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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- Name
- Reboxetine
- Accession Number
- DB00234 (APRD00198)
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Description
Reboxetine is an antidepressant drug used in the treatment of clinical depression, panic disorder and ADD/ADHD. Its mesylate (i.e. methanesulfonate) salt is sold under tradenames including Edronax, Norebox, Prolift, Solvex, Davedax or Vestra. Reboxetine has two chiral centers, but it only exists as two enantiomers, (R,R)-(-)- and (S,S)-(+)-reboxetine.
- Structure
Structure for DB00234 (Reboxetine)
- Synonyms
- Not Available
- Product Ingredients
Ingredient UNII CAS InChI Key Reboxetine mesilate L94J81YNNY 98769-84-7 CGTZMJIMMUNLQD-STYNFMPRSA-N - International/Other Brands
- Davedax / Edronax / Norebox / Prolift / Solvex / Vestra
- Categories
- Adrenergic Agents
- Adrenergic Uptake Inhibitors
- Antidepressive Agents
- Central Nervous System Agents
- Cytochrome P-450 CYP2D6 Inducers
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Membrane Transport Modulators
- Nervous System
- Neurotransmitter Agents
- Neurotransmitter Uptake Inhibitors
- Oxazines
- P-glycoprotein/ABCB1 Inhibitors
- Psychoanaleptics
- Psychotropic Drugs
- UNII
- 947S0YZ36I
- CAS number
- 71620-89-8
- Weight
- Average: 313.397
Monoisotopic: 313.167793605 - Chemical Formula
- C19H23NO3
- InChI Key
- CBQGYUDMJHNJBX-RTBURBONSA-N
- InChI
- InChI=1S/C19H23NO3/c1-2-21-16-10-6-7-11-17(16)23-19(15-8-4-3-5-9-15)18-14-20-12-13-22-18/h3-11,18-20H,2,12-14H2,1H3/t18-,19-/m1/s1
- IUPAC Name
- (2R)-2-[(R)-(2-ethoxyphenoxy)(phenyl)methyl]morpholine
- SMILES
- [H][[email protected]@](OC1=CC=CC=C1OCC)(C1=CC=CC=C1)[[email protected]@]1([H])CNCCO1
Pharmacology
- Indication
For the treatment of clinical depression.
- Structured Indications
- Not Available
- Pharmacodynamics
Reboxetine is a selective noradrenaline reuptake inhibitor (NaRI), the first drug of new antidepressant class. Reboxetine is an a-ariloxybenzyl derivative of morpholine. Reboxetine is primarily used to treat depression but has also been found useful in the treatment of narcolepsy and panic disorders.
- Mechanism of action
Reboxetine is a selective inhibitor of noradrenaline reuptake. It inhibits noradrenaline reuptake in vitro to a similar extent to the tricyclic antidepressant desmethylimipramine. Reboxetine does not affect dopamine or serotonin reuptake and it has low in vivo and in vitro affinity for adrenergic, cholinergic, histaminergic, dopaminergic and serotonergic receptors.
Target Actions Organism ASodium-dependent noradrenaline transporter inhibitorHuman - Absorption
Reboxetine is rapidly and extensively absorbed following oral administration.
- Volume of distribution
- Not Available
- Protein binding
98%
- Metabolism
Reboxetine is metabolized by dealkylation, hydroxylation and oxidation followed by glucuronide or sulphate conjugation. It is metabolized by the cytochrome P450 CYP isoenzyme 3A4.
