• Acetazolamide is an inhibitor of carbonic anhydrase. (wikipedia.org)
  • For the reduction of intraocular pressure (IOP), acetazolamide inactivates carbonic anhydrase and interferes with the sodium pump, which decreases aqueous humor formation and thus lowers IOP. (wikipedia.org)
  • Acetazolamide is a carbonic anhydrase inhibitor. (wikipedia.org)
  • Carbonic anhydrase inhibitors (eg, acetazolamide) and loop diuretics (eg, furosemide) are thought to exert their effect on ICP by reducing cerebrospinal fluid (CSF) production at the choroid plexus. (medscape.com)
  • Acetazolamide is a nonbacteriostatic sulfonamide and a potent CA inhibitor that is effective in diminishing fluid secretion. (medscape.com)
  • Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM. (abmole.com)
  • Carbonic anhydrase inhibitors (CAIs) have been used to treat glaucoma since 1954, when Becker 1 first demonstrated the clinical efficacy of systemically administered acetazolamide. (entokey.com)
  • Acetazolamide (ACZ) is a carbonic anhydrase inhibitor prescribed for the treatment of various pathologies. (unicam.it)
  • In this work we have investigated the effect of 17β-estradiol, an ER activator, and ferulic acid, a carbonic anhydrase inhibitor, as well as ER activator, in the absence and in the presence of the carbonic anhydrase inhibitor acetazolamide on the metabolism of MCF7 cells and MCF7 cells, stably transfected to express HER2 (MCF7HER2). (canada.ca)
  • However, the carbonic anhydrase inhibitor acetazolamide had the largest effect on the profile of lipophilic metabolites. (canada.ca)
  • Inside a transwell assay (Fig.?2a), both anti-CAIX mAbs G37 and G119 showed inhibition of RCC cell migration much like that seen using the CA inhibitor acetazolamide. (monossabios.com)
  • Acetazolamide belongs to a class of drugs known as carbonic anhydrase inhibitors. (webmd.com)
  • This polypharmacology of the CA inhibitors (CAIs) thus affords for novel applications for these drugs, such as for example the antiobesity action of topiramate and zonisamide (thought to be due to inhibition of two mitochondrial CA isoforms) or the antitumor activity of most sulfonamides and also coxibs and kinase inhibitors, which strongly inhibit the tumor-associated isoforms CA IX and XII. (pharmadvances.com)
  • Topical β-blockers, topical carbonic anhydrase inhibitors (CAIs), and prostaglandin analogues are reasonable first-line agents in children. (aao.org)
  • Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. (medscape.com)
  • Inhibition of carbonic anhydrase II in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. (wikipedia.org)
  • The mechanism is thought to involve inhibition of carbonic anhydrase (CA) within the choroidal epithelial cells, reducing the production of protons which are necessary for the osmotic transport of water and ions which constitute CSF. (wikipedia.org)
  • In rare cases, the inhibition of carbonic anhydrase may be strong enough to cause metabolic acidosis of clinical importance. (wikipedia.org)
  • Due to characteristic physicochemical properties of sulphonamide (Inhibition of Carbonic Anhydrase), they are clinically effective against glaucoma. (eurekaselect.com)
  • Zonisamide is another sulfur containing antiseizure drug that weakly inhibits carbonic anhydrase. (wikipedia.org)
  • Reversibly inhibits carbonic anhydrase, reducing hydrogen ion secretion at renal tubule and increasing renal excretion of sodium, potassium bicarbonate, and water to decrease production of aqueous humor. (medscape.com)
  • Ethoxzolamide is an inhibitor of the metalloenzyme carbonic anhydrase, which inhibits hCA I, hCA II, hCA IV, hCA VI and hCA VII with K i of 25 nM, 8 nM, 93 nM, 43 nM and 0.8 nM, respectively. (abmole.com)
  • Fluorometholone acetate potently inhibits carbonic anhydrase (CA) with IC50s of 2.18 μM and 17.5 μM for hCA-I and hCA-II, respectively. (abmole.com)
  • These drugs inhibit carbonic anhydrase (CA), one of the enzymes that regulate aqueous humor formation. (entokey.com)
