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Identification
NameChlorothiazide
Accession NumberDB00880  (APRD00721)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

A thiazide diuretic with actions and uses similar to those of hydrochlorothiazide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p812)

Structure
Thumb
Synonyms
6-Chloro-1,1-dioxo-1,2-dihydro-1lambda*6*-benzo[1,2,4]thiadiazine-7-sulfonic acid amide
6-chloro-7-Sulfamoyl-2H-1,2,4-benzothiadiazine 1,1-dioxide
Chlorothiazid
Chlorothiazide
Chlorothiazidum
Chlorthiazide
Clorotiazida
Mechlozid
Uroflux
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Chlorothiazide Sodiuminjection500 mg/1intravenousAkorn, Inc.2012-08-132016-04-05Us
Diurilsuspension250 mg/5mLoralSalix Pharmaceuticals, Inc.1962-02-152016-04-05Us
Sodium Diurilinjection.5 mg/18mLintravenousOak Pharmaceuticals, Inc. (Subsidiary of Akorn, Inc.)1958-10-032016-04-05Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Chlorothiazidetablet500 mg/1oralGolden State Medical Supply, Inc.2005-08-302016-04-05Us
Chlorothiazidetablet250 mg/1oralWest ward Pharmaceutical Corp2005-08-302016-04-23Us
Chlorothiazidetablet250 mg/1oralGolden State Medical Supply, Inc.2005-08-302016-04-05Us
Chlorothiazidetablet250 mg/1oralAvera Mc Kennan Hospital2015-03-012016-04-05Us
Chlorothiazidetablet500 mg/1oralMylan Pharmaceuticals Inc.1975-07-172016-04-23Us
Chlorothiazidetablet250 mg/1oralMylan Pharmaceuticals Inc.1975-06-262016-04-23Us
Chlorothiazideinjection, powder, lyophilized, for solution500 mg/18mLintravenousFresenius Kabi USA, LLC2009-10-212016-04-05Us
Chlorothiazidetablet500 mg/1oralWest ward Pharmaceutical Corp2005-08-302016-04-23Us
Chlorothiazide Sodiuminjection, powder, lyophilized, for solution500 mg/18mLintravenousSun Pharma Global FZE2011-08-052016-04-05Us
Chlorothiazide Sodiuminjection, powder, lyophilized, for solution500 mg/18mLintravenousSagent Pharmaceuticals2015-10-122016-04-05Us
Chlorothiazide Sodiuminjection, powder, lyophilized, for solution500 mg/18mLintravenousAmerican Regent, Inc.2015-04-012016-04-23Us
Chlorothiazide Sodiuminjection, powder, lyophilized, for solution500 mg/18mLintravenousMylan Institutional LLC2014-08-082016-04-05Us
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
Supres 150 TabMerck Frosst Canada & Cie, Merck Frosst Canada & Co.
Supres 250 TabMerck Frosst Canada & Cie, Merck Frosst Canada & Co.
Salts
Name/CASStructureProperties
Chlorothiazide Sodium
ThumbNot applicableDBSALT000926
Categories
UNII77W477J15H
CAS number58-94-6
WeightAverage: 295.723
Monoisotopic: 294.948824782
Chemical FormulaC7H6ClN3O4S2
InChI KeyInChIKey=JBMKAUGHUNFTOL-UHFFFAOYSA-N
InChI
InChI=1S/C7H6ClN3O4S2/c8-4-1-5-7(2-6(4)16(9,12)13)17(14,15)11-3-10-5/h1-3H,(H,10,11)(H2,9,12,13)
IUPAC Name
6-chloro-1,1-dioxo-4H-1λ⁶,2,4-benzothiadiazine-7-sulfonamide
SMILES
NS(=O)(=O)C1=C(Cl)C=C2NC=NS(=O)(=O)C2=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzothiadiazines. These are organic compounds containing a benzene fused to a thiadiazine ring (a six-member ring with two nitrogen atoms and a sulfur atom).
