Identification
- Summary
Rotigotine is a non-selective dopamine agonist used for the treatment of Parkinson's Disease and Restless Leg Syndrome.
- Brand Names
- Neupro
- Generic Name
- Rotigotine
- DrugBank Accession Number
- DB05271
- Background
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 to Schwarz Pharma of Germany. It was approved by the European Medicines Agency in 2006 and by the FDA in 2007. However, all Neupro patches in the United States and some of Europe were recalled in 2008 due to delivery mechanism issues. Rotigotine has been authorized as a treatment for RLS since August 2008.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Rotigotine (DB05271)
- Weight
- Average: 315.48
Monoisotopic: 315.165685603 - Chemical Formula
- C19H25NOS
- Synonyms
- (6S)-6-(propyl(2-(2-thienyl)ethyl)amino)-5,6,7,8-tetrahydro-1-naphthalenol
- Rotigotina
- Rotigotine
- External IDs
- N-0923
- SPM 962
Pharmacology
- Indication
For use/treatment in neurologic disorders and parkinson's disease as well as moderate-to-severe primary Restless Legs Syndrome.
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 Parkinson's disease •••••••••••• Management of Moderate restless leg syndrome •••••••••••• Management of Severe restless leg syndrome •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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
Target Actions Organism ADopamine D3 receptor agonistHumans ADopamine D4 receptor agonistHumans ADopamine D2 receptor agonistHumans UDopamine D5 receptor agonistHumans UDopamine D1 receptor agonistHumans U5-hydroxytryptamine receptor 1A agonistHumans UAlpha-2B adrenergic receptor antagonistHumans - 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.
Hover over products below to view reaction partners
- 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
- Adverse Effects
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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.
- 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);">
- Not Available
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 software1,2-Benzodiazepine 1,2-Benzodiazepine may increase the sedative activities of Rotigotine. Abaloparatide The risk or severity of adverse effects can be increased when Abaloparatide is combined with Rotigotine. Abametapir The serum concentration of Rotigotine can be increased when it is combined with Abametapir. Abatacept The metabolism of Rotigotine can be increased when combined with Abatacept. Abiraterone The metabolism of Rotigotine can be decreased when combined with Abiraterone. - Food Interactions
- No interactions found.
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.- Product Ingredients
Ingredient UNII CAS InChI Key Rotigotine hydrochloride 6Q1W9573L2 125572-93-2 CEXBONHIOKGWNU-NTISSMGPSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Leganto Patch 4 mg/24h Transdermal Ucb Pharma S.A. 2021-02-11 2022-02-18 EU 
Leganto Patch 8 mg/24h Transdermal Ucb Pharma S.A. 2021-02-11 2022-02-18 EU Leganto Patch 3 mg/24h Transdermal Ucb Pharma S.A. 2021-02-11 2022-02-18 EU Leganto Patch 8 mg/24h Transdermal Ucb Pharma S.A. 2021-02-11 2022-02-18 EU Leganto Patch 2 mg/24h Transdermal Ucb Pharma S.A. 2021-02-11 2022-02-18 EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Neupro Rotigotine (2 mg/24h) + Rotigotine (4 mg/24h) Kit; Patch, extended release Transdermal UCB, Inc. 2012-04-02 Not applicable US 
Neupro Rotigotine (2 mg/24h) + Rotigotine (4 mg/24h) Kit; Patch, extended release Transdermal UCB, Inc. 2012-04-02 Not applicable US NEUPRO TRANSDERMAL 28 FLASTER BASLANGIC TEDAVI PAKETI Rotigotine (2 mg/24h) + Rotigotine (4 mg/24h) + Rotigotine (6 mg/24h) + Rotigotine (8 mg/24h) Kit; Patch Transdermal UCB PHARMA A.Ş. 2012-06-06 2018-04-19 Turkey 
