Carbonic Anhydrase Inhibitors
Acetazolamide
One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)
Carbonic Anhydrases
Methazolamide
Ethoxzolamide
Benzolamide
Carbonic Anhydrase II
Bicarbonates
Carbonic Anhydrase III
Carbon Dioxide
Carbonic Anhydrase I
Ion Exchange
Aqueous Humor
Timolol
Hydrogen-Ion Concentration
Glaucoma
An ocular disease, occurring in many forms, having as its primary characteristics an unstable or a sustained increase in the intraocular pressure which the eye cannot withstand without damage to its structure or impairment of its function. The consequences of the increased pressure may be manifested in a variety of symptoms, depending upon type and severity, such as excavation of the optic disk, hardness of the eyeball, corneal anesthesia, reduced visual acuity, seeing of colored halos around lights, disturbed dark adaptation, visual field defects, and headaches. (Dictionary of Visual Science, 4th ed)
Sodium
Rabbits
Biological Transport
Carbonic Anhydrase V
PubMed
A bibliographic database that includes MEDLINE as its primary subset. It is produced by the National Center for Biotechnology Information (NCBI), part of the NATIONAL LIBRARY OF MEDICINE. PubMed, which is searchable through NLM's Web site, also includes access to additional citations to selected life sciences journals not in MEDLINE, and links to other resources such as the full-text of articles at participating publishers' Web sites, NCBI's molecular biology databases, and PubMed Central.
Molecular Structure
Crystallography, X-Ray
Glaucoma, Open-Angle
Prostanoic Acids
Nevus, Sebaceous of Jadassohn
A syndrome characterized by lesions occurring on the face, scalp, or neck which consist of congenital hypoplastic malformations of cutaneous structures and which over time undergo verrucous hyperplasia. Additionally it is associated with neurological symptoms and skeletal, ophthalmological, urogenital, and cardiovascular abnormalities.
Genes, Dominant
Pedigree
Thermodynamics
A rigorously mathematical analysis of energy relationships (heat, work, temperature, and equilibrium). It describes systems whose states are determined by thermal parameters, such as temperature, in addition to mechanical and electromagnetic parameters. (From Hawley's Condensed Chemical Dictionary, 12th ed)
Reserpine
An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.
Pentylenetetrazole
A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.
Seizures
Does gill boundary layer carbonic anhydrase contribute to carbon dioxide excretion: a comparison between dogfish (Squalus acanthias) and rainbow trout (Oncorhynchus mykiss). (1/420)
In vivo experiments were conducted on spiny dogfish (Squalus acanthias) and rainbow trout (Oncorhynchus mykiss) in sea water to determine the potential role of externally oriented or gill boundary layer carbonic anhydrase in carbon dioxide excretion. This was accomplished by assessing pH changes in expired water using a stopped-flow apparatus. In dogfish, expired water was in acid-base disequilibrium as indicated by a pronounced acidification (delta pH=-0.11+/-0.01; N=22; mean +/- s.e.m.) during the period of stopped flow; inspired water, however, was in acid-base equilibrium (delta pH=-0.002+/-0.01; N=22). The acid-base disequilibrium in expired water was abolished (delta pH=-0.005+/-0.01; N=6) by the addition of bovine carbonic anhydrase (5 mg l-1) to the external medium. Addition of the carbonic anhydrase inhibitor acetazolamide (1 mmol l-1) to the water significantly reduced the magnitude of the pH disequilibrium (from -0.133+/-0.03 to -0.063+/-0.02; N=4). However, after correcting for the increased buffering capacity of the water caused by acetazolamide, the acid-base disequilibrium during stopped flow was unaffected by this treatment (control delta [H+]=99.8+/-22.8 micromol l-1; acetazolamide delta [H+]=81.3+/-21.5 micromol l-1). In rainbow trout, expired water displayed an acid-base disequilibrium (delta pH=0.09+/-0.01; N=6) that also was abolished by the application of external carbonic anhydrase (delta pH=0.02+/-0.01). The origin of the expired water acid-base disequilibrium was investigated further in dogfish. Intravascular injection of acetazolamide (40 mg kg-1) to inhibit internal carbonic anhydrase activity non-specifically and thus CO2 excretion significantly diminished the extent of the expired water disequilibrium pH after 30 min (from -0.123+/-0.01 to -0.065+/-0.01; N=6). Selective inhibition of extracellular carbonic anhydrase activity using a low intravascular dose (1.3 mg kg-1) of the inhibitor benzolamide caused a significant reduction in the acid-base disequilibrium after 5 min (from -0.11+/-0.01 to -0.07+/-0. 01; N=14). These results demonstrate that the expired water acid-base disequilibrium originates, at least in part, from excretory CO2 and that extracellular carbonic anhydrase in dogfish may have a significant role in carbon dioxide excretion. However, externally oriented carbonic anhydrase (if present in dogfish) plays no role in catalysing the hydration of the excretory CO2 in water flowing over the gills and thus is unlikely to facilitate CO2 excretion. (+info)Synaptic activation of GABAA receptors induces neuronal uptake of Ca2+ in adult rat hippocampal slices. (2/420)
Synaptically evoked transmembrane movements of Ca2+ in the adult CNS have almost exclusively been attributed to activation of glutamate receptor channels and the consequent triggering of voltage-gated calcium channels (VGCCs). Using microelectrodes for measuring free extracellular Ca2+ ([Ca2+]o) and extracellular space (ECS) volume, we show here for the first time that synaptic stimulation of gamma-aminobutyric acid-A (GABAA) receptors can result in a decrease in [Ca2+]o in adult rat hippocampal slices. High-frequency stimulation (100-200 Hz, 0.4-0.5 s) applied in stratum radiatum close (+info)Modulation of chloride, potassium and bicarbonate transport by muscarinic receptors in a human adenocarcinoma cell line. (3/420)
1. Short-circuit current (I(SC)) responses to carbachol (CCh) were investigated in Colony 1 epithelia, a subpopulation of the HCA-7 adenocarcinoma cell line. In Krebs-Henseleit (KH) buffer, CCh responses consisted of three I(SC) components: an unusual rapid decrease (the 10 s spike) followed by an upward spike at 30 s and a slower transient increase (the 2 min peak). This response was not potentiated by forskolin; rather, CCh inhibited cyclic AMP-stimulated I(SC). 2. In HCO3- free buffer, the decrease in forskolin-elevated I(SC) after CCh was reduced, although the interactions between CCh and forskolin remained at best additive rather than synergistic. When Cl- anions were replaced by gluconate, both Ca2+- and cyclic AMP-mediated electrogenic responses were significantly inhibited. 3. Basolateral Ba2+ (1-10 mM) and 293B (10 microM) selectively inhibited forskolin stimulation of I(SC), without altering the effects of CCh. Under Ba2+- or 293B-treated conditions, CCh responses were potentiated by pretreatment with forskolin. 4. Basolateral charybdotoxin (50 nM) significantly increased the size of the 10 s spike of CCh responses in both KH and HCO3- free medium, without affecting the 2 min peak. The enhanced 10 s spike was inhibited by prior addition of 5 mM apical Ba2+. Charybdotoxin did not affect forskolin responses. 5. In epithelial layers prestimulated with forskolin, the muscarinic antagonists atropine and 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP, both at 100 nM) abolished subsequent 10 microM CCh responses. Following addition of p-fluoro hexahydro-sila-difenidol (pF-HHSiD, 10 microM) or pirenzepine (1 microM), qualitative changes in the CCh response time-profile also indicated a rightward shift of the agonist concentration-response curve; however, 1 microM gallamine had no effect. These results suggest that a single M3-like receptor subtype mediates the secretory response to CCh. 6. It is concluded that CCh and forskolin activate discrete populations of basolateral K+ channels gated by either Ca2+ or cyclic AMP, but that the Cl- permeability of the apical membrane may limit their combined effects on electrogenic Cl- secretion. In addition, CCh activates a Ba2+-sensitive apical K+ conductance leading to electrogenic K+ transport. Both agents may also modulate HCO3- secretion through a mechanism at least partially dependent on carbonic anhydrase. (+info)Effects of maternal acetazolamide treatment on body weights and incisor development of the fetal rat. (4/420)
The incisor development of fetal rats on gestation day 19 was well correlated with their fetal weights. The number of odontoblasts in the mandibular incisors, an index of incisor development, increased more than that of the maxillary incisors with increase in fetal body weights. Maternal acetazolamide treatments were observed to suppress the mean fetal weight and to retard incisor development. A smaller incisor size, a thinner predentin layer, and fewer odontoblasts were characteristic of the acetazolamide group. There was also a good correlation between the fetal weights and the number of odontoblasts in the acetazolamide group. From these results, we postulated that the retarded incisor development of the fetal rats caused by the maternal acetazolamide treatment was related to their suppressed fetal weights. However, the regression coefficient of the fetal weights and the number of odontoblasts in the acetazolamide group was smaller than that of the vehicle control group. It may indicate that retarded incisor development in response to maternal acetazolamide treatment is to some extent independent of suppressed fetal weight. (+info)Endogenous pH shifts facilitate spreading depression by effect on NMDA receptors. (5/420)
Rapid extracellular alkalinizations accompany normal neuronal activity and have been implicated in the modulation of N-methyl-D-aspartate (NMDA) receptors. Particularly large alkaline transients also occur at the onset of spreading depression (SD). To test whether these endogenous pH shifts can modulate SD, the alkaline shift was amplified using benzolamide, a poorly permeant inhibitor of interstitial carbonic anhydrase. SD was evoked by microinjection of 1.2 M KCl into the CA1 stratum radiatum of rat hippocampal slices and recorded by a proximal double-barreled pH microelectrode and a distal potential electrode. In Ringer solution of pH 7.1 containing picrotoxin (but not at a bath pH of 7.4), addition of 10 microM benzolamide increased the SD alkaline shift from 0.20 +/- 0.07 to 0.38 +/- 0.17 unit pH (means +/- SE). This was correlated with a significant shortening of the latency and an increase in the conduction velocity by 26 +/- 16%. In the presence of the NMDA receptor antagonist DL-2-amino-5-phosphonovaleric acid (APV), benzolamide still amplified the alkaline transient, however, its effect on the SD latency and propagation velocity was abolished. The intrinsic modulation of SD by its alkaline transient may play an important role under focal ischemic conditions by removing the proton block of NMDA receptors where interstitial acidosis would otherwise limit NMDA receptor activity. (+info)Inhibition of carbonic anhydrase accounts for the direct vascular effects of hydrochlorothiazide. (6/420)
