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Identification
NameTolmetin
Accession NumberDB00500  (APRD01268)
TypeSmall Molecule
GroupsApproved
Description

A non-steroidal anti-inflammatory agent (anti-inflammatory agents, NON-steroidal) similar in mode of action to indomethacin. [PubChem]

Structure
Thumb
Synonyms
1-Methyl-5-(4-methylbenzoyl)-pyrrole-2-acetic acid
1-Methyl-5-P-toluoylpyrrole-2-acetic acid
5-(P-Toluoyl)-1-methylpyrrole-2-acetic acid
Tolmetin
Tolmetina
Tolmétine
Tolmetino
Tolmetinum
External Identifiers
  • McN 2559
  • McN 2559-21-98
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Novo-tolmetin Capsules 400mgcapsule400 mgoralNovopharm Limited1994-12-312005-08-10Canada
Tolectin 200 Tab 200mgtablet245 mgoralMcneil Pharmaceutical, Division Of Ortho Mcneil Inc.1976-12-312002-08-02Canada
Tolectin 400 Cap 400mgcapsule400 mgoralMcneil Pharmaceutical, Division Of Ortho Mcneil Inc.1980-12-312002-08-02Canada
Tolectin Tab 600mgtablet600 mgoralJanssen Inc1987-12-312006-02-27Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Tolmetin Sodiumcapsule400 mg/1oralTeva Pharmaceuticals USA Inc2012-07-26Not applicableUs
Tolmetin Sodiumcapsule400 mg/1oralMutual Pharmaceutical Company, Inc.2009-09-04Not applicableUs
Tolmetin Sodiumtablet200 mg/1oralMutual Pharmaceutical Company, Inc.2009-09-04Not applicableUs
Tolmetin Sodiumtablet, film coated600 mg/1oralSTAT Rx USA LLC2009-11-02Not applicableUs
Tolmetin Sodiumcapsule400 mg/1oralMylan Pharmaceuticals Inc.1993-05-27Not applicableUs
Tolmetin Sodiumtablet, film coated600 mg/1oralMylan Pharmaceuticals Inc.1994-08-30Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
TolectinTeva
Tolectin DSTeva
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Tolmetin sodium
64490-92-2
Thumb
  • InChI Key: QGUALMNFRILWRA-UHFFFAOYSA-M
  • Monoisotopic Mass: 279.087137994
  • Average Mass: 279.2663
DBSALT000496
Categories
UNIID8K2JPN18B
CAS number26171-23-3
WeightAverage: 257.2845
Monoisotopic: 257.105193351
Chemical FormulaC15H15NO3
InChI KeyInChIKey=UPSPUYADGBWSHF-UHFFFAOYSA-N
InChI
InChI=1S/C15H15NO3/c1-10-3-5-11(6-4-10)15(19)13-8-7-12(16(13)2)9-14(17)18/h3-8H,9H2,1-2H3,(H,17,18)
IUPAC Name
2-[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetic acid
SMILES
CN1C(CC(O)=O)=CC=C1C(=O)C1=CC=C(C)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as acetophenones. These are organic compounds containing the acetophenone structure.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassAcetophenones
Direct ParentAcetophenones
Alternative Parents
Substituents
  • Acetophenone
  • Aryl ketone
  • Benzoyl
  • Toluene
  • Substituted pyrrole
  • N-methylpyrrole
  • Heteroaromatic compound
  • Pyrrole
  • Ketone
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the relief of signs and symptoms of rheumatoid arthritis and osteoarthritis, including the treatment of acute flares long-term management. Also for treatment of juvenile rheumatoid arthritis.
PharmacodynamicsTolmetin is a nonsteroidal anti-inflammatory agent. Studies in animals have shown tolmetin to possess anti-inflammatory, analgesic and antipyretic activity. In the rat, tolmetin prevents the development of experimentally induced polyarthritis and also decreases established inflammation. In patients with either rheumatoid arthritis or osteaoarthritis, tolmetin is as effective as aspirin and indomethacin in controlling disease activity, but the frequency of the milder gastrointestinal adverse effects and tinnitus was less than in aspirin-treated patients, and the incidence of central nervous system adverse effects was less than in indomethacin-treated patients. In patients with juvenile rheumatoid arthritis, tolmetin is as effective as aspirin in controlling disease activity, with a similar incidence of adverse reactions. tolmetin has produced additional therapeutic benefit when added to a regimen of gold salts and, to a lesser extent, with corticosteroids. Tolmetin should not be used in conjunction with salicylates since greater benefit from the combination is not likely, but the potential for adverse reactions is increased.
