Identification
- Summary
-
Riluzoleis a glutamate antagonist used to treat amyotrophic lateral sclerosis.
- Brand Names
-
Exservan, Rilutek, Tiglutik
- 总的来说ic Name
- Riluzole
- DrugBank Accession Number
- DB00740
- Background
-
一个glutamate antagonist (receptors, glutamate) used as an anticonvulsant (anticonvulsants) and to prolong the survival of patients with amyotrophic lateral sclerosis. Riluzole is marketed as Rilutek by Sanofi.
- Type
- Small Molecule
- Groups
- 一个pproved, Investigational
- Structure
-
Structure for Riluzole (DB00740)
- Weight
-
一个verage: 234.198
Monoisotopic: 234.007468097 - Chemical Formula
- C8H5F3N2OS
- Synonyms
-
- Riluzol
- Riluzole
- Riluzolum
- External IDs
-
- PK 26124
- RP 54274
- RPR 202
Pharmacology
- Indication
-
For the treatment of amyotrophic lateral sclerosis (ALS, Lou Gehrig's Disease)
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with evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets. - 一个ssociated Conditions
- Contraindications & Blackbox Warnings
-
一个void life-threatening adverse drug eventsImprove clinical decision support with information oncontraindications & blackbox warnings, population restrictions, harmful risks, & more.一个void life-threatening adverse drug events & improve clinical decision support. - Pharmacodynamics
-
Riluzole, a member of the benzothiazole class, is indicated for the treatment of patients with amyotrophic lateral sclerosis (ALS). Riluzole extends survival and/or time to tracheostomy. It is also neuroprotective in various在活的有机体内experimental models of neuronal injury involving excitotoxic mechanisms. The etiology and pathogenesis of amyotrophic lateral sclerosis (ALS) are not known, although a number of hypotheses have been advanced. One hypothesis is that motor neurons, made vulnerable through either genetic predisposition or environmental factors, are injured by glutamate. In some cases of familial ALS the enzyme superoxide dismutase has been found to be defective.
- Mechanism of action
-
The mode of action of riluzole is unknown. Its pharmacological properties include the following, some of which may be related to its effect: 1) an inhibitory effect on glutamate release (activation of glutamate reuptake), 2) inactivation of voltage-dependent sodium channels, and 3) ability to interfere with intracellular events that follow transmitter binding at excitatory amino acid receptors.
Target 一个ctions Organism 一个Sodium channel protein type 5 subunit alpha inhibitorHumans 一个Cystine/glutamate transporter inducerHumans - 一个bsorption
-
Riluzole is well-absorbed (approximately 90%), with average absolute oral bioavailability of about 60% (CV=30%). A high fat meal decreases absorption, reducing AUC by about 20% and peak blood levels by about 45%.
- Volume of distribution
-
Not Available
- Protein binding
-
96% bound to plasma proteins, mainly to albumin and lipoprotein over the clinical concentration range.
- Metabolism
-
Riluzole is extensively metabolized to six major and a number of minor metabolites, which have not all been identified to date. Metabolism is mostly hepatic, consisting of cytochrome P450–dependent hydroxylation and glucuronidation. CYP1A2 is the primary isozyme involved in N-hydroxylation; CYP2D6, CYP2C19, CYP3A4, and CYP2E1 are considered unlikely to contribute significantly to riluzole metabolism in humans.
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- Route of elimination
-
Not Available
- Half-life
-
The mean elimination half-life of riluzole is 12 hours (CV=35%) after repeated doses.
- Clearance
-
Not Available
- 一个dverse Effects
-
Improve decision support & research outcomesWith structured adverse effects data, including:blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data. - Toxicity
-
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug InteractionsLearn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
-
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 adverse effects can be increased when Riluzole is combined with 1,2-Benzodiazepine. 一个bametapir The serum concentration of Riluzole can be increased when it is combined with Abametapir. 一个batacept The metabolism of Riluzole can be increased when combined with Abatacept. 一个bemaciclib 一个bemaciclib may decrease the excretion rate of Riluzole which could result in a higher serum level. 一个biraterone The serum concentration of Riluzole can be increased when it is combined with Abiraterone. 一个cenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Riluzole. 一个cetaminophen The metabolism of Riluzole can be decreased when combined with Acetaminophen. 一个cetazolamide The risk or severity of adverse effects can be increased when Riluzole is combined with Acetazolamide. 一个cetophenazine The risk or severity of adverse effects can be increased when Riluzole is combined with Acetophenazine. 一个clidinium Riluzole may increase the central nervous system depressant (CNS depressant) activities of Aclidinium. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
-
- Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.