- Route of elimination
- Not Available
- Half life
12.5 hours
- Clearance
- Not Available
- Toxicity
Reports of seizures (rare) have been reported
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Drug group Afatinib The serum concentration of Afatinib can be increased when it is combined with Reboxetine. Approved Amiodarone The metabolism of Reboxetine can be decreased when combined with Amiodarone. Approved, Investigational Apalutamide The serum concentration of Reboxetine can be decreased when it is combined with Apalutamide. Approved, Investigational Aprepitant The serum concentration of Reboxetine can be increased when it is combined with Aprepitant. Approved, Investigational Atazanavir The metabolism of Reboxetine can be decreased when combined with Atazanavir. Approved, Investigational Atomoxetine The metabolism of Reboxetine can be decreased when combined with Atomoxetine. Approved Boceprevir The metabolism of Reboxetine can be decreased when combined with Boceprevir. Approved, Withdrawn Bortezomib The metabolism of Reboxetine can be decreased when combined with Bortezomib. Approved, Investigational Bosentan The serum concentration of Reboxetine can be decreased when it is combined with Bosentan. Approved, Investigational Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Reboxetine. Approved Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Reboxetine. Approved, Investigational Carbamazepine The metabolism of Reboxetine can be increased when combined with Carbamazepine. Approved, Investigational Ceritinib The serum concentration of Reboxetine can be increased when it is combined with Ceritinib. Approved Clarithromycin The metabolism of Reboxetine can be decreased when combined with Clarithromycin. Approved Clemastine The metabolism of Reboxetine can be decreased when combined with Clemastine. Approved, Investigational Clotrimazole The metabolism of Reboxetine can be decreased when combined with Clotrimazole. Approved, Vet Approved Cobicistat The metabolism of Reboxetine can be decreased when combined with Cobicistat. Approved Colchicine The serum concentration of Colchicine can be increased when it is combined with Reboxetine. Approved Conivaptan The serum concentration of Conivaptan can be increased when it is combined with Reboxetine. Approved, Investigational Crizotinib The metabolism of Reboxetine can be decreased when combined with Crizotinib. Approved Cyclosporine The metabolism of Reboxetine can be decreased when combined with Cyclosporine. Approved, Investigational, Vet Approved Dabigatran etexilate The serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Reboxetine. Approved Dabrafenib The serum concentration of Reboxetine can be decreased when it is combined with Dabrafenib. Approved, Investigational Darunavir The metabolism of Reboxetine can be decreased when combined with Darunavir. Approved Dasatinib The serum concentration of Reboxetine can be increased when it is combined with Dasatinib. Approved, Investigational Deferasirox The serum concentration of Reboxetine can be decreased when it is combined with Deferasirox. Approved, Investigational Delavirdine The metabolism of Reboxetine can be decreased when combined with Delavirdine. Approved Dihydroergotamine The metabolism of Reboxetine can be decreased when combined with Dihydroergotamine. Approved, Investigational Diltiazem The metabolism of Reboxetine can be decreased when combined with Diltiazem. Approved, Investigational Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Reboxetine. Approved, Investigational Doxycycline The metabolism of Reboxetine can be decreased when combined with Doxycycline. Approved, Investigational, Vet Approved Dronedarone The metabolism of Reboxetine can be decreased when combined with Dronedarone. Approved Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Reboxetine. Approved Enzalutamide The serum concentration of Reboxetine can be decreased when it is combined with Enzalutamide. Approved Erythromycin The metabolism of Reboxetine can be decreased when combined with Erythromycin. Approved, Investigational, Vet Approved Everolimus The serum concentration of Everolimus can be increased when it is combined with Reboxetine. Approved Fesoterodine The serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Reboxetine. Approved Fluconazole The metabolism of Reboxetine can be decreased when combined with Fluconazole. Approved, Investigational Fluvoxamine The metabolism of Reboxetine can be decreased when combined with Fluvoxamine. Approved, Investigational Fosamprenavir The metabolism of Reboxetine can be decreased when combined with Fosamprenavir. Approved Fosaprepitant The serum concentration of Reboxetine can be increased when it is combined with Fosaprepitant. Approved Fosphenytoin The