  • Overview of analysis favours substituents with high electronegativity and less bulk at R and R positions of the parent nucleus, provides a basis to design new Sulfamide derivatives possessing potent and selective carbonic anhydrase-II inhibitory activity. (eurekaselect.com)
  • A series of artemisinin-sulfonamide hybrids (1-16) have been designed and synthesized by using molecular hybridization approach and investigated for the inhibitory activity of four human (h) carbonic anhydrases (CAs, EC 4.2.1.1), hCA I, II, IX and XII. (aminer.cn)
  • Selected sulfamides incorporate cluster with inhibitory effects toward CAs (IC50 values in the submicromolar and nanomolar range, some of the inhibitors being more than 50-times more selective toward the tumor-specific CAIX than for CAII abundantly present in normal tissues). (imtm.cz)
  • Methazolamide is also a carbonic anhydrase inhibitor. (wikipedia.org)
  • Other examples are: Dorzolamide Methazolamide Brinzolamide Dichlorphenamide Carbonic anhydrase inhibitors may be used to reduce the production of cerebrospinal fluid (CSF) in the brain. (wikipedia.org)
  • Methazolamide is a carbonic anhydrase inhibitor with K i of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively. (abmole.com)
  • Synthesis and biological evaluation of aminomethyl and alkoxymethyl derivatives as carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase inhibitors. (yyu.edu.tr)
  • It exists as a number of isoenzymes, the most active of which is carbonic anhydrase II (CA-II). (wikipedia.org)
  • In this research, we determined the inhibition property of rosmarinic acid on carbonic anhydrase isoenzymes I and II (hCA I and II) puri ed from human erythrocytes by using Sepharose-4B a nity column chromatography. (gumushane.edu.tr)
  • Human carbonic anhydrases (CAs) play essential roles in many pathological processes and several CA isoenzymes thus represent diagnostic and therapeutic targets. (imtm.cz)
  • We have developed selective CAIX inhibitors with anticancer properties based on carborane scaffold to the structure-assisted design of novel and original inhibitors targeting therapeutically relevant isoenzymes of human carbonic anhydrase. (imtm.cz)
  • Novelty, in brief, is represented by the intended elaboration of carborane, heteroborane and metalloborane compounds as active-site inhibitors of CA isoenzymes. (imtm.cz)
  • the sulfonamide coxibs (celecoxib, valdecoxib and paricoxib), or the protein kinase inhibitors pazopanib, imatinib and nilotinib, also show significant inhibition of many pharmacologically relevant CA isoforms. (pharmadvances.com)
  • This can include beta-blockers and carbonic anhydrase inhibitor. (guidedogs.org.uk)
  • 2 We hypothesized that 1) IOPs would differ between fish species, 2) the ophthalmic carbonic anhydrase inhibitor dorzolamide (Trusopt®) would reduce intraocular pressure in normal eyes, and 3) IOPs of exophthalmic eyes would differ from normal eyes. (vin.com)
  • Dorzolamide HCl is a water-soluble, potent inhibitor of human carbonic anhydrase II and IV with Ki of 1.9 nM and 31 nM, respectively, used as anti-glaucoma agent. (abmole.com)
  • Carbonic anhydrase inhibitors are primarily used for the treatment of glaucoma. (wikipedia.org)
  • citation needed] Brinzolamide (trade name Azopt) is a carbonic anhydrase inhibitor used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension. (wikipedia.org)
  • Carbonic Anhydrase-II is an excellent approach in reducing elevated intraocular pressure, thus treating glaucoma. (eurekaselect.com)
  • SIMBRINZA is a fixed combination of a carbonic anhydrase inhibitor and an alpha-2 adrenergic receptor agonist indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. (nih.gov)
  • SIMBRINZA (brinzolamide and brimonidine tartrate ophthalmic suspension) 1% and 0.2% is a fixed combination of a carbonic anhydrase inhibitor and an alpha-2 adrenergic receptor agonist indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. (nih.gov)
  • Dichlorphenamide is a sulfonamide and a carbonic anhydrase inhibitor of the meta-Disulfamoylbenzene class. (abmole.com)
  • All currently used inhibitors anhydrase inhibitors contain a sulfonamide or a sulfamate moiety connected to so-called 'ring structure' which is usually a 5- or 6-membered aromatic ring or conjugated ring system containing nitrogen, oxygen, and/or sulfur heteroatoms. (imtm.cz)