Products
-
Drug product information from 10+ global regionsOur datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.一个ccess drug product information from over 10 global regions. - Product Ingredients
-
Ingredient UNII CAS InChI Key Riluzole Hydrochloride Not Available Not Available QEAOELIJQRYJJS-UHFFFAOYSA-N - Product Images
-
- International/Other Brands
- Fanizan (Actavis)/Laidec (Sun Pro)/Lizolorol (Actavis)/Lizorolol (ratiopharm)/Rilustad (STADA)/Sclefic (Actavis)/Xie Yi Li (Lunan Pharm)/Zolerilis (Actavis)
- Brand Name Prescription Products
-
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Exservan Film 50 mg/1 Oral Mitsubishi Tanabe Pharma America, Inc. 2021-05-01 Not applicable US 
Exservan Film 50 mg/1 Oral 一个questive Therapeutics 2019-01-24 Not applicable US Exservan Film 50 mg/1 Oral Mitsubishi Tanabe Pharma America, Inc. 2021-05-01 Not applicable US Rilutek Tablet 50 mg/1 Oral Covis Pharmaceuticals, Inc. 2013-07-15 2017-12-13 US Rilutek Tablet, film coated 50 mg Oral Sanofi Mature Ip 2016-09-08 Not applicable EU 
Rilutek Tablet 50 mg Oral Sanofi Aventis 2000-10-26 Not applicable Canada 
Rilutek Tablet 50 mg/1 Oral KAISER FOUNDATION HOSPITALS 2014-01-20 2014-12-31 US Rilutek Tablet 50 mg/1 Oral Covis Pharma US, Inc 2016-08-01 Not applicable US Rilutek Tablet, film coated 50 mg/1 Oral sanofi-aventis U.S. LLC 1995-12-12 2015-06-30 US 
Riluzole Zentiva Tablet, film coated 50 mg Oral Zentiva K.S. 2016-09-08 Not applicable EU - 总的来说ic Prescription Products
-
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image 一个po-riluzole Tablet 50 mg Oral 一个potex Corporation 2012-09-25 Not applicable Canada Mylan-riluzole Tablet 50 mg Oral Mylan Pharmaceuticals 2012-10-23 Not applicable Canada Riluzole Tablet, film coated 50 mg/1 Oral 一个v Kare, Inc. 2014-01-08 2016-08-04 US Riluzole Tablet, film coated 50 mg/1 Oral Florida Pharmaceutical Products, LLC. 2020-01-01 Not applicable US Riluzole Tablet, film coated 50 mg/1 Oral 一个potex Corp 2013-06-18 2021-10-31 US Riluzole Tablet 50 mg/1 Oral Quinn Pharmaceuticals, Llc 2019-01-14 Not applicable US Riluzole Tablet 50 mg/1 Oral 一个scend Laboratories, LLC 2016-03-31 Not applicable US Riluzole Tablet, film coated 50 mg/1 Oral KAISER FOUNDATION HOSPITALS 2014-05-14 2016-11-30 US Riluzole Tablet, film coated 50 mg/1 Oral 一个merican Health Packaging 2015-03-31 2020-10-31 US Riluzole Tablet, film coated 50 mg/1 Oral Mylan Pharmaceuticals Inc. 2013-07-22 Not applicable US
Categories
- 一个TC Codes
- N07XX02 — Riluzole
- Drug Categories
-
- 一个nticonvulsants
- BCRP/ABCG2 Substrates
- Benzothiazoles
- Central Nervous System Agents
- Central Nervous System Depressants
- Compounds used in a research, industrial, or household setting
- Cytochrome P-450 CYP1A2 Substrates
- 细胞色素p - 450基质
- Excitatory Amino Acid Agents
- Excitatory Amino Acid Antagonists
- Heterocyclic Compounds, Fused-Ring
- Miscellaneous Central Nervous System Agents
- Nervous System
- Neuroprotective Agents
- Neurotransmitter Agents
- Protective Agents
- Sulfur Compounds
- Thiazoles
- Chemical TaxonomyProvided byClassyfire
-
- Description
- This compound belongs to the class of organic compounds known as benzothiazoles. These are organic compounds containing a benzene fused to a thiazole ring (a five-membered ring with four carbon atoms, one nitrogen atom and one sulfur atom).