NEUPRO TRANSDERMAL 28 FLASTER BASLANGIC TEDAVI PAKETI Rotigotine (2 mg/24h) + Rotigotine (4 mg/24h) + Rotigotine (6 mg/24h) + Rotigotine (8 mg/24h) Kit; Patch Transdermal UCB PHARMA A.Ş. 2012-06-06 2018-04-19 Turkey NEUPRO TRANSDERMAL 28 FLASTER BASLANGIC TEDAVI PAKETI Rotigotine (2 mg/24h) + Rotigotine (4 mg/24h) + Rotigotine (6 mg/24h) + Rotigotine (8 mg/24h) Kit; Patch Transdermal UCB PHARMA A.Ş. 2012-06-06 2018-04-19 Turkey
Categories
- ATC Codes
- N04BC09 — Rotigotine
- Drug Categories
- Agents that produce hypertension
- Anti-Parkinson Agents (Dopamine Agonist)
- Anti-Parkinson Drugs
- Antidepressive Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 Inhibitors (weak)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Inhibitors (weak)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Dopamine Agents
- Dopamine Agonists
- Hypotensive Agents
- Naphthalenes
- Nervous System
- Neurotransmitter Agents
- Nonergot-derivative Dopamine Receptor Agonists
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 5-HT1 Receptor Agonists
- Serotonin Agents
- Serotonin Receptor Agonists
- Sulfur Compounds
- Chemical TaxonomyProvided by Classyfire
- 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
- 1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / Amine / Aralkylamine / Aromatic heteropolycyclic compound / Heteroaromatic compound / Hydrocarbon derivative / Organic nitrogen compound / Organic oxygen compound / Organoheterocyclic compound
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 87T4T8BO2E
- CAS number
- 99755-59-6
- 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
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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- External Links
- KEGG Drug
- D05768
- PubChem Compound
- 59227
- PubChem Substance
- 99443232
- ChemSpider
- 53406
- BindingDB
- 50123626
- 616739
- ChEBI
- 135351
- ChEMBL
- CHEMBL1303
- ZINC
- ZINC000000004028
- PharmGKB
- PA166165149
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- R5F
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Rotigotine
- PDB Entries
- 8irr / 8irs / 8irt / 8iru / 8irv
- FDA label
- Download (1.34 MB)
- MSDS
- Download (29.9 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 Treatment Advanced Idiopathic Parkinson's Disease 2 4 Completed Treatment Ekbom Syndrome / Restless Legs Syndrome (RLS) / Willis-Ekbom Disease 1 4 Completed Treatment Idiopathic Parkinson's Disease 3 4 Completed Treatment Parkinson's Disease (PD) 2 4 Completed Treatment Restless Legs Syndrome (RLS) 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Kit; patch, extended release Transdermal Patch Transdermal 1 mg / 24 hour Patch Transdermal 2 mg / 24 hour Patch Transdermal 2 MG/24H Patch Transdermal 3 mg / 24 hour Patch Transdermal 4 mg / 24 hour Patch Transdermal 4 MG/24H Patch Transdermal 6 mg / 24 hour Patch Transdermal 8 mg / 24 hour Patch, extended release Transdermal 1 MG/24hr Patch, extended release Transdermal 1 mg/24h Patch, extended release Transdermal 2 MG/24hr Patch, extended release Transdermal 2 mg/24h Patch, extended release Transdermal 3 mg/24h Patch, extended release Transdermal 3 MG/24hr Patch, extended release Transdermal 4 MG/24hr Patch, extended release Transdermal 4 mg/24h Patch, extended release Transdermal 6 MG/24hr Patch, extended release Transdermal 6 mg/24h Patch, extended release Transdermal 8 MG/24hr Patch, extended release Transdermal 8 mg/24h Drug delivery system Transdermal 18 mg Patch Transdermal 1 mg Patch Transdermal 2 mg Patch Transdermal 4.5 mg Patch Transdermal 3 mg Patch Transdermal 4 mg Patch Transdermal 6 mg Patch Transdermal 8 mg Kit; patch Transdermal