Hydrochlorothiazide has been shown to exert direct vasodilator effects by activation of calcium-activated potassium (KCa) channels in human and guinea pig isolated resistance arteries. Since hydrochlorothiazide binds to and inhibits the enzyme carbonic anhydrase and because KCa channel activation is pH sensitive, we investigated the role of intracellular and extracellular carbonic anhydrase in the vascular effects of thiazide diuretics. Small arteries were isolated from guinea pig mesentery and studied by use of a microvascular myograph technique. In some experiments, tone and intracellular pH (pHi) were measured simultaneously with 2', 7'-bis(2-carboxyethyl)-5(6)'-carboxyfluorescein (BCECF-AM). Bendroflumethiazide, a thiazide diuretic with minimal inhibitory effects on carbonic anhydrase, had little effect on noradrenaline-induced tone (16+/-8% relaxation) compared with hydrochlorothiazide (74+/-12% relaxation). In contrast to hydrochlorothiazide, the action of bendroflumethiazide was unaffected by 100 nmol/L charybdotoxin, a selective blocker of KCa channels. All inhibitors of carbonic anhydrase relaxed noradrenaline-induced tone in a concentration-dependent manner, and this effect was blocked by charybdotoxin. Hydrochlorothiazide and the inhibitors of carbonic anhydrase failed to relax tone induced by a depolarizing potassium solution. Acetazolamide and hydrochlorothiazide increased pHi by 0.27+/-0.07 and 0.21+/-0.04, respectively, whereas bendroflumethiazide had a much smaller effect: 0.06+/-0.03. The rise in pHi induced by any agent was not inhibited by charybdotoxin. The vasorelaxant effect of hydrochlorothiazide is shared by other inhibitors of carbonic anhydrase. Inhibitors of carbonic anhydrase, but not bendroflumethiazide, cause intracellular alkalinization, which is associated with KCa channel opening. These data suggest that the vasodilator effect of thiazide diuretics results primarily from inhibition of vascular smooth muscle cell carbonic anhydrase, which results in a rise in pHI, leading to KCa channel activation and vasorelaxation. (+info)Topical therapies for glaucoma: what family physicians need to know. (7/420)
Medication classes historically used in the management of glaucoma include beta blockers, miotics, sympathomimetics and carbonic anhydrase inhibitors. Because topically applied medications are more site specific, they are preferred in the treatment of glaucoma. Compared with oral medications, topical agents are associated with a decreased incidence of systemic side effects. With topical administration, conjunctival and localized skin allergic reactions are relatively common, whereas severe reactions, including death, are rare. Recently introduced topical agents for glaucoma therapy include dorzolamide and brinzolamide, the first topical carbonic anhydrase inhibitors; brimonidine and apraclonidine, more ocular-specific alpha agonists; and latanoprost, a prostaglandin analog, which is a new class of glaucoma medication. Latanoprost has the unique side effect of increasing iris pigmentation. Like their predecessors, the newer agents lower intraocular pressure by a statistically significant degree. Preservation of visual field, the more substantial patient-oriented end point, continues to be studied. (+info)VCO2 and VE kinetics during moderate- and heavy-intensity exercise after acetazolamide administration. (8/420)
The effect of carbonic anhydrase inhibition with acetazolamide (Acz) on CO2 output (VCO2) and ventilation (VE) kinetics was examined during moderate- and heavy-intensity exercise. Seven men [24 +/- 1 (SE) yr] performed cycling exercise during control (Con) and Acz (10 mg/kg body wt iv) sessions. Each subject performed step transitions (6 min) in work rate from 0 to 100 W [below ventilatory threshold (
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Sequence Similarity
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Diuretic
Carbonic anhydrase inhibitors[edit]. Carbonic anhydrase inhibitors inhibit the enzyme carbonic anhydrase which is found in the ... Carbonic anhydrase inhibitors acetazolamide,[16] dorzolamide Inhibits H+ secretion, resultant promotion of Na+ and K+ excretion ...
Diclofenamide
"Carbonic anhydrase inhibitors and osmotic agents in glaucoma. Carbonic anhydrase inhibitors". The British Journal of ... Diclofenamide (or dichlorphenamide) is a sulfonamide and a carbonic anhydrase inhibitor of the meta-disulfamoylbenzene class. ...
Angela Casini
"Carbonic anhydrase inhibitors". Medicinal Research Reviews. 23 (2): 146-189. doi:10.1002/med.10025. PMID 12500287. S2CID ... Casini, Angela (2004). "Hypoxia activates the capacity of tumor‐associated carbonic anhydrase IX to acidify extracellular pH". ... Casini, Angela (2004). "Unexpected nanomolar inhibition of carbonic anhydrase by COX-2-selective celecoxib: new pharmacological ...
Amphetamine
... based upon the clinical use of carbonic anhydrase inhibitors, carbonic anhydrase activation in other tissues may be associated ... CARBONIC ANHYDRASE INHIBITORS (CAIs). The design and development of CAIs represent the most prolific area within the CA ... Bozdag M, Altamimi AA, Vullo D, Supuran CT, Carta F (2019). "State of the Art on Carbonic Anhydrase Modulators for Biomedical ... Amphetamine also activates seven human carbonic anhydrase enzymes, several of which are expressed in the human brain. ...
Ethoxzolamide
Dimazole Dithiazanine iodide Gordon DM (July 1958). "Ethoxzolamide; a new carbonic anhydrase inhibitor". American Journal of ... It also decreases carbonic anhydrase in the CNS, increasing the seizure threshold. This reduction in carbonic anhydrase also ... Ethoxzolamide binds and inhibits carbonic anhydrase I. Carbonic anhydrase plays an essential role in facilitating the transport ... is a sulfonamide medication that functions as a carbonic anhydrase inhibitor. It is used in the treatment of glaucoma and ...
Ciliary body
Carbonic anhydrase inhibitors also decrease fluid production. They are available as eye drops (Trusopt and Azopt) and pills ( ...
Enzyme inhibitor
Reversible inhibitors[edit]. Types of reversible inhibitors[edit]. Reversible inhibitors attach to enzymes with non-covalent ... fraction of the enzyme population bound by inhibitor [. I. ]. [. I. ]. +. K. i. {\displaystyle {\cfrac {{\ce {[I]}}}{[{{\ce {I ... Uses of inhibitors[edit]. Enzyme inhibitors are found in nature and are also designed and produced as part of pharmacology and ... Examples of irreversible inhibitors[edit]. Trypanothione reductase with the lower molecule of an inhibitor bound irreversibly ...
Eye drop
Carbonic anhydrase inhibitors may cause stinging, burning, and eye discomfort. Lubricant eye drops may cause some side effects ... and carbonic anhydrase inhibitors. There are also combination drugs available for those patients who require more than one type ...
Methazolamide
... (trade name Neptazane) is a potent carbonic anhydrase inhibitor. It is indicated in the treatment of increased ...
Granatin A
It is a weak carbonic anhydrase inhibitor. Satomi, H.; Umemura, K.; Ueno, A.; Hatano, T.; Okuda, T.; Noro, T. (1993). "Carbonic ... anhydrase inhibitors from the pericarps of Punica granatum L". Biological & Pharmaceutical Bulletin. 16 (8): 787-790. doi: ...
Corilagin
It is a weak carbonic anhydrase inhibitor. Ellagic acid and corilagin inhibit TGF-β1-dependent EMT and has been shown to ... "Carbonic anhydrase inhibitors from the pericarps of Punica granatum L". Biological & Pharmaceutical Bulletin. 16 (8): 787-90. ...
Indane-5-sulfonamide
... is a carbonic anhydrase inhibitor. Carbonic anhydrase inhibitors: binding of indanesulfonamides to the ...
Punicalin
It is a highly active carbonic anhydrase inhibitor. The molecule contains a gallagic acid component linked to a glucose. Zhang ... Satomi, H.; Umemura, K.; Ueno, A.; Hatano, T.; Okuda, T.; Noro, T. (1993). "Carbonic anhydrase inhibitors from the pericarps of ...
Granatin B
It is a highly active carbonic anhydrase inhibitor. www.chemicalbook.com Satomi, H.; Umemura, K.; Ueno, A.; Hatano, T.; Okuda, ... "Carbonic anhydrase inhibitors from the pericarps of Punica granatum L". Biological & Pharmaceutical Bulletin. 16 (8): 787-790. ...
Casuarinin
It is a highly active carbonic anhydrase inhibitor. In some plants including oak and chestnut, the ellagitannins are formed ... "Carbonic anhydrase inhibitors from the pericarps of Punica granatum L". Biological & Pharmaceutical Bulletin. 16 (8): 787-790. ...
Pedunculagin
It is a highly active carbonic anhydrase inhibitor. It is an isomer of terflavin B. It can be synthesized. Satomi, H.; Umemura ... "Carbonic anhydrase inhibitors from the pericarps of Punica granatum L". Biological & Pharmaceutical Bulletin. 16 (8): 787-790. ... "Further characterization of galloyl pedunculagin as an effective autophosphorylation inhibitor of C-kinase in vitro". ...
Andersen-Tawil syndrome
Periodic paralysis can be treated with carbonic anhydrase inhibitors such as acetazolamide. The condition is very rare and is ... Periodic paralysis may be improved by taking carbonic anhydrase inhibitors such as acetazolamide. Andersen-Tawil syndrome is ...
Punicalagin
Satomi, H.; Umemura, K.; Ueno, A.; Hatano, T.; Okuda, T.; Noro, T. (1993). "Carbonic anhydrase inhibitors from the pericarps of ... In laboratory research, punicalagins had carbonic anhydrase inhibitor activity. Marzouk, M. S. A.; El-Toumy, S. A. A.; Moharram ...
Pomegranate ellagitannin
Satomi, H.; Umemura, K.; Ueno, A.; Hatano, T.; Okuda, T.; Noro, T. (1993). "Carbonic anhydrase inhibitors from the pericarps of ...
Brinzolamide
... is a carbonic anhydrase inhibitor (specifically, carbonic anhydrase II). Carbonic anhydrase is found primarily in ... and thus exhibits carbonic anhydrase inhibitory activity (largely carbonic anhydrase-I, when in the presence of Brinzolamide) ... Brinzolamide (trade names Azopt, Alcon Laboratories, Befardin, Fardi Medicals, ) is a carbonic anhydrase inhibitor used to ... Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion and thus lowers the ...
Aqueous humour
Fluid production can be decreased by beta blockers, alpha2-agonists, and carbonic anhydrase inhibitors. Structures of the eye ... an enzyme inhibited by 5-alpha reductase inhibitors, may be involved in production of aqueous humour. Aqueous humour is ...
Dorzolamide
It is a carbonic anhydrase inhibitor and works by decreasing the production of aqueous humour. Dorzolamide was approved for ... By blocking carbonic anhydrase, the Na/H exchanger can't work, which will decrease Na in the cell and prevent aqueous humor ... It lowers IOP by about 20%. Carbonic Anhydrase can convert H2CO3 into HCO3 (bicarbonate) and H+. The H+ is then exchanged for ...
