School of Pharmacy, Nanjing Medical University, Nanjing, PR China
Drug Dev Ind Pharm 36:1340-7. 2010In this study, a thermosensitive in situ gelling vehicle was prepared to increase the precorneal resident time and the bioavailability of methazolamide (MTA).
- Effects of low-dose methazolamide on the control of breathing in catsJ H L Bijl
Department of Anesthesiology Leiden University Medical Center Leiden, The Netherlands
Adv Exp Med Biol 580:257-62; discussion 351-9. 2006
- Effect of methazolamide on chronic macular edema in patients with retinitis pigmentosaG A Fishman
Department of Ophthalmology and Visual Sciences, University of Illinois, Chicago College of Medicine 60612
Ophthalmology 101:687-93. 1994To determine the effectiveness of methazolamide for improving visual acuity and macular edema in patients with retinitis pigmentosa.
- Methazolamide 1% in cyclodextrin solution lowers IOP in human ocular hypertensionE Gudmundsdottir
Departments of Ophthalmology and Pharmacy, University of Iceland, Reykjavik
Invest Ophthalmol Vis Sci 41:3552-4. 2000To formulate aqueous eye drops containing methazolamide 1% in cyclodextrin solution and to evaluate their effect on intraocular pressure (IOP) in a double-blind randomized trial in humans...
- Methazolamide calcium phosphate nanoparticles in an ocular delivery systemRui Chen
Department of Pharmaceutics, Nanjing Medical University, China
Yakugaku Zasshi 130:419-24. 2010A new system for the local delivery of methazolamide to the eye has been developed based on calcium phosphate (CaP) nanoparticles...
- HLA-B*5901 is strongly associated with methazolamide-induced Stevens-Johnson syndrome/toxic epidermal necrolysisSae Hoon Kim
Department of Internal Medicine, Seoul National University College of Medicine, Seoul, South Korea
Pharmacogenomics 11:879-84. 2010The carbonic anhydrase inhibitor methazolamide infrequently causes Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN). An association between these diseases and the HLA-B59 serotype has been suggested in case reports...
- Inhibition of hypoxia-induced calcium responses in pulmonary arterial smooth muscle by acetazolamide is independent of carbonic anhydrase inhibitionLarissa A Shimoda
Division of Pulmonary and Critical Care Medicine, Johns Hopkins University, Baltimore, MD 21224, USA
Am J Physiol Lung Cell Mol Physiol 292:L1002-12. 2007..These results suggest that AZ attenuates HPV by selectively inhibiting hypoxia-induced Ca2+ responses via a mechanism independent of CA inhibition, changes in pH(i), or membrane potential...
- Treat ankylosing spondylitis with methazolamideXiaotian Chang
National Laboratory for Bio Drugs of Ministry of Health, Provincial Laboratory for Modern Medicine and Technology of Shandong, Research Center for Medicinal Biotechnology of Shandong Academy of Medical Sciences, Jingshi Road 18877, Jinan, Shandong 250062, P R China
Int J Med Sci 8:413-9. 2011..This study aimed to evaluate the effectiveness and safety of methazolamide, an anti-carbonic anhydrase drug, for treating patients with AS.
- Carbonic anhydrase inhibitors are antiarthritic in the ratJ C Nolan
Department of Pharmacology, A H Robins Co, Richmond, VA 23220
Pharmacol Res 24:377-83. 1991..Acetazolamide, ethoxzolamide, methazolamide, and dichlorphenamide reduced paw oedema and attenuated the deterioration of the joints of rats with adjuvant ..
- Double-blind controlled study of methazolamide in the treatment of essential tremorK Busenbark
Department of Neurology, University of Kansas Medical Center, Kansas City 66160 7314
Neurology 43:1045-7. 1993We studied the effect of the carbonic anhydrase inhibitor methazolamide in 25 patients with essential tremor (ET) in a double-blind, placebo-controlled trial...
- Gramicidin-perforated patch analysis on HCO3- secretion through a forskolin-activated anion channel in rat parotid intralobular duct cellsC Hirono
Department of Oral Physiology, Hiroshima University School of Dentistry, Hiroshima 734 8553, Japan
J Membr Biol 180:11-9. 2001..The anion current was markedly suppressed by addition of 1 mM methazolamide, a carbonic anhydrase inhibitor, and removal of external HCO3-...
- Treatment of essential tremor with methazolamideM D Muenter
Lee Silverman Center for Parkinson s Disease and Movement Disorders, Mayo Clinic Scottsdale, AZ 85259
Mayo Clin Proc 66:991-7. 1991We treated 28 patients (16 women and 12 men) who had essential tremor with methazolamide. Their median age was 69 years (range, 34 to 89 years), and the median duration of tremor was 16 years (range, less than 1 to 69 years)...
- Carbonic anhydrases and mucosal vanilloid receptors help mediate the hyperemic response to luminal CO2 in rat duodenumYasutada Akiba
Department of Medicine, School of Medicine, University of California Los Angeles, USA
Gastroenterology 131:142-52. 2006..We examined the hyperemic response to elevated luminal PCO(2) in the duodenum of anesthetized rats luminally exposed to high CO(2) saline to help elucidate luminal acid-sensing mechanisms...
