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Identification
NameTetrabenazine
Accession NumberDB04844
TypeSmall Molecule
GroupsApproved
Description

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.

Structure
Thumb
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
TBZ
Tetra benazin
Tetrabenazina
Tetrabenazinum
Tetrabenzaine
Tetrabenzine
External Identifiers
  • Ro 1-9569
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Nitomantablet25 mgoralValeant Canada Lp Valeant Canada S.E.C.1996-12-09Not applicableCanada
PMS-tetrabenazinetablet25 mgoralPharmascience Inc2013-02-26Not applicableCanada
Tetrabenazinetablet25 mg/1oralOceanside Pharmaceuticals2015-07-20Not applicableUs
Tetrabenazinetablet12.5 mg/1oralOceanside Pharmaceuticals2015-07-20Not applicableUs
Tetrabenazine Tabletstablet25 mgoralSterimax Inc2013-08-29Not applicableCanada
Xenazinetablet12.5 mg/1oralLundbeck Inc.2008-11-24Not applicableUs
Xenazinetablet25 mg/1oralLundbeck Inc.2008-11-24Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-tetrabenazinetablet25 mgoralApotex Inc2013-11-01Not applicableCanada
Tetrabenazinetablet, coated12.5 mg/1oralCamber Pharmaceuticals, Inc.2015-08-17Not applicableUs
Tetrabenazinetablet12.5 mg/1oralSun Pharma Global FZE2015-08-17Not applicableUs
Tetrabenazinetablet25 mg/1oralSun Pharma Global FZE2015-08-17Not applicableUs
Tetrabenazinetablet, coated25 mg/1oralCamber Pharmaceuticals, Inc.2015-08-17Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
RubigenNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIZ9O08YRN8O
CAS number58-46-8
WeightAverage: 317.4226
Monoisotopic: 317.199093735
Chemical FormulaC19H27NO3
InChI KeyInChIKey=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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as tetrahydroisoquinolines. These are tetrahydrogenated isoquinoline derivatives.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassTetrahydroisoquinolines
Sub ClassNot Available
Direct ParentTetrahydroisoquinolines
Alternative Parents
Substituents
  • Tetrahydroisoquinoline
  • Anisole
  • Aralkylamine
  • Piperidinone
  • Alkyl aryl ether
  • Benzenoid
  • Piperidine
  • Cyclic ketone
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ketone
  • Azacycle
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationTreatment of hyperkinetic movement disorders like chorea in Huntington's disease, hemiballismus, senile chorea, Tourette syndrome and other tic disorders, and tardive dyskinesia
PharmacodynamicsProlongation 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 actionTetrabenazine 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).
Related Articles
AbsorptionFollowing 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 bindingTetrabenazine = 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.

SubstrateEnzymesProduct
Tetrabenazine
alpha-dihydrotetrabenazineDetails
Tetrabenazine
Not Available
b-dihydrotetrabenazineDetails
Route of eliminationAfter 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 lifeα-HTBZ = 7 hours; β-HTBZ = 5 hours; 9-desmethyl-β-DHTBZ = 12 hours.
Clearance