  • In biology and biochemistry , protease inhibitors , or antiproteases , [1] are molecules that inhibit the function of proteases ( enzymes that aid the breakdown of proteins ). (wikipedia.org)
  • Estrogen receptor (ER) activity has a profound effect on breast cancer cell growth through a number of metabolic changes driven by its effect on transcription of several enzymes, including carbonic anhydrases, Stearoyl-CoA desaturase-1, and oncogenes including HER2. (canada.ca)
  • Sultiame is a carbonic anhydrase inhibitor, widely used as an antiepileptic agent. (abmole.com)
  • EMAC10101d is a potent and selective toward hCA II inhibitor, with a Ki of 8.1 nM. (abmole.com)
  • Girentuximab (G250) is a chimeric monoclonal antibody that binds carbonic anhydrase IX (CAIX), a cell surface glycoprotein ubiquitously expressed in clear cell renal cell carcinoma (ccRCC). (abmole.com)
  • The development of isoform-specific inhibitor is still an important task in current medicine. (imtm.cz)
  • The use of three-dimensional boron cluster is a novel approach in the development of isoform-specific CA inhibitors. (imtm.cz)
  • The active site cavity contains a cluster of non-conserved residues that may be involved in ligand binding and have significant implications for developing the next-generation of isoform-specific inhibitors. (ox.ac.uk)
  • The sulfur-containing antiseizure and antimigraine drug topiramate is a weak inhibitor of carbonic anhydrase, particularly subtypes II and IV. (wikipedia.org)
  • Risk factors for metformin-associated lactic acidosis include renal impairment, concomitant use of certain drugs (eg, carbonic anhydrase inhibitors such as topiramate ), age 65 years old or greater, having a radiological study with contrast, surgery and other procedures, hypoxic states (eg, acute congestive heart failure), excessive alcohol intake, and hepatic impairment. (medscape.com)
  • Human carbonic anhydrase (hCA) XIV is a membrane-associated protein consisting of an N-terminal extracellular domain, a putative transmembrane region, and a small cytoplasmic tail. (rcsb.org)
  • Background Carbonic anhydrase (CA) IX is normally a surface-expressed protein that's upregulated from the hypoxia inducible factor (HIF) and represents a prototypic tumor-associated antigen that's overexpressed about renal cell carcinoma (RCC). (monossabios.com)
  • Carbonic Anhydrase I from human erythrocytes is a protein which is used as a standard pI (isoelectric point) marker for isoelectric focussing experiments. (sigmaaldrich.com)
  • A more immediate treatment is carbonic anhydrase inhibitors, which prevent bicarbonate uptake in the kidney and help correct the alkalosis. (wikipedia.org)
  • Zn(2+)-dependent carbonic anhydrases (CA) catalyse the reversible hydration of carbon dioxide to bicarbonate and participate in diverse physiological processes, hence having manifold therapeutic potentials. (ox.ac.uk)
  • The GDPSP/C was dependent on the availability of bicarbonate, but not on interstitial or intrapyramidal carbonic anhydrase activity. (jneurosci.org)
  • For the drugs used to treat viral infections, see protease inhibitor (pharmacology) . (wikipedia.org)
  • citation needed] Some diuretics inhibit the activity of carbonic anhydrase in proximal convoluted tubules and prevent reabsorption of bicarbonates from renal tubules. (wikipedia.org)
  • A class of compounds that reduces the secretion of H+ ions by the proximal kidney tubule through inhibition of CARBONIC ANHYDRASES. (bvsalud.org)
  • Proteinase propeptide inhibitors (sometimes referred to as activation peptides) are responsible for the modulation of folding and activity of the peptidase pro-enzyme or zymogen . (wikipedia.org)
  • Many naturally occurring protease inhibitors are proteins . (wikipedia.org)
  • In medicine , protease inhibitor is often used interchangeably with alpha 1-antitrypsin (A1AT, which is abbreviated PI for this reason). (wikipedia.org)
  • [3] A1AT is indeed the protease inhibitor most often involved in disease, namely in alpha-1 antitrypsin deficiency . (wikipedia.org)