- NHE3 inhibition activates duodenal bicarbonate secretion in the ratOsamu Furukawa
Greater Los Angeles Veterans Affairs Healthcare System, Los Angeles, California 90073, USA
Am J Physiol Gastrointest Liver Physiol 286:G102-9. 2004..Coperfusion with 0.1 microM indomethacin, 0.5 mM DIDS, or 1 mM methazolamide did not affect S3226-induced DBS. Nevertheless, coperfusion with 0.1 and 0...
- Effects of oral administration of methazolamide on intraocular pressure and aqueous humor flow rate in clinically normal dogsBrian J Skorobohach
Department of Small Animal Clinical Sciences, College of Veterinary Medicine, The University of Tennessee, Knoxville, TN 37996, USA
Am J Vet Res 64:183-7. 2003To determine magnitude and duration of the effect of oral administration of methazolamide at 2 dosages on intraocular pressure (IOP) in dogs in single-dose and multiple-dose trials and to determine aqueous humor flow rate (AHFR) by use ..
- Degradation and effects of the potential mosquito larvicides methazolamide and acetazolamide in sheepshead minnow (Cyprinodon variegatus)Maria del Pilar Corena
The Whitney Laboratory, University of Florida, St Augustine, FL 32080, USA
Ecotoxicol Environ Saf 64:369-76. 2006..of carbonic anhydrase inhibitors as larvicides, the decomposition and degradation of samples containing methazolamide (MTZ) and acetazolamide (ACZ) in aqueous solution were monitored under different conditions...
- Pharmacological impact on loop gain properties to prevent irregular breathingH Kiwull-Schöne
Department of Physiology, Ruhr University Bochum, Germany
J Physiol Pharmacol 59:37-45. 2008..Acetazolamide significantly reduced G by 42.0 +/- 9.3% and methazolamide by 35.0 +/- 9.5% (each n = 7, P<0.01). Irrespective of the substance, NHE3 inhibition reduced G by 33...
- Carbonic anhydrase in the adult mosquito midgutMaria del Pilar Corena
The Whitney Laboratory, University of Florida, Saint Augustine, FL 32080, USA
J Exp Biol 208:3263-73. 2005..We also tested the effect of CA inhibitors such as methazolamide and acetazolamide in the alkalization of the midgut in females from these species...
- Acid-base effects on electrolyte transport in CA II-deficient mouse colonD S Goldfarb
Nephrology Section, Veterans Affairs Medical Center and New York University School of Medicine, New York, New York 10010, USA
Am J Physiol Gastrointest Liver Physiol 278:G409-15. 2000..Membrane-permeant methazolamide, but not impermeant benzolamide, at 0.1 mM prevented the effects of pH...
- Inhibition of aquaporin-mediated CO2 diffusion and voltage-gated H+ channels by zinc does not alter rabbit lung CO2 and NO excretionErik R Swenson
Department of Medicine, VA Puget Sound Health Care System, University of Washington, Seattle, WA 98108, USA
Clin Sci (Lond) 103:567-75. 2002..For comparison, red cell and lung carbonic anhydrases (CAs) were inhibited by 0.1 mM methazolamide. ZnCl(2) had no effect on CO(2) exchange when inspired CO(2) was altered between 2% and 5% in 5-min intervals...
- Carbachol-induced fluid movement through methazolamide-sensitive bicarbonate production in rat parotid intralobular ducts: quantitative analysis of fluorescence images using fluorescent dye sulforhodamine under a confocal laser scanning microscopeTetsuji Nakamoto
Department of Removable Prosthodontics, Hiroshima University Faculty of Dentistry, Japan
Eur J Cell Biol 81:497-504. 2002..clearance of the fluorescent dye was divided into two phases by the sensitivity to external Ca2+ and methazolamide, an inhibitor for carbonic anhydrase...
- Carbonic anhydrase II and alveolar fluid reabsorption during hypercapniaJiwang Chen
Division of Pulmonary and Critical Care Medicine, Department of Medicine, Feinberg School of Medicine, Northwestern University, Chicago, Illinois, USA
Am J Respir Cell Mol Biol 38:32-7. 2008..Inhibition of CAII by acetazolamide or methazolamide delayed the decrease in the intracellular pH observed during hypercapnia in cultured AECI, AECII, and AECI-..
- Topical inhibition of nasal carbonic anhydrase affects the CO2 detection threshold in ratsKatheryn E Ferris
Neuroscience Program, Allegheny College, Meadville, PA 16335, USA
Chem Senses 32:263-71. 2007..2) to determine the rats' CO(2) detection thresholds before and after nasal perfusion of mammalian Ringers or methazolamide, a CA inhibitor...
- Inhibitors of cytochrome c release with therapeutic potential for Huntington's diseaseXin Wang
Neuroapoptosis Laboratory and Department of Neurosurgery, Brigham and Women s Hospital, Harvard Medical School, Boston, Massachusetts 02115, USA
J Neurosci 28:9473-85. 2008..Given that many of these compounds have been approved by the Food and Drug Administration for clinical usage and cross the blood-brain barrier, these drugs may lead to trials in patients...