Accommodative excess
Use of systemic drugs like Morphine, Digitalis, Sulfonamides, Carbonic anhydrase inhibitors may cause accommodative excess. ...
Timolol
It can also be used in combination with pilocarpine, carbonic anhydrase inhibitors or prostaglandin analogs. A Cochrane review ... For ophthalmic use, timolol is also available combined: with carbonic anhydrase inhibitors: timolol and brinzolamide timolol ...
Sultiame
... , also known as sulthiame, is a sulfonamide and inhibitor of the enzyme carbonic anhydrase. It is used as an ... Hansen JM, Kristensen M, Skovsted L (March 1968). "Sulthiame (Ospolot) as inhibitor of diphenylhydatoin metabolism". Epilepsia ...
Acetazolamide
... is a carbonic anhydrase inhibitor, hence causing the accumulation of carbonic acid. Carbonic anhydrase is an ... Other carbonic anhydrase inhibitors - potential for additive inhibitory effects on carbonic anhydrase and hence potential for ... Acetazolamide is in the diuretic and carbonic anhydrase inhibitor families of medication. It works by decreasing the formation ... The enzyme carbonic anhydrase is found here, allowing the reabsorption of bicarbonate, sodium, and chloride. By inhibiting this ...
Zonisamide
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Dynamic combinatorial chemistry
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he proposed the use of carbonic anhydrase (CA) inhibitor acetazolamide to heal peptic ulcers. In 1972 patented the first 100% ...
Competitive inhibition
is modified to include binding of the inhibitor to the free enzyme:. EI. +. S. ⇌. k. 3. k. −. 3. E. +. S. +. I. ⇌. k. −. 1. k. ... is the inhibitor concentration.. V. max. {\displaystyle V_{\max }}. remains the same because the presence of the inhibitor can ... To compute the concentration of competitive inhibitor [. I. ]. {\displaystyle {\ce {[I]}}}. that yields a fraction f. V. 0. {\ ... At this point, we can define the dissociation constant for the inhibitor as K. i. =. k. −. 3. /. k. 3. {\displaystyle K_{i}=k ...
Diuretic
Carbonic anhydrase inhibitorsEdit. Carbonic anhydrase inhibitors inhibit the enzyme carbonic anhydrase which is found in the ... Carbonic anhydrase inhibitors acetazolamide,[17] dorzolamide Inhibits H+ secretion, resultant promotion of Na+ and K+ excretion ...
효소 - 위키백과, 우리 모두의 백과사전
"Structural and kinetic characterization of active-site histidine as a proton shuttle in catalysis by human carbonic anhydrase ... Wlodawer A, Vondrasek J (1998). "Inhibitors of HIV-1 protease: a major success of structure-assisted drug design". 》Annual ... "The discovery and development of HMG-CoA reductase inhibitors" (PDF). 》J. Lipid Res.》 33 (11): 1569-82. PMID 1464741 ... "Allosteric small-molecule kinase inhibitors" (PDF). 》Pharmacology & Therapeutics》 (영어) 156: 59-68. doi:10.1016/j.pharmthera. ...
Karbonatna dehidrataza
Murakami, H. and Sly, W.S. (1987). "Purification and characterization of human salivary carbonic anhydrase". J. Biol. Chem. 262 ... Robert A. Copeland (2013). Evaluation of Enzyme Inhibitors in Drug Discovery: A Guide for Medicinal Chemists and ... Keilin, D. and Mann, T. (1939). "Carbonic anhydrase". Nature 144: 442-443. ... http://books.google.com/books/about/Evaluation_of_Enzyme_Inhibitors_in_Drug.html?id=l2rMy8QNUk0C. ...
Medication
Anti-allergy: mast cell inhibitors. *Anti-glaucoma: adrenergic agonists, beta-blockers, carbonic anhydrase inhibitors/ ... HMG-CoA reductase inhibitors (statins) for lowering LDL cholesterol inhibitors: hypolipidaemic agents. ... cytotoxic drugs, therapeutic antibodies, sex hormones, aromatase inhibitors, somatostatin inhibitors, recombinant interleukins ... monoamine oxidase inhibitors, lithium salts, and selective serotonin reuptake inhibitors (SSRIs)), antiemetics, Anticonvulsants ...
Phosphogluconate dehydratase
Carbonic anhydrase. *Fumarase. *Aconitase. *Enolase *Alpha. *Enolase 2. *Enoyl-CoA hydratase/3-Hydroxyacyl ACP dehydrase ...
Hemoglobin
Through the enzyme carbonic anhydrase, carbon dioxide reacts with water to give carbonic acid, which decomposes into ... hemoglobin ligands also include competitive inhibitors such as carbon monoxide (CO) and allosteric ligands such as carbon ...
Red blood cell
Band 3 - also assembles various glycolytic enzymes, the presumptive CO2 transporter, and carbonic anhydrase into a ... Inhibitors of eryptosis include erythropoietin, nitric oxide, catecholamines and high concentrations of urea. ...
Primary polydipsia
... a carbonic anhydrase inhibitor Lithium was previously used for treatment of PPD as a direct competitive ADH agonist, but is now ... ACE Inhibitors, such as enalapril Clonidine, an alpha-2 adrenergic agonist Irbesartan, an angiotensin II receptor antagonist ...
Carbonic anhydrase
... inhibitor. ReferencesEdit. *^ Badger MR, Price GD (1994). "The role of carbonic anhydrase in photosynthesis ... The reaction catalyzed by carbonic anhydrase is: HCO3- + H+ ↽. −. ⇀. {\displaystyle {\ce {,=,,}}}. CO2 + H2O. Carbonic acid has ... Cadmium-containing carbonic anhydraseEdit. Marine diatoms have been found to express a new form of ζ carbonic anhydrase. T. ... Several forms of carbonic anhydrase occur in nature. In the best-studied α-carbonic anhydrase form present in animals, the zinc ...
Levobunolol
Carbonic anhydrase inhibitors/. (sulfonamides). *Acetazolamide. *Brinzolamide (+timolol). *Diclofenamide. *Dorzolamide (+ ... It can also cause severe hypertension (high blood pressure) when combined with sympathomimetic drugs or MAO-A inhibitors, ... Combination with MAO-A inhibitors is also contraindicated because it could cause a dangerous rise in blood pressure.[1] ...
Aqueous humour
Fluid production can be decreased by beta blockers, alpha2-agonists, and carbonic anhydrase inhibitors.[7] ... an enzyme inhibited by 5-alpha reductase inhibitors, may be involved in production of aqueous humour.[4] ...
Thiazide
... or direct vasodilator actions either through inhibition of carbonic anhydrase or by desensitizing the vascular smooth muscle ... Therefore, ACE inhibitor and thiazide combination is used to prevent hypokalemia. Hyperglycemia Hyperlipidemia Hyperuricemia - ... Thiazides have also been replaced by angiotensin converting enzyme (ACE) inhibitors in Australia due to their propensity to ...
Biomineralization
Carbonic anhydrase serves a role in mineralization in sponges, as well as metazoans, implying an ancestral role.[44] Far from ... inhibitors, and transcription factors - many elements of this 'toolkit' are shared between phyla as diverse as corals, molluscs ... "Sponge paleogenomics reveals an ancient role for carbonic anhydrase in skeletogenesis". Science. 316 (5833): 1893-1895. Bibcode ...
COX-2 inhibitor
... of NSAID expenditures were for COX-2 inhibitors. Over the period of the study, COX-2 inhibitors rose from 10.03% of total ... "COX-2 Inhibitors and Cancer". Fact Sheet. United States National Cancer Institute. Archived from the original on May 9, 2008.. ... COX-2 inhibitors appear to work as well as nonselective NSAIDS.[5] They have not been compared to other treatment options such ... COX-2 inhibitors and cardiovascular risk". Science. 336 (6087): 1386-7. Bibcode:2012Sci...336.1386C. doi:10.1126/science. ...
Drug design
... example of the application of structure-based drug design leading to an approved drug is the carbonic anhydrase inhibitor ... Another important case study in rational drug design is imatinib, a tyrosine kinase inhibitor designed specifically for the bcr ... Small molecules (for example receptor agonists, antagonists, inverse agonists, or modulators; enzyme activators or inhibitors; ... "AutoDock's role in Developing the First Clinically-Approved HIV Integrase Inhibitor". Press Release. The Scripps Research ...
Atropine
Carbonic anhydrase inhibitors/. (sulfonamides). *Acetazolamide. *Brinzolamide (+timolol, +brimonidine). *Diclofenamide. * ... Also indirect D2 agonists, such as dopamine reuptake inhibitors (cocaine, methylphenidate), releasing agents (amphetamine, ...
Enzyme promiscuity
... and human carbonic anhydrase II (CAII)) has shown the main activity is "robust" towards change, whereas the promiscuous ...
5α-Reductase inhibitor
Neurosteroidogenesis inhibitor. References[edit]. *^ a b Ulrike Blume-Peytavi; David A. Whiting; Ralph M. Trüeb (26 June 2008 ... 5α-Reductase inhibitors (5-ARIs), also known as dihydrotestosterone (DHT) blockers, are a class of medications with ... Lee JY, Cho KS (May 2018). "Effects of 5-alpha reductase inhibitors: new insights on benefits and harms". Curr Opin Urol. 28 (3 ... Liu, L; Zhao, S; Li, F; Li, E; Kang, R; Luo, L; Luo, J; Wan, S; Zhao, Z (September 2016). "Effect of 5α-Reductase Inhibitors on ...
Diffusion limited enzyme
In 1972, it was observed that in the dehydration of H2CO3 catalyzed by carbonic anhydrase, the second-order rate constant ... "H2CO3 as Substrate for Carbonic Anhydrase in the Dehydration of HCO3−". Proceedings of the National Academy of Sciences of the ...
Carbachol
Carbonic anhydrase inhibitors/. (sulfonamides). *Acetazolamide. *Brinzolamide (+timolol). *Diclofenamide. *Dorzolamide (+ ...
Ketogenic diet
A class of anticonvulsants known as carbonic anhydrase inhibitors (topiramate, zonisamide) are known to increase the risk of ...
Ribonuclease inhibitor
Guanidinium thiocyanate - a chemical RNase inhibitor.. References[edit]. *^ a b PDB: 2BNH; Kobe B, Deisenhofer J (1993). " ... Ribonuclease inhibitor (RI) is a large (~450 residues, ~49 kDa), acidic (pI ~4.7), leucine-rich repeat protein that forms ... Top view of porcine ribonuclease inhibitor, showing its horseshoe shape.[1] The outer layer is composed of α-helices and the ... Shapiro R (2001). "Cytoplasmic ribonuclease inhibitor". Methods in Enzymology. 341: 611-28. doi:10.1016/S0076-6879(01)41180-3. ...
