Identification
- Summary
Tetrabenazine is a vesicular monoamine transporter 2 (VMAT) inhibitor used for the management of chorea associated with Huntington's Disease.
- Brand Names
- Nitoman, Xenazine
- Generic Name
- Tetrabenazine
- DrugBank Accession Number
- DB04844
- Background
A drug formerly used as an antipsychotic but now used primarily in the symptomatic treatment of various hyperkinetic disorders. It is a monoamine depletor and used as symptomatic treatment of chorea associated with Huntington's disease. FDA approved on August 15, 2008.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Tetrabenazine (DB04844)
- Weight
- Average: 317.4226
Monoisotopic: 317.199093735 - Chemical Formula
- C19H27NO3
- Synonyms
- 1,2,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy-2H-benzo[a]quinolizin-2-one
- 2-oxo-3-isobutyl-9,10-dimethoxy-1,2,3,4,6,7-hexahydro-11bH-benzo[a]quinolizine
- 2-oxo-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-benzoquinolizine
- Tetrabenazina
- Tetrabenazine
- Tetrabenazinum
- External IDs
- RO 1-9569
- RO-1-9569
- RO-19569
Pharmacology
- Indication
Treatment of hyperkinetic movement disorders like chorea in Huntington's disease, hemiballismus, senile chorea, Tourette syndrome and other tic disorders, and tardive dyskinesia
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 Management of Hemiballismus •••••••••••• Management of Huntington's chorea •••••••••••• Management of Tardive dyskinesia •••••••••••• Management of Tourette syndrome •••••••••••• Management of Senile chorea •••••••••••• - Contraindications & Blackbox Warnings
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Prolongation of the QTc interval has been observed at doses of 50 mg. In rats, it has been observed that tetrabenazine or its metabolites bind to melanin-containing tissues such as the eyes and skin. After a single oral dose of radiolabeled tetrabenazine, radioactivity was still detected in eye and fur at 21 days post dosing.
- Mechanism of action
Tetrabenazine is a reversible human vesicular monoamine transporter type 2 inhibitor (Ki = 100 nM). It acts within the basal ganglia and promotes depletion of monoamine neurotransmitters serotonin, norepinephrine, and dopamine from stores. It also decreases uptake into synaptic vesicles. Dopamine is required for fine motor movement, so the inhibition of its transmission is efficacious for hyperkinetic movement. Tetrabenazine exhibits weak in vitro binding affinity at the dopamine D2 receptor (Ki = 2100 nM).
Target Actions Organism ASynaptic vesicular amine transporter inhibitorHumans UDopamine D2 receptor inhibitorHumans - Absorption
Following oral administration of tetrabenazine, the extent of absorption is at least 75%. After single oral doses ranging from 12.5 to 50 mg, plasma concentrations of tetrabenazine are generally below the limit of detection because of the rapid and extensive hepatic metabolism of tetrabenazine. Food does not affect the absorption of tetrabenazine. Cmax, oral = 4.8 ng/mL in HD or tardive dyskinesia patients;
Tmax, oral = 69 min in HD or tardive dyskinesia patients- Volume of distribution
Steady State, IV, in HD or tardive dyskinesia patients: 385L. Tetrabenazine is rapidly distributed to the brain following IV injection. The site with the highest binding is the striatum, while the lowest binding was observed in the cortex.
- Protein binding
Tetrabenazine = 82 - 88%; α-HTBZ = 60 - 68%; β-HTBZ = 59 - 63%.
- Metabolism
Tetrabenazine is hepatically metabolized. Carbonyl reductase in the liver is responsible for the formation of two major active metabolites: α-dihydrotetrabenazine (α-HTBZ) and β-dihydrotetrabenazine (β-HTBZ). α-HTBZ is further metabolized into 9-desmethyl-α-DHTBZ, a minor metabolite by CYP2D6 and with some contribution of CYP1A2. β-HTBZ is metabolized to another major circulating metabolite, 9-desmethyl-β-DHTBZ, by CYP2D6. The Tmax of this metabolite is 2 hours post-administration of tetrabenazine.
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- Route of elimination
After oral administration, tetrabenazine is extensively hepatically metabolized, and the metabolites are primarily renally eliminated (75%). Tetrabenazine is also cleared fecally (7% to 16%). Unchanged tetrabenazine has not been found in human urine. Urinary excretion of α-HTBZ or β-HTBZ (the major metabolites) accounted for less than 10% of the administered dose.