- Carbonic anhydrase inhibitors: X-ray crystallographic structure of the adduct of human isozyme II with the perfluorobenzoyl analogue of methazolamide. Implications for the drug design of fluorinated inhibitorsFrancesco Abbate
Universita degli Studi di Firenze, Polo Scientifico, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Via della Lastruccia, 3, Rm 188, 1 50019 Sesto Fiorentino, Firenze, Italy
J Enzyme Inhib Med Chem 18:303-8. 2003..5 nM) compared to the lead molecule, methazolamide, a clinically used drug (KI of 14 nM)...
- Gramicidin-perforated patch recording revealed the oscillatory nature of secretory Cl- movements in salivary acinar cellsMakoto Sugita
Department of Oral Physiology, Graduate School of Biomedical Sciences, Hiroshima University, Kasumi 1 2 3, Minami Ku, Hiroshima 734 8553, Japan
J Gen Physiol 124:59-69. 2004..In contrast, neither methazolamide, a carbonic anhydrase inhibitor, nor elimination of external HCO(3)(-) had significant effects, suggesting ..
- [Diuretic therapy in heart failure]G Splendiani
Dipartimento di Nefrologia e Dialisi, Policlinico Tor Vergata, Rome
G Ital Nefrol 23:S74-6. 2006..divide the diuretics into six categories: 1) carbonic anhydrase inhibitors: acetazolamide, dichlorphenamide, methazolamide; 2) osmotic diuretics: glycerol, mannitol, urea; 3) loop diuretics: furosemide, bumetanide, ethacrynic acid, ..
- Carbonic anhydrase inhibitors. Inhibition studies of a coral secretory isoform by sulfonamidesAnthony Bertucci
Centre Scientifique de Monaco, Avenue Saint Martin, MC 98000 Principality of Monaco, Monaco
Bioorg Med Chem 17:5054-8. 2009..been investigated with a series of sulfonamides, including some clinically used derivatives (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, benzolamide, and sulpiride, or indisulam, a ..
- The development of topically acting carbonic anhydrase inhibitors as antiglaucoma agentsFrancesco Mincione
U O Oculistica Az USL 3, Val di Nievole, Ospedale di Pescia, Pescia, Italy
Curr Pharm Des 14:649-54. 2008..2.1.1) isoforms present in the eyes (CA I, II, IV and XII), with sulfonamides such as acetazolamide, methazolamide, ethoxzolamide and dichlorophenamide, is still widely used for the systemic treatment of glaucoma...
- Theoretical study of gas-phase acidity, pKa, lipophilicity, and solubility of some biologically active sulfonamidesMilan Remko
Department of Pharmaceutical Chemistry, Comenius University, Odbojarov 10, SK 832 32 Bratislava, Slovakia
Bioorg Med Chem 12:5395-403. 2004The geometries of 19 biologically active substituted sulfonamides (including clinically useful acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, and brinzolamide) in both neutral and deprotonated forms, were ..
- The development of topically acting carbonic anhydrase inhibitors as anti-glaucoma agentsFrancesco Mincione
U O Oculistica Az USL 3, Val di Nievole, Ospedale di Pescia, Pescia, Italy
Curr Top Med Chem 7:849-54. 2007Carbonic anhydrase inhibitors (CAIs) such as acetazolamide, methazolamide, ethoxzolamide and dichlorophenamide were and still are widely used systemic antiglaucoma drugs...
- Saccharomyces cerevisiae β-carbonic anhydrase: inhibition and activation studiesSemra Isik
Science and Art Faculty, Department of Biology, Balikesir University, Balikesir, Turkey
Curr Pharm Des 16:3327-36. 2010..The clinically used sulfonamides/sulfamate (acetazolamide, ethoxzolamide, methazolamide, dorzolamide, topiramate, celecoxib, etc...
- Design of a carbonic anhydrase IX active-site mimic to screen inhibitors for possible anticancer propertiesCaroli Genis
Department of Biochemistry and Molecular Biology, College of Medicine, University of Florida, Gainesville, Florida 32610, USA
Biochemistry 48:1322-31. 2009..with five CA sulfonamide-based inhibitors (acetazolamide, benzolamide, chlorzolamide, ethoxzolamide, and methazolamide), and compared to CA II...
- Studies on bicarbonate transporters and carbonic anhydrase in porcine nonpigmented ciliary epitheliumMohammad Shahidullah
Department of Physiology, University of Arizona, Tucson, Arizona 85724, USA
Invest Ophthalmol Vis Sci 50:1791-800. 2009..Bicarbonate transport plays a role in aqueous humor (AH) secretion. The authors examined bicarbonate transport mechanisms and carbonic anhydrase (CA) in porcine nonpigmented ciliary epithelium (NPE)...
- PAT-1 (Slc26a6) is the predominant apical membrane Cl-/HCO3- exchanger in the upper villous epithelium of the murine duodenumJanet E Simpson
Department of Biomedical Sciences, University of Missouri, Columbia, MO, USA
Am J Physiol Gastrointest Liver Physiol 292:G1079-88. 2007..in the PAT-1(-) villous epithelium but increased to WT levels in the absence of CO(2)/HCO(3)(-) or during methazolamide treatment...
