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Identification
Name Ropinirole
Accession Number DB00268 (APRD00302)
Type small molecule
Groups approved
Description

Ropinirole is a non-ergoline dopamine agonist, manufactured by GlaxoSmithKline. It is used in the treatment of Parkinson’s disease, and is also one of two medications in the United States with an FDA-approved indication for the treatment of restless legs syndrome (the other being Pramipexole). [Wikipedia]
Structure Thumb
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms
Ropinirol [INN-Spanish]
Ropinirole HCl
Ropinirole hydrochloride
Ropinirolum [INN-Latin]
Salts Not Available
Brand names
Name Company
Requip GlaxoSmithKline
ReQuip CR GlaxoSmithKline
ReQuip XL GlaxoSmithKline
Brand mixtures Not Available
Categories
  • Central Nervous System Agents
  • Antiparkinson Agents
  • Antidyskinetics
  • Dopamine Agonists
CAS number 91374-21-9
Weight Average: 260.3746
Monoisotopic: 260.1888634
Chemical Formula C16H24N2O
InChI Key InChIKey=UHSKFQJFRQCDBE-UHFFFAOYSA-N
InChI
InChI=1S/C16H24N2O/c1-3-9-18(10-4-2)11-8-13-6-5-7-15-14(13)12-16(19)17-15/h5-7H,3-4,8-12H2,1-2H3,(H,17,19)
Plain Text
IUPAC Name
4-[2-(dipropylamino)ethyl]-2,3-dihydro-1H-indol-2-one
SMILES
CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Organic
Classes
  • Indoles and Indole Derivatives
  • Phenethylamines
  • Lactams
Substructures
  • Indoles and Indole Derivatives
  • Amino Ketones
  • Benzene and Derivatives
  • Carboxylic Acids and Derivatives
  • Aliphatic and Aryl Amines
  • Phenethylamines
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Lactams
  • Anilines
  • Pyrrolines
Pharmacology
Indication For the treatment of the signs and symptoms of idiopathic Parkinson's disease. Also used for the treatment of restless legs syndrome.
Pharmacodynamics Ropinirole is a nonergot dopamine agonist with high relative in vitro specificity and full intrinsic activity at the D2 subfamily of dopamine receptors, binding with higher affinity to D3 than to D2 or D4 receptor subtypes. The relevance of D3 receptor binding in Parkinson's disease is unknown. The mechanism of ropinirole-induced postural hypotension is presumed to be due to a D2 -mediated blunting of the noradrenergic response to standing and subsequent decrease in peripheral vascular resistance.
Mechanism of action Ropinirole binds the dopamine receptors D3 and D2. Although the precise mechanism of action of ropinirole as a treatment for Parkinson's disease is unknown, it is believed to be related to its ability to stimulate these receptors in the striatum. This conclusion is supported by electrophysiologic studies in animals that have demonstrated that ropinirole influences striatal neuronal firing rates via activation of dopamine receptors in the striatum and the substantia nigra, the site of neurons that send projections to the striatum.
Absorption Absolute bioavailability is 55%, indicating a first pass effect. Food does not affect the extent of absorption.
Volume of distribution
  • 7.5 L/kg
  • 525 L
Protein binding 40% bound to plasma proteins with a blood-to-plasma ratio of 1:1.
Metabolism
Hepatic. Ropinirole is extensively metabolized to inactive metabolites via N -despropylation and hydroxylation pathways, largely by the P450 isoenzyme CYP1A2. N-despropyl ropinirole is the predominant metabolite found in urine (40%), followed by the carboxylic acid metabolite (10%), and the glucuronide of the hydroxy metabolite (10%).