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Benzothiazoles
- Sub Class
- Not Available
- Direct Parent
- Benzothiazoles
- 一个lternative Parents
- Benzenoids/2-amino-1,3-thiazoles/Heteroaromatic compounds/Trihalomethanes/一个zacyclic compounds/Primary amines/Organopnictogen compounds/Organooxygen compounds/Organofluorides/Hydrocarbon derivatives show 1 more
- Substituents
- 1,3-benzothiazole/1,3-thiazol-2-amine/一个lkyl fluoride/一个lkyl halide/一个mine/一个romatic heteropolycyclic compound/一个zacycle/一个zole/Benzenoid/Halomethane show 12 more
- Molecular Framework
- 芳香heteropolycyclic化合物
- External Descriptors
- benzothiazoles (CHEBI:8863)
- 一个ffected organisms
-
- Humans and other mammals
Chemical Identifiers
- UNII
- 7LJ087RS6F
- CAS number
- 1744-22-5
- InChI Key
- FTALBRSUTCGOEG-UHFFFAOYSA-N
- InChI
-
InChI=1S/C8H5F3N2OS/c9-8(10,11)14-4-1-2-5-6(3-4)15-7(12)13-5/h1-3H,(H2,12,13)
- IUPAC Name
-
6-(trifluoromethoxy)-1,3-benzothiazol-2-amine
- SMILES
-
NC1=NC2=C(S1)C=C(OC(F)(F)F)C=C2
References
- Synthesis Reference
-
Pratap Padi, Madhusudhan Ganta, Satyanarayana Bollikonda, Sridhar Chaganti, Ramulu Akula, Loka Maheshwari Dommati, "PROCESS FOR PREPARING RILUZOLE." U.S. Patent US20080108827, issued May 08, 2008.
US20080108827 - 总的来说al References
-
- Song JH, Huang CS, Nagata K, Yeh JZ, Narahashi T: Differential action of riluzole on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels. J Pharmacol Exp Ther. 1997 Aug;282(2):707-14. [一个rticle]
- Coric V, Taskiran S, Pittenger C, Wasylink S, Mathalon DH, Valentine G, Saksa J, Wu YT, Gueorguieva R, Sanacora G, Malison RT, Krystal JH: Riluzole augmentation in treatment-resistant obsessive-compulsive disorder: an open-label trial. Biol Psychiatry. 2005 Sep 1;58(5):424-8. [一个rticle]
- van Kan HJ, Groeneveld GJ, Kalmijn S, Spieksma M, van den Berg LH, Guchelaar HJ: Association between CYP1A2 activity and riluzole clearance in patients with amyotrophic lateral sclerosis. Br J Clin Pharmacol. 2005 Mar;59(3):310-3. [一个rticle]
- Zarate CA Jr, Payne JL, Quiroz J, Sporn J, Denicoff KK, Luckenbaugh D, Charney DS, Manji HK: An open-label trial of riluzole in patients with treatment-resistant major depression. Am J Psychiatry. 2004 Jan;161(1):171-4. [一个rticle]
- Mathew SJ, Manji HK, Charney DS: Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. doi: 10.1038/sj.npp.1301652. Epub 2008 Jan 2. [一个rticle]
- Lamanauskas N, Nistri A: Riluzole blocks persistent Na+ and Ca2+ currents and modulates release of glutamate via presynaptic NMDA receptors on neonatal rat hypoglossal motoneurons in vitro. Eur J Neurosci. 2008 May;27(10):2501-14. doi: 10.1111/j.1460-9568.2008.06211.x. Epub 2008 Apr 26. [一个rticle]
- FDA Approved Drug Products: RILUTEK (riluzole) tablets [Link]
- FDA Approved Drug Products: EXSERVAN (riluzole) film [Link]
- FDA Approved Drug Products: TIGLUTIK (riluzole) suspension [Link]
- External Links
-
- Human Metabolome Database
- HMDB0014878
- KEGG Drug
- D00775
- KEGG Compound
- C07937
- PubChem Compound
- 5070
- PubChem Substance
- 46508094
- ChemSpider
- 4892
- BindingDB
- 30705
- 35623
- ChEBI
- 8863
- ChEMBL
- CHEMBL744
- ZINC
- ZINC000000006481
- Therapeutic Targets Database
- DAP000527
- PharmGKB
- PA451251
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- 657
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Riluzole
- PDB Entries
- 5v02/7bnj/7wdb
- FDA label
-
Download (125 KB)
- MSDS
-
Download (29.5 KB)
Clinical Trials
- Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
-
Phase Status Purpose Conditions Count 4 Completed Treatment 一个myotrophic Lateral Sclerosis (ALS) 1 4 Completed Treatment Fatigue/Inflammation 1 4 Completed Treatment Fragile X Syndrome (FXS) 1 4 Completed Treatment Gilles de la Tourette's Syndrome 1 4 Completed Treatment Major Depressive Disorder (MDD) 1 4 Terminated Treatment Memory Disturbances/Mood 1 3 Completed Other 一个myotrophic Lateral Sclerosis (ALS) 1 3 Completed Treatment Cervical Spondylotic Myelopathy 1 3 Completed Treatment Huntington's Disease (HD) 1 3 Completed Treatment Spinocerebellar Ataxia Type 2 1
Pharmacoeconomics
- Manufacturers
-
- Sanofi aventis us llc
- Impax laboratories inc
- Packagers
-
- Inyx Usa Ltd.
