You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameRocuronium
Accession NumberDB00728  (APRD01221)
TypeSmall Molecule
GroupsApproved
Description

Rocuronium (rapid onset-curonium) is a desacetoxy analogue of vecuronium with a more rapid onset of action. It is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation.
Introduced in 1994, rocuronium has rapid onset, and intermediate duration of action. It is marketed under the trade name of Zemuron in the United States and Esmeron in most other countries.
There is considered to be a risk of allergic reaction to the drug in some patients (particularly those with asthma), but a similar incidence of allergic reactions has been observed by using other members of the same drug class (non-depolarizing neuromuscular blocking drugs). The γ-cyclodextrin derivative sugammadex (trade name Bridion) has been recently introduced as a novel agent to reverse the action of rocuronium.

Structure
Thumb
Synonyms
Rocuronium
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Rocuronium Bromide Injectionsolution10 mgintravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Rocuronium Bromide Injectionsolution10 mgintravenousOmega Laboratories Ltd2012-08-02Not applicableCanada
Rocuronium Bromide Injectionsolution10 mgintravenousSandoz Canada Incorporated2008-10-24Not applicableCanada
Rocuronium Bromide Injectionliquid10 mgintravenousHospira Healthcare Corporation2009-02-10Not applicableCanada
Rocuronium Bromide Injection Sdzsolution10 mgintravenousSandoz Canada IncorporatedNot applicableNot applicableCanada
Zemuroninjection, solution10 mg/mLintravenousOrganon USA Inc.1994-03-17Not applicableUs
Zemuronsolution10 mgintravenousMerck Canada Inc1995-12-31Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Rocuroniuminjection, solution10 mg/mLintravenousThe Medicines Company2009-12-13Not applicableUs
Rocuroniuminjection, solution10 mg/mLintravenousFresenius Kabi USA, LLC2009-12-13Not applicableUs
Rocuroniuminjection, solution10 mg/mLintravenousThe Medicines Company2009-12-13Not applicableUs
Rocuronium Bromideinjection, solution10 mg/mLintravenousHospira, Inc.2008-11-26Not applicableUs
Rocuronium Bromideinjection10 mg/mLintravenousREMEDYREPACK INC.2015-03-112016-03-29Us
Rocuronium Bromidesolution10 mg/mLintravenousX Gen Pharmaceuticals, Inc.2012-12-01Not applicableUs
Rocuronium Bromideinjection10 mg/mLintravenousMylan Institutional LLC2014-09-29Not applicableUs
Rocuronium Bromideinjection, solution10 mg/mLintravenousSagent Pharmaceuticals2011-12-20Not applicableUs
Rocuronium Bromideinjection10 mg/mLintravenousMylan Institutional LLC2014-09-29Not applicableUs
Rocuronium Bromideinjection, solution10 mg/mLintravenousSandoz Inc2008-12-05Not applicableUs
Rocuronium Bromideinjection10 mg/mLintravenousMylan Institutional LLC2012-02-06Not applicableUs
Rocuronium Bromideinjection, solution10 mg/mLintravenousTeva Parenteral Medicines, Inc.2008-12-01Not applicableUs
Rocuronium Bromideinjection, solution10 mg/mLintravenousTeva Parenteral Medicines, Inc.2008-12-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Rocuronium Bromideinjection, solution10 mg/mLintravenousCantrell Drug Company2015-01-29Not applicableUs
International Brands
NameCompany
EsmeronNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Rocuronium bromide
119302-91-9
Thumb
  • InChI Key: OYTJKRAYGYRUJK-FMCCZJBLSA-M
  • Monoisotopic Mass: 608.318870841
  • Average Mass: 609.678
DBSALT000575
Categories
UNIIWRE554RFEZ
CAS number143558-00-3
WeightAverage: 529.7742
Monoisotopic: 529.400533194
Chemical FormulaC32H53N2O4
InChI KeyInChIKey=YXRDKMPIGHSVRX-OOJCLDBCSA-N
InChI
InChI=1S/C32H53N2O4/c1-5-14-34(15-6-7-16-34)28-20-26-24-9-8-23-19-29(36)27(33-12-17-37-18-13-33)21-32(23,4)25(24)10-11-31(26,3)30(28)38-22(2)35/h5,23-30,36H,1,6-21H2,2-4H3/q+1/t23-,24+,25-,26-,27-,28-,29-,30-,31-,32-/m0/s1