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassThiadiazines
Sub ClassBenzothiadiazines
Direct ParentBenzothiadiazines
Alternative Parents
Substituents
  • Benzothiadiazine
  • Benzenesulfonamide
  • Chlorobenzene
  • Benzenoid
  • Aryl halide
  • Aryl chloride
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Azacycle
  • Amidine
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationChlorothiazide is indicated as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. It is also indicated in the management of hypertension either as the sole therapeutic agent or to enhance the effectiveness of other antihypertensive drugs in the more severe forms of hypertension.
PharmacodynamicsLike other thiazides, chlorothiazide promotes water loss from the body (diuretics). It inhibits Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue. Chlorothiazide affects the distal renal tubular mechanism of electrolyte reabsorption. At maximal therapeutic dosages, all thiazides are approximately equal in their diuretic efficacy. Chlorothiazide increases excretion of sodium and chloride in approximately equivalent amounts. Natriuresis may be accompanied by some loss of potassium and bicarbonate. After oral doses, 10-15 percent of the dose is excreted unchanged in the urine. Chlorothiazide crosses the placental but not the blood-brain barrier and is excreted in breast milk.
Mechanism of actionAs a diuretic, chlorothiazide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like chlorothiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of chlorothiazide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle.
Related Articles
AbsorptionRapidly absorbed following oral administration.
Volume of distributionNot Available
Protein bindingApproximately 40% bound to plasma proteins.
Metabolism

Chlorothiazide is not metabolized but is eliminated rapidly by the kidney.

Route of eliminationChlorothiazide is not metabolized but is eliminated rapidly by the kidney. After oral doses, 10 to 15 percent of the dose is excreted unchanged in the urine. Chlorothiazide crosses the placental but not the blood-brain barrier and is excreted in breast milk.
Half life45-120 minutes
ClearanceNot Available
ToxicityOral, rat LD50: > 10 g/kg. Signs of overdose include those caused by electrolyte depletion (hypokalemia, hypochloremia, hyponatremia) and dehydration resulting from excessive diuresis. If digitalis has also been administered hypokalemia may accentuate cardiac arrhythmias.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Chlorothiazide Action PathwayDrug actionSMP00078
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9119
Blood Brain Barrier-0.9506
Caco-2 permeable-0.7368
P-glycoprotein substrateNon-substrate0.706
P-glycoprotein inhibitor INon-inhibitor0.8482
P-glycoprotein inhibitor IINon-inhibitor0.8381
Renal organic cation transporterNon-inhibitor0.8177
CYP450 2C9 substrateNon-substrate0.755
CYP450 2D6 substrateNon-substrate0.8379
CYP450 3A4 substrateNon-substrate0.6308
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.923
CYP450 2C19 inhibitorNon-inhibitor0.9382
CYP450 3A4 inhibitorNon-inhibitor0.8901
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8658
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.7792
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.5023 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9654
hERG inhibition (predictor II)Non-inhibitor0.9352
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Salix pharmaceuticals inc
  • Abc holding corp
  • Lederle laboratories div american cyanamid co
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Watson laboratories inc
  • West ward pharmaceutical corp
  • Lundbeck inc
  • App pharmaceuticals llc
Packagers
Dosage forms
FormRouteStrength
Tabletoral250 mg/1
Tabletoral500 mg/1
Injectionintravenous500 mg/1
Injection, powder, lyophilized, for solutionintravenous500 mg/18mL
Suspensionoral250 mg/5mL
Injectionintravenous.5 mg/18mL
Tabletoral
Prices
Unit descriptionCostUnit
Diuril sodium 500 mg vial519.62USD vial
Chlorothiazide sod 500 mg vial357.24USD vial
Microzide 12.5 mg capsule0.95USD capsule
Aldoclor 250-250 mg tablet0.67USD tablet
Chlorothiazide 500 mg tablet0.36USD tablet
Chlorothiazide 250 mg tablet0.28USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point342.5-343Novello, F.C.; US. Patent 2,809,194; October 8,1957; assigned to Merck & Co.,Inc. Hinkley, D.F.; US. Patent 2,937,169; May 17,1960; assigned to Merck & Co., Inc.
water solubility266 mg/L (at 30 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP-0.24HANSCH,C ET AL. (1995)
logS-3.05ADME Research, USCD
Caco2 permeability-6.72ADME Research, USCD
pKa6.85MERCK INDEX (1996)
Predicted Properties
PropertyValueSource
Water Solubility0.398 mg/mLALOGPS
logP0.41ALOGPS
logP-0.44ChemAxon
logS-2.9ALOGPS
pKa (Strongest Acidic)9.1ChemAxon
pKa (Strongest Basic)1.15ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area118.69 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity62.51 m3·mol-1ChemAxon
Polarizability24.55 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (10.1 KB)
SpectraNot Available
References
Synthesis Reference

Eugene S. Barabas, “Water soluble complex of a poly (vinyl lactam) and chlorothiazide and process for producing same.” U.S. Patent US4713238, issued December, 1985.

