Identification

Name
Ropinirole
Accession Number
DB00268  (APRD00302)
Type
Small Molecule
Groups
Approved, Investigational
Description

Ropinirole is a non-ergoline dopamine agonist, manufactured by GlaxoSmithKline. It is used in the treatment of Parkinson's disease, and is also one of two medications in the United States with an FDA-approved indication for the treatment of restless legs syndrome (the other being Pramipexole).

Structure
Thumb
Synonyms
  • Ropinirol
  • Ropinirolum
External IDs
SK&F 101468 / SK&F-101468
Product Ingredients
IngredientUNIICASInChI Key
Ropinirole HydrochlorideD7ZD41RZI991374-20-8XDXHAEQXIBQUEZ-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act RopiniroleTablet0.25 mgOralActavis Pharma Company2009-07-22Not applicableCanada
Act RopiniroleTablet2 mgOralActavis Pharma Company2009-07-22Not applicableCanada
Act RopiniroleTablet1 mgOralActavis Pharma Company2009-07-22Not applicableCanada
Act RopiniroleTablet5 mgOralActavis Pharma Company2009-07-22Not applicableCanada
RequipTablet, film coated0.5 mg/1OralGlaxosmithkline Inc1997-10-102018-11-30Us00007 4891 20 nlmimage10 cd18e6d7
RequipTablet, film coated1 mg/1OralGlaxo Wellcome SA1997-10-012019-07-31Us
RequipTablet1 mgOralGlaxosmithkline Inc1997-09-25Not applicableCanada
RequipTablet, film coated2 mg/1OralPhysicians Total Care, Inc.2006-01-302008-12-31Us
RequipTablet, film coated3 mg/1OralGlaxo Wellcome SA2001-06-192018-10-31Us
RequipTablet5 mgOralGlaxosmithkline Inc1997-09-25Not applicableCanada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-ropiniroleTablet0.25 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-ropiniroleTablet5.0 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-ropiniroleTablet1.0 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-ropiniroleTablet3.0 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-ropiniroleTablet0.5 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-ropiniroleTablet2.0 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-ropiniroleTablet4.0 mgOralApotex CorporationNot applicableNot applicableCanada
Dom-ropiniroleTablet0.25 mgOralDominion PharmacalNot applicableNot applicableCanada
Dom-ropiniroleTablet1.0 mgOralDominion PharmacalNot applicableNot applicableCanada
Dom-ropiniroleTablet5.0 mgOralDominion PharmacalNot applicableNot applicableCanada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
RequipRopinirole Hydrochloride + Ropinirole Hydrochloride + Ropinirole HydrochlorideTablet, film coatedOralGlaxoSmithKline2006-10-062006-10-06Us
RequipRopinirole Hydrochloride + Ropinirole Hydrochloride + Ropinirole HydrochlorideTablet, film coatedOralGlaxoSmithKline2006-10-062006-10-06Us
RequipRopinirole Hydrochloride + Ropinirole Hydrochloride + Ropinirole HydrochlorideTablet, film coatedOralGlaxoSmithKline2006-10-062006-10-06Us
International/Other Brands
Adartrel / ReQuip CR (GlaxoSmithKline) / Ronirol
Categories
UNII
030PYR8953
CAS number
91374-21-9
Weight
Average: 260.3746
Monoisotopic: 260.1888634
Chemical Formula
C16H24N2O
InChI Key
UHSKFQJFRQCDBE-UHFFFAOYSA-N
InChI
InChI=1S/C16H24N2O/c1-3-9-18(10-4-2)11-8-13-6-5-7-15-14(13)12-16(19)17-15/h5-7H,3-4,8-12H2,1-2H3,(H,17,19)
IUPAC Name
4-[2-(dipropylamino)ethyl]-2,3-dihydro-1H-indol-2-one
SMILES
CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1

Pharmacology

Indication

For the treatment of the signs and symptoms of idiopathic Parkinson's disease. Also used for the treatment of restless legs syndrome.

Associated Conditions
Pharmacodynamics

Ropinirole is a nonergot dopamine agonist with high relative in vitro specificity and full intrinsic activity at the D2 subfamily of dopamine receptors, binding with higher affinity to D3 than to D2 or D4 receptor subtypes. The relevance of D3 receptor binding in Parkinson's disease is unknown. The mechanism of ropinirole-induced postural hypotension is presumed to be due to a D2 -mediated blunting of the noradrenergic response to standing and subsequent decrease in peripheral vascular resistance.