- Focal CO2/H+ alters phrenic motor output response to chemical stimulation of cat pre-Botzinger complex in vivoIrene C Solomon
Department of Physiology and Biophysics, State University of New York at Stony Brook, Stony Brook, New York 11794 8661, USA
J Appl Physiol (1985) 94:2151-7. 2003..Focal tissue acidosis was produced by blockade of carbonic anhydrase with either focal acetazolamide (AZ) or methazolamide (MZ) microinjection...
- Carbonic anhydrase inhibitors. Inhibition and homology modeling studies of the fungal beta-carbonic anhydrase from Candida albicans with sulfonamidesAlessio Innocenti
Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino, Florence, Italy
Bioorg Med Chem 17:4503-9. 2009..6 microM. The best Nce103 inhibitors were acetazolamide, methazolamide, bromosulfanilamide, and 4-hydroxymethylbenzenesulfonamide (K(I)s<500 nM)...
- Molecular cloning, characterization, and inhibition studies of the Rv1284 beta-carbonic anhydrase from Mycobacterium tuberculosis with sulfonamides and a sulfamateTomoko Minakuchi
Department of Gastroenterology, Kochi Medical School, Nankoku, Kochi 783 8505, Japan, and Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Room 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
J Med Chem 52:2226-32. 2009..values in the range of 1-10 microM, but several derivatives, including sulfanilyl-sulfonamides acetazolamide, methazolamide, dichlorophenamide, dorzolamide, brinzolamide, benzolamide, and the sulfamate topiramate, exhibited ..
- The alpha and beta classes carbonic anhydrases from Helicobacter pylori as novel drug targetsIsao Nishimori
Department of Gastroenterology and Hepatology, Kochi Medical Schoo, Nankoku, Kochi 783 8505, Japan
Curr Pharm Des 14:622-30. 2008..Furthermore, certain CA inhibitors, such as acetazolamide and methazolamide, were shown to inhibit the bacterial growth in vitro...
- Muscarinic receptor-induced acidification in sublingual mucous acinar cells: loss of pH recovery in Na+-H+ exchanger-1 deficient miceH V Nguyen
Center for Oral Biology, University of Rochester School of Medicine and Dentistry, Rochester, NY 14642, USA
J Physiol 523:139-46. 2000..niflumate, and was prevented in the absence of HCO3- by treatment with the carbonic anhydrase inhibitor methazolamide. These results indicate that the muscarinic-induced acidification is due to HCO3- loss, probably mediated by ..
- Discovery of molecular mechanisms of neuroprotection using cell-based bioassays and oligonucleotide arraysSatinder S Sarang
Biotechnology Center, Center for Neurologic Diseases, Brigham and Women s Hospital, Harvard Medical School, Cambridge, Massachusetts 02139, USA
Physiol Genomics 11:45-52. 2002..We identified 26 neuroprotective compounds, of which megestrol, meclizine, verapamil, methazolamide, sulindac, and retinol were examined in greater detail...
- Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XVMika Hilvo
Institute of Medical Technology, University of Tampere and Tampere University Hospital, Biokatu 6, FI 33520, Tampere, Finland
J Med Chem 52:646-54. 2009..Best mCA XV inhibitors were celecoxib, sulfanilyl-sulfonamides, methazolamide, ethoxzolamide, dorzolamide, brinzolamide, and sulthiame, with K(I)s in the range of 45-65 nM...
- Forskolin-induced HCO3- current across apical membrane of the frog corneal epitheliumO A Candia
Department of Ophthalmology, Mount Sinai School of Medicine, New York, New York 10029
Am J Physiol 259:C215-23. 1990..b>Methazolamide also inhibited Isc...
- Bicarbonate transport along the loop of Henle. I. Microperfusion studies of load and inhibitor sensitivityG Capasso
Department of Cellular and Molecular Physiology, Yale University School of Medicine, New Haven, Connecticut 06510 8026
J Clin Invest 88:430-7. 1991..min-1 was reached. Methazolamide (2 x 10(-4) M) reduced JHCO3 by 70%; the amiloride analogue ethylisopropylamiloride (EIPA) (2 x 10(-4) M) ..
- Biochemical, histological, and inhibitor studies of membrane carbonic anhydrase in frog gastric acid secretionE R Swenson
Department of Medicine, Department of Veterans Affairs Medical Center, University of Washington, Seattle, Washington 98108, USA
Am J Physiol Gastrointest Liver Physiol 281:G61-8. 2001..isolated mucosa was measured before and after mucosal addition of a permeant CA inhibitor (methazolamide) and before and after mucosal or serosal addition of two impermeant CA inhibitors of differing molecular mass: ..
- Methazolamide does not impair respiratory work performance in anesthetized rabbitsHeidrun F Kiwull-Schöne
Dept of Physiology, Faculty of Medicine, Ruhr Univ, 44780 Bochum, Germany
Am J Physiol Regul Integr Comp Physiol 297:R648-54. 2009..Among others, the highly diffusible CA-inhibitor methazolamide differs from acetazolamide in that it fails to activate Ca(2+)-dependent potassium channels in skeletal ..
- Carbonic anhydrase inhibitors. Inhibition of the human cytosolic isozyme VII with aromatic and heterocyclic sulfonamidesDaniela Vullo
Universita degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
Bioorg Med Chem Lett 15:971-6. 2005..of aromatic and heterocyclic sulfonamides, including some of the clinically used derivatives (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide and benzolamide), as well as the sulfamate ..