IUPAC Name
1-[(1S,2S,4S,5S,7S,10R,11S,13S,14R,15S)-14-(acetyloxy)-5-hydroxy-2,15-dimethyl-4-(morpholin-4-yl)tetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadecan-13-yl]-1-(prop-2-en-1-yl)pyrrolidin-1-ium
SMILES
[H][C@@]12C[C@@H]([[email protected]](OC(C)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC[C@@]2([H])C[[email protected]](O)[[email protected]](C[C@]12C)N1CCOCC1)[N+]1(CC=C)CCCC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as steroid esters. These are compounds containing a steroid moiety which bears a carboxylic acid ester group.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassSteroid esters
Direct ParentSteroid esters
Alternative Parents
Substituents
  • Steroid ester
  • Androgen-skeleton
  • Androstane-skeleton
  • 3-alpha-hydroxysteroid
  • Hydroxysteroid
  • 3-hydroxysteroid
  • Cyclohexylamine
  • N-alkylpyrrolidine
  • Oxazinane
  • Morpholine
  • Acetate salt
  • Quaternary ammonium salt
  • Pyrrolidine
  • Cyclic alcohol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary alcohol
  • Carboxylic acid ester
  • 1,2-aminoalcohol
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Ether
  • Dialkyl ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Organic cation
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor inpatients and outpatients as an adjunct to general anesthesia to facilitate both rapid sequence and routine tracheal intubation, and to provide skeletal muscle relaxation during surgery or mechanical ventilation.
PharmacodynamicsNeuromuscular blocking agents are drugs that cause skeletal muscle relaxation primarily by causing a decreased response to the neurotransmitter acetylcholine (ACh) at the myoneural (neuromuscular) junction of skeletal muscle. At that site, ACh normally produces electrical depolarization of the postjunctional membrane of motor end-plate, which leads to conduction of muscle action potential and subsequently induces skeletal muscle contraction. Neuromuscular agents are classified as depolarizing or nondepolarizing. Rocuronium is a nondepolarizing neuromuscular blocking agent with a rapid to intermediate onset depending on dose and intermediate duration. Rocuronium, like vecuronium is longer acting in infants than in children. However, unlike vecuronium, rocuronium retains the characteristics of an intermediate-acting NMBD in infants.
Mechanism of actionRocuronium acts by competing for cholinergic receptors at the motor end-plate. This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine and edrophonium. Rocuronium acts by competitively binding to nicotinic cholinergic receptors. The binding of vecuronium decreases the opportunity for acetylcholine to bind to the nicotinic receptor at the postjunctional membrane of the myoneural junction. As a result, depolarization is prevented, calcium ions are not released and muscle contraction does not occur. Evidence also suggests that nondepolarizing agents can affect ACh release. It has been hypothesized that nondepolarzing agents bind to postjunctional ("curare") receptors and may therefore interfere with the sodium and potassium flux, which is responsible for depolarization and repolarization of the membranes involved in muscle contraction.
Related Articles
AbsorptionPoorly absorbed from the GI tract.
Volume of distribution
  • 0.3 L/kg [3 to <12 mos]
  • 0.26 L/kg [1 to <3 yrs]
  • 0.21 L/kg [3 to <8 yrs]
Protein bindingApproximately 30% bound to human plasma proteins.
Metabolism

Rocuronium is metabolized to a less active metabolite, 17-desacetyl-rocuronium, and is eliminated primarily by the liver.

SubstrateEnzymesProduct
Rocuronium
Not Available
17-desacetyl-rocuroniumDetails
Route of eliminationStudies of distribution, metabolism, and excretion in cats and dogs indicate that rocuronium is eliminated primarily by the liver.