Mechanism of action

Ropinirole binds the dopamine receptors D3 and D2. Although the precise mechanism of action of ropinirole as a treatment for Parkinson's disease is unknown, it is believed to be related to its ability to stimulate these receptors in the striatum. This conclusion is supported by electrophysiologic studies in animals that have demonstrated that ropinirole influences striatal neuronal firing rates via activation of dopamine receptors in the striatum and the substantia nigra, the site of neurons that send projections to the striatum.

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

Absolute bioavailability is 55%, indicating a first pass effect. Food does not affect the extent of absorption.

Volume of distribution
  • 7.5 L/kg
  • 525 L
Protein binding

40% bound to plasma proteins with a blood-to-plasma ratio of 1:1.

Metabolism

Hepatic. Ropinirole is extensively metabolized to inactive metabolites via N -despropylation and hydroxylation pathways, largely by the P450 isoenzyme CYP1A2. N-despropyl ropinirole is the predominant metabolite found in urine (40%), followed by the carboxylic acid metabolite (10%), and the glucuronide of the hydroxy metabolite (10%).

Route of elimination

Ropinirole is extensively metabolized by the liver to inactive metabolites, and less than 10% of the administered dose is excreted as unchanged drug in urine.

Half life

6 hours

Clearance
  • 47 L/hr [after oral administration to Parkinson's disease patients and patients with Restless Legs Syndrome]
Toxicity

Symptoms of overdose include agitation, chest pain, confusion, drowsiness, facial muscle movements, grogginess, increased jerkiness of movement, symptoms of low blood pressure (dizziness, light-headedness)upon standing, nausea, and vomiting.

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

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Ropinirole.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Ropinirole.
2,5-Dimethoxy-4-ethylamphetamineThe risk or severity of serotonin syndrome can be increased when Ropinirole is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may increase the sedative activities of Ropinirole.
3-isobutyl-1-methyl-7H-xanthineThe serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be increased when it is combined with Ropinirole.
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may increase the sedative activities of Ropinirole.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Ropinirole.
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may increase the sedative activities of Ropinirole.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Ropinirole.
4-Methoxyamphetamine4-Methoxyamphetamine may increase the sedative activities of Ropinirole.
Food Interactions
Not Available

References

Synthesis Reference
US4452808
General References
Not Available
External Links
Human Metabolome Database
HMDB0014413
KEGG Drug
D08489
KEGG Compound
C07564
PubChem Compound
5095
PubChem Substance
46507918
ChemSpider
4916
BindingDB
50020680
ChEBI
8888
ChEMBL
CHEMBL589
Therapeutic Targets Database
DAP001515
PharmGKB
PA164749035
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Ropinirole
ATC Codes
N04BC04 — Ropinirole
AHFS Codes
  • 28:36.20.08 — Nonergot-derivative Dopamine Receptor Agonists
FDA label
Download (267 KB)
MSDS
Download (29.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers2
1CompletedNot AvailablePharmacokinetic Study2
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentParkinson's Disease (PD)1
1CompletedTreatmentRestless Legs Syndrome (RLS)2
1, 2RecruitingTreatmentParkinson's Disease (PD)1
1, 2RecruitingTreatmentIdiopathic hyperprolactinemic disorder / Prolactinoma1
2CompletedTreatmentCerebrovascular Accidents / Hemiparesis1
2CompletedTreatmentDependence, Cocaine1
2CompletedTreatmentFibromyalgia Syndrome, Primary1
2CompletedTreatmentParkinson's Disease (PD)1
2CompletedTreatmentPeripheral T-Cell Lymphoma (PTCL)1
2Not Yet RecruitingTreatmentEnd Stage Renal Disease (ESRD) / Restless Legs Syndrome (RLS)1
2TerminatedTreatmentRestless Legs Syndrome (RLS)1
2Unknown StatusTreatmentUnverricht-Lundborg Syndrome1
3CompletedTreatmentIdiopathic Parkinson's Disease1
3CompletedTreatmentModerate to Severe Idiopathic Restless Legs Syndrome (RLS) / Restless Legs Syndrome (RLS)1
3CompletedTreatmentParkinson's Disease (PD)5
3CompletedTreatmentRestless Legs Syndrome (RLS)6
3TerminatedTreatmentLymphoma, Large-Cell, Diffuse1
3Unknown StatusTreatmentParkinson's Disease (PD)1
4CompletedDiagnosticParkinson's Disease (PD)1
4CompletedTreatmentBipolar Disorder (BD)1
4CompletedTreatmentParkinson's Disease (PD)1
4CompletedTreatmentRestless Legs Syndrome (RLS)1
4CompletedTreatmentSexual Dysfunctions1
4Enrolling by InvitationSupportive CareLiver Cirrhosis / Muscle Cramps1
4Unknown StatusTreatmentBipolar Disorder (BD) / Major Depressive Disorder (MDD)1
Not AvailableCompletedNot AvailableRestless Legs Syndrome (RLS)1
Not AvailableCompletedTreatmentParkinson's Disease (PD) / Restless Legs Syndrome (RLS)2
Not AvailableRecruitingNot AvailableAtypical Parkinson Disease / Corticobasal Degeneration / Gait, Frontal / Multiple System Atrophy (MSA) / Parkinson's Disease (PD) / Parkinsonian Disorders / Progressive Supranuclear Palsy (PSP)1