- Alkalinization in the isolated and perfused anterior midgut of the larval mosquito, Aedes aegyptiHorst Onken
Department of Biological Sciences, Wagner College, Staten Island, NY 10301, USA
J Insect Sci 8:1-20. 2008..The carbonic anhydrase inhibitor, methazolamide (50 micromol l(-1)), on either the luminal or hemolymph-side, or the inhibitor of anion transport, DIDS (1 ..
- Carbonic anhydrase inhibitors. Design of anticonvulsant sulfonamides incorporating indane moietiesCeline Chazalette
Universite Joseph Fourier de Grenoble, Laboratoire d Etudes Dynamiques et Structurales de la Sélectivité, Bât C Chimie, 301 rue de la Chimie, Domaine Universitaire, 38400 Saint Martin d Hères Grenoble, France
Bioorg Med Chem Lett 14:5781-6. 2004..of these sulfonamides was rather low as compared to that of other sulfonamide/sulfamate CA inhibitors, such as methazolamide. Furthermore, the 2-amino/acetamido-indane-5-sulfonic acids prepared during this work also showed interesting ..
- Volume-activated taurine efflux from skate erythrocytes: possible band 3 involvementL Goldstein
Section of Physiology, Brown University, Providence, Rhode Island 02912
Am J Physiol 260:R1014-20. 1991..Thus there is considerable evidence in favor of the involvement of band 3 in VA taurine efflux, but the issue of the sulfate fluxes remains to be resolved...
- Glutathione conjugation of methazolamide and subsequent reactions in the ciliary body in vitroK Kishida
Department of Ophthalmology, Osaka University Medical School, Japan
J Pharm Sci 79:638-42. 1990Conjugation reaction of methazolamide with glutathione and its subsequent reactions were studied in vitro. Glutathione, cysteinylglycine, and cysteine conjugates of methazolamide were chemically synthesized...
- Purification and characterization of human salivary carbonic anhydraseH Murakami
J Biol Chem 262:1382-8. 1987..iodide, sulfanilamide, and bromopyruvic acid, but the salivary enzyme is less sensitive to acetazolamide and methazolamide than CA II...
- Methazolamide for essential voice tremorK Busenbark
Department of Neurology, University of Kansas Medical Center, Kansas City 66160 7314, USA
Neurology 47:1331-2. 1996We studied the safety and efficacy of methazolamide (average dose 168 mg/day) in a placebo-controlled blinded investigation in nine patients with essential voice tremor...
- A comparison between the effect of topical and systemic carbonic anhydrase inhibitors on aqueous humor secretionW F Brechue
University of Florida Health Science Center, College of Medicine, Department of Pharmacology and Therapeutics, Gainesville 32610 0267
Exp Eye Res 57:67-78. 1993..We studied methazolamide (25 mg kg-1), ethoxzolamide (4 mg kg-1), and MK-927 (2% in 0.5% hydroxyethylcellulose, topical, pH 4.8)...
- Electroretinal changes in the presence of a carbonic anhydrase inhibitorG C Broeders
Department of Ophthalmology, College of Medicine, University of Florida, Gainesville
Ophthalmologica 196:103-10. 1988A specific carbonic anhydrase activity inhibitor (methazolamide) was injected into one vitreous body each of 4 New Zealand White rabbits. Electroretinograms (ERG) were recorded before and several times after the methazolamide injection...
- Carbonic anhydrase inhibitors ameliorate the symptoms of hypokalaemic periodic paralysis in rats by opening the muscular Ca2+-activated-K+ channelsDomenico Tricarico
Unit of Pharmacology, Department of Pharmacobiology, Faculty of Pharmacy, University of Bari, via Orabona no 4, 70126 Bari, Italy
Neuromuscul Disord 16:39-45. 2006..K+ -deficient rats treated in vivo with dichlorphenamide (DCP), ethoxzolamide (ETX), hydrochlorthiazide (HCT), methazolamide (MTZ), bendroflumethiazide (BFT) and acetazolamide (ACTZ)...
- Topical dorzolamide for the treatment of cystoid macular edema in patients with retinitis pigmentosaSandeep Grover
Department of Ophthalmology and Visual Sciences, University of Illinois at Chicago, 1855 West Taylor Street, Chicago, IL 60612, USA
Am J Ophthalmol 141:850-8. 2006To determine if topical dorzolamide, as observed with the use of systemic acetazolamide and methazolamide, would be effective in treating cystoid macular edema (CME) in patients with retinitis pigmentosa (RP).
- A role for carbonic anhydrase in early eye morphogenesisP J Linser
Whitney Laboratory, St Augustine, FL 32086
Invest Ophthalmol Vis Sci 30:783-5. 1989The carbonic anhydrase inhibitor methazolamide was used to test the hypothesis that carbonic anhydrase activity plays a role in the early morphogenesis of the chick eye...