IV, 1.67 L/min in HD or tardive dyskinesia patients

ToxicityDose-limiting adverse effects are sedation, parkinsonism, akathsia, and depression. LD50 oral, mouse: 550 mg/kg
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.995
Blood Brain Barrier+0.9639
Caco-2 permeable+0.8608
P-glycoprotein substrateSubstrate0.7819
P-glycoprotein inhibitor IInhibitor0.8908
P-glycoprotein inhibitor IIInhibitor0.7631
Renal organic cation transporterInhibitor0.6484
CYP450 2C9 substrateNon-substrate0.8444
CYP450 2D6 substrateSubstrate0.6448
CYP450 3A4 substrateSubstrate0.8091
CYP450 1A2 substrateNon-inhibitor0.7482
CYP450 2C9 inhibitorNon-inhibitor0.9042
CYP450 2D6 inhibitorInhibitor0.7084
CYP450 2C19 inhibitorNon-inhibitor0.8191
CYP450 3A4 inhibitorNon-inhibitor0.8308
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8718
Ames testNon AMES toxic0.6674
CarcinogenicityNon-carcinogens0.9083
BiodegradationNot ready biodegradable0.9974
Rat acute toxicity2.8540 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6451
hERG inhibition (predictor II)Inhibitor0.7524
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral25 mg
Tabletoral12.5 mg/1
Tabletoral25 mg/1
Tablet, coatedoral12.5 mg/1
Tablet, coatedoral25 mg/1
Prices
Unit descriptionCostUnit
Xenazine 25 mg tablet74.57USD tablet
Xenazine 12.5 mg tablet37.29USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point126 °CMSDS
water solubilitySparingly solubleFDA label
pKa6.51FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.361 mg/mLALOGPS
logP3.23ALOGPS
logP3.4ChemAxon
logS-2.9ALOGPS
pKa (Strongest Acidic)18.24ChemAxon
pKa (Strongest Basic)7.41ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area38.77 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity91.31 m3·mol-1ChemAxon
Polarizability36.59 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
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
  1. Jankovic J, Beach J: Long-term effects of tetrabenazine in hyperkinetic movement disorders. Neurology. 1997 Feb;48(2):358-62. [PubMed:9040721 ]
  2. 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. [PubMed:20869622 ]
External Links
ATC CodesN07XX06
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (269 KB)
MSDSDownload (79.6 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Tetrabenazine can be increased when it is combined with Abiraterone.
AcepromazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Acetophenazine.
AmisulprideThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Amisulpride.
AripiprazoleThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Aripiprazole.
AzelastineTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Tetrabenazine.
BenzquinamideThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Benzquinamide.
BrexpiprazoleThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Brexpiprazole.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Tetrabenazine.
BuprenorphineTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
BupropionThe serum concentration of Tetrabenazine can be increased when it is combined with Bupropion.
CarphenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Carphenazine.
ChlormezanoneThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Chlorprothixene.
CinacalcetThe serum concentration of Tetrabenazine can be increased when it is combined with Cinacalcet.
CitalopramCitalopram may increase the QTc-prolonging activities of Tetrabenazine.
ClozapineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Clozapine.
CobicistatThe serum concentration of Tetrabenazine can be increased when it is combined with Cobicistat.
CocaineThe serum concentration of Tetrabenazine can be increased when it is combined with Cocaine.
DarunavirThe serum concentration of Tetrabenazine can be increased when it is combined with Darunavir.
DelavirdineThe serum concentration of Tetrabenazine can be increased when it is combined with Delavirdine.
DofetilideDofetilide may increase the QTc-prolonging activities of Tetrabenazine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Tetrabenazine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Tetrabenazine.
DroperidolThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Droperidol.
EthanolTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FencamfamineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Fencamfamine.
FluoxetineThe serum concentration of Tetrabenazine can be increased when it is combined with Fluoxetine.
FlupentixolThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Fluspirilene.
GoserelinGoserelin may increase the QTc-prolonging activities of Tetrabenazine.
HaloperidolThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Haloperidol.
HydrocodoneTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
IsocarboxazidThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Isocarboxazid.
IvabradineIvabradine may increase the QTc-prolonging activities of Tetrabenazine.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Tetrabenazine.
LinezolidThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Linezolid.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Tetrabenazine.
LoxapineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Loxapine.
LurasidoneThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Lurasidone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Tetrabenazine.
MesoridazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Mesoridazine.
MethotrimeprazineThe serum concentration of Tetrabenazine can be increased when it is combined with Methotrimeprazine.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Tetrabenazine.
MetyrosineThe risk or severity of adverse effects can be increased when Metyrosine is combined with Tetrabenazine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Tetrabenazine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Tetrabenazine.
MoclobemideThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Moclobemide.
MolindoneThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Molindone.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Tetrabenazine.
OctreotideOctreotide may increase the QTc-prolonging activities of Tetrabenazine.
OlanzapineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Ondansetron.
OrphenadrineTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PaliperidoneThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Paliperidone.
ParaldehydeTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe serum concentration of Tetrabenazine can be increased when it is combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Tetrabenazine can be decreased when it is combined with Peginterferon alfa-2b.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Tetrabenazine.
PerphenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Perphenazine.
PhenelzineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Phenelzine.
PimozideThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Piperacetazine.
PramipexoleTetrabenazine may increase the sedative activities of Pramipexole.
ProcarbazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Procarbazine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Promazine.
QuetiapineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Quetiapine.
RasagilineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Rasagiline.
RemoxiprideThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Tetrabenazine.
RisperidoneThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Risperidone.
RitonavirThe serum concentration of Tetrabenazine can be increased when it is combined with Ritonavir.
RopiniroleTetrabenazine may increase the sedative activities of Ropinirole.
RotigotineTetrabenazine may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tetrabenazine.
SelegilineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Selegiline.
SertindoleThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Sertindole.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Tetrabenazine.
StiripentolThe serum concentration of Tetrabenazine can be increased when it is combined with Stiripentol.
SulpirideThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Sulpiride.
SuvorexantTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tetrabenazine.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Tedizolid Phosphate.
TerbinafineThe serum concentration of Tetrabenazine can be increased when it is combined with Terbinafine.
ThalidomideTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Thiothixene.
TiclopidineThe metabolism of Tetrabenazine can be decreased when combined with Ticlopidine.
TipranavirThe serum concentration of Tetrabenazine can be increased when it is combined with Tipranavir.
TranylcypromineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Tranylcypromine.
TrifluoperazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Triflupromazine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Ziprasidone.
ZolpidemTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Zuclopenthixol.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
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. Requisite for vesicular amine storage prior to secretion via exocytosis.
Gene Name:
SLC18A2
Uniprot ID:
Q05940
Molecular Weight:
55712.075 Da
References
  1. 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. [PubMed:17233532 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  3. 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. [PubMed:19571144 ]
  4. 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. [PubMed:19223416 ]
  5. 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. [PubMed:20007701 ]
  6. 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. [PubMed:20135628 ]
Kind
Protein
Organism
Human
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
Molecular Weight:
50618.91 Da
References
  1. FDA label

Enzymes

Kind
Protein
Organism
Human
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. 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. [PubMed:20442355 ]
Kind
Protein
Organism
Human
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. Catalyzes the reduction of the antitumor anthracyclines doxorubicin and daunorubicin to the cardiotoxic compounds doxorubicinol and daunorubicinol. Can convert prostaglandin E2 to prostaglandin F2-alp...
Gene Name:
CBR1
Uniprot ID:
P16152
Molecular Weight:
30374.73 Da
References
  1. 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. [PubMed:22014129 ]
Comments
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Drug created on October 16, 2007 11:37 / Updated on September 16, 2013 17:26