Rocuronium
Explore a selection of our essential drug information below, or:
Overview
- Description
- A medication used in surgery to relax the muscles.
- Description
- A medication used in surgery to relax the muscles.
- DrugBank ID
- DB00728
- Type
- Small Molecule
- Clinical Trials
- Phase 0
- 4
- Phase 1
- 2
- Phase 2
- 20
- Phase 3
- 46
- Phase 4
- 109
- Mechanism of Action
- Neuronal acetylcholine receptor subunit alpha-2Antagonist
- Muscarinic acetylcholine receptor M2Antagonist
- Neuronal acetylcholine receptor subunit alpha-2
Identification
- Summary
Rocuronium is a vecuronium analog used to facilitate tracheal intubation and to relax skeletal muscles during surgery.
- Generic Name
- Rocuronium
- DrugBank Accession Number
- DB00728
- Background
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 commonly marketed under the trade names Zemuron and Esmeron. The drug is associated with the risk of developing allergic reactions in some high-risk patients, such as those with asthma. However, there was a similar incidence of allergic reactions associated with other non-depolarizing neuromuscular blocking agents. Sugammadex is a γ-cyclodextrin derivative that has been introduced as a novel agent to reverse the action of rocuronium.
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 529.7742
Monoisotopic: 529.400533194 - Chemical Formula
- C32H53N2O4
- Synonyms
- Rocuronio
- Rocuronium
- External IDs
- ORG 9426
Pharmacology
- Indication
For 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.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Prophylaxis of Muscle fasciculation caused by succinylcholine ••• ••••• - Associated Therapies
- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Neuromuscular 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 action
Rocuronium 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.
Target Actions Organism ANeuronal acetylcholine receptor subunit alpha-2 antagonistHumans AMuscarinic acetylcholine receptor M2 antagonistHumans U5-hydroxytryptamine receptor 3A antagonistHumans - Absorption
Poorly 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 binding
Approximately 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.
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- Route of elimination
Studies of distribution, metabolism, and excretion in cats and dogs indicate that rocuronium is eliminated primarily by the liver.
- Half-life
The 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]
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
No 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.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Rocuronium is combined with 1,2-Benzodiazepine. Acetazolamide The risk or severity of CNS depression can be increased when Rocuronium is combined with Acetazolamide. Acetophenazine The risk or severity of CNS depression can be increased when Rocuronium is combined with Acetophenazine. Acetylcholine The risk or severity of adverse effects can be increased when Rocuronium is combined with Acetylcholine. Acetyldigitoxin The risk or severity of Cardiac Arrhythmia can be increased when Rocuronium is combined with Acetyldigitoxin. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Rocuronium bromide I65MW4OFHZ 119302-91-9 OYTJKRAYGYRUJK-FMCCZJBLSA-M - International/Other Brands
- Esmeron
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Injectable Rocuronium Bromide Solution 10 mg / mL Intravenous Omega Laboratories Ltd Not applicable Not applicable Canada Rocuronium Bromide Injection, solution 10 mg/1mL Intravenous Cantrell Drug Company 2015-01-29 2017-12-06 US Rocuronium Bromide Injection Solution 10 mg / mL Intravenous Hikma Canada Limited 2023-09-29 Not applicable Canada Rocuronium Bromide Injection Solution 10 mg / mL Intravenous Pfizer Italia S.R.L. 2009-02-10 Not applicable Canada Rocuronium Bromide Injection Solution 10 mg / mL Intravenous Jamp Pharma Corporation 2024-02-26 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Rocuronium Injection, solution 100 mg/10mL Intravenous Piramal Critical Care Italia S.P.A. 2020-07-20 Not applicable US Rocuronium Injection, solution 10 mg/1mL Intravenous Fresenius Kabi Italia S.R.L. 2022-03-07 Not applicable US Rocuronium Injection, solution 10 mg/1mL Intravenous The Medicines Company 2009-12-13 2015-03-31 US Rocuronium Injection, solution 10 mg/1mL Intravenous Fresenius Kabi Italia S.R.L. 2009-12-13 Not applicable US Rocuronium Injection, solution 10 mg/1mL Intravenous Phlow Corporation 2022-02-08 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Rocuronium Bromide Rocuronium bromide (10 mg/1mL) Injection, solution Intravenous Cantrell Drug Company 2015-01-29 2017-12-06 US