- Measurement of aqueous humor flow following scleral injection of sulfacetamide as marker: effect of methazolamide, timolol, and pilocarpineB P Vogh
University of Florida College of Medicine, Department of Pharmacology and Therapeutics, Gainesville
J Ocul Pharmacol 5:293-302. 1989..37 S.E. overall. The data show that inhibition of carbonic anhydrase (CA) in ciliary processes by systemic methazolamide reduces flow 38%. Topical timolol reduces flow 35%...
- The effects of topical and general anesthesia on ocular drug levels and intraocular pressure lowering activity of topically applied carbonic anhydrase inhibitorsA Bar-Ilan
Department of Pharmacology and Therapeutics, University of Florida College of Medicine, Gainesville
J Ocul Pharmacol 4:1-12. 1988..This did not affect the permeability and activity of other, more lipophilic, CAI like methazolamide and ethoxzolamide (E)...
- Cyclodextrin solubilization of carbonic anhydrase inhibitor drugs: formulation of dorzolamide eye drop microparticle suspensionPhatsawee Jansook
Faculty of Pharmaceutical Sciences, University of Iceland, Reykjavik, Iceland
Eur J Pharm Biopharm 76:208-14. 2010..Phase-solubility of each drug tested (i.e. methazolamide, brinzolamide and dorzolamide HCl) was determined in either pure water or an aqueous eye drop medium...
- Regulation of anion transport across the uterine epithelium of Gallus domesticusK Brockmeier
Institute for Veterinary Physiology, Justus Liebig Universität Gießen, D 35392 Gießen, Germany
Poult Sci 90:618-23. 2011..In addition, methazolamide, a blocker of carboanhydrases, significantly reduced baseline I(sc)...
- Changes in intraocular pressure associated with topical dorzolamide and oral methazolamide in glaucomatous dogsK N Gelatt
Department of Small Animal Clinical Sciences, College of Veterinary Medicine, University of Florida, Gainesville, FL 32610 0126, USA
Vet Ophthalmol 4:61-7. 2001To compare the reduction in intraocular pressure (IOP) by topical 2% dorzolamide to oral methazolamide (5 mg/kg) in dogs, and determine if the combination of both drugs would reduce IOP more than either drug administered alone.
- DNA cloning, characterization, and inhibition studies of an α-carbonic anhydrase from the pathogenic bacterium Vibrio choleraeSonia Del Prete
Istituto di Biochimica delle Proteine CNR, Via P Castellino 111, 80131 Napoli, Italy
J Med Chem 55:10742-8. 2012..and sulfamates led to the detection of a large number of low nanomolar inhibitors, among which are methazolamide, acetazolamide, ethoxzolamide, dorzolamide, brinzolamide, benzolamide, and indisulam (KI values in the range 0...
- Interactions between carbonic anhydrase and its inhibitors revealed by gel electrophoresis and circular dichroismE Gianazza
Istituto di Scienze Farmacologiche, Universita di Milano, Italy
Electrophoresis 21:1435-45. 2000..of complexes between carbonic anhydrase (CA) and three sulfonamide inhibitors, acetazolamide, dorzolamide and methazolamide, were investigated by spectroscopic and electrophoretic techniques...
- The ocular distribution of methazolamide after corneal and scleral administration: the effect of ionization stateC W Conroy
University of Florida College of Medicine, Department of Pharmacology and Therapeutics, Gainesville 32610, USA
J Ocul Pharmacol Ther 14:565-73. 1998The accession of methazolamide in ionized and unionized form to cornea, sclera, aqueous humor and ciliary process was studied 10 minutes following separate application to either sclera or cornea of a 1 mM solution...
- Dual role of CFTR in cAMP-stimulated HCO3- secretion across murine duodenumL L Clarke
Dalton Cardiovascular Research Center, University of Missouri Columbia 65211, USA
Am J Physiol 274:G718-26. 1998..b>Methazolamide also reduced the Js-->m by 39% but did not affect the delta Isc...
- Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IVAngela Casini
Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Universita degli Studi di Firenze, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino, Florence, Italy
Bioorg Med Chem Lett 13:841-5. 2003..good inhibitory properties against the other two isozymes investigated here, similarly with acetazolamide, methazolamide or dichlorophenamide...
- The effect of transport-blocking drugs on secretion of fluid and electrolytes by the mandibular gland of red kangaroos, Macropus rufusA M Beal
School of Biological Science, University of New South Wales, Sydney, Australia
Arch Oral Biol 42:705-16. 1997..b>Methazolamide (0...
- Barium- or quinine-induced depolarization activates K+, Na+ and cationic conductances in frog proximal tubular cellsF Discala
INSERM U 323, Faculte de Medecine Necker Enfants Malades, Paris, France
J Physiol 448:525-37. 1992..1 mM-methazolamide, to inhibit the rheogenic Na(+)-HCO3-symport, and 1 microM-amiloride, to block Na+ conductance (GNa)...
- Purification and inhibition studies with anions and sulfonamides of an α-carbonic anhydrase from the Antarctic seal Leptonychotes weddelliiAlessandra Cincinelli
Universita degli Studi di Firenze, Dipartimento di Chimica Ugo Schiff, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
Bioorg Med Chem 19:1847-51. 2011..Many clinically used sulfonamides, such as acetazolamide, methazolamide, dorzolamide, brinzolamide and benzolamide were low nanomolar inhibitors, with K(I)s in the range of 5.7-67 nM...