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Ropinirole
    		N-despropyl ropinirole Details
    Route of elimination Ropinirole is extensively metabolized by the liver to inactive metabolites, and less than 10% of the administered dose is excreted as unchanged drug in urine.
    Half life 6 hours
    Clearance
    • 47 L/hr [after oral administration to Parkinson’s disease patients and patients with Restless Legs Syndrome]
    Toxicity Symptoms of overdose include agitation, chest pain, confusion, drowsiness, facial muscle movements, grogginess, increased jerkiness of movement, symptoms of low blood pressure (dizziness, light-headedness)upon standing, nausea, and vomiting.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    Pharmacoeconomics
    Manufacturers
    • Smithkline beecham corp dba glaxosmithkline
    • Glaxosmithkline
    • Alembic ltd
    • Corepharma llc
    • Glenmark generics ltd
    • Huahai us inc
    • Mylan pharmaceuticals inc
    • Roxane laboratories inc
    • Teva pharmaceuticals usa inc
    • Wockhardt ltd
    • Zydus pharmaceuticals usa inc
    Packagers
    Dosage forms
    Form Route Strength
    Tablet, film coated Oral 0.25 mg
    Tablet, film coated Oral 1 mg
    Tablet, film coated Oral 2 mg
    Tablet, film coated Oral 3 mg
    Tablet, film coated Oral 4 mg
    Tablet, film coated Oral 5 mg
    Prices
    Unit description Cost Unit
    Requip XL 12 mg 24 Hour tablet 14.92 USD tablet
    Requip xl 12 mg tablet 14.35 USD tablet
    Requip XL 8 mg 24 Hour tablet 8.96 USD tablet
    Requip xl 6 mg tablet 8.61 USD tablet
    Requip xl 8 mg tablet 8.61 USD tablet
    Requip XL 4 mg 24 Hour tablet 5.97 USD tablet
    Requip xl 4 mg tablet 5.74 USD tablet
    Requip 5 mg Tablet 3.87 USD tablet
    Requip 3 mg tablet 3.41 USD tablet
    Requip 4 mg tablet 3.41 USD tablet
    Requip 5 mg tablet 3.41 USD tablet
    Requip 0.25 mg tablet 3.29 USD tablet
    Requip 0.5 mg tablet 3.29 USD tablet
    Requip 1 mg tablet 3.29 USD tablet
    Requip 2 mg tablet 3.29 USD tablet
    Requip xl 2 mg tablet 2.87 USD tablet
    Ropinirole hcl 3 mg tablet 2.65 USD tablet
    Ropinirole hcl 4 mg tablet 2.65 USD tablet
    Ropinirole hcl 5 mg tablet 2.65 USD tablet
    Ropinirole hcl 0.25 mg tablet 2.55 USD tablet
    Ropinirole hcl 0.5 mg tablet 2.55 USD tablet
    Ropinirole hcl 1 mg tablet 2.55 USD tablet
    Ropinirole hcl 2 mg tablet 2.55 USD tablet
    Co Ropinirole 5 mg Tablet 1.8 USD tablet
    Pms-Ropinirole 5 mg Tablet 1.8 USD tablet
    Ran-Ropinirole 5 mg Tablet 1.8 USD tablet
    Ropinirole 5 mg Tablet 1.8 USD tablet
    Requip 2 mg Tablet 1.41 USD tablet
    Requip 1 mg Tablet 1.28 USD tablet
    Co Ropinirole 2 mg Tablet 0.65 USD tablet
    Pms-Ropinirole 2 mg Tablet 0.65 USD tablet
    Ran-Ropinirole 2 mg Tablet 0.65 USD tablet
    Ropinirole 2 mg Tablet 0.65 USD tablet
    Co Ropinirole 1 mg Tablet 0.59 USD tablet
    Pms-Ropinirole 1 mg Tablet 0.59 USD tablet
    Ran-Ropinirole 1 mg Tablet 0.59 USD tablet
    Ropinirole 1 mg Tablet 0.59 USD tablet
    Requip 0.25 mg Tablet 0.32 USD tablet
    Co Ropinirole 0.25 mg Tablet 0.15 USD tablet
    Pms-Ropinirole 0.25 mg Tablet 0.15 USD tablet
    Ran-Ropinirole 0.25 mg Tablet 0.15 USD tablet
    Ropinirole 0.25 mg Tablet 0.15 USD tablet
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    DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
    Patents
    Country Patent Number Approved Expires (estimated)
    United States 5422123 1995-06-06 2012-06-06
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 243-250 °C Not Available
    water solubility 133 mg/mL Not Available
    logP 2.70 ADLARD,M ET AL. (1995)
    Predicted Properties
    Property Value Source
    water solubility 3.53e-01 g/l ALOGPS
    logP 3.16 ALOGPS
    logP 3.06 ChemAxon
    logS -2.9 ALOGPS
    pKa (strongest acidic) 13.24 ChemAxon
    pKa (strongest basic) 10.17 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 2 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 32.34 ChemAxon
    rotatable bond count 7 ChemAxon
    refractivity 81.43 ChemAxon
    polarizability 31.19 ChemAxon
    References
    Synthesis Reference Not Available
    General Reference Not Available
    External Links
    Resource Link
    KEGG Compound C07564 Link_out
    PubChem Compound 5095 Link_out
    PubChem Substance 46507918 Link_out
    ChemSpider 4916 Link_out
    ChEBI 8888 Link_out
    ChEMBL 8888 Link_out
    Therapeutic Targets Database DAP001515 Link_out
    PharmGKB PA164749035 Link_out
    Drug Product Database 2232567 Link_out
    RxList http://www.rxlist.com/cgi/generic/ropinirole.htm Link_out
    Drugs.com http://www.drugs.com/cdi/ropinirole.html Link_out
    PDRhealth http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/req1372.shtml Link_out
    Wikipedia http://en.wikipedia.org/wiki/Ropinirole Link_out
    ATC Codes
    • N04BC04
    AHFS Codes
    • 28:36.20.08
    PDB Entries Not Available
    FDA label show (267 KB)
    MSDS show (29.6 KB)
    Interactions
    Drug Interactions
    Drug Interaction
    Ciprofloxacin Ciprofloxacin may increase the effect and toxicity of ropinirole.
    Fluvoxamine Increases the effect and toxicity of ropinirole
    Paliperidone The atypical antipsychotic agent, paliperidone, may decrease the therapeutic effect of the anti-Parkinson's agent, ropinirole. This interaction may be due to the dopamine antagonist properties of paliperidone. Consider an alternate antipsychotic in those with Parkinson's disease or consider using clozapine or quetiapine if an atypical antipsychotic is necessary.
    Thiothixene Thiothixene may antaonize the effects of the anti-Parkinsonian agent, Ropinirole. Consider alternate therapy or monitor for decreased effects of both agents.
    Ziprasidone The atypical antipsychotic, ziprasidone, may antagonize the effect of the dopamine agonist, ropinirole. Consider alternate therapy or monitor for worsening of movement disorder.
    Zuclopenthixol Antagonism may occur between zuclopenthixol, a dopamine D2 receptor antagonist, and ropinirole, a dopamine agonist. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of both agents if concurrent therapy is initiated, discontinued or dose(s) changed.
    Food Interactions Not Available
    Targets