5α-Reductase inhibitor
Neurosteroidogenesis inhibitor. References[edit]. *^ a b Ulrike Blume-Peytavi; David A. Whiting; Ralph M. Trüeb (26 June 2008 ... 5α-Reductase inhibitors (5-ARIs), also known as dihydrotestosterone (DHT) blockers, are a class of medications with ... Liu, L; Zhao, S; Li, F; Li, E; Kang, R; Luo, L; Luo, J; Wan, S; Zhao, Z (September 2016). "Effect of 5α-Reductase Inhibitors on ... Trost L, Saitz TR, Hellstrom WJ (2013). "Side Effects of 5-Alpha Reductase Inhibitors: A Comprehensive Review". Sex Med Rev. 1 ...
Histidine
In carbonic anhydrases, a histidine proton shuttle is utilized to rapidly shuttle protons away from a zinc-bound water molecule ... See also: Receptor/signaling modulators • Monoamine metabolism modulators • Monoamine reuptake inhibitors. Wikimedia Commons ...
Bronchodilator
carbonic anhydrase (chloride shift). *oxyhemoglobin. *respiratory quotient. *arterial blood gas. *diffusion capacity (DLCO) ... ACE inhibitors. *Angiotensin II receptor antagonists. *Renin inhibitors. *Antihyperlipidemics *Statins. *Fibrates. *Bile acid ...
Cofactor (biochemistry)
... and even cadmium in the carbonic anhydrase from the marine diatom Thalassiosira weissflogii.[19][20] ... Mack M, Grill S (2006). "Riboflavin analogs and inhibitors of riboflavin biosynthesis". Appl. Microbiol. Biotechnol. 71 (3): ...
Avermitilol synthase
Carbonic anhydrase. *Fumarase. *Aconitase. *Enolase *Alpha. *Enolase 2. *Enoyl-CoA hydratase/3-Hydroxyacyl ACP dehydrase ...
Loop diuretic
... and carbonic anhydrase inhibitors (blockade of chloride-bicarbonate exchanger pendrin) has been suggested to complement the ... Loop diuretics may also precipitate kidney failure in patients concurrently taking an NSAID and an ACE inhibitor-the so-called ... Thomas MC (February 2000). "Diuretics, ACE inhibitors and NSAIDs--the triple whammy". Med. J. Aust. 172 (4): 184-5. doi:10.5694 ...
Carbonic anhydrase inhibitor - Wikipedia
... are carbonic anhydrase inhibitors. Supuran CT, Scozzafava A, Conway J, eds. (2004). Carbonic anhydrase: its inhibitors and ... Carbonic anhydrase inhibitors are a class of pharmaceuticals that suppress the activity of carbonic anhydrase. Their clinical ... "Carbonic Anhydrase Inhibitors and High Altitude Illnesses". In Frost, Susan C.; McKenna, Robert (eds.). Carbonic Anhydrase: ... Carbonic anhydrase inhibitors are primarily used for the treatment of glaucoma. They may also be used to treat seizure disorder ...
RCSB PDB - 1BNQ: CARBONIC ANHYDRASE II INHIBITOR
Structural analysis of inhibitor binding to human carbonic anhydrase II.. Boriack-Sjodin, P.A., Zeitlin, S., Chen, H.H., ... X-ray crystal structures of carbonic anhydrase II (CAII) complexed with sulfonamide inhibitors illuminate the structural ... X-ray crystal structures of carbonic anhydrase II (CAII) complexed with sulfonamide inhibitors illuminate the structural ... the newest carbonic anhydrase inhibitor approved for the treatment of glaucoma.. Organizational Affiliation: Department of ...
RCSB PDB - 3NI5: Carbonic anhydrase inhibitor: C1 family
Carbonic anhydrase 2. A. 260. Homo sapiens. Mutation(s): 0 Gene Names: CA2. EC: 4.2.1.1. ... which have been investigated for the inhibition of five physiologically relevant human carbonic anhydrase (hCA, EC 4.2.1.1) ... which have been investigated for the inhibition of five physiologically relevant human carbonic a ... ... Carbonic anhydrase inhibitor: C1 family. *DOI: 10.2210/pdb3NI5/pdb. *Classification: Lyase/Lyase INHIBITOR ...
List of Carbonic anhydrase inhibitor anticonvulsants - Drugs.com
Compare carbonic anhydrase inhibitor anticonvulsants. View important safety information, ratings, user reviews, popularity and ... Carbonic anhydrase inhibitor anticonvulsants. What are Carbonic anhydrase inhibitor anticonvulsants. Carbonic anhydrase ... inhibitor anticonvulsants inhibit the enzyme carbonic anhydrase. Generally carbonic anhydrase inhibitors are used to treat ... Home › Drug Classes › Central Nervous System Agents › Anticonvulsants › Carbonic Anhydrase Inhibitor Anticonvulsants ...
Systemic carbonic anhydrase inhibitors - American Academy of Ophthalmology
Carbonic anhydrase inhibitors decrease aqueous production by inhibiting ion transport associated with the secretion of aqueous ... Carbonic anhydrase inhibitors decrease aqueous production by inhibiting ion transport associated with the secretion of aqueous ... Adequate inhibition of carbonic anhydrase with systemic administration has been shown to cause a decrease in aqueous humor ...
Intraocular Carbonic Anhydrase Inhibitor - Trip Database
Helping you find trustworthy answers on Intraocular Carbonic Anhydrase Inhibitor , Latest evidence made easy ... Find all the evidence you need on Intraocular Carbonic Anhydrase Inhibitor via the Trip Database. ... of Drugs Anti-Arrhythmia Agents Antihypertensive Agents Carbonic Anhydrase Inhibitors Enzyme Inhibitors (...) ) surgery the ... Angle-Closure Ocular Hypertension Eye Diseases Acetazolamide Anticonvulsants Carbonic Anhydrase Inhibitors Enzyme Inhibitors ...
Molecules | Free Full-Text | Phenols and Polyphenols as Carbonic Anhydrase Inhibitors
... such as the Carbonic Anhydrases (CAs, EC 4.2.1.1). CAs reversibly catalyze the fundamental reaction of CO2 hydration to ... Keywords: carbonic anhydrase inhibitors (CAIs); metalloenzymes; phenols; polyphenols; flavonoids carbonic anhydrase inhibitors ... Phenols and Polyphenols as Carbonic Anhydrase Inhibitors by Anastasia Karioti 1,*, Fabrizio Carta 2. and Claudiu T. Supuran 2,* ... Karioti, A.; Carta, F.; Supuran, C.T. Phenols and Polyphenols as Carbonic Anhydrase Inhibitors. Molecules 2016, 21, 1649. ...
Interactions between Excedrin Extra Strength Oral and aspirin-81-mg-salicylates-carbonic-anhydrase-inhibitors
WebMD provides information about interactions between Excedrin Extra Strength Oral and aspirin-81-mg-salicylates-carbonic- ... Carbonic Anhydrase Inhibitors/Aspirin (, 81 mg); Salicylates Interactions. This information is generalized and not intended as ... Metabolic acidosis induced by carbonic anhydrase inhibitors and salicylates in patients with normal renal function. Br Med J ( ... Toxicity of combined therapy with carbonic anhydrase inhibitors and aspirin. Am J Ophthalmol 1978 Oct; 86(4):516-9. ...
A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects. - PubMed - NCBI
A class of sulfonamide carbonic anhydrase inhibitors with neuropathic pain modulating effects.. Carta F1, Di Cesare Mannelli L2 ... A series of benzene sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitors which incorporate lipophilic 4-alkoxy- and 4- ... These derivatives were investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) of which multiple ... In a mice model of neuropathic pain induced by oxaliplatin, one of the strong CA II/VII inhibitors reported here induced a long ...
Carbonic Anhydrase as Drug Target - Thermodynamics and Structure of Inhibitor Binding | Daumantas Matulis | Springer
... with a particular focus on inhibitor binding for drug design. Illustrated with numerous X-ray crystallographic structures. ... deep insights into the thermodynamics and molecular structures of the twelve catalytically active isoforms of human carbonic ... Carbonic Anhydrase as Drug Target. Book Subtitle. Thermodynamics and Structure of Inhibitor Binding. Editors. * Daumantas ... Carbonic Anhydrase as Drug Target. Thermodynamics and Structure of Inhibitor Binding. Editors: Matulis, Daumantas (Ed.) ...
CARBONIC ANHYDRASE INHIBITORS | Pharmacological Reviews
Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions. - PubMed - NCBI
Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions.. Innocenti A1, Firnges MA, Antel ... The membrane-associated human isozyme of carbonic anhydrase, hCA IV, has been investigated for its interaction with anion ... Sulfate was a good hCA IV inhibitor (K(i) of 9 mM), although it is a much weaker inhibitor of isozymes I, II, V and IX. ... the best hCA IV inhibitor among the halides, are weak inhibitors of other isozymes, such as hCA I, II and V. The metal poisons ...
Carbonic Anhydrase Inhibitor (Oral Route, Parenteral Route) Description and Brand Names - Mayo Clinic
3D-QSAR study of benzene sulfonamide analogs as carbonic anhydrase II inhibitors
... studies were performed for a series of carbonic anhydrase inhibitors using comparative molecular field analysis (CoMFA) and ... 3D-QSAR study of benzene sulfonamide analogs as carbonic anhydrase II inhibitors Bioorg Med Chem Lett. 2010 May 15;20(10):3089- ... The large set of 37 different aromatic/heterocyclic sulfonamides carbonic anhydrase (CA, EC 4.2.1.1) inhibitors, such as CA II ... studies were performed for a series of carbonic anhydrase inhibitors using comparative molecular field analysis (CoMFA) and ...
Unilateral Glaucoma Medication: Beta-adrenergic blockers, Alpha 2-adrenergic agonists, Carbonic anhydrase inhibitors,...
Carbonic anhydrase inhibitors. Class Summary. Enzyme found in many tissues of the body, including the eye. Catalyzes a ... Medications used to decrease aqueous production include beta-blockers (topical), carbonic anhydrase inhibitors (topical and/or ... Cultured Cells and Inhibitor May Restore Cornea in Patients with Bullous Keratopathy ... Catalyzes reversible reaction involving hydration of carbon dioxide and dehydration of carbonic acid. May use concomitantly ...
Azobenzene-based inhibitors of human carbonic anhydrase II
... In: Beilstein Journal of Organic Chemistry, Vol. 11: pp. 1129-1135 ... Aryl sulfonamides are a widely used drug class for the inhibition of carbonic anhydrases. In the context of our program of ... interested in the exploration of azobenzene-containing sulfonamides to block the catalytic activity of human carbonic anhydrase ...