- Half-life
There is interindividual variability in elimination half-life.3 The elimination half-life of tetrabenazine was 10 hours following intravenous bolus administration.4 The oral half-lives of its metabolites, α-HTBZ, β-HTBZ and 9-desmethyl-β-DHTBZ, are seven hours, five hours and 12 hours, respectively.5 Following a single oral dose of 25 mg tetrabenazine, the elimination half-life was approximately 17.5 hours in subjects with hepatic impairment.5
- Clearance
IV, 1.67 L/min in HD or tardive dyskinesia patients
- 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
Dose-limiting adverse effects are sedation, parkinsonism, akathsia, and depression. LD50 oral, mouse: 550 mg/kg
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Cytochrome P450 2D6 CYP2D6*3 Not Available C allele Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*4 Not Available C allele Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*5 Not Available Whole-gene deletion Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*6 Not Available 1707delT Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*7 Not Available 2935A>C Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*8 Not Available 1758G>T Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*11 Not Available 883G>C Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*12 Not Available 124G>A Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*13 Not Available CYP2D7/2D6 hybrid gene structure Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*14A Not Available 1758G>A Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*15 Not Available 137insT, 137_138insT Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*19 Not Available 2539_2542delAACT Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*20 Not Available 1973_1974insG Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*21 Not Available 2573insC Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*31 Not Available -1770G>A / -1584C>G … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*36 Not Available 100C>T / -1426C>T … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*38 Not Available 2587_2590delGACT Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*40 Not Available 1863_1864ins(TTT CGC CCC)2 Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*42 Not Available 3259_3260insGT Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*44 Not Available 2950G>C Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*47 Not Available 100C>T / -1426C>T … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*51 Not Available -1584C>G / -1235A>G … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*56 Not Available 3201C>T Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*57 Not Available 100C>T / 310G>T … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*62 Not Available 4044C>T Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*68A Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*68B Not Available Similar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4. Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*69 Not Available 2988G>A / -1426C>T … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*92 Not Available 1995delC Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*100 Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details Cytochrome P450 2D6 CYP2D6*101 Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer, lower dose requirement. Details
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" 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 softwareAbatacept The metabolism of Tetrabenazine can be increased when combined with Abatacept. Abiraterone The metabolism of Tetrabenazine can be decreased when combined with Abiraterone. Acebutolol The metabolism of Tetrabenazine can be decreased when combined with Acebutolol. Acetaminophen The metabolism of Tetrabenazine can be decreased when combined with Acetaminophen. Acetophenazine The risk or severity of adverse effects can be increased when Acetophenazine is combined with Tetrabenazine. - Food Interactions
- Avoid alcohol. Ingesting alcohol may increase the drowsiness caused by tetrabenazine.
- Take with or without food.
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.- International/Other Brands
- Rubigen
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Nitoman Tablet 25 mg Oral Bausch Health, Canada Inc. 1996-12-09 Not applicable Canada 
Tetrabenazine Tablets Tablet 25 mg Oral Sterimax Inc 2013-08-29 Not applicable Canada Xenazine Tablet 12.5 mg/1 Oral Lundbeck Pharmaceuticals Llc 2008-11-24 Not applicable US 
Xenazine Tablet 25 mg/1 Oral Lundbeck Pharmaceuticals Llc 2008-11-24 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-tetrabenazine Tablet 25 mg Oral Apotex Corporation 2013-11-01 Not applicable Canada PMS-tetrabenazine Tablet 25 mg Oral Pharmascience Inc 2013-02-26 Not applicable Canada Tetrabenazine Tablet 12.5 mg/1 Oral Ingenus Pharmaceuticals Nj, Llc 2017-03-01 2017-03-01 US Tetrabenazine Tablet 25 mg/1 Oral TAGI Pharma, Inc. 2017-02-01 2025-07-31 US Tetrabenazine Tablet 25 mg/1 Oral Oceanside Pharmaceuticals 2015-07-20 Not applicable US
Categories
- ATC Codes
- N07XX06 — Tetrabenazine
- Drug Categories
- Adrenergic Agents
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 Substrates
- Heterocyclic Compounds, Fused-Ring
- Highest Risk QTc-Prolonging Agents
- Membrane Transport Modulators
- Miscellaneous Central Nervous System Agents
- Nervous System
- Neurotransmitter Agents
- Neurotransmitter Uptake Inhibitors
- QTc Prolonging Agents
- Quinolizines
- Vesicular Monoamine Transporter 2 Inhibitor
- Vesicular Monoamine Transporter 2 Inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as tetrahydroisoquinolines. These are tetrahydrogenated isoquinoline derivatives.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Tetrahydroisoquinolines
- Sub Class
- Not Available
- Direct Parent
- Tetrahydroisoquinolines
- Alternative Parents
- Anisoles / Piperidinones / Aralkylamines / Alkyl aryl ethers / Trialkylamines / Cyclic ketones / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives
- Substituents
- Alkyl aryl ether / Amine / Anisole / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Carbonyl group / Cyclic ketone / Ether
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- cyclic ketone, tertiary amino compound, benzoquinolizine (CHEBI:64028)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- Z9O08YRN8O
- CAS number
- 58-46-8
- InChI Key
- MKJIEFSOBYUXJB-UHFFFAOYSA-N
- InChI
- InChI=1S/C19H27NO3/c1-12(2)7-14-11-20-6-5-13-8-18(22-3)19(23-4)9-15(13)16(20)10-17(14)21/h8-9,12,14,16H,5-7,10-11H2,1-4H3
- IUPAC Name
- 9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11bH-pyrido[2,1-a]isoquinolin-2-one
- SMILES
- COC1=C(OC)C=C2C3CC(=O)C(CC(C)C)CN3CCC2=C1
References
- Synthesis Reference
Michael James Rishel, Kande Kankananamalage Dayarathna Amarasinghe, Sean Richard Dinn, Bruce Fletcher Johnson, "METHOD FOR MAKING TETRABENAZINE COMPOUNDS." U.S. Patent US20080306267, issued December 11, 2008.
