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Identification
NameSparfloxacin
Accession NumberDB01208  (APRD01231)
TypeSmall Molecule
GroupsApproved
Description

Sparfloxacin is a fluoroquinolone antibiotic used in the treatment of bacterial infections. Sparfloxacin exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. DNA gyrase is an essential enzyme which controls DNA topology and assists in DNA replication, repair, deactivation, and transcription.

Structure
Thumb
Synonyms
cis-5-Amino-1-cyclopropyl-7-(3,5-dimethyl-1-piperazinyl)-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
Sparfloxacin
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ZagamNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIQ90AGA787L
CAS number110871-86-8
WeightAverage: 392.3998
Monoisotopic: 392.165997
Chemical FormulaC19H22F2N4O3
InChI KeyInChIKey=DZZWHBIBMUVIIW-DTORHVGOSA-N
InChI
InChI=1S/C19H22F2N4O3/c1-8-5-24(6-9(2)23-8)17-13(20)15(22)12-16(14(17)21)25(10-3-4-10)7-11(18(12)26)19(27)28/h7-10,23H,3-6,22H2,1-2H3,(H,27,28)/t8-,9+
IUPAC Name
5-amino-1-cyclopropyl-7-[(3R,5S)-3,5-dimethylpiperazin-1-yl]-6,8-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
SMILES
C[[email protected]]1CN(C[C@@H](C)N1)C1=C(F)C(N)=C2C(=O)C(=CN(C3CC3)C2=C1F)C(O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as quinoline carboxylic acids. These are quinolines in which the quinoline ring system is substituted by a carboxyl group at one or more positions.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassQuinolines and derivatives
Sub ClassQuinoline carboxylic acids
Direct ParentQuinoline carboxylic acids
Alternative Parents
Substituents
  • Quinoline-3-carboxylic acid
  • N-arylpiperazine
  • Fluoroquinolone
  • Dihydroquinolone
  • Aminoquinoline
  • Dihydroquinoline
  • Pyridine carboxylic acid or derivatives
  • Pyridine carboxylic acid
  • Dialkylarylamine
  • Fluorobenzene
  • Benzenoid
  • Pyridine
  • Primary aromatic amine
  • Piperazine
  • 1,4-diazinane
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Vinylogous amide
  • Tertiary amine
  • Azacycle
  • Secondary amine
  • Monocarboxylic acid or derivatives
  • Secondary aliphatic amine
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of adults with the following infections caused by susceptible strains microorganisms: community-acquired pneumonia (caused by Chlamydia pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, or Streptococcus pneumoniae) and acute bacterial exacerbations of chronic bronchitis (caused by Chlamydia pneumoniae, Enterobacter cloacae, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Staphylococcus aureus, or Streptococcus pneumoniae).
PharmacodynamicsSparfloxacin is a synthetic fluoroquinolone broad-spectrum antimicrobial agent in the same class as ofloxacin and norfloxacin. Sparfloxacin has in vitro activity against a wide range of gram-negative and gram-positive microorganisms. Sparfloxacin exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. DNA gyrase is an essential enzyme which controls DNA topology and assists in DNA replication, repair, deactivation, and transcription. Quinolones differ in chemical structure and mode of action from (beta)-lactam antibiotics. Quinolones may, therefore, be active against bacteria resistant to (beta)-lactam antibiotics. Although cross-resistance has been observed between sparfloxacin and other fluoroquinolones, some microorganisms resistant to other fluoroquinolones may be susceptible to sparfloxacin. In vitro tests show that the combination of sparfloxacin and rifampin is antagonistic against Staphylococcus aureus.
Mechanism of actionThe bactericidal action of sparfloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination.
Related Articles
AbsorptionWell absorbed following oral administration with an absolute oral bioavailability of 92%. Unaffected by administration with milk or food, however concurrent administration of antacids containing magnesium hydroxide and aluminum hydroxide reduces the oral bioavailability of sparfloxacin by as much as 50%.
Volume of distributionNot Available
Protein bindingLow plasma protein binding in serum at about 45%.
Metabolism

Hepatic. Metabolized primarily by phase II glucuronidation to form a glucuronide conjugate. Metabolism does not utilize or interfere with the cytochrome P450 enzyme system.