    1. D(3) dopamine receptor

    Pharmacological action: yes
    Actions: agonist

    This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase

    Organism class: human
    UniProt ID: P35462 Link_out
    Gene: DRD3 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
    2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed
    3. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed

    2. D(2) dopamine receptor

    Pharmacological action: yes
    Actions: agonist

    This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase

    Organism class: human
    UniProt ID: P14416 Link_out
    Gene: DRD2 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
    2. de Mey C, Enterling D, Meineke I, Yeulet S: Interactions between domperidone and ropinirole, a novel dopamine D2-receptor agonist. Br J Clin Pharmacol. 1991 Oct;32(4):483-8. Pubmed
    3. Iida M, Miyazaki I, Tanaka K, Kabuto H, Iwata-Ichikawa E, Ogawa N: Dopamine D2 receptor-mediated antioxidant and neuroprotective effects of ropinirole, a dopamine agonist. Brain Res. 1999 Aug 14;838(1-2):51-9. Pubmed
    4. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed
    5. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed
    6. Matsukawa N, Maki M, Yasuhara T, Hara K, Yu G, Xu L, Kim KM, Morgan JC, Sethi KD, Borlongan CV: Overexpression of D2/D3 receptors increases efficacy of ropinirole in chronically 6-OHDA-lesioned Parkinsonian rats. Brain Res. 2007 Jul 30;1160:113-23. Epub 2007 May 26. Pubmed