metabolism of Reboxetine can be increased when combined with Fosphenytoin. Approved, Investigational Fusidic Acid The serum concentration of Reboxetine can be increased when it is combined with Fusidic Acid. Approved, Investigational Idelalisib The metabolism of Reboxetine can be decreased when combined with Idelalisib. Approved Imatinib The metabolism of Reboxetine can be decreased when combined with Imatinib. Approved Indinavir The metabolism of Reboxetine can be decreased when combined with Indinavir. Approved Isavuconazole The serum concentration of Reboxetine can be increased when it is combined with Isavuconazole. Approved, Investigational Isavuconazonium The metabolism of Reboxetine can be decreased when combined with Isavuconazonium. Approved, Investigational Isocarboxazid The therapeutic efficacy of Reboxetine can be increased when used in combination with Isocarboxazid. Approved Isradipine The metabolism of Reboxetine can be decreased when combined with Isradipine. Approved, Investigational Itraconazole The metabolism of Reboxetine can be decreased when combined with Itraconazole. Approved, Investigational Ivacaftor The serum concentration of Reboxetine can be increased when it is combined with Ivacaftor. Approved Ketoconazole The metabolism of Reboxetine can be decreased when combined with Ketoconazole. Approved, Investigational Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Reboxetine. Approved Lopinavir The metabolism of Reboxetine can be decreased when combined with Lopinavir. Approved Lorpiprazole The serum concentration of Reboxetine can be increased when it is combined with Lorpiprazole. Approved Lovastatin The metabolism of Reboxetine can be decreased when combined with Lovastatin. Approved, Investigational Luliconazole The serum concentration of Reboxetine can be increased when it is combined with Luliconazole. Approved Lumacaftor The metabolism of Reboxetine can be increased when combined with Lumacaftor. Approved Metoprolol The serum concentration of Metoprolol can be increased when it is combined with Reboxetine. Approved, Investigational Mifepristone The serum concentration of Reboxetine can be increased when it is combined with Mifepristone. Approved, Investigational Mitotane The serum concentration of Reboxetine can be decreased when it is combined with Mitotane. Approved Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Reboxetine. Approved Nefazodone The metabolism of Reboxetine can be decreased when combined with Nefazodone. Approved, Withdrawn Nelfinavir The metabolism of Reboxetine can be decreased when combined with Nelfinavir. Approved Netupitant The serum concentration of Reboxetine can be increased when it is combined with Netupitant. Approved, Investigational Nevirapine The metabolism of Reboxetine can be increased when combined with Nevirapine. Approved Nilotinib The metabolism of Reboxetine can be decreased when combined with Nilotinib. Approved, Investigational Olaparib The metabolism of Reboxetine can be decreased when combined with Olaparib. Approved Osimertinib The serum concentration of Reboxetine can be increased when it is combined with Osimertinib. Approved Palbociclib The serum concentration of Reboxetine can be increased when it is combined with Palbociclib. Approved, Investigational Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Reboxetine. Approved Pentobarbital The metabolism of Reboxetine can be increased when combined with Pentobarbital. Approved, Investigational, Vet Approved Phenobarbital The metabolism of Reboxetine can be increased when combined with Phenobarbital. Approved, Investigational Phenytoin The metabolism of Reboxetine can be increased when combined with Phenytoin. Approved, Vet Approved Pitolisant The serum concentration of Pitolisant can be increased when it is combined with Reboxetine. Approved, Investigational Posaconazole The metabolism of Reboxetine can be decreased when combined with Posaconazole. Approved, Investigational, Vet Approved Primidone The metabolism of Reboxetine can be increased when combined with Primidone. Approved, Vet Approved Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Reboxetine. Approved Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Reboxetine. Approved, Investigational Rifabutin The metabolism of Reboxetine can be increased when combined with Rifabutin. Approved, Investigational Rifampicin The metabolism of Reboxetine can be increased when combined with Rifampicin. Approved Rifapentine The metabolism of Reboxetine can be increased when combined with Rifapentine. Approved, Investigational Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Reboxetine. Approved, Investigational Rucaparib The metabolism of Reboxetine can be decreased when combined with Rucaparib. Approved, Investigational