Route of eliminationNot Available
Half lifeMean terminal elimination half-life of 20 hours (range 16-30 hours). Prolonged in patients with renal impairment (creatinine clearance <50 mL/min).
ClearanceNot Available
ToxicitySingle doses of sparfloxacin were relatively non-toxic via the oral route of administration in mice, rats, and dogs. No deaths occurred within a 14-day post-treatment observation period at the highest oral doses tested, up to 5000 mg/kg in either rodent species, or up to 600 mg/kg in the dog. Clinical signs observed included inactivity in mice and dogs, diarrhea in both rodent species, and vomiting, salivation, and tremors in dogs.
Affected organisms
  • Enteric bacteria and other eubacteria
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9845
Blood Brain Barrier-0.967
Caco-2 permeable+0.8866
P-glycoprotein substrateSubstrate0.8118
P-glycoprotein inhibitor INon-inhibitor0.9345
P-glycoprotein inhibitor IINon-inhibitor0.9183
Renal organic cation transporterNon-inhibitor0.8154
CYP450 2C9 substrateNon-substrate0.8794
CYP450 2D6 substrateNon-substrate0.8787
CYP450 3A4 substrateNon-substrate0.6465
CYP450 1A2 substrateNon-inhibitor0.82
CYP450 2C9 inhibitorNon-inhibitor0.84
CYP450 2D6 inhibitorNon-inhibitor0.89
CYP450 2C19 inhibitorNon-inhibitor0.8339
CYP450 3A4 inhibitorNon-inhibitor0.85
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7377
Ames testAMES toxic0.6341
CarcinogenicityNon-carcinogens0.8044
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.9265 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.967
hERG inhibition (predictor II)Non-inhibitor0.7961
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US4795751 No1993-02-042010-02-04Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityPractically insolubleNot Available
logP2.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.113 mg/mLALOGPS
logP-0.07ALOGPS
logP-0.043ChemAxon
logS-3.5ALOGPS
pKa (Strongest Acidic)5.75ChemAxon
pKa (Strongest Basic)8.79ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area98.9 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity101.69 m3·mol-1ChemAxon
Polarizability38.98 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Guillaume Conrath, “Solution of sparfloxacin, its preparation and salt of which it is composed.” U.S. Patent US5478829, issued May, 1987.

US5478829
General ReferencesNot Available
External Links
ATC CodesJ01MA09
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (13.3 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcarboseSparfloxacin may increase the hypoglycemic activities of Acarbose.
AcenocoumarolSparfloxacin may increase the anticoagulant activities of Acenocoumarol.
AlbiglutideSparfloxacin may increase the hypoglycemic activities of Albiglutide.
AlogliptinSparfloxacin may increase the hypoglycemic activities of Alogliptin.
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
BetamethasoneThe risk or severity of adverse effects can be increased when Betamethasone is combined with Sparfloxacin.
BromocriptineSparfloxacin may increase the hypoglycemic activities of Bromocriptine.
Calcium AcetateCalcium Acetate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium citrateCalcium citrate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium gluconateCalcium gluconate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
CanagliflozinSparfloxacin may increase the hypoglycemic activities of Canagliflozin.
CelecoxibCelecoxib may increase the neuroexcitatory activities of Sparfloxacin.
ChlorpropamideSparfloxacin may increase the hypoglycemic activities of Chlorpropamide.
CorticotropinThe risk or severity of adverse effects can be increased when Corticotropin is combined with Sparfloxacin.
Cortisone acetateThe risk or severity of adverse effects can be increased when Cortisone acetate is combined with Sparfloxacin.
DapagliflozinSparfloxacin may increase the hypoglycemic activities of Dapagliflozin.
DexamethasoneThe risk or severity of adverse effects can be increased when Dexamethasone is combined with Sparfloxacin.
DiclofenacDiclofenac may increase the neuroexcitatory activities of Sparfloxacin.
DidanosineThe serum concentration of Didanosine can be decreased when it is combined with Sparfloxacin.
DiflunisalDiflunisal may increase the neuroexcitatory activities of Sparfloxacin.
DisopyramideSparfloxacin may increase the hypoglycemic activities of Disopyramide.
DulaglutideSparfloxacin may increase the hypoglycemic activities of Dulaglutide.