Half lifeThe rapid distribution half-life is 1-2 minutes and the slower distribution half-life is 14-18 minutes. Renal impairment has no net effect on half-life, however, half-life is almost doubled in patients with impaired liver function.
Clearance
  • 0.25 L/kg/hr [Adults (Ages 27 to 58 years)]
  • 0.21 L/kg/hr [Geriatrics (>=65 yrs)]
  • 0.16 L/kg/hr [Normal ewnal and hepatice function]
  • 0.13 L/kg/hr [Renal transplant patients]
  • 0.13 L/kg/hr [Hepatic dysfunction patients]
  • 0.35 +/- 0.08 L/kg/hr [Pediatric Patients 3 to <12 mos]
  • 0.32 +/- 0.07 L/kg/hr [Pediatric Patients 1 to 3 yrs]
  • 0.44 +/- 0.16 L/kg/hr [Pediatric Patients 3 to 8 yrs]
ToxicityNo cases of significant accidental or intentional overdose have been reported. Overdosage with neuromuscular blocking agents may result in neuromuscular block beyond the time needed for surgery and anesthesia.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.9444
Blood Brain Barrier+0.8569
Caco-2 permeable-0.5336
P-glycoprotein substrateSubstrate0.8559
P-glycoprotein inhibitor IInhibitor0.7889
P-glycoprotein inhibitor IIInhibitor0.9009
Renal organic cation transporterNon-inhibitor0.7222
CYP450 2C9 substrateNon-substrate0.8008
CYP450 2D6 substrateNon-substrate0.7534
CYP450 3A4 substrateSubstrate0.7272
CYP450 1A2 substrateNon-inhibitor0.9103
CYP450 2C9 inhibitorNon-inhibitor0.8856
CYP450 2D6 inhibitorNon-inhibitor0.8763
CYP450 2C19 inhibitorNon-inhibitor0.8423
CYP450 3A4 inhibitorNon-inhibitor0.8582
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9119
Ames testNon AMES toxic0.7601
CarcinogenicityNon-carcinogens0.9353
BiodegradationNot ready biodegradable0.946
Rat acute toxicity2.9310 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8607
hERG inhibition (predictor II)Non-inhibitor0.8146
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • App pharmaceuticals llc
  • Bioniche pharma usa llc
  • Hospira inc
  • Sagent pharmaceuticals inc
  • Sandoz canada inc
  • Teva parenteral medicines inc
  • Schering corp
Packagers
Dosage forms
FormRouteStrength
Injectionintravenous10 mg/mL
Solutionintravenous10 mg/mL
Liquidintravenous10 mg
Injection, solutionintravenous10 mg/mL
Solutionintravenous10 mg
Prices
Unit descriptionCostUnit
Zemuron 10 mg/ml vial4.62USD ml
Rocuronium 100 mg/10 ml vial2.66USD ml
Rocuronium 50 mg/5 ml vial1.08USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityCompleteNot Available
Predicted Properties
PropertyValueSource
Water Solubility2.84e-05 mg/mLALOGPS
logP2.71ALOGPS
logP-0.33ChemAxon
logS-7.3ALOGPS
pKa (Strongest Acidic)14.59ChemAxon
pKa (Strongest Basic)7.96ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area59 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity161.65 m3·mol-1ChemAxon
Polarizability62.87 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Eliezer Adar, David Sondack, Oded Friedman, Iosef Manascu, Tamir Fizitzki, Boris Freger, Oded Arad, Alexander Weisman, Joseph Kaspi, “Processes for the preparation of rocuronium bromide and intermediates thereof.” U.S. Patent US20050159398, issued July 21, 2005.