Mechanism of actionThe mode of action of tolmetin is not known. However, studies in laboratory animals and man have demonstrated that the anti-inflammatory action of tolmetin is not due to pituitary-adrenal stimulation. Tolmetin inhibits prostaglandin synthetase in vitro and lowers the plasma level of prostaglandin E in man. This reduction in prostaglandin synthesis may be responsible for the anti-inflammatory action. Tolmetin does not appear to alter the course of the underlying disease in man.
Related Articles
AbsorptionRapidly and almost completely absorbed with peak plasma levels being reached within 30-60 minutes after an oral therapeutic dose.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Essentially all of the administered dose is recovered in the urine in 24 hours either as an inactive oxidative metabolite or as conjugates of tolmetin.

SubstrateEnzymesProduct
Tolmetin
Not Available
Tolmetin glucuronideDetails
Route of eliminationNot Available
Half lifeBiphasic elimination from the plasma consisting of a rapid phase with a half-life of one to 2 hours followed by a slower phase with a half-life of about 5 hours.
ClearanceNot Available
ToxicitySymptoms of overdose include lethargy, drowsiness, nausea, vomiting, and epigastric pain.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Tolmetin Action PathwayDrug actionSMP00704
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9752
Blood Brain Barrier+0.8387
Caco-2 permeable+0.8867
P-glycoprotein substrateNon-substrate0.7277
P-glycoprotein inhibitor INon-inhibitor0.9062
P-glycoprotein inhibitor IINon-inhibitor0.9542
Renal organic cation transporterNon-inhibitor0.7999
CYP450 2C9 substrateNon-substrate0.7091
CYP450 2D6 substrateNon-substrate0.7867
CYP450 3A4 substrateNon-substrate0.6233
CYP450 1A2 substrateNon-inhibitor0.9159
CYP450 2C9 inhibitorNon-inhibitor0.9353
CYP450 2D6 inhibitorNon-inhibitor0.9449
CYP450 2C19 inhibitorNon-inhibitor0.9389
CYP450 3A4 inhibitorNon-inhibitor0.9563
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9346
Ames testNon AMES toxic0.8887
CarcinogenicityNon-carcinogens0.8992
BiodegradationReady biodegradable0.5
Rat acute toxicity2.9129 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9535
hERG inhibition (predictor II)Non-inhibitor0.9545
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Ortho mcneil janssen pharmaceuticals inc
  • Actavis elizabeth llc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
Packagers
Dosage forms
FormRouteStrength
Capsuleoral400 mg
Tabletoral245 mg
Tabletoral600 mg
Capsuleoral400 mg/1
Tabletoral200 mg/1
Tablet, film coatedoral600 mg/1
Prices
Unit descriptionCostUnit
Tolectin 600 mg tablet2.43USD tablet
Tolmetin sodium 600 mg tablet2.06USD tablet
Tolmetin Sodium 400 mg capsule1.77USD capsule
Tolmetin sodium 200 mg tablet0.77USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point156 dec °CPhysProp
water solubility222 mg/LNot Available
logP2.79SANGSTER (1993)
pKa3.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.131 mg/mLALOGPS
logP2.81ALOGPS
logP2.73ChemAxon
logS-3.3ALOGPS
pKa (Strongest Acidic)3.96ChemAxon
pKa (Strongest Basic)-7.8ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area59.3 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity72.39 m3·mol-1ChemAxon
Polarizability27.67 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (9.07 KB)
SpectraNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesM01AB03M02AA21
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (77.4 KB)
MSDSDownload (44.3 KB)
Interactions
Drug Interactions
Drug
AbciximabTolmetin may increase the anticoagulant activities of Abciximab.