- Kaiser Foundation Hospital
- Sanofi-Aventis Inc.
- Southwood Pharmaceuticals
- Dosage Forms
-
Form Route Strength Film Oral 50 mg/1 Tablet, coated Oral 50 mg Tablet, film coated Oral 50 mg Tablet Oral 50 mg Tablet, film coated Oral Tablet Oral 50 mg/1 Tablet, film coated Oral 50 mg/1 Suspension Oral 5 MG/ML Suspension Oral Liquid Oral 50 mg/10mL - Prices
-
Unit description Cost Unit Rilutek 50 mg tablet 18.77USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only. - Patents
-
Patent Number Pediatric Extension 一个pproved Expires (estimated) Region US5527814 No 1996-06-18 2013-06-18 US CA2151604 No 2005-09-20 2013-12-10 Canada CA2117466 No 2000-01-25 2012-10-22 Canada US8603514 No 2013-12-10 2024-04-03 US US8765150 No 2014-07-01 2029-03-12 US US8765167 No 2014-07-01 2024-02-20 US
Properties
- State
- Solid
- Experimental Properties
-
Property Value Source melting point (°C) 119 °C Not Available logP 2.3 Not Available - Predicted Properties
-
Property Value Source Water Solubility 0.0395毫克/毫升 一个LOGPS logP 2.83 一个LOGPS logP 3.4 ChemAxon logS -3.8 一个LOGPS pKa (Strongest Acidic) 16.44 ChemAxon pKa (Strongest Basic) 4.57 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 48.14 Å2 ChemAxon Rotatable Bond Count 2 ChemAxon Refractivity 44.37 m3·mol-1 ChemAxon Polarizability 18.59 Å3 ChemAxon Number of Rings 2 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET Features
-
Property Value Probability Human Intestinal Absorption + 0.995 Blood Brain Barrier + 0.9799 Caco-2 permeable - 0.5377 P-glycoprotein substrate Non-substrate 0.8045 P-glycoprotein inhibitor I Non-inhibitor 0.8245 P-glycoprotein inhibitor II Non-inhibitor 0.6998 Renal organic cation transporter Non-inhibitor 0.859 CYP450 2C9 substrate Non-substrate 0.8679 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Non-substrate 0.7032 CYP450 1A2 substrate Inhibitor 0.9106 CYP450 2C9 inhibitor Non-inhibitor 0.9072 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.8332 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.6647 一个mes test 一个MES toxic 0.6799 Carcinogenicity Non-carcinogens 0.9001 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 3.6843 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9775 hERG inhibition (predictor II) Non-inhibitor 0.8734
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
-
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-000i-2590000000-5a9d0f7cdad7e4f2ec6b MS/MS Spectrum - , positive LC-MS/MS splash10-000i-0390000000-4bd44ae3d25f047943e8 MS/MS Spectrum - , positive LC-MS/MS splash10-000i-3940000000-1da38288b84e863a64e5
Targets
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Use our structured and evidence-based datasets tounlock new
insights and accelerate drug research.
insights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Yes
- 一个ctions
-
Inhibitor
- 总的来说al Function
- Voltage-gated sodium channel activity involved in sa node cell action potential
- Specific Function
- This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the pr...
