Identification

Name
Rotigotine
Accession Number
DB05271
Type
Small Molecule
Groups
Approved
Description

Rotigotine (Neupro) is a non-ergoline dopamine agonist indicated for the treatment of Parkinson's disease (PD) and restless legs syndrome (RLS) in Europe and the United States. It is formulated as a once-daily transdermal patch which provides a slow and constant supply of the drug over the course of 24 hours.

Like other dopamine agonists, rotigotine has been shown to possess antidepressant effects and may be useful in the treatment of depression as well.

Rotigotine was developed by Aderis Pharmaceuticals. In 1998, Aderis licensed worldwide development and commercialization rights for rotigotine to the German pharmaceutical company Schwarz Pharma (today a subsidiary of the Belgian company UCB S.A.). The drug has been approved by the EMEA for use in Europe in 2006 and is today being sold in several European countries. In 2007, the Neupro patch was approved by the Food and Drug Administration (FDA) as the first transdermal treatment of Parkinson's disease in the United States. However, as of 2008, Schwarz Pharma has recalled all Neupro patches in the United States and some in Europe because of problems with the delivery mechanism. Rotigotine has been authorized as a treatment for RLS since August 2008.

Structure
Thumb
Synonyms
  • (6S)-6-(propyl(2-(2-thienyl)ethyl)amino)-5,6,7,8-tetrahydro-1-naphthalenol
External IDs
N-0923 / SPM 962
Product Ingredients
IngredientUNIICASInChI Key
Rotigotine hydrochloride6Q1W9573L2125572-93-2CEXBONHIOKGWNU-NTISSMGPSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NeuproPatch4 mgTransdermalUcb Inc2013-06-27Not applicableCanada
NeuproPatch1 mgTransdermalUcb Inc2013-12-19Not applicableCanada
NeuproPatch, extended release8 mg/24hTransdermalUcb Inc2012-04-02Not applicableUs
NeuproPatch, extended release3 mg/24hTransdermalUcb Inc2012-04-02Not applicableUs
NeuproPatch8 mgTransdermalUcb Inc2013-06-27Not applicableCanada
NeuproPatch3 mgTransdermalUcb Inc2013-12-19Not applicableCanada
NeuproPatch, extended release6 mg/24hTransdermalUcb Inc2012-04-02Not applicableUs
NeuproPatch, extended release2 mg/24hTransdermalUcb Inc2012-04-02Not applicableUs
NeuproPatch6 mgTransdermalUcb Inc2013-06-27Not applicableCanada
NeuproPatch2 mgTransdermalUcb Inc2013-06-27Not applicableCanada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
NeuproRotigotine (2 mg/24h) + Rotigotine (4 mg/24h)KitUcb Inc2012-04-02Not applicableUs
NeuproRotigotine (2 mg/24h) + Rotigotine (4 mg/24h)KitUcb Inc2012-04-02Not applicableUs
Categories
UNII
87T4T8BO2E
CAS number
99755-59-6
Weight
Average: 315.48
Monoisotopic: 315.165685603
Chemical Formula
C19H25NOS
InChI Key
KFQYTPMOWPVWEJ-INIZCTEOSA-N
InChI
InChI=1S/C19H25NOS/c1-2-11-20(12-10-17-6-4-13-22-17)16-8-9-18-15(14-16)5-3-7-19(18)21/h3-7,13,16,21H,2,8-12,14H2,1H3/t16-/m0/s1
IUPAC Name
(6S)-6-{propyl[2-(thiophen-2-yl)ethyl]amino}-5,6,7,8-tetrahydronaphthalen-1-ol
SMILES
CCCN(CCC1=CC=CS1)[C@H]1CCC2=C(O)C=CC=C2C1

Pharmacology

Indication

For use/treatment in neurologic disorders and parkinson's disease as well as moderate-to-severe primary Restless Legs Syndrome.

Associated Conditions
Pharmacodynamics

Rotigotine is an agonist at all 5 dopamine receptor subtypes (D1-D5) but binds to the D3 receptor with the highest affinity. It is also an antagonist at α-2-adrenergic receptors and an agonist at the 5HT1A receptors. Rotigotine also inhibits dopamine uptake and prolactin secretion. There is no indication of a QT/QTc prolonging effect of Neupro in doses up to 24 mg/24 hours. The effects of Neupro at doses up to 24 mg/24 hours (supratherapeutic doses) on the QT/QTc interval was evaluated in a double-blind, randomized, placebo- and positive-controlled (moxifloxacin 400 mg IV, single dose) parallel-group trial with an overall treatment period of 52 days in male and female patients with advanced-stage Parkinson's disease. Assay sensitivity was confirmed by significant QTc prolongation by moxifloxacin.