Patch Transdermal 4.5 mg/10cm2 Patch Transdermal 9.0 mg/20cm2 Patch Transdermal 13.5 mg/30cm2 Patch Transdermal 18 mg/40cm2 Drug delivery system Transdermal 9 mg Drug delivery system Transdermal 13.5 mg Drug delivery system Transdermal 4.5 mg Patch Transdermal 4.5000 mg Plaster Transdermal 1 mg/24stunde Plaster Transdermal 2 mg/24stunde Plaster Transdermal 3 mg/24stunde Plaster Transdermal 4 mg/24stunde Plaster Transdermal 6 mg/24stunde Plaster Transdermal 8 mg/24stunde Patch Transdermal 1 mg/24h Patch Transdermal 3 mg/24h Patch Transdermal 6 mg/24h Patch Transdermal 8 mg/24h Patch Transdermal 2 mg/24hr Patch Transdermal 4 mg/24hr Patch Transdermal 6 mg/24hr Patch Transdermal 8 mg/24hr - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8246979 No 2012-08-21 2027-09-01 US US8617591 No 2013-12-31 2023-07-22 US US7413747 No 2008-08-19 2019-03-18 US US6884434 No 2005-04-26 2021-03-30 US US6699498 No 2004-03-02 2020-11-27 US US8246980 No 2012-08-21 2025-11-27 US US9925150 No 2018-03-27 2032-03-01 US US10130589 No 2018-11-20 2030-12-22 US US10350174 No 2019-07-16 2030-12-22 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 4.70 BIOBYTE STARLIST (2009) - Predicted Properties
Property Value Source Water Solubility 0.00904 mg/mL ALOGPS logP 5.01 ALOGPS logP 4.34 Chemaxon logS -4.5 ALOGPS pKa (Strongest Acidic) 10.03 Chemaxon pKa (Strongest Basic) 10.97 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 23.47 Å2 Chemaxon Rotatable Bond Count 6 Chemaxon Refractivity 94.56 m3·mol-1 Chemaxon Polarizability 36.56 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 + 0.9808 Caco-2 permeable + 0.5864 P-glycoprotein substrate Substrate 0.7351 P-glycoprotein inhibitor I Non-inhibitor 0.6945 P-glycoprotein inhibitor II Inhibitor 0.6398 Renal organic cation transporter Inhibitor 0.6722 CYP450 2C9 substrate Non-substrate 0.5674 CYP450 2D6 substrate Non-substrate 0.5502 CYP450 3A4 substrate Substrate 0.5937 CYP450 1A2 substrate Inhibitor 0.724 CYP450 2C9 inhibitor Non-inhibitor 0.7855 CYP450 2D6 inhibitor Inhibitor 0.8238 CYP450 2C19 inhibitor Non-inhibitor 0.7351 CYP450 3A4 inhibitor Inhibitor 0.5691 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.8638 Ames test Non AMES toxic 0.5 Carcinogenicity Non-carcinogens 0.9255 Biodegradation Not ready biodegradable 0.9912 Rat acute toxicity 2.6229 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6074 hERG inhibition (predictor II) Inhibitor 0.7098
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0109000000-ca52e9f21427895310e0 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-02t9-0906000000-5dcfea96f1844607f62e Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0496000000-6a079e20ffab97090232 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-5942000000-caf759018013d9d27f0c Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-01ot-2910000000-82102304754d6af41353 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-024j-3910000000-c6c78631a474f0a7e2e6 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]- 184.2886082 predictedDarkChem Lite v0.1.0 [M-H]- 171.20937 predictedDeepCCS 1.0 (2019) [M+H]+ 185.4024082 predictedDarkChem Lite v0.1.0 [M+H]+ 173.56737 predictedDeepCCS 1.0 (2019) [M+Na]+ 184.7890082 predictedDarkChem Lite v0.1.0 [M+Na]+ 179.6605 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- 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
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- 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
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- FDA Approved Drug Products: Neupro (rotigotine transdermal system) for topical application [Link]
Drug created at November 18, 2007 18:23 / Updated at February 20, 2024 23:55