EmpagliflozinSparfloxacin may increase the hypoglycemic activities of Empagliflozin.
ErythromycinSparfloxacin may increase the hypoglycemic activities of Erythromycin.
EtodolacEtodolac may increase the neuroexcitatory activities of Sparfloxacin.
ExenatideSparfloxacin may increase the hypoglycemic activities of Exenatide.
FenoprofenFenoprofen may increase the neuroexcitatory activities of Sparfloxacin.
Ferric CitrateThe serum concentration of Sparfloxacin can be decreased when it is combined with Ferric Citrate.
FloctafenineFloctafenine may increase the neuroexcitatory activities of Sparfloxacin.
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Sparfloxacin.
FlurbiprofenFlurbiprofen may increase the neuroexcitatory activities of Sparfloxacin.
GliclazideSparfloxacin may increase the hypoglycemic activities of Gliclazide.
GlimepirideSparfloxacin may increase the hypoglycemic activities of Glimepiride.
GlipizideSparfloxacin may increase the hypoglycemic activities of Glipizide.
GlyburideSparfloxacin may increase the hypoglycemic activities of Glyburide.
HydrocortisoneThe risk or severity of adverse effects can be increased when Hydrocortisone is combined with Sparfloxacin.
IbuprofenIbuprofen may increase the neuroexcitatory activities of Sparfloxacin.
IndomethacinIndomethacin may increase the neuroexcitatory activities of Sparfloxacin.
Insulin AspartSparfloxacin may increase the hypoglycemic activities of Insulin Aspart.
Insulin DegludecSparfloxacin may increase the hypoglycemic activities of Insulin degludec.
Insulin DetemirSparfloxacin may increase the hypoglycemic activities of Insulin Detemir.
Insulin GlargineSparfloxacin may increase the hypoglycemic activities of Insulin Glargine.
Insulin GlulisineSparfloxacin may increase the hypoglycemic activities of Insulin Glulisine.
Insulin HumanSparfloxacin may increase the hypoglycemic activities of Insulin Regular.
Insulin LisproSparfloxacin may increase the hypoglycemic activities of Insulin Lispro.
KetoprofenKetoprofen may increase the neuroexcitatory activities of Sparfloxacin.
KetorolacKetorolac may increase the neuroexcitatory activities of Sparfloxacin.
LanreotideSparfloxacin may increase the hypoglycemic activities of Lanreotide.
LanthanumThe serum concentration of Sparfloxacin can be decreased when it is combined with Lanthanum.
Lanthanum carbonateThe serum concentration of Sparfloxacin can be decreased when it is combined with Lanthanum carbonate.
LiraglutideSparfloxacin may increase the hypoglycemic activities of Liraglutide.
Magnesium chlorideThe serum concentration of Sparfloxacin can be decreased when it is combined with Magnesium chloride.
Magnesium citrateThe serum concentration of Sparfloxacin can be decreased when it is combined with Magnesium citrate.
Magnesium hydroxideMagnesium hydroxide can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium oxideThe serum concentration of Sparfloxacin can be decreased when it is combined with Magnesium oxide.
Magnesium salicylateThe serum concentration of Sparfloxacin can be decreased when it is combined with Magnesium salicylate.
Magnesium SulfateThe serum concentration of Sparfloxacin can be decreased when it is combined with Magnesium Sulfate.
MecaserminSparfloxacin may increase the hypoglycemic activities of Mecasermin.
Mefenamic acidMefenamic acid may increase the neuroexcitatory activities of Sparfloxacin.
MeloxicamMeloxicam may increase the neuroexcitatory activities of Sparfloxacin.
MetforminSparfloxacin may increase the hypoglycemic activities of Metformin.
MethylprednisoloneThe risk or severity of adverse effects can be increased when Methylprednisolone is combined with Sparfloxacin.
MifepristoneSparfloxacin may increase the hypoglycemic activities of Mifepristone.
MiglitolSparfloxacin may increase the hypoglycemic activities of Miglitol.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be decreased when it is combined with Sparfloxacin.
Mycophenolic acidThe serum concentration of Mycophenolic acid can be decreased when it is combined with Sparfloxacin.
NabumetoneNabumetone may increase the neuroexcitatory activities of Sparfloxacin.