US4713238
General ReferencesNot Available
External Links
ATC CodesC03AA04C03AB04C03AH01
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (72.7 KB)
Interactions
Drug Interactions
Drug
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Chlorothiazide.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Chlorothiazide.
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Chlorothiazide.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Chlorothiazide.
AlfuzosinAlfuzosin may increase the hypotensive activities of Chlorothiazide.
AllopurinolThe risk of a hypersensitivity reaction to Allopurinol is increased when it is combined with Chlorothiazide.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Chlorothiazide.
AmifostineChlorothiazide may increase the hypotensive activities of Amifostine.
BrimonidineBrimonidine may increase the antihypertensive activities of Chlorothiazide.
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Chlorothiazide.
ButabarbitalButabarbital may increase the orthostatic hypotensive activities of Chlorothiazide.
ButethalButethal may increase the orthostatic hypotensive activities of Chlorothiazide.
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Chlorothiazide.
CaffeineThe risk or severity of adverse effects can be increased when Caffeine is combined with Chlorothiazide.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Chlorothiazide.
CarbamazepineThe risk or severity of adverse effects can be increased when Chlorothiazide is combined with Carbamazepine.
ChlorphenamineThe risk or severity of adverse effects can be increased when Chlorphenamine is combined with Chlorothiazide.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Chlorothiazide.
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Chlorothiazide.
ColesevelamColesevelam can cause a decrease in the absorption of Chlorothiazide resulting in a reduced serum concentration and potentially a decrease in efficacy.
CyclophosphamideThe risk or severity of adverse effects can be increased when Chlorothiazide is combined with Cyclophosphamide.
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Chlorothiazide.
DiazoxideThe risk or severity of adverse effects can be increased when Chlorothiazide is combined with Diazoxide.
DigoxinThe risk or severity of adverse effects can be increased when Chlorothiazide is combined with Digoxin.
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Chlorothiazide.
DihydrotachysterolChlorothiazide may increase the hypercalcemic activities of Dihydrotachysterol.
DofetilideChlorothiazide may increase the QTc-prolonging activities of Dofetilide.
DuloxetineChlorothiazide may increase the orthostatic hypotensive activities of Duloxetine.
EthanolEthanol may increase the orthostatic hypotensive activities of Chlorothiazide.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Chlorothiazide.
FludrocortisoneFludrocortisone may increase the hypokalemic activities of Chlorothiazide.
FlunisolideFlunisolide may increase the hypokalemic activities of Chlorothiazide.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Chlorothiazide.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Chlorothiazide.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Chlorothiazide.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Chlorothiazide.
HeptabarbitalHeptabarbital may increase the orthostatic hypotensive activities of Chlorothiazide.
HexobarbitalHexobarbital may increase the orthostatic hypotensive activities of Chlorothiazide.
HydrocodoneThe risk or severity of adverse effects can be increased when Hydrocodone is combined with Chlorothiazide.
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Chlorothiazide.
InfliximabThe therapeutic efficacy of Chlorothiazide can be decreased when used in combination with Infliximab.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Chlorothiazide.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Chlorothiazide.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Chlorothiazide.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Chlorothiazide.
Insulin HumanThe therapeutic efficacy of Insulin Regular can be decreased when used in combination with Chlorothiazide.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Chlorothiazide.
IvabradineChlorothiazide may increase the arrhythmogenic activities of Ivabradine.
LevodopaChlorothiazide may increase the orthostatic hypotensive activities of Levodopa.
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Chlorothiazide.
LicoriceLicorice may increase the hypokalemic activities of Chlorothiazide.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Chlorothiazide.