Categories
- ATC Codes
- M03AC09 — Rocuronium bromide
- Drug Categories
- Agents producing tachycardia
- Androstanes
- Androstanols
- Anticholinergic Agents
- Central Nervous System Depressants
- Fused-Ring Compounds
- Muscarinic Antagonists
- Muscle Relaxants
- Muscle Relaxants, Peripherally Acting Agents
- Musculo-Skeletal System
- Neuromuscular Agents
- Neuromuscular Blocking Agents
- Neuromuscular Nondepolarizing Blockade
- Neuromuscular-Blocking Agents (Nondepolarizing)
- Nicotinic Antagonists
- OCT1 inhibitors
- OCT1 substrates
- Peripheral Nervous System Agents
- Steroids
- Chemical TaxonomyProvided by Classyfire
- Description
- This 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.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Steroid esters
- Direct Parent
- Steroid esters
- Alternative Parents
- Androgens and derivatives / 3-alpha-hydroxysteroids / N-alkylpyrrolidines / Morpholines / Tetraalkylammonium salts / Trialkylamines / Secondary alcohols / 1,2-aminoalcohols / Amino acids and derivatives / Cyclic alcohols and derivatives show 11 more
- Substituents
- 1,2-aminoalcohol / 3-alpha-hydroxysteroid / 3-hydroxysteroid / Alcohol / Aliphatic heteropolycyclic compound / Amine / Amino acid or derivatives / Androgen-skeleton / Androstane-skeleton / Azacycle show 29 more
- Molecular Framework
- Aliphatic heteropolycyclic compounds
- External Descriptors
- quaternary ammonium ion, androstane, 3alpha-hydroxy steroid (CHEBI:8884)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- WRE554RFEZ
- CAS number
- 143558-00-3
- InChI Key
- 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-[(1R,2S,3aS,3bR,5aS,7S,8S,9aS,9bS,11aS)-1-(acetyloxy)-7-hydroxy-9a,11a-dimethyl-8-(morpholin-4-yl)-hexadecahydro-1H-cyclopenta[a]phenanthren-2-yl]-1-(prop-2-en-1-yl)pyrrolidin-1-ium
- SMILES
- [H][C@@]12C[C@@H]([C@H](OC(C)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CC[C@@]2([H])C[C@H](O)[C@H](C[C@]12C)N1CCOCC1)[N+]1(CC=C)CCCC1
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
- Agoston S, Vandenbrom RH, Wierda JM: Clinical pharmacokinetics of neuromuscular blocking drugs. Clin Pharmacokinet. 1992 Feb;22(2):94-115. [Article]
- Khuenl-Brady KS, Sparr H: Clinical pharmacokinetics of rocuronium bromide. Clin Pharmacokinet. 1996 Sep;31(3):174-83. [Article]
- Alvarez-Gomez JA: [Rocuronium]. Rev Esp Anestesiol Reanim. 1997 Oct;44(8):310-4. [Article]
- Wicks TC: The pharmacology of rocuronium bromide (ORG 9426). AANA J. 1994 Feb;62(1):33-8. [Article]
- Sparr HJ, Beaufort TM, Fuchs-Buder T: Newer neuromuscular blocking agents: how do they compare with established agents? Drugs. 2001;61(7):919-42. [Article]
- 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. [Article]
- FDA Approved Drug Products: ZEMURON (rocuronium bromide) injection [Link]
- External Links
- Human Metabolome Database
- HMDB0014866
- KEGG Drug
- D00765
- KEGG Compound
- C07556
- PubChem Compound
- 441290
- PubChem Substance
- 46506855
- ChemSpider
- 390053
- 68139
- ChEBI
- 8884
- ChEMBL
- CHEMBL1201244
- ZINC
- ZINC000053229445
- Therapeutic Targets Database
- DAP000349
- PharmGKB
- PA164754992
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- RBR
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Rocuronium_bromide
- PDB Entries
- 8esk / 8f2s / 8s4h / 8s4k
- MSDS
- Download (46.3 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package
Pharmacoeconomics
- Manufacturers
- App pharmaceuticals llc
- Bioniche pharma usa llc
- Hospira inc
- Sagent pharmaceuticals inc
- Sandoz canada inc
- Teva parenteral medicines inc
- Schering corp
- Packagers
- Baxter International Inc.