Pharmacoeconomics

Manufacturers
  • Smithkline beecham corp dba glaxosmithkline
  • Glaxosmithkline
  • Alembic ltd
  • Corepharma llc
  • Glenmark generics ltd
  • Huahai us inc
  • Mylan pharmaceuticals inc
  • Roxane laboratories inc
  • Teva pharmaceuticals usa inc
  • Wockhardt ltd
  • Zydus pharmaceuticals usa inc
Packagers
  • Amerisource Health Services Corp.
  • A-S Medication Solutions LLC
  • Atlantic Biologicals Corporation
  • Bryant Ranch Prepack
  • Cadila Healthcare Ltd.
  • Cardinal Health
  • Corepharma LLC
  • GlaxoSmithKline Inc.
  • Glenmark Generics Ltd.
  • Heartland Repack Services LLC
  • Heritage Pharmaceuticals
  • Innoviant Pharmacy Inc.
  • Kaiser Foundation Hospital
  • Lake Erie Medical and Surgical Supply
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Nucare Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Rebel Distributors Corp.
  • Resource Optimization and Innovation LLC
  • Roxane Labs
  • Stat Rx Usa
  • Teva Pharmaceutical Industries Ltd.
  • Vangard Labs Inc.
  • Wockhardt Ltd.
  • Zydus Pharmaceuticals
Dosage forms
FormRouteStrength
TabletOral1 mg
TabletOral2 mg
TabletOral5 mg
TabletOral3.0 mg
TabletOral4.0 mg
TabletOral0.25 mg
TabletOral0.5 mg
TabletOral1.0 mg
TabletOral2.0 mg
TabletOral5.0 mg
Tablet, film coatedOral
Tablet, film coatedOral0.25 mg/1
Tablet, film coatedOral0.5 mg/1
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral2 mg/1
Tablet, film coatedOral3 mg/1
Tablet, film coatedOral4 mg/1
Tablet, film coated, extended releaseOral2 mg/1
TabletOral4 mg/1
TabletOral5 mg/1
TabletOral0.25 mg/1
TabletOral0.5 mg/1
TabletOral1 mg/1
TabletOral2 mg/1
TabletOral3 mg/1
Tablet, coatedOral0.25 mg/1
Tablet, coatedOral0.5 mg/1
Tablet, coatedOral1 mg/1
Tablet, coatedOral2 mg/1
Tablet, coatedOral3 mg/1
Tablet, coatedOral4 mg/1
Tablet, coatedOral5 mg/1
Tablet, film coatedOral5 mg/1
Tablet, film coated, extended releaseOral12 mg/1
Tablet, film coated, extended releaseOral3 mg/1
Tablet, film coated, extended releaseOral4 mg/1
Tablet, film coated, extended releaseOral6 mg/1
Tablet, film coated, extended releaseOral8 mg/1
Prices
Unit descriptionCostUnit
Requip XL 12 mg 24 Hour tablet14.92USD tablet
Requip xl 12 mg tablet14.35USD tablet
Requip XL 8 mg 24 Hour tablet8.96USD tablet
Requip xl 6 mg tablet8.61USD tablet
Requip xl 8 mg tablet8.61USD tablet
Requip XL 4 mg 24 Hour tablet5.97USD tablet
Requip xl 4 mg tablet5.74USD tablet
Requip 5 mg Tablet3.87USD tablet
Requip 3 mg tablet3.41USD tablet
Requip 4 mg tablet3.41USD tablet
Requip 5 mg tablet3.41USD tablet
Requip 0.25 mg tablet3.29USD tablet
Requip 0.5 mg tablet3.29USD tablet
Requip 1 mg tablet3.29USD tablet
Requip 2 mg tablet3.29USD tablet
Requip xl 2 mg tablet2.87USD tablet
Ropinirole hcl 3 mg tablet2.65USD tablet
Ropinirole hcl 4 mg tablet2.65USD tablet
Ropinirole hcl 5 mg tablet2.65USD tablet