- Carbonic anhydrase inhibitors: aromatic and heterocyclic sulfonamides incorporating adamantyl moieties with strong anticonvulsant activityMarc A Ilies
University of Agricultural Sciences and Veterinary Medicine, Faculty of Biotechnologies, Department of Chemistry, B dul Marasti nr 59, 71331 Bucharest, Romania
Bioorg Med Chem 12:2717-26. 2004..processes, CA I, and CA II, of the same order of magnitude as the clinically used drugs acetazolamide and methazolamide. The lipophilicity of the best CA inhibitors was determined and expressed as their experimental log k' IAM and ..
- Carbonic anhydrase inhibitors. Inhibition of mitochondrial isozyme V with aromatic and heterocyclic sulfonamidesDaniela Vullo
Laboratorio di Chimica Bioinorganica, Universita degli Studi di Firenze, Rm 188, Via della Lastruccia 3, I 50019 Sesto Fiorentino Firenze, Italy
J Med Chem 47:1272-9. 2004..The clinically used inhibitors acetazolamide, methazolamide, ethoxzolamide, dorzolamide, brinzolamide, and topiramate on the other hand were less effective CA V ..
- A case of paclitaxel-induced maculopathy treated with methazolamideNam Kyun Koo
Department of Ophthalmology, Dongkang Hospital, Ulsan, Korea
Korean J Ophthalmol 26:394-7. 2012..is significant, replacing paclitaxel with another agent was not warranted; therefore, maintenance therapy with methazolamide was performed before and after administering the anti-cancer agent...
- Interactions of human organic anion transporters with diureticsHabib Hasannejad
Department of Pharmacology and Toxicology, Kyorin University School of Medicine, Tokyo, Japan
J Pharmacol Exp Ther 308:1021-9. 2004..bumetanide, ethacrynic acid, and furosemide; and carbonic anhydrase inhibitors, including acetazolamide and methazolamide. These diuretics inhibited organic anion uptake mediated by hOAT1, hOAT2, hOAT3, and hOAT4 in a competitive ..
- The extremo-α-carbonic anhydrase from the thermophilic bacterium Sulfurihydrogenibium azorense is highly inhibited by sulfonamidesDaniela Vullo
Universita degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm 188, Via della Lastruccia 3, 50019 Sesto Fiorentino Florence, Italy
Bioorg Med Chem 21:4521-5. 2013..Many clinically used sulfonamides, such as acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, topiramate, celecoxib and sulpiride were low ..
- Impact of hemolysis during sample collection: how different is drug concentration in hemolyzed plasma from that of normal plasma?Aimin Tan
PharmaNet Canada Inc, Quebec, Canada
J Chromatogr B Analyt Technol Biomed Life Sci 901:79-84. 2012..Among the ten different drug compounds tested, only methazolamide, which binds strongly to RBCs, showed significant change in plasma concentration due to hemolysis.
- Acute bilateral angle closure glaucoma induced by methazolamideAhmad A Aref
Bascom Palmer Eye Institute, University of Miami Miller School of Medicine, Miami, FL Illinois Eye and Ear Infirmary, University of Illinois at Chicago School of Medicine, Chicago, IL, USA
Clin Ophthalmol 7:279-82. 2013To report a case of bilateral acute myopia and angle closure glaucoma after ingestion of methazolamide.
- Anticonvulsant/antiepileptic carbonic anhydrase inhibitors: a patent reviewMayank Aggarwal
University of Florida, Department of Biochemistry and Molecular Biology, College of Medicine, 1600 SW Archer Rd, PO Box 100245, Gainesville, FL 32610, USA
Expert Opin Ther Pat 23:717-24. 2013..One indirect pathway for the treatment of epilepsy includes the inhibition of carbonic anhydrase (CA), thereby increasing CO(2) levels in the brain...
- Differential contribution of isoaspartate post-translational modifications to the fibrillization and toxic properties of amyloid β and the Asn23 Iowa mutationSilvia Fossati
Department of Pathology, New York University School of Medicine, New York, NY 10016, U S A
Biochem J 456:347-60. 2013..b>Methazolamide, a cytochrome c release inhibitor, exerted a protective effect in both cell types, suggesting that ..
- Inhibition profiling of human carbonic anhydrase II by high-throughput screening of structurally diverse, biologically active compoundsRema Iyer
Department of Biological Sciences, Western Michigan University, Kalamazoo, Michigan 49008 5410, USA
J Biomol Screen 11:782-91. 2006..Three known sulfonamide CA inhibitors were identified: acetazolamide, methazolamide, and celecoxib...
- Determination of memantine in rat plasma by HPLC-fluorescence method and its application to study of the pharmacokinetic interaction between memantine and methazolamideMohamed G Hassan
Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Al Azhar University, Assiut Branch, Assiut 71524, Egypt
Biomed Chromatogr 26:214-9. 2012..The fluorescence property and reaction yield of authentic DIB-MT were also examined. The proposed method was successfully applied to study the pharmacokinetic interaction between MT and methazolamide.
- Effect of thiazides on colonic NaCl absorption: role of carbonic anhydraseD S Goldfarb
Nephrology Section, Department of Veteran Affairs Medical Center, New York, New York 10010
Am J Physiol 261:F452-8. 1991..Prior exposure of the colon to the carbonic anhydrase inhibitor methazolamide (0...