    3. D(4) dopamine receptor

    Pharmacological action: unknown
    Actions: agonist

    This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase

    Organism class: human
    UniProt ID: P21917 Link_out
    Gene: DRD4 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
    2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed

    4. 5-hydroxytryptamine 1A receptor

    Pharmacological action: unknown
    Actions: agonist

    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. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity

    Organism class: human
    UniProt ID: P08908 Link_out
    Gene: HTR1A Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed

    5. 5-hydroxytryptamine 1D receptor

    Pharmacological action: unknown
    Actions: agonist

    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. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity

    Organism class: human
    UniProt ID: P28221 Link_out
    Gene: HTR1D Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed

    6. 5-hydroxytryptamine 2B receptor

    Pharmacological action: unknown
    Actions: agonist

    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 mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system

    Organism class: human
    UniProt ID: P41595 Link_out
    Gene: HTR2B Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed

    7. D(1A) dopamine receptor

    Pharmacological action: unknown
    Actions: agonist

    This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase

    Organism class: human
    UniProt ID: P21728 Link_out
    Gene: DRD1 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed

    8. D(1B) dopamine receptor

    Pharmacological action: unknown
    Actions: agonist

    This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase

    Organism class: human
    UniProt ID: P21918 Link_out
    Gene: DRD5 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed

    9. 5-hydroxytryptamine 1B receptor

    Pharmacological action: unknown
    Actions: agonist

    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. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity

    Organism class: human
    UniProt ID: P28222 Link_out
    Gene: HTR1B Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed

    10. 5-hydroxytryptamine 2A receptor

    Pharmacological action: unknown
    Actions: agonist

    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 mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. This receptor is involved in tracheal smooth muscle contraction, bronchoconstriction, and control of aldosterone production

    Organism class: human
    UniProt ID: P28223 Link_out
    Gene: HTR2A Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed

    11. 5-hydroxytryptamine 2C receptor

    Pharmacological action: unknown
    Actions: agonist

    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 mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system

    Organism class: human
    UniProt ID: P28335 Link_out
    Gene: HTR2C Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed

    12. Alpha-2A adrenergic receptor

    Pharmacological action: unknown
    Actions: agonist

    Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol

    Organism class: human
    UniProt ID: P08913 Link_out
    Gene: ADRA2A Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed

    13. Alpha-2B adrenergic receptor

    Pharmacological action: unknown
    Actions: agonist

    Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol

    Organism class: human
    UniProt ID: P18089 Link_out
    Gene: ADRA2B Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed

    14. Alpha-2C adrenergic receptor

    Pharmacological action: unknown
    Actions: agonist

    Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins

    Organism class: human
    UniProt ID: P18825 Link_out
    Gene: ADRA2C Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed
    Enzymes

    1. Cytochrome P450 1A2

    Actions: substrate, inhibitor

    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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N3-demethylation. Also acts in the metabolism of aflatoxin B1 and acetaminophen

    UniProt ID: P05177 Link_out
    Gene: CYP1A2
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed
    2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

    2. Cytochrome P450 3A4

    Actions: substrate

    Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4- hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. The enzyme also hydroxylates etoposide

    UniProt ID: P08684 Link_out
    Gene: CYP3A4
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed
    2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

    3. Cytochrome P450 2D6

    Actions: inhibitor

    Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants

    UniProt ID: P10635 Link_out
    Gene: CYP2D6 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. Pubmed
    2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
    Comments
    Drug created on June 13, 2005 07:24 / Updated on February 08, 2013 16:19