Saccharin Sulfonamides as Inhibitors of Carbonic Anhydrases I, II, VII, XII, and XIII
W. S. Sly and P. Y. Hu, "Human carbonic anhydrases and carbonic anhydrase deficiencies," Annual Review of Biochemistry, vol. 64 ... Saccharin Sulfonamides as Inhibitors of Carbonic Anhydrases I, II, VII, XII, and XIII. Vaida Morkūnaitė,1 Lina Baranauskienė,1 ... C. T. Supuran, "Carbonic anhydrases: novel therapeutic applications for inhibitors and activators," Nature Reviews Drug ... Sulfonamides are the most investigated inhibitors of carbonic anhydrases. Primary SO2NH2 group binds to zinc atom in the active ...
Carbonic anhydrase inhibitor legal definition of Carbonic anhydrase inhibitor
What is Carbonic anhydrase inhibitor? Meaning of Carbonic anhydrase inhibitor as a legal term. What does Carbonic anhydrase ... Definition of Carbonic anhydrase inhibitor in the Legal Dictionary - by Free online English dictionary and encyclopedia. ... Carbonic anhydrase inhibitor legal definition of Carbonic anhydrase inhibitor https://legal-dictionary.thefreedictionary.com/ ... inhibitor. (redirected from Carbonic anhydrase inhibitor). Also found in: Dictionary, Thesaurus, Medical, Acronyms, ...
Which medications in the drug class Antiglaucoma, Carbonic Anhydrase Inhibitors are used in the treatment of Sturge-Weber...
Dorzolamide inhibits carbonic anhydrase in the ciliary processes, which decrease... more ... Carbonic Anhydrase InhibitorsThese agents lower IOP by decreasing aqueous production.Dorzolamide (Trusopt) ... Which medications in the drug class Antiglaucoma, Carbonic Anhydrase Inhibitors are used in the treatment of Sturge-Weber ... Antiglaucoma, Carbonic Anhydrase Inhibitors. These agents lower IOP by decreasing aqueous production. ...
Juvenile Glaucoma Medication: Prostaglandin Agonists, Antiglaucoma, Beta-Blockers, Alpha Agonists, Ophthalmic, Antiglaucoma,...
Antiglaucoma, Carbonic Anhydrase Inhibitors. Class Summary. By slowing the formation of bicarbonate ions, causing a reduction ... Dorzolamide is a carbonic anhydrase inhibitor that decreases aqueous humor secretion, causing a decrease in IOP. This agent ... Oral carbonic anhydrase inhibitors have significant adverse effects, including tiredness, malaise, and anorexia. Because of an ... Oral carbonic anhydrase inhibitors have significant adverse effects, including tiredness, malaise, and anorexia. Because of an ...
Novel Carborane Based Inhibitors of Carbonic Anhydrase IX » Linkos.cz
CAIX is a transmembrane isoform of carbonic anhydrase with an extracellular-facing catalytic site and therefore is well ... inhibitors. The aim of this study is to evaluate the effect of new carboranes with functional sulfonamide residues on CAIX ... Introduction Carborane-based compounds have emerged as promising lead structures for the development of carbonic anhydrase (CA ... Novel Carborane Based Inhibitors of Carbonic Anhydrase IX. Konference: 2015 XI. Dny diagnostické, prediktivní a experimentální ...
Intrinsic thermodynamics of sulfonamide inhibitor binding to human carbonic anhydrases I and II. | Sigma-Aldrich
Intrinsic thermodynamics of sulfonamide inhibitor binding to human carbonic anhydrases I and II.. [Vaida Morkūnaitė, Joana ... Carbonic Anhydrase Isozyme II human, ≥80%, powder, ≥3,000 W-A units/mg protein pricing ... Human carbonic anhydrase (CA) I and II are cytosolic proteins, where their expression disorders can cause diseases such as ... There are numerous inhibitors that target these isozymes, but it is difficult to design compounds that could bind to one of ...
Carbonic anhydrase inhibitor d's | definition of carbonic anhydrase inhibitor d's by Medical dictionary
... carbonic anhydrase inhibitor ds explanation free. What is carbonic anhydrase inhibitor ds? Meaning of carbonic anhydrase ... inhibitor ds medical term. What does carbonic anhydrase inhibitor ds mean? ... Looking for online definition of carbonic anhydrase inhibitor ds in the Medical Dictionary? ... carbonic anhydrase inhibitor ds. inhibit carbonic anhydrase activity and inhibit ion exchange mechanisms especially that of ...
Leki refundowane - Cena i zamienniki leku carbonic anhydrase inhibitor Oral, Parenteral
Enhanced Ocular Bioavailability Of Carbonic Anhydrase Inhibitor Formulation With Novel Nanopolymers | IOVS | ARVO Journals
Enhanced Ocular Bioavailability Of Carbonic Anhydrase Inhibitor Formulation With Novel Nanopolymers You will receive an email ... Tapan Shah, Jun Inoue; Enhanced Ocular Bioavailability Of Carbonic Anhydrase Inhibitor Formulation With Novel Nanopolymers. ... of this paper is to present a novel ophthalmic composition comprising a hyperbranched polymer with carbonic anhydrase inhibitor ...
Inhibition of Human Aquaporin-1 Water Channel Activity by Carbonic Anhydrase Inhibitors | IOVS | ARVO Journals
Conclusions:: Water permeability of AQP1 cRNA injected oocytes was inhibited by three different carbonic anhydrase inhibitors. ... Inhibition of Human Aquaporin-1 Water Channel Activity by Carbonic Anhydrase Inhibitors ... Inhibition of Human Aquaporin-1 Water Channel Activity by Carbonic Anhydrase Inhibitors ... a carbonic anhydrase (CA) inhibitor, inhibits AQP1 activity. The purpose of this study was to determine if the effect of ...
PRIME PubMed | 4-Functionalized 1,3-diarylpyrazoles bearing 6-aminosulfonylbenzothiazole moiety as potent inhibitors of...
3-diarylpyrazoles bearing 6-aminosulfonylbenzothiazole moiety as potent inhibitors of carbonic anhydrase isoforms hCA I, II, IX ... BenzothiazolesCarbonic Anhydrase ICarbonic Anhydrase IICarbonic Anhydrase IXCarbonic Anhydrase InhibitorsCarbonic Anhydrases ... selective inhibitors of the tumor-associated carbonic anhydrases IX and XII.. *Carbonic anhydrase inhibitors. Inhibition of the ... Inhibition of carbonic anhydrase isoforms I, II, IX and XII with novel Schiff bases: identification of selective inhibitors for ...
A Patients Guide to Glaucoma: Section 7-C-4: Carbonic Anhydrase Inhibitors (CAIs)
Section 7-C-4: Carbonic Anhydrase Inhibitors (CAIs) The topical CAIs include dorzolamide (Trusopt) and brinzolamide (Azopt). ... Combination beta-blocker and carbonic anhydrase inhibitor: timolol maleate/dorzolamide hydrochloride (Cosopt, Merck Co., ... The CAIs inhibit the enzyme carbonic anhydrase, which in turn, reduces aqueous humor formation. Patients are typically placed ...
Phenolic Compounds as Antioxidants: Carbonic Anhydrase Isoenzymes Inhibitors | Bentham Science
Phenolic Compounds as Antioxidants: Carbonic Anhydrase Isoenzymes Inhibitors. Author(s): Ilhami Gulcin, Sukru Beydemir Ataturk ... Ilhami Gulcin and Sukru Beydemir, "Phenolic Compounds as Antioxidants: Carbonic Anhydrase Isoenzymes Inhibitors", Mini-Reviews ... Carbonic anhydrase (EC 4.2.1.1., CA) is a pH regulatory/metabolic enzyme in all life kingdoms, being found in organisms all ... Carbonic anhydrase (EC 4.2.1.1., CA) is a pH regulatory/metabolic enzyme in all life kingdoms, being found in organisms all ...
THE ANTICONVULSANT ACTION OF CARBON DIOXIDE: INTERACTION WITH RESERPINE AND INHIBITORS OF CARBONIC ANHYDRASE | Journal of...
THE ANTICONVULSANT ACTION OF CARBON DIOXIDE: INTERACTION WITH RESERPINE AND INHIBITORS OF CARBONIC ANHYDRASE. WILLIAM D. GRAY ... THE ANTICONVULSANT ACTION OF CARBON DIOXIDE: INTERACTION WITH RESERPINE AND INHIBITORS OF CARBONIC ANHYDRASE. WILLIAM D. GRAY ... THE ANTICONVULSANT ACTION OF CARBON DIOXIDE: INTERACTION WITH RESERPINE AND INHIBITORS OF CARBONIC ANHYDRASE. WILLIAM D. GRAY ... The results support the belief that the anticonvulsant action of carbonic anhydrase inhibitors is mediated by disequilibrium of ...