NaproxenNaproxen may increase the neuroexcitatory activities of Sparfloxacin.
NateglinideSparfloxacin may increase the hypoglycemic activities of Nateglinide.
OctreotideSparfloxacin may increase the hypoglycemic activities of Octreotide.
OxaprozinOxaprozin may increase the neuroexcitatory activities of Sparfloxacin.
PasireotideSparfloxacin may increase the hypoglycemic activities of Pasireotide.
PentamidineSparfloxacin may increase the hypoglycemic activities of Pentamidine.
PioglitazoneSparfloxacin may increase the hypoglycemic activities of Pioglitazone.
PiroxicamPiroxicam may increase the neuroexcitatory activities of Sparfloxacin.
PramlintideSparfloxacin may increase the hypoglycemic activities of Pramlintide.
PrednisoloneThe risk or severity of adverse effects can be increased when Prednisolone is combined with Sparfloxacin.
PrednisoneThe risk or severity of adverse effects can be increased when Prednisone is combined with Sparfloxacin.
ProbenecidThe serum concentration of Sparfloxacin can be increased when it is combined with Probenecid.
QuinaprilThe serum concentration of Sparfloxacin can be decreased when it is combined with Quinapril.
QuinineSparfloxacin may increase the hypoglycemic activities of Quinine.
RepaglinideSparfloxacin may increase the hypoglycemic activities of Repaglinide.
Repository corticotropinThe risk or severity of adverse effects can be increased when Repository corticotropin is combined with Sparfloxacin.
RosiglitazoneSparfloxacin may increase the hypoglycemic activities of Rosiglitazone.
SaxagliptinSparfloxacin may increase the hypoglycemic activities of Saxagliptin.
SevelamerSevelamer can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
SitagliptinSparfloxacin may increase the hypoglycemic activities of Sitagliptin.
SucralfateThe serum concentration of Sparfloxacin can be decreased when it is combined with Sucralfate.
SulfadiazineSparfloxacin may increase the hypoglycemic activities of Sulfadiazine.
SulfamethoxazoleSparfloxacin may increase the hypoglycemic activities of Sulfamethoxazole.
SulfisoxazoleSparfloxacin may increase the hypoglycemic activities of Sulfisoxazole.
SulindacSulindac may increase the neuroexcitatory activities of Sparfloxacin.
SunitinibSparfloxacin may increase the hypoglycemic activities of Sunitinib.
Tiaprofenic acidTiaprofenic acid may increase the neuroexcitatory activities of Sparfloxacin.
TolazamideSparfloxacin may increase the hypoglycemic activities of Tolazamide.
TolbutamideSparfloxacin may increase the hypoglycemic activities of Tolbutamide.
TolmetinTolmetin may increase the neuroexcitatory activities of Sparfloxacin.
TriamcinoloneThe risk or severity of adverse effects can be increased when Triamcinolone is combined with Sparfloxacin.
TrimethoprimSparfloxacin may increase the hypoglycemic activities of Trimethoprim.
VareniclineThe serum concentration of Varenicline can be increased when it is combined with Sparfloxacin.
WarfarinSparfloxacin may increase the anticoagulant activities of Warfarin.
ZincThe serum concentration of Sparfloxacin can be decreased when it is combined with Zinc.
Zinc gluconateThe serum concentration of Sparfloxacin can be decreased when it is combined with Zinc gluconate.
Zinc sulfateThe serum concentration of Sparfloxacin can be decreased when it is combined with Zinc sulfate.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Pharmacological action
yes
Actions
inhibitor
General Function:
Dna topoisomerase type ii (atp-hydrolyzing) activity
Specific Function:
DNA gyrase negatively supercoils closed circular double-stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, including catenanes and knotted rings.