AcenocoumarolTolmetin may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Tolmetin is combined with Acetylsalicylic acid.
AliskirenTolmetin may decrease the antihypertensive activities of Aliskiren.
AlteplaseTolmetin may increase the anticoagulant activities of Alteplase.
AmikacinTolmetin may decrease the excretion rate of Amikacin which could result in a lower serum level and potentially a reduction in efficacy.
AmitriptylineAmitriptyline may increase the antiplatelet activities of Tolmetin.
AnistreplaseTolmetin may increase the anticoagulant activities of Anistreplase.
ApixabanThe risk or severity of adverse effects can be increased when Tolmetin is combined with Apixaban.
ArbekacinTolmetin may decrease the excretion rate of Arbekacin which could result in a lower serum level and potentially a reduction in efficacy.
BalsalazideTolmetin may increase the nephrotoxic activities of Balsalazide.
Citric AcidTolmetin may increase the anticoagulant activities of Citric Acid.
ColesevelamColesevelam can cause a decrease in the absorption of Tolmetin resulting in a reduced serum concentration and potentially a decrease in efficacy.
CollagenaseThe risk or severity of adverse effects can be increased when Tolmetin is combined with Collagenase.
CyclosporineTolmetin may increase the nephrotoxic activities of Cyclosporine.
Dabigatran etexilateTolmetin may increase the anticoagulant activities of Dabigatran etexilate.
DalteparinTolmetin may increase the anticoagulant activities of Dalteparin.
DasatinibDasatinib may increase the anticoagulant activities of Tolmetin.
DeferasiroxThe risk or severity of adverse effects can be increased when Tolmetin is combined with Deferasirox.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Tolmetin is combined with Deoxycholic Acid.
DesmopressinThe risk or severity of adverse effects can be increased when Tolmetin is combined with Desmopressin.
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Tolmetin.
DiclofenacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Tolmetin.
DicoumarolTolmetin may increase the anticoagulant activities of Dicoumarol.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Tolmetin.
DrospirenoneTolmetin may increase the hyperkalemic activities of Drospirenone.
Edetic AcidTolmetin may increase the anticoagulant activities of Edetic Acid.
EnoxaparinTolmetin may increase the anticoagulant activities of Enoxaparin.
EplerenoneTolmetin may decrease the antihypertensive activities of Eplerenone.
Ethyl biscoumacetateTolmetin may increase the anticoagulant activities of Ethyl biscoumacetate.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Tolmetin.
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Tolmetin.
Fondaparinux sodiumTolmetin may increase the anticoagulant activities of Fondaparinux sodium.
FramycetinTolmetin may decrease the excretion rate of Framycetin which could result in a lower serum level and potentially a reduction in efficacy.
GentamicinTolmetin may decrease the excretion rate of Gentamicin which could result in a lower serum level and potentially a reduction in efficacy.
GlucosamineGlucosamine may increase the antiplatelet activities of Tolmetin.
HaloperidolThe risk or severity of adverse effects can be increased when Tolmetin is combined with Haloperidol.
HeparinTolmetin may increase the anticoagulant activities of Heparin.
HomoharringtonineThe risk or severity of adverse effects can be increased when Tolmetin is combined with Homoharringtonine.
HydralazineTolmetin may decrease the antihypertensive activities of Hydralazine.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Tolmetin is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Tolmetin.
IcosapentThe risk or severity of adverse effects can be increased when Tolmetin is combined with Icosapent.
InfliximabThe risk or severity of adverse effects can be increased when Infliximab is combined with Tolmetin.
KanamycinTolmetin may decrease the excretion rate of Kanamycin which could result in a lower serum level and potentially a reduction in efficacy.
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Tolmetin.
LimaprostLimaprost may increase the antiplatelet activities of Tolmetin.
LithiumThe serum concentration of Lithium can be increased when it is combined with Tolmetin.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Tolmetin.
MorniflumateThe risk or severity of adverse effects can be increased when Morniflumate is combined with Tolmetin.
NadololTolmetin may decrease the antihypertensive activities of Nadolol.
NeomycinTolmetin may decrease the excretion rate of Neomycin which could result in a lower serum level and potentially a reduction in efficacy.