US20050159398
General References
  1. Agoston S, Vandenbrom RH, Wierda JM: Clinical pharmacokinetics of neuromuscular blocking drugs. Clin Pharmacokinet. 1992 Feb;22(2):94-115. [PubMed:1551294 ]
  2. Khuenl-Brady KS, Sparr H: Clinical pharmacokinetics of rocuronium bromide. Clin Pharmacokinet. 1996 Sep;31(3):174-83. [PubMed:8877248 ]
  3. Alvarez-Gomez JA: [Rocuronium]. Rev Esp Anestesiol Reanim. 1997 Oct;44(8):310-4. [PubMed:9424684 ]
  4. Wicks TC: The pharmacology of rocuronium bromide (ORG 9426). AANA J. 1994 Feb;62(1):33-8. [PubMed:8122487 ]
  5. Sparr HJ, Beaufort TM, Fuchs-Buder T: Newer neuromuscular blocking agents: how do they compare with established agents? Drugs. 2001;61(7):919-42. [PubMed:11434449 ]
  6. Hemmerling TM, Russo G, Bracco D: Neuromuscular blockade in cardiac surgery: an update for clinicians. Ann Card Anaesth. 2008 Jul-Dec;11(2):80-90. [PubMed:18603747 ]
External Links
ATC CodesM03AC09
AHFS Codes
  • 12:20.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (46.3 KB)
Interactions
Drug Interactions
Drug
AmikacinAmikacin may increase the activities of Rocuronium.
AmlodipineAmlodipine may increase the neuromuscular blocking activities of Rocuronium.
AmrinoneAmrinone may increase the neuromuscular blocking activities of Rocuronium.
ArbekacinArbekacin may increase the activities of Rocuronium.
BepridilBepridil may increase the neuromuscular blocking activities of Rocuronium.
Botulinum Toxin Type ABotulinum Toxin Type A may increase the neuromuscular blocking activities of Rocuronium.
Botulinum Toxin Type BRocuronium may increase the neuromuscular blocking activities of Botulinum Toxin Type B.
CapreomycinCapreomycin may increase the neuromuscular blocking activities of Rocuronium.
ClindamycinClindamycin may increase the neuromuscular blocking activities of Rocuronium.
ColistimethateColistimethate may increase the neuromuscular blocking activities of Rocuronium.
CyclosporineCyclosporine may increase the neuromuscular blocking activities of Rocuronium.
DigoxinRocuronium may increase the arrhythmogenic activities of Digoxin.
FelodipineFelodipine may increase the neuromuscular blocking activities of Rocuronium.
FludrocortisoneRocuronium may increase the adverse neuromuscular activities of Fludrocortisone.
FlunarizineFlunarizine may increase the neuromuscular blocking activities of Rocuronium.
FramycetinFramycetin may increase the activities of Rocuronium.
GabapentinGabapentin may increase the neuromuscular blocking activities of Rocuronium.
GentamicinGentamicin may increase the activities of Rocuronium.
IsofluraneIsoflurane may increase the neuromuscular blocking activities of Rocuronium.
IsradipineIsradipine may increase the neuromuscular blocking activities of Rocuronium.
KanamycinKanamycin may increase the activities of Rocuronium.
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Rocuronium.
LamotrigineLamotrigine may increase the neuromuscular blocking activities of Rocuronium.
LercanidipineLercanidipine may increase the neuromuscular blocking activities of Rocuronium.
LincomycinLincomycin may increase the neuromuscular blocking activities of Rocuronium.
LithiumLithium may increase the neuromuscular blocking activities of Rocuronium.
Magnesium SulfateMagnesium Sulfate may increase the neuromuscular blocking activities of Rocuronium.
MinocyclineMinocycline may increase the neuromuscular blocking activities of Rocuronium.
NeomycinNeomycin may increase the activities of Rocuronium.
NetilmicinNetilmicin may increase the activities of Rocuronium.
NicardipineNicardipine may increase the neuromuscular blocking activities of Rocuronium.
NimodipineNimodipine may increase the neuromuscular blocking activities of Rocuronium.
NisoldipineNisoldipine may increase the neuromuscular blocking activities of Rocuronium.
NitrendipineNitrendipine may increase the neuromuscular blocking activities of Rocuronium.
OxytetracyclineOxytetracycline may increase the neuromuscular blocking activities of Rocuronium.
PerhexilinePerhexiline may increase the neuromuscular blocking activities of Rocuronium.
PhenytoinPhenytoin may decrease the neuromuscular blocking activities of Rocuronium.
Polymyxin B SulfatePolymyxin B Sulfate may increase the neuromuscular blocking activities of Rocuronium.