- Generamedix Inc.
- Gland Pharma Ltd.
- Hospira Inc.
- Organon Pharmaceuticals
- Sandoz
- Teva Pharmaceutical Industries Ltd.
- Dosage Forms
Form Route Strength Solution Intravenous 25 mg Solution Intravenous 10 mg Solution Intravenous 50 mg Solution 50 mg/5ml Solution 50.000 mg Solution Parenteral 50.00 mg Solution Parenteral 50.000 mg Injection Intravenous 50 mg Injection, solution Intravenous 100 mg Injection, solution Intravenous 50 mg Solution Parenteral 250 mg Injection Intravenous Solution Intravenous 50 mg/5ml Injection Intravenous 10 mg/ml Injection, solution Intravenous bolus 50 mg/5ml Injection, solution Solution Intravenous 50.000 mg Injection, solution 50 mg/5ml Solution Intravenous 100 mg Injection, solution Parenteral 10 MG/ML Injection, solution Intravenous bolus; Intravenous drip 10 MG/ML Solution Parenteral 50 mg Solution 10 mg/ml Injection Intravenous 10 mg/1mL Injection Intravenous 100 mg/10mL Injection Intravenous 50 mg/5mL Injection, solution Intravenous 10 mg/1mL Injection, solution Intravenous 100 mg/10mL Injection, solution Intravenous 50 mg/5mL Solution Intravenous 10 mg/1mL Solution Intravenous 10 mg / mL Solution 10 mg/1ml Injection, solution Intravenous Injection, solution Intravenous 10 mg/ml Solution Intravenous 10 mg/ml Injection Parenteral 10 mg/ml Injection, solution 10 mg/1ml Solution Intravenous 25.000 mg - Prices
Unit description Cost Unit Zemuron 10 mg/ml vial 4.62USD ml Rocuronium 100 mg/10 ml vial 2.66USD ml Rocuronium 50 mg/5 ml vial 1.08USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Complete Not Available - Predicted Properties
Property Value Source Water Solubility 2.84e-05 mg/mL ALOGPS logP 2.71 ALOGPS logP -0.33 Chemaxon logS -7.3 ALOGPS pKa (Strongest Acidic) 14.59 Chemaxon pKa (Strongest Basic) 7.96 Chemaxon Physiological Charge 2 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 59 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 161.65 m3·mol-1 Chemaxon Polarizability 62.78 Å3 Chemaxon Number of Rings 6 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.9444 Blood Brain Barrier + 0.8569 Caco-2 permeable - 0.5336 P-glycoprotein substrate Substrate 0.8559 P-glycoprotein inhibitor I Inhibitor 0.7889 P-glycoprotein inhibitor II Inhibitor 0.9009 Renal organic cation transporter Non-inhibitor 0.7222 CYP450 2C9 substrate Non-substrate 0.8008 CYP450 2D6 substrate Non-substrate 0.7534 CYP450 3A4 substrate Substrate 0.7272 CYP450 1A2 substrate Non-inhibitor 0.9103 CYP450 2C9 inhibitor Non-inhibitor 0.8856 CYP450 2D6 inhibitor Non-inhibitor 0.8763 CYP450 2C19 inhibitor Non-inhibitor 0.8423 CYP450 3A4 inhibitor Non-inhibitor 0.8582 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9119 Ames test Non AMES toxic 0.7601 Carcinogenicity Non-carcinogens 0.9353 Biodegradation Not ready biodegradable 0.946 Rat acute toxicity 2.9310 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8607 hERG inhibition (predictor II) Non-inhibitor 0.8146
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-001i-1439520000-efed63eab6ab3907f152 - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 228.90265 predictedDeepCCS 1.0 (2019) [M+H]+ 230.79805 predictedDeepCCS 1.0 (2019) [M+Na]+ 236.5675 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General 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
- Specific Function
- acetylcholine receptor activity
- Gene Name
- CHRNA2
- Uniprot ID
- Q15822
- Uniprot Name
- Neuronal acetylcholine receptor subunit alpha-2
- Molecular Weight
- 59764.82 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General 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 triggers calcium ion release into the cytosol
- Specific Function
- arrestin family protein binding
- Gene Name
- CHRM2
- Uniprot ID
- P08172
- Uniprot Name
- Muscarinic acetylcholine receptor M2
- Molecular Weight
- 51714.605 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Forms serotonin (5-hydroxytryptamine/5-HT3)-activated cation-selective channel complexes, which when activated cause fast, depolarizing responses in neurons
- Specific Function
- excitatory extracellular ligand-gated monoatomic ion channel activity
- Gene Name
- HTR3A
- Uniprot ID
- P46098
- Uniprot Name
- 5-hydroxytryptamine receptor 3A
- Molecular Weight
- 55279.835 Da
References