LithiumChlorothiazide may decrease the excretion rate of Lithium which could result in a lower serum level and potentially a reduction in efficacy.
MecamylamineThe risk or severity of adverse effects can be increased when Chlorothiazide is combined with Mecamylamine.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Chlorothiazide.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Chlorothiazide.
MethohexitalMethohexital may increase the orthostatic hypotensive activities of Chlorothiazide.
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Chlorothiazide.
MolsidomineMolsidomine may increase the hypotensive activities of Chlorothiazide.
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Chlorothiazide.
MoxonidineMoxonidine may increase the hypotensive activities of Chlorothiazide.
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Chlorothiazide.
NicorandilNicorandil may increase the hypotensive activities of Chlorothiazide.
ObinutuzumabChlorothiazide may increase the hypotensive activities of Obinutuzumab.
OrciprenalineOrciprenaline may increase the hypokalemic activities of Chlorothiazide.
OxcarbazepineThe risk or severity of adverse effects can be increased when Chlorothiazide is combined with Oxcarbazepine.
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Chlorothiazide.
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Chlorothiazide.
ParoxetineParoxetine may increase the activities of Chlorothiazide.
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Chlorothiazide.
PentobarbitalPentobarbital may increase the orthostatic hypotensive activities of Chlorothiazide.
PentoxifyllinePentoxifylline may increase the hypotensive activities of Chlorothiazide.
PerindoprilChlorothiazide may increase the hypotensive activities of Perindopril.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Chlorothiazide.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Chlorothiazide.
PorfimerChlorothiazide may increase the photosensitizing activities of Porfimer.
PrimidonePrimidone may increase the orthostatic hypotensive activities of Chlorothiazide.
ProcyclidineThe serum concentration of Chlorothiazide can be increased when it is combined with Procyclidine.
QuinineQuinine may increase the hypotensive activities of Chlorothiazide.
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Chlorothiazide.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Chlorothiazide.
RisperidoneChlorothiazide may increase the hypotensive activities of Risperidone.
RituximabChlorothiazide may increase the hypotensive activities of Rituximab.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Chlorothiazide.
SecobarbitalSecobarbital may increase the orthostatic hypotensive activities of Chlorothiazide.
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Chlorothiazide.
SulpirideThe risk or severity of adverse effects can be increased when Chlorothiazide is combined with Sulpiride.
TadalafilTadalafil may increase the antihypertensive activities of Chlorothiazide.
TapentadolThe risk or severity of adverse effects can be increased when Tapentadol is combined with Chlorothiazide.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Chlorothiazide.
TopiramateChlorothiazide may increase the hypokalemic activities of Topiramate.
ToremifeneChlorothiazide may increase the hypercalcemic activities of Toremifene.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Chlorothiazide.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Chlorothiazide.
TreprostinilTreprostinil may increase the hypotensive activities of Chlorothiazide.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Chlorothiazide.
VardenafilVardenafil may increase the antihypertensive activities of Chlorothiazide.
VerteporfinChlorothiazide may increase the photosensitizing activities of Verteporfin.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Chlorothiazide.
YohimbineYohimbine may decrease the antihypertensive activities of Chlorothiazide.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Key mediator of sodium and chloride reabsorption in this nephron segment, accounting for a significant fraction of renal sodium reabsorption.
Gene Name:
SLC12A3
Uniprot ID:
P55017
Molecular Weight:
113138.04 Da
References
  1. Thakker RV: Molecular pathology of renal chloride channels in Dent's disease and Bartter's syndrome. Exp Nephrol. 2000 Nov-Dec;8(6):351-60. [PubMed:11014932 ]
  2. Schmidt H, Kabesch M, Schwarz HP, Kiess W: Clinical, biochemical and molecular genetic data in five children with Gitelman's syndrome. Horm Metab Res. 2001 Jun;33(6):354-7. [PubMed:11456284 ]
  3. Wilson FH, Kahle KT, Sabath E, Lalioti MD, Rapson AK, Hoover RS, Hebert SC, Gamba G, Lifton RP: Molecular pathogenesis of inherited hypertension with hyperkalemia: the Na-Cl cotransporter is inhibited by wild-type but not mutant WNK4. Proc Natl Acad Sci U S A. 2003 Jan 21;100(2):680-4. Epub 2003 Jan 6. [PubMed:12515852 ]
  4. Maki N, Komatsuda A, Wakui H, Ohtani H, Kigawa A, Aiba N, Hamai K, Motegi M, Yamaguchi A, Imai H, Sawada K: Four novel mutations in the thiazide-sensitive Na-Cl co-transporter gene in Japanese patients with Gitelman's syndrome. Nephrol Dial Transplant. 2004 Jul;19(7):1761-6. Epub 2004 Apr 6. [PubMed:15069170 ]
  5. Reinalter SC, Jeck N, Peters M, Seyberth HW: Pharmacotyping of hypokalaemic salt-losing tubular disorders. Acta Physiol Scand. 2004 Aug;181(4):513-21. [PubMed:15283765 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Reversible hydration of carbon dioxide. Can hydrates cyanamide to urea.