Mechanism of action

Rotigotine, a member of the dopamine agonist class of drugs, is delivered continuously through the skin (transdermal) using a silicone-based patch that is replaced every 24 hours. A dopamine agonist works by activating dopamine receptors in the body, mimicking the effect of the neurotransmitter dopamine. The precise mechanism of action of rotigotine as a treatment for Restless Legs Syndrome is unknown but is thought to be related to its ability to stimulate dopamine

TargetActionsOrganism
AD(3) dopamine receptor
agonist
Human
AD(4) dopamine receptor
agonist
Human
UD(1B) dopamine receptor
agonist
Human
AD(2) dopamine receptor
agonist
Human
UD(1A) dopamine receptor
agonist
Human
U5-hydroxytryptamine receptor 1A
agonist
Human
UAlpha-2B adrenergic receptor
antagonist
Human
Absorption

Bioavailability varies depending on the application site. Differences in bioavailability were very small between the abdomen and hip (<1%). In contrast, the shoulder and thigh had a very large different in measured bioavailability (46%), with the shoulder showing the higher value. Tmax, 8 mg dose = 15 - 18 hours (it take approximately 3 hours until rotigotine reaches detectable levels in the plasma). The peak concentration cannot be observered. Steady state is reached in 2-3 days.

Volume of distribution

The weight normalized apparent volume of distribution, (Vd/F), in humans is approximately 84 L/kg after repeated dose administration.

Protein binding

92% in vitro and 89.5% in vivo.

Metabolism

Hepatic (CYP-mediated). Rotigotine is extensively and rapidly metabolized by conjugation and N-dealkylation. After intravenous dosing the predominant metabolites in human plasma are sulfate conjugates of rotigotine, glucuronide conjugates of rotigotine, sulfate conjugates of the N-despropyl-rotigotine and conjugates of N-desthienylethyl-rotigotine. Multiple CYP isoenzymes, sulfotransferases and two UDP-glucuronosyltransferases catalyze the metabolism of rotigotine.

Route of elimination

Urine (71%), Fecal (23%). Most of rotigotine that is excreted in the urine is in the form of inactive conjugates. Unchanged drug made up less <1%.

Half life

After removal of the patch, plasma levels decreased with a terminal half-life of 5 to 7 hours. The pharmacokinetic profile showed a biphasic elimination with an initial half-life of 3 hours.

Clearance
Not Available
Toxicity

The most likely symptoms of overdose would be those related to the pharmacodynamic profile of a dopamine agonist, including nausea, vomiting, hypotension, involuntary movements, hallucinations, confusion, convulsions, and other signs of excessive dopaminergic stimulation.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
7-Nitroindazole7-Nitroindazole may increase the sedative activities of Rotigotine.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe metabolism of Rotigotine can be decreased when combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
AbirateroneThe serum concentration of Rotigotine can be increased when it is combined with Abiraterone.
AcebutololThe risk or severity of adverse effects can be increased when Rotigotine is combined with Acebutolol.
AcepromazineAcepromazine may increase the sedative activities of Rotigotine.
AceprometazineAceprometazine may increase the sedative activities of Rotigotine.
AcetazolamideAcetazolamide may increase the sedative activities of Rotigotine.
Acetyl sulfisoxazoleThe metabolism of Rotigotine can be decreased when combined with Acetyl sulfisoxazole.
AdipiplonAdipiplon may increase the sedative activities of Rotigotine.
AgomelatineAgomelatine may increase the sedative activities of Rotigotine.
Food Interactions
  • Because rotigotine is administered transdermally, food should not affect absorption, and the product may be administered without regard to the timing of meals.

References

Synthesis Reference

Hans-Michael Wolff, Luc Quere, Jens Riedner, "NOVEL POLYMORPHIC FORM OF ROTIGOTINE AND PROCESS FOR PRODUCTION." U.S. Patent US20090143460, issued June 04, 2009.