NetilmicinTolmetin may decrease the excretion rate of Netilmicin which could result in a lower serum level and potentially a reduction in efficacy.
ObinutuzumabThe risk or severity of adverse effects can be increased when Tolmetin is combined with Obinutuzumab.
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Tolmetin.
PamidronateThe risk or severity of adverse effects can be increased when Tolmetin is combined with Pamidronate.
ParoxetineParoxetine may increase the antiplatelet activities of Tolmetin.
PemetrexedThe serum concentration of Pemetrexed can be increased when it is combined with Tolmetin.
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Tolmetin.
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Tolmetin.
PerindoprilThe risk or severity of adverse effects can be increased when Perindopril is combined with Tolmetin.
PhenindioneTolmetin may increase the anticoagulant activities of Phenindione.
PhenprocoumonTolmetin may increase the anticoagulant activities of Phenprocoumon.
PorfimerTolmetin may increase the photosensitizing activities of Porfimer.
PralatrexateThe serum concentration of Pralatrexate can be increased when it is combined with Tolmetin.
ProbenecidThe serum concentration of Tolmetin can be increased when it is combined with Probenecid.
ReteplaseTolmetin may increase the anticoagulant activities of Reteplase.
RibostamycinTolmetin may decrease the excretion rate of Ribostamycin which could result in a lower serum level and potentially a reduction in efficacy.
RidogrelTolmetin may increase the anticoagulant activities of Ridogrel.
RivaroxabanTolmetin may increase the anticoagulant activities of Rivaroxaban.
SparfloxacinTolmetin may increase the neuroexcitatory activities of Sparfloxacin.
SpectinomycinTolmetin may decrease the excretion rate of Spectinomycin which could result in a lower serum level and potentially a reduction in efficacy.
StreptokinaseTolmetin may increase the anticoagulant activities of Streptokinase.
StreptomycinTolmetin may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
SulodexideTolmetin may increase the anticoagulant activities of Sulodexide.
TacrolimusTolmetin may increase the nephrotoxic activities of Tacrolimus.
TalniflumateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Tolmetin.
TenecteplaseTolmetin may increase the anticoagulant activities of Tenecteplase.
TenofovirThe risk or severity of adverse effects can be increased when Tolmetin is combined with Tenofovir.
TipranavirTipranavir may increase the antiplatelet activities of Tolmetin.
TobramycinTolmetin may decrease the excretion rate of Tobramycin which could result in a lower serum level and potentially a reduction in efficacy.
TorasemideTolmetin may decrease the diuretic activities of Torasemide.
TositumomabThe risk or severity of adverse effects can be increased when Tolmetin is combined with Tositumomab.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Tolmetin.
TriamtereneTolmetin may decrease the antihypertensive activities of Triamterene.
TrichlormethiazideThe therapeutic efficacy of Trichlormethiazide can be decreased when used in combination with Tolmetin.
UnoprostoneThe therapeutic efficacy of Unoprostone can be decreased when used in combination with Tolmetin.
UrokinaseTolmetin may increase the anticoagulant activities of Urokinase.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Tolmetin.
VancomycinThe serum concentration of Vancomycin can be increased when it is combined with Tolmetin.
VenlafaxineVenlafaxine may increase the antiplatelet activities of Tolmetin.
VerteporfinTolmetin may increase the photosensitizing activities of Verteporfin.
Vitamin EVitamin E may increase the antiplatelet activities of Tolmetin.
WarfarinTolmetin may increase the anticoagulant activities of Warfarin.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and brain, and in pathological conditions, such as in cancer. PTGS2 is responsible for production of inflammatory prostaglandins. Up-regulation of PTGS2 is also associated with increased cell adhesion, p...