AcetazolamideDorzolamideEnzymeCAIsIsoenzymesCarbon dioxideBeta-blockersDiureticsIntraocular pressureActivity of carbonicBrinzolamideMethazolamideDrug that weakly inhibits carbonic anhydraseSulfonamidesAntiglaucomaTopical carbonicTopiramateCompoundsPotent inhibitorsBicarbonateHydrationRenalInhibition of carbonic anhydraseDefinition of carbonicCAIXInhibitTreatment of glaucomaAnticonvulsantsMammalian carbonic anhydraseOphthalmicDrugsDecrease aqueous productionCrystallographyDiureticIsozymeHumanIsozymesAbstractSulfonamide CA inhibitorsCAIIOralBenzeneAcidDerivatives
Acetazolamide17
- Müller cells have bicarbonate-related transport mechanisms that control movement of potassium and sodium ions (and thus fluid), partly explaining the role for carbonic anhydrase inhibitors such as acetazolamide in the treatment of cystoid macular edema. (tripdatabase.com)
- 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)
- Earlier reports have claimed that acetazolamide, a carbonic anhydrase (CA) inhibitor, inhibits AQP1 activity. (arvojournals.org)
- The purpose of this study was to determine if the effect of acetazolamide was a compound-specific or other CA inhibitors have the same effect on AQP1 activity. (arvojournals.org)
- The Pf values for AQP1 cRNA injected oocytes in the presence of acetazolamide and two other CA inhibitors, AL-5733A and AL-6950 were 144 +/- 37 (p = 0.0143), 111 +/- 3 (p = 0.0015) and 83 +/- 12 (p = 0.0006), respectively. (arvojournals.org)
- The inhibition of the tumor-associated transmembrane carbonic anhydrase IX (CA IX) isozyme has been investigated with a series of aromatic and heterocyclic sulfonamides, including the six clinically used derivatives acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide and brinzolamide. (nih.gov)
- Similarly to the clinically used drugs acetazolamide, methazolamide and topiramate, E7070 showed inhibition constants in the range of 15-31nM against isozymes I, II and IX, being slightly less effective as a CA IV inhibitor (K(i) of 65nM). (semanticscholar.org)
- The best Zn-Cam inhibitors were sulfamic acid and acetazolamide, with inhibition constants in the range of 63-96 nM, whereas other investigated aromatic/heterocylic sulfonamides showed a rather levelled behavior, with K I s in the range of 0.12-1.70 μM. (elsevier.com)
- Acetazolamide exerts its diuretic effect by inhi- bition of renal carbonic anhydrase (Maren. (kidneytreatment.site)
- infused acetazolamide (a CA inhibitor) in CA 11-deficient pa- tients. (kidneytreatment.site)
- Acetazolamide is a carbonic anhydrase inhibitor which can cause partial renal tubular acidosis and hypokalemia as a side effect. (kidneytreatment.site)
- Acetazolamide is a potent carbonic anhydrase inhibitor, effective in the control of fluid secretion, in the treatment of certain convulsive disorders and in the promotion of diuresis in instances of abnormal fluid retention. (pharmacycode.com)
- In contrast to acetazolamide and methazolamide, it is a very weak inhibitor of human CA isoenzyme I. Dorzolamide has been observed to be a very good ocular penetrator in rabbits following topical dosing. (elsevier.com)
- Acetazolamide belongs to a group of drugs called carbonic anhydrase inhibitors, which help to reduce amount of fluid in the eye and to reduce adverse symptoms when at high altitudes. (medicineshoppe.com)
- The effect of carbonic anhydrase inhibition with acetazolamide (Acz, 10 mg/kg) on the ventilatory response to an abrupt switch into hyperoxia (end-tidal PO2 = 450 Torr) and hypoxia (end-tidal PO2 = 50 Torr) was examined in five male subjects [30 +/- 3 (SE) yr]. (biomedsearch.com)
Dorzolamide8
- dorzolamide/timolol) Alpha agonist/ carbonic anhydrase inhibitor (eg, brimonidine/brinzolamide) Laser therapy Laser can be used as primary or adjunctive treatment. (tripdatabase.com)
- Dorzolamide is a sulfonamide and topical carbonic anhydrase II inhibitor. (wikipedia.org)
- Topical carbonic anhydrase inhibitors (dorzolamide, brinzolamide) are used as second-line therapy in the treatment of POAG. (thefreedictionary.com)
- Dorzolamide inhibits carbonic anhydrase in the ciliary processes, which decreases aqueous humor formation. (medscape.com)
- Dorzolamide is a reversible carbonic anhydrase inhibitor that may decrease aqueous humor secretion, causing a decrease in IOP. (medscape.com)
- Dorzolamide (TRUSOPT) and brinzolamide (AZOPT) both work by inhibiting carbonic anhydrase (isoenzyme II), which is found in the ciliary body epithelium . (eyewiki.org)
- Dorzolamide hydrochloride is a water-soluble potent inhibitor of human carbonic anhydrase (CA) isoenzymes II and IV. (elsevier.com)
- Dorzolamide is metabolized in the liver by N-deethylation and N- deethyldorzolamide is an inhibitor of CA isoenzymes I, II and IV. (elsevier.com)
Enzyme15
- Carbonic anhydrase inhibitor anticonvulsants inhibit the enzyme carbonic anhydrase. (drugs.com)
- X-ray crystallographic structures in combination with enzyme kinetic testing provide information on the interaction of CAs and their inhibitors, knowledge which is crucial for rational drug design. (springer.com)
- The membrane-associated human isozyme of carbonic anhydrase, hCA IV, has been investigated for its interaction with anion inhibitors, for the CO(2) hydration reaction catalyzed by this enzyme. (nih.gov)
- The CAIs inhibit the enzyme carbonic anhydrase, which in turn, reduces aqueous humor formation. (medrounds.org)
- Carbonic anhydrase inhibitors inhibit the enzyme carbonic anhydrase which is found in the proximal convoluted tubule. (wikipedia.org)
- Carbonic anhydrase (CAse) is an enzyme which catalyses the reversible reaction H2O + CO2 ←→ H2CO3. (pharmacy180.com)
- In support of Ray's views of CO2 as one of the main factors in mitochondrial biogenesis and health, and as such in a host of health conditions, this study found that carbonic anhydrase levels are higher and the enzyme itself is more active in both aging and degenerative conditions. (raypeatforum.com)
- Sitagliptin is an orally-active inhibitor of the dipeptidyl peptidase -4 (DPP-4) enzyme. (rxlist.com)
- Their results shown that the resection of enzyme-inhibitor is prevailed by the short-range van der Waals forces (7). (orientjchem.org)
- Carbonic anhydrase (CA) is a seemingly ubiquitous enzyme of profound physiological importance, which plays essential roles in respiration, acid-base homeostasis, bone resorption, calcification, photosynthesis, several biosynthetic pathways and a variety of processes involving ion, gas and fluid transfer. (springer.com)
- Since the early use of CA inhibitors as diuretics and in treating congestive heart failure, the enzyme has been target of considerable clinical attention. (springer.com)
- As a result, monophenyl indenoquinolines 16-18 may have promising anti-Alzheimer drug potential and 3,8-dibromoindenoquinoline amine (15f) can be novel hCA I and hCA II enzyme inhibitors. (cumhuriyet.edu.tr)
- Carbonic anhydrase inhibitors are pharmaceutical substances that repress the action of carbonic anhydrase , which is an enzyme that plays a major role in regulating pH and fluid levels in the human body. (visionaware.org)
- An anhydrase is defined as an enzyme that catalyzes the removal of a water molecule from a compound, and so it is this "reverse" reaction that gives carbonic anhydrase its name, because it removes a water molecule from carbonic acid. (wikipedia.org)
- Carbonic anhydrase (CA) is an enzyme which converts carbon dioxide (CO2) to bicarbonate and a proton (hydrogen ion. (rainbow.coop)
CAIs6
- Topical carbonic anhydrase inhibitors (CAI) took many years to develop - due to the poor side-effect profile of oral CAIs - but were an important addition to the treatment of POAG. (eyewiki.org)
- Blockade of carbonic anhydrase by CAIs in local tissues reduces the formation of bicarbonate ions, thus reducing fluid transport and IOP. (eyewiki.org)
- Carbonic anhydrase inhibitors (CAIs) reduce eye pressure by decreasing the production of intraocular fluid. (kidneytreatment.site)
- As such, a subset of these mercaptoquinazolin-4(3H)-one compounds represented interesting leads for developing new efficient and selective carbonic anhydrase inhibitors (CAIs) for the management of a variety of diseases including glaucoma , epilepsy , arthritis and cancer . (bvsalud.org)
- Carbonic Anhydrase Inhibitors (CAIs) have been used to lower intraocular pressure (IOP) for over 70 years. (new-glaucoma-treatments.com)
- Thus, carbonic anhydrase inhibitors (CAIs) are drugs that decrease pressure in the eye by reducing the amount of fluid produced by the eye itself. (visionaware.org)
Isoenzymes8
- It exists as a number of isoenzymes, the most active of which is carbonic anhydrase II (CA-II). (wikipedia.org)
- In addition, there are given some chemical and kinetic basis and technical details related to phenolic antioxidant compounds and carbonic anhydrase isoenzymes. (eurekaselect.com)
- Then the wild thought just came out of nowhere - what if thiamine was also a carbonic anhydrase inhibitor but at different isoenzymes and with different. (raypeatforum.com)
- Topiramate as an inhibitor of carbonic anhydrase isoenzymes. (kidneytreatment.site)
- 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)
- Novelty, in brief, is represented by the intended elaboration of carborane, heteroborane and metallaborane compounds as active-site inhibitors of CA isoenzymes. (imtm.cz)
Carbon dioxide9
- Catalyzes a reversible reaction where carbon dioxide becomes hydrated and carbonic acid dehydrated. (medscape.com)
- Catalyzes reversible reaction involving hydration of carbon dioxide and dehydration of carbonic acid. (medscape.com)
- Carbonic anhydrases (CAs) belong to the lyase family of enzymes and catalyze the reversible reaction of carbon dioxide hydration to bicarbonate ion and proton. (hindawi.com)
- Chemically, carbonic anhydrase catalyzes carbon dioxide (CO2) hydration and conversion to carbonic acid (H2CO3), which freely dissociates into bicarbonate anions and protons. (eyewiki.org)
- dissociation of carbonic acid into water and carbon dioxide in the proximal. (kidneytreatment.site)
- The carbonic anhydrases (CA) form a family of enzymes that catalyze the rapid interconversion of carbon dioxide and water to bicarbonate and protons (or vice versa), a reversible reaction that occurs relatively slowly in the absence of a catalyst. (orientjchem.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 carbonic anhydrases (or carbonate dehydratases ) form a family of enzymes that catalyze the interconversion between carbon dioxide and water and the dissociated ions of carbonic acid (i.e. bicarbonate and hydrogen ions ). (wikipedia.org)
- In the lungs carbonic anhydrase converts bicarbonate to carbon dioxide, suited for exhalation. (wikipedia.org)
Beta-blockers4
- Medications used to decrease aqueous production include beta-blockers (topical), carbonic anhydrase inhibitors (topical and/or oral), and alpha 2-agonists. (medscape.com)