- Biochemical and molecular characterization of stress-induced β-carbonic anhydrase from a C(4) plant, Pennisetum glaucumTanushri Kaul
Plant Molecular Biology Group, International Centre for Genetic Engineering and Biotechnology ICGEB, Aruna Asaf Ali Marg, New Delhi 110 067, India
J Plant Physiol 168:601-10. 2011..Recombinant PgCA esterase activity is inhibited by standard CA inhibitors acetazolamide, methazolamide and azide. Subcellular immunostaining studies revealed a chloroplastic localization of PgCA protein...
- Calcium metabolism in acidotic patients induced by carbonic anhydrase inhibitors: responses to citrateE Higashihara
Department of Urology, Faculty of Medicine, University of Tokyo, Japan
J Urol 145:942-8. 1991..citrate were examined in 51 patients with glaucoma receiving carbonic anhydrase inhibitors (acetazolamide or methazolamide). Metabolic acidosis, hypocitraturia and increased incidence of nephrolithiasis were induced by both drugs...
- Inhibition of mitochondrial carbonic anhydrase and ureagenesis: a discrepancy examinedS J Dodgson
Department of Physiology, School of Medicine, University of Pennsylvania, Philadelphia 19104 6085
J Appl Physiol (1985) 63:2134-41. 1987..07 ethoxzolamide, 0.5 methazolamide, 0.7 acetazolamide, and 5.0 p-aminomethylbenzenesulfonamide...
- Penetration into the anterior chamber via the conjunctival/scleral pathwayR D Schoenwald
Division of Pharmaceutics, College of Pharmacy, University of Iowa, Iowa City, USA
J Ocul Pharmacol Ther 13:41-59. 1997..A constant concentration of methazolamide analogs as well as 6-carboxyfluorescein (6-CB) and rhodamine B (RB) was maintained on either the cornea or the ..
- Larvae of the midge Chironomus riparius possess two distinct mechanisms for ionoregulation in response to ion-poor conditionsHang Nguyen
Department of Biology, York University, Toronto, Ontario, Canada
Am J Physiol Regul Integr Comp Physiol 299:R762-73. 2010..Inhibitors of the Na(+)/H(+) exchangers (EIPA) and carbonic anhydrase (methazolamide) provide evidence for Na(+)/H(+) and Cl(-)/HCO(3)(-) exchange mechanisms in the anal papillae...
- A novel system to measure labelled CO2 and HCO3- fluxes across epithelia: corneal epithelium as model tissueO A Candia
Department of Ophthalmology, Mount Sinai School of Medicine, New York, NY 10029, USA
Exp Eye Res 63:137-49. 1996..These fluxes were independent of the presence of Cl- in the bathing solutions. The bilateral addition of methazolamide (10(-4) M) reduced both unidirectional fluxes to about 2.0 mu eq h-1 cm-2...
- The hypoxia-induced facilitation of augmented breaths is suppressed by the common effect of carbonic anhydrase inhibitionHarold J Bell
Department of Medicine, Penn State University College of Medicine, Milton S Hershey Medical Centre, Hershey, PA, USA
Respir Physiol Neurobiol 171:201-11. 2010..addressed this question by studying the effects of treatment with an alternative carbonic anhydrase inhibitor, methazolamide, which has been reported to leave carotid body responsiveness to hypoxia intact...
- HCO3- secretion in the esophageal submucosal glandsSolange Abdulnour-Nakhoul
The VA Medical Center, Attn Research, Rm 5F151, 1601 Perdido St, New Orleans, LA 70112 2699, USA
Am J Physiol Gastrointest Liver Physiol 288:G736-44. 2005..and carbachol-stimulated secretions were also blocked by serosal application of atropine, pirenzipine, DIDS, methazolamide, and ethoxzolamide...
- Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: solution and X-ray crystallographic studiesGiuseppina De Simone
Dipartimento di Chimica Biologica Sezione Biostrutture and Istituto di Biostrutture e Bioimmagini CNR, University of Naples Federico II, Via Mezzocannone 16, 80134 Naples, Italy
Bioorg Med Chem Lett 15:2315-20. 2005..2 nM, of the same order of magnitude as that of the clinically used sulfonamides/sulfamates acetazolamide, methazolamide, ethoxzolamide and topiramate (K(I)s in the range of 5.4-15.4 nM)...
- Methazolamide-induced deliriumM Cyr
College of Pharmacy, University of Tennessee, Memphis, USA
Pharmacotherapy 17:387-9. 1997A 74-year-old man became delirious 2 days after beginning oral therapy with methazolamide. The delirium was manifested by intermittent psychosis, incontinence of bowel and bladder, lethargy, and disorientation...
- Alkalization of larval mosquito midgut and the role of carbonic anhydrase in different species of mosquitoesMaria del Pilar Corena
The Whitney Laboratory, University of Florida, St Augustine, USA
Comp Biochem Physiol C Toxicol Pharmacol 137:207-25. 2004..We also tested the effect of CA inhibitors such as methazolamide and acetazolamide in the alkalization of the midgut for these species...