US20090143460
General References
  1. Giladi N, Boroojerdi B, Korczyn AD, Burn DJ, Clarke CE, Schapira AH: Rotigotine transdermal patch in early Parkinson's disease: a randomized, double-blind, controlled study versus placebo and ropinirole. Mov Disord. 2007 Dec;22(16):2398-404. [PubMed:17935234]
  2. Chen JJ, Swope DM, Dashtipour K, Lyons KE: Transdermal rotigotine: a clinically innovative dopamine-receptor agonist for the management of Parkinson's disease. Pharmacotherapy. 2009 Dec;29(12):1452-67. doi: 10.1592/phco.29.12.1452. [PubMed:19947805]
  3. Perez-Lloret S, Rey MV, Ratti PL, Rascol O: Rotigotine transdermal patch for the treatment of Parkinson's Disease. Fundam Clin Pharmacol. 2013 Feb;27(1):81-95. doi: 10.1111/j.1472-8206.2012.01028.x. Epub 2012 Feb 9. [PubMed:22320451]
  4. de Biase S, Merlino G, Lorenzut S, Valente M, Gigli GL: ADMET considerations for restless leg syndrome drug treatments. Expert Opin Drug Metab Toxicol. 2012 Oct;8(10):1247-61. doi: 10.1517/17425255.2012.708023. Epub 2012 Jul 18. [PubMed:22808933]
External Links
KEGG Drug
D05768
PubChem Compound
59227
PubChem Substance
99443232
ChemSpider
53406
BindingDB
50123626
ChEBI
135351
ChEMBL
CHEMBL1303
PharmGKB
PA166165149
IUPHAR
941
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Rotigotine
ATC Codes
N04BC09 — Rotigotine
AHFS Codes
  • 28:36.20.08 — Nonergot-derivative Dopamine Receptor Agonists
FDA label
Download (1.34 MB)
MSDS
Download (29.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers3
1CompletedBasic ScienceHealthy Volunteers3
1CompletedBasic ScienceParkinson's Disease (PD)1
1CompletedTreatmentBioequivalence - Irritation and Sensitization Potential of Transdermal Patch1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentParkinson's Disease (PD)5
1RecruitingTreatmentParkinson's Disease (PD)1
2CompletedNot AvailableRestless Legs Syndrome (RLS)1
2CompletedTreatmentFibromyalgia Syndrome1
2CompletedTreatmentHemispatial Neglect / Motor Deficits / Right Hemisphere Stroke1
2CompletedTreatmentIdiopathic Restless Legs Syndrome2
2CompletedTreatmentParkinson's Disease (PD)5
2CompletedTreatmentRestless Legs Syndrome (RLS)2
2Not Yet RecruitingTreatmentPost-op Pain1
2RecruitingTreatmentAlzheimer's Disease (AD)1
2TerminatedTreatmentParkinson's Disease (PD)1
2, 3CompletedTreatmentEarly Parkinson's Disease1
2, 3CompletedTreatmentParkinson's Disease (PD)1
3Active Not RecruitingTreatmentApathy / Parkinson's Disease (PD)1
3CompletedTreatmentAdvanced Parkinson's Disease1
3CompletedTreatmentAdvanced Stage Parkinson's Disease1
3CompletedTreatmentEarly Stage Parkinson's Disease1
3CompletedTreatmentEarly-Stage Parkinson's Disease1
3CompletedTreatmentEnd-Stage Renal Disease (ESRD) / Restless Legs Syndrome (RLS)1
3CompletedTreatmentIdiopathic Parkinson's Disease4
3CompletedTreatmentIdiopathic Restless Legs Syndrome2
3CompletedTreatmentParkinson's Disease (PD)8
3CompletedTreatmentParkinson's Disease, Idiopathic1
3CompletedTreatmentRestless Legs Syndrome (RLS)5
3TerminatedTreatmentAdvanced Parkinson's Disease1
3TerminatedTreatmentParkinson's Disease (PD)1
4Active Not RecruitingTreatmentNocturnal Hypokinesia1
4CompletedTreatmentAdvanced Idiopathic Parkinson's Disease2
4CompletedTreatmentEkbom Syndrome / Restless Legs Syndrome (RLS) / Willis-Ekbom Disease1
4CompletedTreatmentIdiopathic Parkinson's Disease3
4CompletedTreatmentParkinson's Disease (PD)1
4CompletedTreatmentParkinson´s Disease1
4CompletedTreatmentRestless Legs Syndrome (RLS)2
4RecruitingTreatmentAnxiety Disorders / Parkinson's Disease (PD)1
Not AvailableCompletedNot AvailableConditions for Which There is a Documented Medical Necessity to Receive Treatment With Rotigotine1
Not AvailableCompletedNot AvailableIdiopathic Parkinson's Disease1
Not AvailableCompletedNot AvailableIdiopathic Restless Legs Syndrome1
Not AvailableUnknown StatusNot AvailableParkinson's Disease (PD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Kit
PatchTransdermal1 mg
PatchTransdermal2 mg
PatchTransdermal3 mg
PatchTransdermal4 mg
PatchTransdermal6 mg
PatchTransdermal8 mg
Patch, extended releaseTransdermal1 mg/24h
Patch, extended releaseTransdermal2 mg/24h
Patch, extended releaseTransdermal3 mg/24h
Patch, extended releaseTransdermal4 mg/24h
Patch, extended releaseTransdermal6 mg/24h
Patch, extended releaseTransdermal8 mg/24h
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8246979No2007-09-012027-09-01Us
US8617591No2003-07-222023-07-22Us