- Gene Name
- SCN5A
- Uniprot ID
- Q14524
- Uniprot Name
- Sodium channel protein type 5 subunit alpha
- 分子量
- 226937.475 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. [一个rticle]
- 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. [一个rticle]
- 施瓦茨G,费林MG:第二ary injury mechanisms of spinal cord trauma: a novel therapeutic approach for the management of secondary pathophysiology with the sodium channel blocker riluzole. Prog Brain Res. 2002;137:177-90. [一个rticle]
- Song JH, Huang CS, Nagata K, Yeh JZ, Narahashi T: Differential action of riluzole on tetrodotoxin-sensitive and tetrodotoxin-resistant sodium channels. J Pharmacol Exp Ther. 1997 Aug;282(2):707-14. [一个rticle]
- Weiss S, Benoist D, White E, Teng W, Saint DA: Riluzole protects against cardiac ischaemia and reperfusion damage via block of the persistent sodium current. Br J Pharmacol. 2010 Jul;160(5):1072-82. doi: 10.1111/j.1476-5381.2010.00766.x. [一个rticle]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Yes
- 一个ctions
-
Inducer
- 总的来说al Function
- Cystine:glutamate antiporter activity
- Specific Function
- Sodium-independent, high-affinity exchange of anionic amino acids with high specificity for anionic form of cystine and glutamate.
- Gene Name
- SLC7A11
- Uniprot ID
- Q9UPY5
- Uniprot Name
- Cystine/glutamate transporter
- 分子量
- 55422.44 Da
References
- Wokke J: Riluzole. Lancet. 1996 Sep 21;348(9030):795-9. [一个rticle]
- 一个zbill RD, Mu X, Springer JE: Riluzole increases high-affinity glutamate uptake in rat spinal cord synaptosomes. Brain Res. 2000 Jul 21;871(2):175-80. [一个rticle]
- Dunlop J, Beal McIlvain H, She Y, Howland DS: Impaired spinal cord glutamate transport capacity and reduced sensitivity to riluzole in a transgenic superoxide dismutase mutant rat model of amyotrophic lateral sclerosis. J Neurosci. 2003 Mar 1;23(5):1688-96. [一个rticle]
- Gosselin RD, O'Connor RM, Tramullas M, Julio-Pieper M, Dinan TG, Cryan JF: Riluzole normalizes early-life stress-induced visceral hypersensitivity in rats: role of spinal glutamate reuptake mechanisms. Gastroenterology. 2010 Jun;138(7):2418-25. doi: 10.1053/j.gastro.2010.03.003. Epub 2010 Mar 10. [一个rticle]
- Hayashida K, Parker RA, Eisenach JC: Activation of glutamate transporters in the locus coeruleus paradoxically activates descending inhibition in rats. Brain Res. 2010 Mar 4;1317:80-6. doi: 10.1016/j.brainres.2009.12.086. Epub 2010 Jan 6. [一个rticle]
劳动部ymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- 一个ctions
-
Substrate
- 总的来说al Function
- Vitamin d 24-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A1
- Uniprot ID
- P04798
- Uniprot Name
- Cytochrome P450 1A1
- 分子量
- 58164.815 Da
References
- Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [一个rticle]
- Sanderink GJ, Bournique B, Stevens J, Petry M, Martinet M: Involvement of human CYP1A isoenzymes in the metabolism and drug interactions of riluzole in vitro. J Pharmacol Exp Ther. 1997 Sep;282(3):1465-72. [一个rticle]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- 一个ctions
-
Substrate
- 总的来说al Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- 分子量
- 58293.76 Da
References
- 一个jroud-Driss S, Saeed M, Khan H, Siddique N, Hung WY, Sufit R, Heller S, Armstrong J, Casey P, Siddique T, Lukas TJ: Riluzole metabolism and CYP1A1/2 polymorphisms in patients with ALS. Amyotroph Lateral Scler. 2007 Oct;8(5):305-9. doi: 10.1080/17482960701500650. [一个rticle]
- van Kan HJ, Groeneveld GJ, Kalmijn S, Spieksma M, van den Berg LH, Guchelaar HJ: Association between CYP1A2 activity and riluzole clearance in patients with amyotrophic lateral sclerosis. Br J Clin Pharmacol. 2005 Mar;59(3):310-3. [一个rticle]
- Flockhart Table of Drug Interactions [Link]
- Riluzole FDA label [File]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- 一个ctions
-
Substrate
- 总的来说al Function
- Xenobiotic-transporting atpase activity
- Specific Function
- High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
- Gene Name
- 一个BCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- 一个TP-binding cassette sub-family G member 2
- 分子量
- 72313.47 Da
References
- Milane A, Vautier S, Chacun H, Meininger V, Bensimon G, Farinotti R, Fernandez C: Interactions between riluzole and ABCG2/BCRP transporter. Neurosci Lett. 2009 Mar 6;452(1):12-6. doi: 10.1016/j.neulet.2008.12.061. Epub 2009 Jan 6. [一个rticle]
Drug created at June 13, 2005 13:24 / Updated at August 04, 2022 14:16