US20080306267- General References
- Jankovic J, Beach J: Long-term effects of tetrabenazine in hyperkinetic movement disorders. Neurology. 1997 Feb;48(2):358-62. [Article]
- Guay DR: Tetrabenazine, a monoamine-depleting drug used in the treatment of hyperkinetic movement disorders. Am J Geriatr Pharmacother. 2010 Aug;8(4):331-73. doi: 10.1016/j.amjopharm.2010.08.006. [Article]
- Yero T, Rey JA: Tetrabenazine (Xenazine), An FDA-Approved Treatment Option For Huntington's Disease-Related Chorea. P T. 2008 Dec;33(12):690-4. [Article]
- Roberts MS, McLean S, Millingen KS, Galloway HM: The pharmacokinetics of tetrabenazine and its hydroxy metabolite in patients treated for involuntary movement disorders. Eur J Clin Pharmacol. 1986;29(6):703-8. doi: 10.1007/BF00615962. [Article]
- FDA Approved Drug Products: XENAZINE (tetrabenazine) tablets, for oral use [Link]
- External Links
- Human Metabolome Database
- HMDB0015592
- KEGG Drug
- D08575
- KEGG Compound
- C11168
- PubChem Compound
- 6018
- PubChem Substance
- 46506426
- ChemSpider
- 5796
- BindingDB
- 50017701
- 10390
- ChEBI
- 64028
- ChEMBL
- CHEMBL117785
- Therapeutic Targets Database
- DAP000756
- PharmGKB
- PA140222719
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Tetrabenazine
- FDA label
- Download (456 KB)
- MSDS
- Download (79.6 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Supportive Care Cerebral Palsy (CP) / Excessive crying / Pain 1 4 Completed Treatment Huntington's Disease (HD) 1 4 Recruiting Treatment Huntington's Disease (HD) 1 3 Completed Treatment Huntington's Disease (HD) 1 3 Completed Treatment Tardive Dyskinesia (TD) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Laboratories Fournier Sca
- Lundbeck Inc.
- Dosage Forms
Form Route Strength Tablet Oral Tablet Oral 25 mg Tablet Oral 2500000 mg Tablet Oral 12.5 MG Tablet Oral 12.5 mg/1 Tablet Oral 25 mg/1 Tablet, coated Oral 12.5 mg/1 Tablet, coated Oral 25 mg/1 Tablet, coated Oral 25 mg - Prices
Unit description Cost Unit Xenazine 25 mg tablet 74.57USD tablet Xenazine 12.5 mg tablet 37.29USD tablet 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 melting point (°C) 126 °C MSDS water solubility Sparingly soluble FDA label pKa 6.51 FDA label - Predicted Properties
Property Value Source Water Solubility 0.361 mg/mL ALOGPS logP 3.23 ALOGPS logP 3.4 Chemaxon logS -2.9 ALOGPS pKa (Strongest Acidic) 19.3 Chemaxon pKa (Strongest Basic) 7.33 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 38.77 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 91.31 m3·mol-1 Chemaxon Polarizability 36.59 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 No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.995 Blood Brain Barrier + 0.9639 Caco-2 permeable + 0.8608 P-glycoprotein substrate Substrate 0.7819 P-glycoprotein inhibitor I Inhibitor 0.8908 P-glycoprotein inhibitor II Inhibitor 0.7631 Renal organic cation transporter Inhibitor 0.6484 CYP450 2C9 substrate Non-substrate 0.8444 CYP450 2D6 substrate Substrate 0.6448 CYP450 3A4 substrate Substrate 0.8091 CYP450 1A2 substrate Non-inhibitor 0.7482 CYP450 2C9 inhibitor Non-inhibitor 0.9042 CYP450 2D6 inhibitor Inhibitor 0.7084 CYP450 2C19 inhibitor Non-inhibitor 0.8191 CYP450 3A4 inhibitor Non-inhibitor 0.8308 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8718 Ames test Non AMES toxic 0.6674 Carcinogenicity Non-carcinogens 0.9083 Biodegradation Not ready biodegradable 0.9974 Rat acute toxicity 2.8540 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6451 hERG inhibition (predictor II) Inhibitor 0.7524