- Many current treatments to lower intraocular pressure (IOP) associated with glaucoma -- beta blockers and carbonic anhydrase inhibitors --work by suppressing the production or inflow of fluid (aqueous humor). (thefreedictionary.com)
- Glaucoma Pharmaceuticals Markets, forecasts the market and identifies key issues, trends, and competitive analysis for such products as: pilocarpine drugs, andrenergic agonists, beta blockers, carbonic anhydrase inhibitors (CAI) and prostaglandin analogues. (thefreedictionary.com)
- Carbonic anhydrase inhibitors typically have a weaker effect than beta blockers. (medscape.com)
Diuretics4
- citation needed] Some diuretics inhibit the activity of carbonic anhydrase in proximal convoluted tubules and prevent reabsorption of bicarbonates from renal tubules. (wikipedia.org)
- For the same degree of natriuresis CAse inhibitors cause the most marked kaliuresis compared to other diuretics. (pharmacy180.com)
- T50.2X4S is a billable diagnosis code used to specify a medical diagnosis of poisoning by carbonic-anhydrase inhibitors, benzothiadiazides and other diuretics, undetermined, sequela. (icdlist.com)
- T50.2X4S is a sequela code, includes a 7th character and should be used for complications that arise as a direct result of a condition like poisoning by carbonic-anhydrase inhibitors benzothiadiazides and other diuretics undetermined. (icdlist.com)
Intraocular pressure2
- citation needed] Brinzolamide (trade names Azopt, Alcon Laboratories, Inc, Befardin Fardi Medicals) is a carbonic anhydrase inhibitor used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension. (wikipedia.org)
- MK-417, a potent carbonic anhydrase inhibitor capable of reducing intraocular pressure after topical application, is currently under investigation for the treatment of glaucoma. (aspetjournals.org)
Activity of carbonic5
- Carbonic anhydrase inhibitors are a class of pharmaceuticals that suppress the activity of carbonic anhydrase. (wikipedia.org)
- Darzi N, Morsali A, Beyramabadi S. A. Prediction of activity of carbonic anhydrase inhibitor drugs based on QSAR studies. (orientjchem.org)
- They investigated the effects of Balabanindexesin predicting activity of carbonic anhydrase inhibitor (10).Also,Felegari,Quantum chemical calculations performed another research based on DFT method for evaluation of anticancer drugs Cyclophosphamide.The results of this work revealed that quantum parameters affecting anticancer activity (11). (orientjchem.org)
- Binary Logistic Regression (BLR) has been developed as non-linear models to establish quantitative structure- activity relationships (QSAR) between structural descriptors and biochemical activity of carbonic anhydrase inhibitors. (ac.ir)
- Appearance and Activity of Carbonic Anhydrase IX Is normally Connected with Metabolic Dysfunction in MDA-MB-231. (aksumuniversity.org)
Brinzolamide2
- Structure-activity relationships rationalize affinity trends observed during the development of brinzolamide (Azopt), the newest carbonic anhydrase inhibitor approved for the treatment of glaucoma. (rcsb.org)
- Topical carbonic anhydrase inhibitors (Brinzolamide) and alpha 2 agonists (Brimonidine) are common choices as additive medicines. (clinicaltrials.gov)
Methazolamide2
- Methazolamide is also a carbonic anhydrase inhibitor. (wikipedia.org)
- Methazolamide is topical carbonic anhydrase inhibitor. (pharmacycode.com)
Drug that weakly inhibits carbonic anhydrase1
- Zonisamide is another sulfur containing antiseizure drug that weakly inhibits carbonic anhydrase. (wikipedia.org)
Sulfonamides14
- These sulfonamides showed modest inhibition against the cytosolic isoform CA I, but were generally effective, low nanomolar CA II, VII, IX and XII inhibitors. (nih.gov)
- The large set of 37 different aromatic/heterocyclic sulfonamides carbonic anhydrase (CA, EC 4.2.1.1) inhibitors, such as CA II chosen for the present study. (nih.gov)
- Aryl sulfonamides are a widely used drug class for the inhibition of carbonic anhydrases. (uni-muenchen.de)
- In the context of our program of photochromic pharmacophores we were interested in the exploration of azobenzene-containing sulfonamides to block the catalytic activity of human carbonic anhydrase II (hCAII). (uni-muenchen.de)
- A series of modified saccharin sulfonamides have been designed as carbonic anhydrase (CA) inhibitors and synthesized. (hindawi.com)
- Heterocyclic sulfonamides are the most investigated CA inhibitors. (hindawi.com)
- Here, we describe the binding properties of saccharin sulfonamides [ 10 ] as CA inhibitors. (hindawi.com)
- The binding of four saccharin sulfonamides (including saccharin itself, chemical structures shown in Figure 1 ) to five isoforms of human recombinant catalytic domains of carbonic anhydrases (CAs) was determined by the fluorescent thermal shift assay (FTSA) and isothermal titration calorimetry (ITC). (hindawi.com)
- Several nanomolar (K(I)-s in the range of 14-50 nM) CA IX inhibitors have been detected, both among the aromatic (such as orthanilamide, homosulfonilamide, 4-carboxy-benzenesulfonamide, 1-naphthalenesulfonamide and 1,3-benzenedisulfonamide derivatives) as well as the heterocylic (such as 1,3,4-thiadizole-2-sulfonamide, etc.) sulfonamides examined. (nih.gov)
- A large number of new sulfonamides have been synthesized and assayed as possible inhibitors of CA isoforms involved in lipogenesis. (eurekaselect.com)
- A detailed inhibition study of carbonic anhydrases (CAs, EC 4.2.1.1) belonging to the β- and γ-families from Archaea with sulfonamides has been performed. (elsevier.com)
- Thus, the three CA families investigated up to now possess a very diverse affinity for sulfonamides, the inhibitors with important medicinal, and environmental applications. (elsevier.com)
- 2] Guzel O., Salman A., Supuran C.T., Synthesis of 2,4,6-Trimethylpyridinium Derivatives of 2- Hydrazinocarbonyl)-3-Aryl-1H-Indole-5-Sulfonamides Acting as Potent Inhibitors of the Tumor-Associated Isoform IX and XII, Bioorganic & Medicinal Chemistry Letters , 19 , p.2931 (2009). (ac.ir)
- o-Benzenedisulfonimido-sulfonamides are potent inhibitors of the tumor-associated carbonic anhydrase isoforms CA IX and CA XII. (bezmialem.edu.tr)
Antiglaucoma2
- Several aromatic/heterocyclic sulfonamide scaffolds have been used to synthesize compounds incorporating NO-donating moieties of the nitrate ester type, which have been investigated for the inhibition of five physiologically relevant human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms: hCA I (offtarget), II, IV and XII (antiglaucoma targets) and IX (antitumor target). (rcsb.org)
- Which medications in the drug class Antiglaucoma, Carbonic Anhydrase Inhibitors are used in the treatment of Sturge-Weber Syndrome? (medscape.com)
Topical carbonic1
- Topical carbonic anhydrase inhibitors MK-507 and sezolamide hydrochloride (previously known as MK-417) were compared in a double-masked, randomized, placebo-controlled study in 82 patients with bilateral primary openangle glaucoma or ocular hypertension. (nyu.edu)
Topiramate4
- The sulfur-containing antiseizure and antimigraine drug topiramate is a weak inhibitor of carbonic anhydrase, particularly subtypes II and IV. (wikipedia.org)
- It has been proved that topiramate also inhibits lipogenesis in adipocytes, similarly to other sulfonamide CA inhibitors investigated earlier. (eurekaselect.com)
- The best Co-Cam inhibitors were topiramate and p-aminoethyl-benzenesulfonamide, with K I s in the range of 0.12-0.13 μM, whereas the worst one was homosulfanilamide (K I of 8.50 μM). (elsevier.com)
- Risk factors for metformin-associated lactic acidosis include renal impairment, concomitant use of certain drugs (e.g., carbonic anhydrase inhibitors such as topiramate), age 65 years old or greater, having a radiological study with contrast, surgery and other procedures, hypoxic states (e.g., acute congestive heart failure), excessive alcohol intake, and hepatic impairment. (rxlist.com)
Compounds11
- The physical and chemical properties of phenolic compounds make these molecules versatile ligands, capable of interacting with a wide range of targets, such as the Carbonic Anhydrases (CAs, EC 4.2.1.1). (mdpi.com)
- Carborane-based compounds have emerged as promising lead structures for the development of carbonic anhydrase (CA) inhibitors. (linkos.cz)
- There are numerous inhibitors that target these isozymes, but it is difficult to design compounds that could bind to one of these proteins specifically. (sigmaaldrich.com)
- These three compounds share some features important for both CA and AQP1 inhibition suggesting that these inhibitors may play a role in IOP regulation partly by modulating water flow via AQP1 channel. (arvojournals.org)
- The phenolic compounds and acids had marked especially CA I and CA II inhibitory effects and might be used as leads for generating CA isoenzyme inhibitors. (eurekaselect.com)
- This class of compounds may lead to isoform-selective inhibitors targeting just one or few of the medicinally relevant CAs. (eurekaselect.com)
- In the case of Cab, the inhibitory power of these compounds varied to a much larger extent, with sulfamic acid and sulfamide showing millimolar affinities (K I s in the range of 44-103 mM), whereas the best inhibitor was ethoxzolamide, with a K I of 5.35 μM. (elsevier.com)
- Coordination Compounds of Chlorothiazide With Transition Metal Ions Behave as Strong Carbonic Anhydrase Inhibitors," Metal-Based Drugs , vol. 3, no. 2, pp. 79-83, 1996. (hindawi.com)
- Inhibitory action of newly synthesised 4-(2-(2-substituted-thio-4-oxoquinazolin-3(4H)-yl)ethyl)benzenesulfonamides compounds 2-13 against human carbonic anhydrase (CA, EC 4.2.1.1) (hCA) isoforms I, II, IX, and XII, was evaluated. (bvsalud.org)
- The beta-lactam compounds were tested as inhibitors of the CA isoenzyme activity. (comu.edu.tr)
- Carbonic Anhydrase Inhibitors in Natural Food Compounds. (rainbow.coop)
Potent inhibitors2
- TY - JOUR T1 - 4-Functionalized 1,3-diarylpyrazoles bearing 6-aminosulfonylbenzothiazole moiety as potent inhibitors of carbonic anhydrase isoforms hCA I, II, IX and XII. (unboundmedicine.com)
- CA II/IX potent inhibitors belonging to the sulfamate class are thus valuable clinical candidates with potential for development as antitumor agents with a multifactorial mechanism of action. (proteopedia.org)
Bicarbonate8
- 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)
- A more immediate treatment is carbonic anhydrase inhibitors, which prevent bicarbonate uptake in the kidney and help correct the alkalosis. (wikipedia.org)
- By slowing the formation of bicarbonate ions, causing a reduction in sodium and fluid transport, these agents may inhibit carbonic anhydrase in the ciliary processes of the eye. (medscape.com)
- Systemic absorption can affect carbonic anhydrase in the kidney, reducing hydrogen ion secretion at the renal tubule and increasing renal excretion of sodium, potassium bicarbonate, and water. (medscape.com)
- Aqueous humor secretion depends on the production of bicarbonate (HCO-3) from carbonic anhydrase II, an isoenzyme found in the non-pigmented ciliary body epithelium. (eyewiki.org)