  • Protease inhibitors may be classified either by the type of protease they inhibit, or by their mechanism of action. (wikipedia.org)
  • In 2004 Rawlings and colleagues introduced a classification of protease inhibitors based on similarities detectable at the level of amino acid sequence. (wikipedia.org)
  • This is a family of protease suicide inhibitors called the serpins . (wikipedia.org)
  • It contains inhibitors of multiple cysteine and serine protease families. (wikipedia.org)
  • The nature of carbonic anhydrase inhibition by aromatic sulfonamides is briefly discussed, as it may relate to certain variables in the analytical method. (aspetjournals.org)
  • Carbonic anhydrase inhibitors are a class of pharmaceuticals that suppress the activity of carbonic anhydrase. (wikipedia.org)
  • Whether carbonic anhydrase inhibition contributes to its clinical activity is not known. (wikipedia.org)
  • The method is suitable for estimating the activity of carbonic anhydrase inhibitors and for their determination in biological material. (aspetjournals.org)
  • In this paper we have represented "Three Dimensional Quantitative Structure Activity Relationship" study to characterize structural features of Sulfamide derivative [RRNSO2NH2] as inhibitors, that are required for selective binding of carbonic anhydrase isozymes (CAI and CAII). (eurekaselect.com)
  • Carbonic anhydrase activity has been observed in both the cytoplasm and around the plasma membranes of the corneal endothelium. (nih.gov)
  • hCAI/II-IN-6 is an orally active human carbonic anhydrase (CA) inhibitor. (abmole.com)
  • Carbonic anhydrase isoform XIV (CA XIV) is the last member of the human (h) CA family discovered so far, being localized in brain, kidneys, colon, small intestine, urinary bladder, liver, and spinal cord. (rcsb.org)
  • Structural Analysis of Charge Discrimination in the Binding of Inhibitors to Human Carbonic Anhydrases I and II. (expasy.org)
  • Carbonic Anhydrase I from human erythrocytes has been used as a pI (isoelectric point) marker in two-dimensional gel electrophoresis. (sigmaaldrich.com)
  • One mechanism by which carbonic anhydrase inhibitors could cause adverse effects in fish is by inducing plasma electrolyte imbalances, as has been reported in alewife. (vin.com)
  • A single application of the carbonic anhydrase inhibitor did not reduce IOP at either 4 h or 24 h, but neither were any adverse effects of treatment noted by visual examination or plasma electrolytes. (vin.com)
  • Crystal structure of the secretory isozyme of mammalian carbonic anhydrases CA VI: implications for biological assembly and inhibitor development. (ox.ac.uk)
  • Epilepsy and belongs to the drug class carbonic anhydrase inhibitor anticonvulsants . (drugs.com)
  • [4] This classification initially identified 48 families of inhibitors that could be grouped into 26 related superfamily (or clans) by their structure. (wikipedia.org)
  • Cardiovascular Drugs / Antilipemic Agents / HMG-CoA Reductase Inhibitors (i.e. (tevausa.com)
  • It catalyzes a reversible reaction whereby carbon dioxide becomes hydrated and carbonic acid becomes dehydrated. (medscape.com)
  • CA catalyzes the reversible reaction in which carbon dioxide (CO 2 ) is hydrated (H 2 O) to form carbonic acid (H 2 CO 3 ) (i.e. (entokey.com)
  • This paper describes the use of electrospray ionization-mass spectrometry (ESI-MS) to screen two libraries of soluble compounds to search for tight binding inhibitors for carbonic anhydrase II (EC 4.2.1.1). (figshare.com)
  • The binding mode observed for these molecules is distinct when compared to other non-metal-binding CA inhibitors. (rcsb.org)
  • Carbonic anhydrase inhibitors have been proposed as a potential treatment for gaseous exophthalmia in fish by modifying gas exchange between the pseudobranch and the eye. (vin.com)
  • 1,8 However, carbonic anhydrase inhibitors may cause buoyancy disorders through their effects on swim bladder function, 3 and there are some anecdotal reports of fatal treatment outcomes, though fish may have been compromised by systemic disease prior to treatment. (vin.com)