US7413747No1999-03-182019-03-18Us
US6884434No2001-03-302021-03-30Us
US6699498No2000-11-272020-11-27Us
US8246980No2005-11-272025-11-27Us
US9925150No2012-03-012032-03-01Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP4.70BIOBYTE STARLIST (2009)
Predicted Properties
PropertyValueSource
Water Solubility0.00904 mg/mLALOGPS
logP5.01ALOGPS
logP4.34ChemAxon
logS-4.5ALOGPS
pKa (Strongest Acidic)10.03ChemAxon
pKa (Strongest Basic)10.97ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area23.47 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity94.56 m3·mol-1ChemAxon
Polarizability36.56 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9968
Blood Brain Barrier+0.9808
Caco-2 permeable+0.5864
P-glycoprotein substrateSubstrate0.7351
P-glycoprotein inhibitor INon-inhibitor0.6945
P-glycoprotein inhibitor IIInhibitor0.6398
Renal organic cation transporterInhibitor0.6722
CYP450 2C9 substrateNon-substrate0.5674
CYP450 2D6 substrateNon-substrate0.5502
CYP450 3A4 substrateSubstrate0.5937
CYP450 1A2 substrateInhibitor0.724
CYP450 2C9 inhibitorNon-inhibitor0.7855
CYP450 2D6 inhibitorInhibitor0.8238
CYP450 2C19 inhibitorNon-inhibitor0.7351
CYP450 3A4 inhibitorInhibitor0.5691
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8638
Ames testNon AMES toxic0.5
CarcinogenicityNon-carcinogens0.9255
BiodegradationNot ready biodegradable0.9912
Rat acute toxicity2.6229 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6074
hERG inhibition (predictor II)Inhibitor0.7098
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as tetralins. These are polycyclic aromatic compounds containing a tetralin moiety, which consists of a benzene fused to a cyclohexane.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Tetralins
Sub Class
Not Available
Direct Parent
Tetralins
Alternative Parents
Aralkylamines / 1-hydroxy-4-unsubstituted benzenoids / 1-hydroxy-2-unsubstituted benzenoids / Thiophenes / Heteroaromatic compounds / Trialkylamines / Organopnictogen compounds / Organooxygen compounds / Hydrocarbon derivatives
Substituents
Tetralin / 1-hydroxy-4-unsubstituted benzenoid / 1-hydroxy-2-unsubstituted benzenoid / Aralkylamine / Thiophene / Heteroaromatic compound / Tertiary amine / Tertiary aliphatic amine / Organoheterocyclic compound / Hydrocarbon derivative
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Details
1. D(3) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
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:18691132]
Details
2. D(4) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Sh3 domain binding
Specific Function
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
Molecular Weight
48359.86 Da
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:18691132]
Details
3. D(1B) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD5
Uniprot ID
P21918
Uniprot Name
D(1B) dopamine receptor
Molecular Weight
52950.5 Da
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:18691132]
Details
4. D(2) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
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
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:18691132]
Details
5. D(1A) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD1
Uniprot ID
P21728
Uniprot Name
D(1A) dopamine receptor
Molecular Weight
49292.765 Da
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:18691132]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
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:18691132]
  2. Scheller D, Ullmer C, Berkels R, Gwarek M, Lubbert H: The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):73-86. doi: 10.1007/s00210-008-0341-4. Epub 2008 Aug 14. [PubMed:18704368]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Epinephrine binding
Specific Function
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...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 Da
References
  1. Scheller D, Ullmer C, Berkels R, Gwarek M, Lubbert H: The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):73-86. doi: 10.1007/s00210-008-0341-4. Epub 2008 Aug 14. [PubMed:18704368]

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
  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:18691132]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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
  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:18691132]

Drug created on November 18, 2007 11:23 / Updated on October 16, 2018 08:38