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-0f6x-4292000000-399e16e38421335dc45d Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0009000000-ba78836c58b00ab4e6c4 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-0009000000-f189fc658abb8f999018 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-0139000000-13d752e602ef6e4c3252 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0049000000-e25754af93da67965901 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0w29-0390000000-12b1bea577b46f85cc04 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-01p9-2390000000-c94ee9cdbabd19c82d12 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 195.2707439 predictedDarkChem Lite v0.1.0 [M-H]- 175.79955 predictedDeepCCS 1.0 (2019) [M+H]+ 196.1049439 predictedDarkChem Lite v0.1.0 [M+H]+ 178.15755 predictedDeepCCS 1.0 (2019) [M+Na]+ 195.5142439 predictedDarkChem Lite v0.1.0 [M+Na]+ 184.25069 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Monoamine transmembrane transporter activity
- Specific Function
- Involved in the ATP-dependent vesicular transport of biogenic amine neurotransmitters. Pumps cytosolic monoamines including dopamine, norepinephrine, serotonin, and histamine into synaptic vesicles...
- Gene Name
- SLC18A2
- Uniprot ID
- Q05940
- Uniprot Name
- Synaptic vesicular amine transporter
- Molecular Weight
- 55712.075 Da
References
- Zheng G, Dwoskin LP, Crooks PA: Vesicular monoamine transporter 2: role as a novel target for drug development. AAPS J. 2006 Nov 10;8(4):E682-92. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kim YS, Shin JH, Hall FS, Linden DJ: Dopamine signaling is required for depolarization-induced slow current in cerebellar Purkinje cells. J Neurosci. 2009 Jul 1;29(26):8530-8. doi: 10.1523/JNEUROSCI.0468-09.2009. [Article]
- Goland R, Freeby M, Parsey R, Saisho Y, Kumar D, Simpson N, Hirsch J, Prince M, Maffei A, Mann JJ, Butler PC, Van Heertum R, Leibel RL, Ichise M, Harris PE: 11C-dihydrotetrabenazine PET of the pancreas in subjects with long-standing type 1 diabetes and in healthy controls. J Nucl Med. 2009 Mar;50(3):382-9. doi: 10.2967/jnumed.108.054866. Epub 2009 Feb 17. [Article]
- Gros Y, Schuldiner S: Directed evolution reveals hidden properties of VMAT, a neurotransmitter transporter. J Biol Chem. 2010 Feb 12;285(7):5076-84. doi: 10.1074/jbc.M109.081216. Epub 2009 Dec 10. [Article]
- Wimalasena K: Vesicular monoamine transporters: structure-function, pharmacology, and medicinal chemistry. Med Res Rev. 2011 Jul;31(4):483-519. doi: 10.1002/med.20187. Epub 2010 Feb 4. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Potassium channel regulator activity
- Specific Function
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
- Gene Name
- DRD2
- Uniprot ID
- P14416
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 Da
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Prostaglandin-e2 9-reductase activity
- Specific Function
- NADPH-dependent reductase with broad substrate specificity. Catalyzes the reduction of a wide variety of carbonyl compounds including quinones, prostaglandins, menadione, plus various xenobiotics. ...
- Gene Name
- CBR1
- Uniprot ID
- P16152
- Uniprot Name
- Carbonyl reductase [NADPH] 1
- Molecular Weight
- 30374.73 Da
References
- Jankovic J, Clarence-Smith K: Tetrabenazine for the treatment of chorea and other hyperkinetic movement disorders. Expert Rev Neurother. 2011 Nov;11(11):1509-23. doi: 10.1586/ern.11.149. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- Poon LH, Kang GA, Lee AJ: Role of tetrabenazine for Huntington's disease-associated chorea. Ann Pharmacother. 2010 Jun;44(6):1080-9. doi: 10.1345/aph.1M582. Epub 2010 May 4. [Article]
Drug created at October 16, 2007 17:37 / Updated at February 20, 2024 23:55