PrenylaminePrenylamine may increase the neuromuscular blocking activities of Rocuronium.
ProcainamideProcainamide may increase the neuromuscular blocking activities of Rocuronium.
QuinidineQuinidine may increase the neuromuscular blocking activities of Rocuronium.
QuinineQuinine may increase the neuromuscular blocking activities of Rocuronium.
RibostamycinRibostamycin may increase the activities of Rocuronium.
RisedronateRisedronate may increase the neuromuscular blocking activities of Rocuronium.
SpectinomycinSpectinomycin may increase the activities of Rocuronium.
SpironolactoneSpironolactone may increase the neuromuscular blocking activities of Rocuronium.
StreptomycinStreptomycin may increase the activities of Rocuronium.
TacrineTacrine may decrease the neuromuscular blocking activities of Rocuronium.
TobramycinTobramycin may increase the activities of Rocuronium.
TorasemideTorasemide may decrease the neuromuscular blocking activities of Rocuronium.
VancomycinVancomycin may increase the neuromuscular blocking activities of Rocuronium.
VerapamilVerapamil may increase the neuromuscular blocking activities of Rocuronium.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Drug binding
Specific Function:
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
Gene Name:
CHRNA2
Uniprot ID:
Q15822
Molecular Weight:
59764.82 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. Jonsson Fagerlund M, Dabrowski M, Eriksson LI: Pharmacological characteristics of the inhibition of nondepolarizing neuromuscular blocking agents at human adult muscle nicotinic acetylcholine receptor. Anesthesiology. 2009 Jun;110(6):1244-52. doi: 10.1097/ALN.0b013e31819fade3. [PubMed:19417616 ]
  4. Jonsson M, Gurley D, Dabrowski M, Larsson O, Johnson EC, Eriksson LI: Distinct pharmacologic properties of neuromuscular blocking agents on human neuronal nicotinic acetylcholine receptors: a possible explanation for the train-of-four fade. Anesthesiology. 2006 Sep;105(3):521-33. [PubMed:16931985 ]
  5. Liu M, Dilger JP: Synergy between pairs of competitive antagonists at adult human muscle acetylcholine receptors. Anesth Analg. 2008 Aug;107(2):525-33. doi: 10.1213/ane.0b013e31817b4469. [PubMed:18633030 ]
  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
yes
Actions
antagonist
General Function:
G-protein coupled acetylcholine receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51714.605 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. Milchert M, Spassov A, Meissner K, Nedeljkov V, Lehmann C, Wendt M, Loster BW, Mazurkiewicz-Janik M, Gedrange T, Pavlovic D: Skeletal muscle relaxants inhibit rat tracheal smooth muscle tone in vitro. J Physiol Pharmacol. 2009 Dec;60 Suppl 8:5-11. [PubMed:20400785 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Voltage-gated potassium channel activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel.
Gene Name:
HTR3A
Uniprot ID:
P46098
Molecular Weight:
55279.835 Da
References
  1. Min KT, Wu CL, Yang J: Nondepolarizing neuromuscular blockers inhibit the serotonin-type 3A receptor expressed in Xenopus oocytes. Anesth Analg. 2000 Feb;90(2):476-81. [PubMed:10648343 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. van Montfoort JE, Muller M, Groothuis GM, Meijer DK, Koepsell H, Meier PJ: Comparison of "type I" and "type II" organic cation transport by organic cation transporters and organic anion-transporting polypeptides. J Pharmacol Exp Ther. 2001 Jul;298(1):110-5. [PubMed:11408531 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibited by the grapefruit juice component naringin.
Gene Name:
SLCO1A2
Uniprot ID:
P46721
Molecular Weight:
74144.105 Da
References
  1. van Montfoort JE, Hagenbuch B, Fattinger KE, Muller M, Groothuis GM, Meijer DK, Meier PJ: Polyspecific organic anion transporting polypeptides mediate hepatic uptake of amphipathic type II organic cations. J Pharmacol Exp Ther. 1999 Oct;291(1):147-52. [PubMed:10490898 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on January 15, 2016 17:38