- Carbonic anhydrase inhibitors reduce the body's uptake of bicarbonate ions and decrease salt absorption, which has the effect of lowering fluid levels in the body. (visionaware.org)
- Cancer cells utilize carbonic anhydrases (CAs) to maintain a balance between intracellular alkalization for their proliferation and extracellular acidification of tumor microenvironment for their invasiveness by catalyzing the reversible hydration of CO2 to bicarbonate (HCO 3 - ) and protons (H + ), serving their critical role in tumor progression [ 9 - 14 ]. (medsci.org)
- Carbonic acid has a pK a of around 6.36 (the exact value depends on the medium) so at pH 7 a small percentage of the bicarbonate is protonated. (wikipedia.org)
Hydration2
- Carbonic anhydrase catalyzes reversible hydration of. (kidneytreatment.site)
- Carbonic anhydrase catalyzes cyanamide hydration to urea: is it mimicking the physiological reaction? (proteopedia.org)
Renal5
- 1.Cowan RA, Hartnell GG, Lowdell CP, Baird IM, Leak AM. Metabolic acidosis induced by carbonic anhydrase inhibitors and salicylates in patients with normal renal function. (webmd.com)
- Carbonic anhydrase inhibitor suppresses invasion of renal cancer cells in vitro. (kidneytreatment.site)
- also known as osteopetrosis with renal tubular acidosis, carbonic anhydrase II deficiency syndrome, Guibaud-Vainsel syndrome or marble brain disease. (proteopedia.org)
- Carbonic anhydrase II deficiency syndrome (osteopetrosis with renal tubular acidosis and brain calcification): novel mutations in CA2 identified by direct sequencing expand the opportunity for genotype-phenotype correlation. (proteopedia.org)
- Carbonic Anhydrase IX Appearance in apparent Cell Renal Cell Carcinoma: An Immunohistochemical Research Evaluating 2 Antibodies. (aksumuniversity.org)
Inhibition of carbonic anhydrase1
- In rare cases, the inhibition of carbonic anhydrase may be strong enough to cause metabolic acidosis of clinical importance. (wikipedia.org)
Definition of carbonic1
- Looking for online definition of carbonic anhydrase inhibitor in the Medical. (kidneytreatment.site)
CAIX5
- CAIX is a transmembrane isoform of carbonic anhydrase with an extracellular-facing catalytic site and therefore is well positioned to act in the control of tumor pH, and is overexpressed in various solid tumors. (linkos.cz)
- In future, novel carboranes with functional sulfonamide residues may serve as selective inhibitors of CAIX, and potential drugs in anticancer treatment. (linkos.cz)
- 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)
- Carborane-based carbonic anhydrase inhibitors: insight into CAII/CAIX specificity from a high-resolution crystal structure, modeling, and quantum chemical calculations. (imtm.cz)
- PubMed] [15] Pastorekova S, Parkkila S, Parkkila A, Opavsky R, Zelnik V, Saarnio J, Pastorek J. Carbonic Anhydrase IX, MN/CAIX: Evaluation of Tummy Complementary DNA Series and Appearance in Individual and Rat Alimentary Tracts Gastroenterology. (aksumuniversity.org)
Inhibit1
- To explore the structure-activity relationship (SAR), their inhibition potentials to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase cyctosolic (hCA I and II) enzymes were determined. (cumhuriyet.edu.tr)
Treatment of glaucoma1
- Carbonic anhydrase inhibitors are primarily used for the treatment of glaucoma. (wikipedia.org)
Anticonvulsants1
- Zonisamide, brand name Zonegran, is in a class of medications called carbonic anhydrase inhibitor anticonvulsants. (healthcentral.com)
Mammalian carbonic anhydrase2
- The new antitumor sulfamate EMD 486019 was investigated for its interaction with twelve catalytically active mammalian carbonic anhydrase (CA, EC 4.2.1.1) isozymes, hCA I - XIV. (proteopedia.org)
- Interaction of the antitumor sulfamate EMD 486019 with twelve mammalian carbonic anhydrase isoforms: Kinetic and X-ray crystallographic studies. (proteopedia.org)
Ophthalmic1
- The purpose of this paper is to present a novel ophthalmic composition comprising a hyperbranched polymer with carbonic anhydrase inhibitor (CAI). (arvojournals.org)
Drugs1
- In between, Benzene sulphonamides important group of drugs that is capable of inhibiting carbonic anhydrase. (orientjchem.org)
Decrease aqueous production1
- Carbonic anhydrase inhibitors decrease aqueous production by inhibiting ion transport associated with the secretion of aqueous humor. (aao.org)
Crystallography1
- X-Ray Crystallography of Carbonic Anhydrase Inhibitors and Its Importance in Drug Design (Vincenzo Alterio, Anna Di Fiore, Katia D'Ambrosio, Claudiu T. (thefreedictionary.com)
Diuretic1
- Generally carbonic anhydrase inhibitors are used to treat epilepsy , glaucoma , mountain sickness, and is used as a diuretic. (drugs.com)
Isozyme6
- Carbonic anhydrase inhibitors: inhibition of the membrane-bound human isozyme IV with anions. (nih.gov)
- Because CA IX is a highly active isozyme predominantly expressed in tumor tissues with poor prognosis of disease progression, this finding is very promising for the potential design of CA IX-specific inhibitors with applications as anti-tumor agents. (nih.gov)
- Carbonic anhydrase inhibitors: E7070, a sulfonamide anticancer agent, potently inhibits cytosolic isozymes I and II, and transmembrane, tumor-associated isozyme IX. (semanticscholar.org)
- 1] Fiore A.D., Simone G.D., Menchise V., Pedone C., Supuran C.T., Carbonic Anhydrase Inhibitors: X-ray Crystal Structure of a Benzenesulfonamide Strong CA II and CA IX Inhibitor Bearing a Pentafluorophenylaminothioureido Tail in Complex with Isozyme II, Bioorganic & Medicinal Chemistry Letters, 15 , p.1937 (2005). (ac.ir)
- Crystal structure of the secretory isozyme of mammalian carbonic anhydrases CA VI: implications for biological assembly and inhibitor development. (ox.ac.uk)
- Immunohistochemistry of Carbonic Anhydrase Isozyme IX (MN/CA IX) in Individual Gut Reveals Polarized Appearance in Epithelial Cells with the best Proliferative Capability. (aksumuniversity.org)
Human15
- This book offers deep insights into the thermodynamics and molecular structures of the twelve catalytically active isoforms of human carbonic anhydrase (CA) with a particular focus on inhibitor binding for drug design. (springer.com)
- Intrinsic thermodynamics of sulfonamide inhibitor binding to human carbonic anhydrases I and II. (sigmaaldrich.com)
- Human carbonic anhydrase (CA) I and II are cytosolic proteins, where their expression disorders can cause diseases such as glaucoma, edema, epilepsy or cancer. (sigmaaldrich.com)
- Carbonic anhydrase gene family expression in normal human brain and GBM patient-derived xenografts. (jci.org)
- Photoswitchable: The activity of a dithienylethene-based human carbonic anhydrase inhibitor (hCAI) can be regulated using light. (uni-regensburg.de)
- Carbonic anhydrase II (gene name CA2), is one of fourteen forms of human α carbonic anhydrases. (kidneytreatment.site)
- provided the QSAR model that consisted of formula for binding constant of benzene sulphonamides as the human carbonic anhydrase (6). (orientjchem.org)
- Docking studies of sulphamate inhibitors of estrone sulphatase in human carbonic anhydrase II. (ox.ac.uk)
- We describe the docking of selected steroidal and non-steroidal estrone sulphatase inhibitors, including the Phase I clinical trial candidate 667COUMATE (6), into the active site of human carbonic anhydrase II (hCA II). (ox.ac.uk)
- Exploring structure-activity relationship of S-substituted 2-mercaptoquinazolin-4(3H)-one including 4-ethylbenzenesulfonamides as human carbonic anhydrase inhibitors. (bvsalud.org)
- Carbonic anhydrase II deficiency syndrome in a Belgian family is caused by a point mutation at an invariant histidine residue (107 His----Tyr): complete structure of the normal human CA II gene. (proteopedia.org)
- Molecular basis of human carbonic anhydrase II deficiency. (proteopedia.org)
- A new series of phthalazine substituted beta-lactam derivatives were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase (hCA I and II) were evaluated. (comu.edu.tr)
- Close-up rendering of active site of human carbonic anhydrase II, showing three histidine residues and a hydroxide group coordinating (dashed lines) the zinc ion at center. (wikipedia.org)
- Ribbon diagram of human carbonic anhydrase II. (wikipedia.org)
Isozymes2
- Sulfate was a good hCA IV inhibitor (K(i) of 9 mM), although it is a much weaker inhibitor of isozymes I, II, V and IX. (nih.gov)
- Diazenylbenzenesulfonamides are Potent and Selective Inhibitors of the Tumor-Associated Isozymes IX and XII over the Cytosolic Isoforms I and II, Bioorganic & Medicinal Chemistry , 17 , p. 7093 (2009). (ac.ir)
Abstract1
- ABSTRACT In this work, we performed a structure-based virtual screening against five carbonic anhydrase isoforms using, as a ligand library, natural components of Citrus. (raypeatforum.com)
Sulfonamide CA inhibitors1
- This is the first report of rationally designed sulfonamide CA inhibitors with pain effective modulating effects. (nih.gov)
CAII2
- X-ray crystal structures of carbonic anhydrase II (CAII) complexed with sulfonamide inhibitors illuminate the structural determinants of high affinity binding in the nanomolar regime. (rcsb.org)
- The regression analysis consequences indicated that the activities of the inhibiting carbonic anhydrase II (CAII) activity can be modeled excellently in multi parametric model (8). (orientjchem.org)
Oral3
- Erleada Erleada (apalutamide) is an oral androgen receptor inhibitor for the treatment of men with. (drugs.com)
- If additional medication is needed to control eye pressure, carbonic anhydrase inhibitors are also prescribed in oral, or pill, forms. (visionaware.org)
- If eyedrops are not effective enough, the doctor may prescribe an oral carbonic anhydrase inhibitor. (medicalnewstoday.com)
Benzene1
- A series of benzene sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitors which incorporate lipophilic 4-alkoxy- and 4-aryloxy moieties, together with several derivatives of ethoxzolamide and sulfanilamide are reported. (nih.gov)
Acid3
- Carboxylic acid 6e was found to be an excellent inhibitor of both hCA IX and XII, with Ki values of 2.8nM and 5.5nM, respectively. (unboundmedicine.com)
- Carbonic acid spontaneously ionizes H 2 CO 3 ←→H + +HCO¯ 3 (Fig. IX.2). (pharmacy180.com)
- For example, carbonic anhydrase produces acid in the stomach lining. (wikipedia.org)
Derivatives2
- These derivatives were investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) of which multiple isoforms are known, and some appear to be involved in pain. (nih.gov)
- On the other hand, these novel arylated indenoquinoline-based derivatives were effective inhibitors of the BChE, hCA I and II, BChE and AChE enzymes with K-i values in the range of 37 +/- 2.04 to 88640 +/- 1990nM for AChE, 120.94 +/- 37.06 to 1150.95 +/- 304.48nM for hCA I, 267.58 +/- 98.05 to 1568.16 +/- 438.67nM for hCA II, and 84 +/- 3.86 to 144120 +/- 2910nM for BChE. (cumhuriyet.edu.tr)