- 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. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics (PubMed:11388889, PubMed:11408531, PubMed:12439218, PubMed:12719534, PubMed:15389554, PubMed:16263091, PubMed:16272756, PubMed:16581093, PubMed:19536068, PubMed:21128598, PubMed:23680637, PubMed:24961373, PubMed:34040533, PubMed:9187257, PubMed:9260930, PubMed:9655880). Functions as a pH- and Na(+)-independent, bidirectional transporter (By similarity). Cation cellular uptake or release is driven by the electrochemical potential (i.e. membrane potential and concentration gradient) and substrate selectivity (By similarity). Hydrophobicity is a major requirement for recognition in polyvalent substrates and inhibitors (By similarity). Primarily expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (By similarity). Most likely functions as an uptake carrier in enterocytes contributing to the intestinal elimination of organic cations from the systemic circulation (PubMed:16263091). Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, histamine, neurotransmitters dopamine, serotonin and adrenaline (PubMed:12439218, PubMed:24961373, PubMed:35469921, PubMed:9260930). Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover (PubMed:21128598). Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism (PubMed:24961373). Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium (PubMed:15817714). Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with lower efficency (PubMed:17460754). Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) (PubMed:11907186). May contribute to the transport of cationic compounds in testes across the blood-testis-barrier (Probable). Also involved in the uptake of xenobiotics tributylmethylammonium (TBuMA), quinidine, N-methyl-quinine (NMQ), N-methyl-quinidine (NMQD) N-(4,4-azo-n-pentyl)-quinuclidine (APQ), azidoprocainamide methoiodide (AMP), N-(4,4-azo-n-pentyl)-21-deoxyajmalinium (APDA) and 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) (PubMed:11408531, PubMed:15389554, PubMed:35469921, PubMed:9260930)
- Specific Function
- (R)-carnitine transmembrane transporter activity
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
References
- 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. [Article]
- Lozano E, Herraez E, Briz O, Robledo VS, Hernandez-Iglesias J, Gonzalez-Hernandez A, Marin JJ: Role of the plasma membrane transporter of organic cations OCT1 and its genetic variants in modern liver pharmacology. Biomed Res Int. 2013;2013:692071. doi: 10.1155/2013/692071. Epub 2013 Jul 31. [Article]
- Wagner DJ, Hu T, Wang J: Polyspecific organic cation transporters and their impact on drug intracellular levels and pharmacodynamics. Pharmacol Res. 2016 Sep;111:237-246. doi: 10.1016/j.phrs.2016.06.002. Epub 2016 Jun 16. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Na(+)-independent transporter that mediates the cellular uptake of a broad range of organic anions such as the endogenous bile salts cholate and deoxycholate, either in their unconjugated or conjugated forms (taurocholate and glycocholate), at the plasmam membrane (PubMed:19129463, PubMed:7557095). Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) (PubMed:11159893, PubMed:12568656, PubMed:19129463, PubMed:23918469, PubMed:25560245, PubMed:9539145). Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision (PubMed:25560245). Involved in the uptake of clinically used drugs (PubMed:17301733, PubMed:20686826, PubMed:27777271). Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) (PubMed:19129463, PubMed:20358049). Also transports prostaglandin E2 (PubMed:19129463). Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons (PubMed:25132355). May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel (PubMed:23243220). Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment (PubMed:19129463). Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions (PubMed:19129463). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
- Specific Function
- bile acid transmembrane transporter activity
- Gene Name
- SLCO1A2
- Uniprot ID
- P46721
- Uniprot Name
- Solute carrier organic anion transporter family member 1A2
- Molecular Weight
- 74144.105 Da
References
- 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. [Article]
Drug created at June 13, 2005 13:24 / Updated at November 09, 2024 06:17