Saquinavir The metabolism of Reboxetine can be decreased when combined with Saquinavir. Approved, Investigational Sarilumab The therapeutic efficacy of Reboxetine can be decreased when used in combination with Sarilumab. Approved, Investigational Sildenafil The metabolism of Reboxetine can be decreased when combined with Sildenafil. Approved, Investigational Silodosin The serum concentration of Silodosin can be increased when it is combined with Reboxetine. Approved Siltuximab The serum concentration of Reboxetine can be decreased when it is combined with Siltuximab. Approved, Investigational Simeprevir The serum concentration of Reboxetine can be increased when it is combined with Simeprevir. Approved St. John's Wort The serum concentration of Reboxetine can be decreased when it is combined with St. John's Wort. Approved, Investigational, Nutraceutical Stiripentol The serum concentration of Reboxetine can be increased when it is combined with Stiripentol. Approved Sulfisoxazole The metabolism of Reboxetine can be decreased when combined with Sulfisoxazole. Approved, Vet Approved Telaprevir The metabolism of Reboxetine can be decreased when combined with Telaprevir. Approved, Withdrawn Telithromycin The metabolism of Reboxetine can be decreased when combined with Telithromycin. Approved Thioridazine The serum concentration of Thioridazine can be increased when it is combined with Reboxetine. Approved, Withdrawn Ticlopidine The metabolism of Reboxetine can be decreased when combined with Ticlopidine. Approved Tocilizumab The serum concentration of Reboxetine can be decreased when it is combined with Tocilizumab. Approved Topotecan The serum concentration of Topotecan can be increased when it is combined with Reboxetine. Approved, Investigational Vemurafenib The risk or severity of QTc prolongation can be increased when Vemurafenib is combined with Reboxetine. Approved Venlafaxine The metabolism of Reboxetine can be decreased when combined with Venlafaxine. Approved Verapamil The metabolism of Reboxetine can be decreased when combined with Verapamil. Approved Vincristine The excretion of Vincristine can be decreased when combined with Reboxetine. Approved, Investigational Voriconazole The metabolism of Reboxetine can be decreased when combined with Voriconazole. Approved, Investigational Ziprasidone The metabolism of Reboxetine can be decreased when combined with Ziprasidone. Approved - Food Interactions
- Not Available
References
- General References
- Fleishaker JC: Clinical pharmacokinetics of reboxetine, a selective norepinephrine reuptake inhibitor for the treatment of patients with depression. Clin Pharmacokinet. 2000 Dec;39(6):413-27. [PubMed:11192474]
- Edwards DM, Pellizzoni C, Breuel HP, Berardi A, Castelli MG, Frigerio E, Poggesi I, Rocchetti M, Dubini A, Strolin Benedetti M: Pharmacokinetics of reboxetine in healthy volunteers. Single oral doses, linearity and plasma protein binding. Biopharm Drug Dispos. 1995 Aug;16(6):443-60. [PubMed:7579027]
- Wienkers LC, Allievi C, Hauer MJ, Wynalda MA: Cytochrome P-450-mediated metabolism of the individual enantiomers of the antidepressant agent reboxetine in human liver microsomes. Drug Metab Dispos. 1999 Nov;27(11):1334-40. [PubMed:10534319]
- Kasper S, el Giamal N, Hilger E: Reboxetine: the first selective noradrenaline re-uptake inhibitor. Expert Opin Pharmacother. 2000 May;1(4):771-82. [PubMed:11249515]
- External Links
- PubChem Compound
- 127151
- PubChem Substance
- 46504845
- ChemSpider
- 112870
- ChEBI
- 135342
- ChEMBL
- CHEMBL383921
- Therapeutic Targets Database
- DAP000720
- PharmGKB
- PA144614921
- HET
- 41X
- Wikipedia
- Reboxetine
- ATC Codes
- N06AX18 — Reboxetine
- PDB Entries
- 4xnx
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 1 Completed Basic Science Amphetamine-Related Disorders / Moods Disorders / Substance-Related Disorders 1 1 Unknown Status Treatment Schizophrenic Disorders 1 3 Completed Supportive Care Bone Mineral Density Quantitative Trait Locus 7 1 3 Terminated Treatment Anxiety Disorders / Dementias / Depression / Psychosomatic Disorders / Schizophrenic Disorders 1 4 Completed Treatment Cerebral Stroke 1 4 Unknown Status Treatment Abdominal Pain (AP) / Major Depressive Disorder (MDD) / Pain 1 4 Unknown Status Treatment Depression 1 4 Unknown Status Treatment Schizophrenic Disorders 1 Not Available Completed Basic Science Cognitive Performance in Major Depression 1 Not Available Completed Treatment Major Depressive Disorder (MDD) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 170-171 °C (Mesylate salt) Not Available water solubility 8 mg/mL (Mesylate salt) Not Available logP 3.1 Not Available - Predicted Properties