Gene Name:
gyrA
Uniprot ID:
P43700
Molecular Weight:
97817.145 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Schmitz FJ, Hofmann B, Hansen B, Scheuring S, Luckefahr M, Klootwijk M, Verhoef J, Fluit A, Heinz HP, Kohrer K, Jones ME: Relationship between ciprofloxacin, ofloxacin, levofloxacin, sparfloxacin and moxifloxacin (BAY 12-8039) MICs and mutations in grlA, grlB, gyrA and gyrB in 116 unrelated clinical isolates of Staphylococcus aureus. J Antimicrob Chemother. 1998 Apr;41(4):481-4. [PubMed:9598779 ]
  4. Taba H, Kusano N: Sparfloxacin resistance in clinical isolates of Streptococcus pneumoniae: involvement of multiple mutations in gyrA and parC genes. Antimicrob Agents Chemother. 1998 Sep;42(9):2193-6. [PubMed:9736534 ]
  5. Fukuda H, Hori S, Hiramatsu K: Antibacterial activity of gatifloxacin (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquired quinolone-resistant mutants and the norA transformant of Staphylococcus aureus. Antimicrob Agents Chemother. 1998 Aug;42(8):1917-22. [PubMed:9687384 ]
Kind
Protein
Organism
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Pharmacological action
yes
Actions
inhibitor
General Function:
Dna topoisomerase type ii (atp-hydrolyzing) activity
Specific Function:
Topoisomerase IV is essential for chromosome segregation. It relaxes supercoiled DNA. Performs the decatenation events required during the replication of a circular DNA molecule.
Gene Name:
parC
Uniprot ID:
P43702
Molecular Weight:
83366.24 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Galbraith KM, Ng AC, Eggers BJ, Kuchel CR, Eggers CH, Samuels DS: parC mutations in fluoroquinolone-resistant Borrelia burgdorferi. Antimicrob Agents Chemother. 2005 Oct;49(10):4354-7. [PubMed:16189120 ]
  4. Oyamada Y, Ito H, Fujimoto K, Asada R, Niga T, Okamoto R, Inoue M, Yamagishi J: Combination of known and unknown mechanisms confers high-level resistance to fluoroquinolones in Enterococcus faecium. J Med Microbiol. 2006 Jun;55(Pt 6):729-36. [PubMed:16687591 ]
  5. Pan XS, Yague G, Fisher LM: Quinolone resistance mutations in Streptococcus pneumoniae GyrA and ParC proteins: mechanistic insights into quinolone action from enzymatic analysis, intracellular levels, and phenotypes of wild-type and mutant proteins. Antimicrob Agents Chemother. 2001 Nov;45(11):3140-7. [PubMed:11600369 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Ubiquitin binding
Specific Function:
Control of topological states of DNA by transient breakage and subsequent rejoining of DNA strands. Topoisomerase II makes double-strand breaks. Essential during mitosis and meiosis for proper segregation of daughter chromosomes. May play a role in regulating the period length of ARNTL/BMAL1 transcriptional oscillation (By similarity).
Gene Name:
TOP2A
Uniprot ID:
P11388
Molecular Weight:
174383.88 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Symporter activity
Specific Function:
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Also relative uptake activity ratio of carnitine to TEA is 11.3.
Gene Name:
SLC22A5
Uniprot ID:
O76082
Molecular Weight:
62751.08 Da
References
  1. Ohashi R, Tamai I, Yabuuchi H, Nezu JI, Oku A, Sai Y, Shimane M, Tsuji A: Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. J Pharmacol Exp Ther. 1999 Nov;291(2):778-84. [PubMed:10525100 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name:
ABCC2
Uniprot ID:
Q92887
Molecular Weight:
174205.64 Da
References
  1. Sasabe H, Tsuji A, Sugiyama Y: Carrier-mediated mechanism for the biliary excretion of the quinolone antibiotic grepafloxacin and its glucuronide in rats. J Pharmacol Exp Ther. 1998 Mar;284(3):1033-9. [PubMed:9495864 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Naruhashi K, Tamai I, Inoue N, Muraoka H, Sai Y, Suzuki N, Tsuji A: Active intestinal secretion of new quinolone antimicrobials and the partial contribution of P-glycoprotein. J Pharm Pharmacol. 2001 May;53(5):699-709. [PubMed:11370709 ]
  2. Cormet-Boyaka E, Huneau JF, Mordrelle A, Boyaka PN, Carbon C, Rubinstein E, Tome D: Secretion of sparfloxacin from the human intestinal Caco-2 cell line is altered by P-glycoprotein inhibitors. Antimicrob Agents Chemother. 1998 Oct;42(10):2607-11. [PubMed:9756763 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:13