Gene Name:
PTGS2
Uniprot ID:
P35354
Molecular Weight:
68995.625 Da
References
  1. Burdan F, Szumilo J, Klepacz R, Dudka J, Korobowicz A, Tokarska E, Cendrowska-Pinkosz M, Madej B, Klepacz L: Gastrointestinal and hepatic toxicity of selective and non-selective cyclooxygenase-2 inhibitors in pregnant and non-pregnant rats. Pharmacol Res. 2004 Nov;50(5):533-43. [PubMed:15458776 ]
  2. Capasso A, Sorrentino L: Arachidonic acid and its metabolites are involved in the expression of morphine dependence in guinea-pig isolated ileum. Eur J Pharmacol. 1997 Jul 9;330(2-3):199-204. [PubMed:9253954 ]
  3. Kirkova M, Alexandova A, Kesiova M, Todorov S: In vivo effects of amtolmetin guacyl on lipid peroxidation and antioxidant defence systems. Comparison with non-selective and COX-2 selective NSAIDs. Auton Autacoid Pharmacol. 2007 Apr;27(2):99-104. [PubMed:17391279 ]
  4. Kennedy JH, Korn N, Thurston RJ: Prostaglandin levels in seminal plasma and sperm extracts of the domestic turkey, and the effects of cyclooxygenase inhibitors on sperm mobility. Reprod Biol Endocrinol. 2003 Oct 9;1:74. [PubMed:14613550 ]
  5. Capasso A: Further studies on the involvement of the arachidonic acid cascade in the acute dependence produced by mu, kappa and delta opioid agonists in isolated tissues. Neuropharmacology. 1999 Jun;38(6):871-7. [PubMed:10465690 ]
  6. 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
unknown
Actions
inhibitor
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
References
  1. Capasso A, Sorrentino L: Arachidonic acid and its metabolites are involved in the expression of morphine dependence in guinea-pig isolated ileum. Eur J Pharmacol. 1997 Jul 9;330(2-3):199-204. [PubMed:9253954 ]
  2. Kennedy JH, Korn N, Thurston RJ: Prostaglandin levels in seminal plasma and sperm extracts of the domestic turkey, and the effects of cyclooxygenase inhibitors on sperm mobility. Reprod Biol Endocrinol. 2003 Oct 9;1:74. [PubMed:14613550 ]
  3. Capasso A: Further studies on the involvement of the arachidonic acid cascade in the acute dependence produced by mu, kappa and delta opioid agonists in isolated tissues. Neuropharmacology. 1999 Jun;38(6):871-7. [PubMed:10465690 ]
  4. Burdan F, Szumilo J, Marzec B, Klepacz R, Dudka J: Skeletal developmental effects of selective and nonselective cyclooxygenase-2 inhibitors administered through organogenesis and fetogenesis in Wistar CRL:(WI)WUBR rats. Toxicology. 2005 Dec 15;216(2-3):204-23. Epub 2005 Sep 22. [PubMed:16182428 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Tryptophan 2,3-dioxygenase activity
Specific Function:
Incorporates oxygen into the indole moiety of tryptophan. Has a broad specificity towards tryptamine and derivatives including D- and L-tryptophan, 5-hydroxytryptophan and serotonin (By similarity).
Gene Name:
TDO2
Uniprot ID:
P48775
Molecular Weight:
47871.215 Da
References
  1. Dairam A, Antunes EM, Saravanan KS, Daya S: Non-steroidal anti-inflammatory agents, tolmetin and sulindac, inhibit liver tryptophan 2,3-dioxygenase activity and alter brain neurotransmitter levels. Life Sci. 2006 Nov 10;79(24):2269-74. Epub 2006 Aug 1. [PubMed:16952380 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Peroxidase activity
Specific Function:
Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production of hypohalous acids, primarily hypochlorous acid in physiologic situations, and other toxic intermediates that greatly enhance PMN microbicidal activity.
Gene Name:
MPO
Uniprot ID:
P05164
Molecular Weight:
83867.71 Da
References
  1. Anderson R, Oosthuizen R, Grabow G: Prevention of peroxidase mediated inhibition of neutrophil motility and lymphocyte transformation by levamisole, OMPI, sodium aurothiomalate, indomethacin and tolmetin in vitro. Int J Immunopharmacol. 1981;3(2):123-32. [PubMed:6266970 ]

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. Apiwattanakul N, Sekine T, Chairoungdua A, Kanai Y, Nakajima N, Sophasan S, Endou H: Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes. Mol Pharmacol. 1999 May;55(5):847-54. [PubMed:10220563 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on May 06, 2016 14:07