Gene Name:
CA1
Uniprot ID:
P00915
Molecular Weight:
28870.0 Da
References
  1. Puscas I, Coltau M, Baican M, Domuta G, Hecht A: Vasodilatory effect of diuretics is dependent on inhibition of vascular smooth muscle carbonic anhydrase by a direct mechanism of action. Drugs Exp Clin Res. 1999;25(6):271-9. [PubMed:10713865 ]
  2. Puscas I, Coltau M, Baican M, Pasca R, Domuta G: The inhibitory effect of diuretics on carbonic anhydrases. Res Commun Mol Pathol Pharmacol. 1999;105(3):213-36. [PubMed:10954127 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Essential for bone resorption and osteoclast differentiation (By similarity). Reversible hydration of carbon dioxide. Can hydrate cyanamide to urea. Involved in the regulation of fluid secretion into the anterior chamber of the eye. Contributes to intracellular pH regulation in the duodenal upper villous epithelium during proton-coupled peptide absorption. Stimulates the chloride-bicarbonate ex...
Gene Name:
CA2
Uniprot ID:
P00918
Molecular Weight:
29245.895 Da
References
  1. Weiner ID, Verlander JW: Renal and hepatic expression of the ammonium transporter proteins, Rh B Glycoprotein and Rh C Glycoprotein. Acta Physiol Scand. 2003 Dec;179(4):331-8. [PubMed:14656370 ]
  2. Puscas I, Coltau M, Baican M, Pasca R, Domuta G: The inhibitory effect of diuretics on carbonic anhydrases. Res Commun Mol Pathol Pharmacol. 1999;105(3):213-36. [PubMed:10954127 ]
  3. Verlander JW, Miller RT, Frank AE, Royaux IE, Kim YH, Weiner ID: Localization of the ammonium transporter proteins RhBG and RhCG in mouse kidney. Am J Physiol Renal Physiol. 2003 Feb;284(2):F323-37. Epub 2002 Oct 8. [PubMed:12388412 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Reversible hydration of carbon dioxide. May stimulate the sodium/bicarbonate transporter activity of SLC4A4 that acts in pH homeostasis. It is essential for acid overload removal from the retina and retina epithelium, and acid release in the choriocapillaris in the choroid.
Gene Name:
CA4
Uniprot ID:
P22748
Molecular Weight:
35032.075 Da
References
  1. Puscas I, Coltau M, Baican M, Domuta G, Hecht A: Vasodilatory effect of diuretics is dependent on inhibition of vascular smooth muscle carbonic anhydrase by a direct mechanism of action. Drugs Exp Clin Res. 1999;25(6):271-9. [PubMed:10713865 ]
  2. Puscas I, Coltau M, Baican M, Pasca R, Domuta G: The inhibitory effect of diuretics on carbonic anhydrases. Res Commun Mol Pathol Pharmacol. 1999;105(3):213-36. [PubMed:10954127 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS) (By similarity). Mediates the sodium-in...
Gene Name:
SLC22A6
Uniprot ID:
Q4U2R8
Molecular Weight:
61815.78 Da
References
  1. Uwai Y, Saito H, Hashimoto Y, Inui KI: Interaction and transport of thiazide diuretics, loop diuretics, and acetazolamide via rat renal organic anion transporter rOAT1. J Pharmacol Exp Ther. 2000 Oct;295(1):261-5. [PubMed:10991988 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:12