Property Value Source Water Solubility 0.0223 mg/mL ALOGPS logP 3.06 ALOGPS logP 3.28 ChemAxon logS -4.2 ALOGPS pKa (Strongest Basic) 7.91 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 4 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 39.72 Å2 ChemAxon Rotatable Bond Count 6 ChemAxon Refractivity 89.48 m3·mol-1 ChemAxon Polarizability 34.51 Å3 ChemAxon Number of Rings 3 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule Yes ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9968 Blood Brain Barrier + 0.9381 Caco-2 permeable + 0.575 P-glycoprotein substrate Substrate 0.7914 P-glycoprotein inhibitor I Inhibitor 0.8825 P-glycoprotein inhibitor II Non-inhibitor 0.5968 Renal organic cation transporter Non-inhibitor 0.5581 CYP450 2C9 substrate Non-substrate 0.8237 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Non-substrate 0.5402 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.8063 CYP450 2D6 inhibitor Non-inhibitor 0.5687 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Inhibitor 0.6318 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.5218 Ames test Non AMES toxic 0.9141 Carcinogenicity Non-carcinogens 0.9083 Biodegradation Not ready biodegradable 0.9372 Rat acute toxicity 2.0972 LD50, mol/kg Not applicable hERG inhibition (predictor I) Strong inhibitor 0.7754 hERG inhibition (predictor II) Inhibitor 0.717
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key 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
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as phenol ethers. These are aromatic compounds containing an ether group substituted with a benzene ring.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Phenol ethers
- Sub Class
- Not Available
- Direct Parent
- Phenol ethers
- Alternative Parents
- Phenoxy compounds / Aralkylamines / Alkyl aryl ethers / Morpholines / Oxacyclic compounds / Dialkylamines / Dialkyl ethers / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
- Substituents
- Phenoxy compound / Phenol ether / Alkyl aryl ether / Aralkylamine / Monocyclic benzene moiety / Morpholine / Oxazinane / Dialkyl ether / Secondary aliphatic amine / Ether
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
Targets
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Norepinephrine:sodium symporter activity
- Specific Function
- Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
- Gene Name
- SLC6A2
- Uniprot ID
- P23975
- Uniprot Name
- Sodium-dependent noradrenaline transporter
- Molecular Weight
- 69331.42 Da
References
- Rauhut AS, Mullins SN, Dwoskin LP, Bardo MT: Reboxetine: attenuation of intravenous nicotine self-administration in rats. J Pharmacol Exp Ther. 2002 Nov;303(2):664-72. [PubMed:12388649]
- Wilson AA, Johnson DP, Mozley D, Hussey D, Ginovart N, Nobrega J, Garcia A, Meyer J, Houle S: Synthesis and in vivo evaluation of novel radiotracers for the in vivo imaging of the norepinephrine transporter. Nucl Med Biol. 2003 Feb;30(2):85-92. [PubMed:12623106]
- Lin KS, Ding YS, Kim SW, Kil KE: Synthesis, enantiomeric resolution, F-18 labeling and biodistribution of reboxetine analogs: promising radioligands for imaging the norepinephrine transporter with positron emission tomography. Nucl Med Biol. 2005 May;32(4):415-22. [PubMed:15878511]
- Spivak B, Strous RD, Shaked G, Shabash E, Kotler M, Weizman A: Reboxetine versus fluvoxamine in the treatment of motor vehicle accident-related posttraumatic stress disorder: a double-blind, fixed-dosage, controlled trial. J Clin Psychopharmacol. 2006 Apr;26(2):152-6. [PubMed:16633143]
- Mitchell HA, Ahern TH, Liles LC, Javors MA, Weinshenker D: The effects of norepinephrine transporter inactivation on locomotor activity in mice. Biol Psychiatry. 2006 Nov 15;60(10):1046-52. Epub 2006 Aug 7. [PubMed:16893531]
- Kasper S, el Giamal N, Hilger E: Reboxetine: the first selective noradrenaline re-uptake inhibitor. Expert Opin Pharmacother. 2000 May;1(4):771-82. [PubMed:11249515]
Enzymes
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-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 performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- 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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- InhibitorInducer
- General Function
- Steroid hydroxylase activity
- Specific Function
- 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...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- 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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Transporters
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Weiss J, Dormann SM, Martin-Facklam M, Kerpen CJ, Ketabi-Kiyanvash N, Haefeli WE: Inhibition of P-glycoprotein by newer antidepressants. J Pharmacol Exp Ther. 2003 Apr;305(1):197-204. [PubMed:12649369]
Drug created on June 13, 2005 07:24 / Updated on March 02, 2018 05:12