Ropinirole hcl 0.25 mg tablet2.55USD tablet
Ropinirole hcl 0.5 mg tablet2.55USD tablet
Ropinirole hcl 1 mg tablet2.55USD tablet
Ropinirole hcl 2 mg tablet2.55USD tablet
Co Ropinirole 5 mg Tablet1.8USD tablet
Pms-Ropinirole 5 mg Tablet1.8USD tablet
Ran-Ropinirole 5 mg Tablet1.8USD tablet
Ropinirole 5 mg Tablet1.8USD tablet
Requip 2 mg Tablet1.41USD tablet
Requip 1 mg Tablet1.28USD tablet
Co Ropinirole 2 mg Tablet0.65USD tablet
Pms-Ropinirole 2 mg Tablet0.65USD tablet
Ran-Ropinirole 2 mg Tablet0.65USD tablet
Ropinirole 2 mg Tablet0.65USD tablet
Co Ropinirole 1 mg Tablet0.59USD tablet
Pms-Ropinirole 1 mg Tablet0.59USD tablet
Ran-Ropinirole 1 mg Tablet0.59USD tablet
Ropinirole 1 mg Tablet0.59USD tablet
Requip 0.25 mg Tablet0.32USD tablet
Co Ropinirole 0.25 mg Tablet0.15USD tablet
Pms-Ropinirole 0.25 mg Tablet0.15USD tablet
Ran-Ropinirole 0.25 mg Tablet0.15USD tablet
Ropinirole 0.25 mg Tablet0.15USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5422123No1995-06-062012-06-06Us
US7927624No2011-04-192021-12-02Us
US8303986No2012-11-062021-04-12Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)243-250 °CNot Available
water solubility133 mg/mLNot Available
logP2.70ADLARD,M ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.353 mg/mLALOGPS
logP3.16ALOGPS
logP3.06ChemAxon
logS-2.9ALOGPS
pKa (Strongest Acidic)13.24ChemAxon
pKa (Strongest Basic)10.17ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area32.34 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity81.43 m3·mol-1ChemAxon
Polarizability31.19 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9971
Caco-2 permeable+0.6087
P-glycoprotein substrateSubstrate0.7604
P-glycoprotein inhibitor IInhibitor0.5458
P-glycoprotein inhibitor IINon-inhibitor0.8641
Renal organic cation transporterNon-inhibitor0.602
CYP450 2C9 substrateNon-substrate0.8593
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6903
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6959
Ames testNon AMES toxic0.7302
CarcinogenicityNon-carcinogens0.905
BiodegradationNot ready biodegradable0.9966
Rat acute toxicity2.6400 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8959
hERG inhibition (predictor II)Non-inhibitor0.7066
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 GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-0190000000-7e072cf65f341641938c
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-3960000000-47d2311adfeeacf4062d
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0006-7900000000-0891c66db163729a5360
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a4i-0090000000-88c0fa3d93090a0d06c6
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0pb9-3590000000-8fb5fc766313ee6bbd9e
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0k96-9400000000-f1b50dacd59a9bfe90b7

Taxonomy

Description
This compound belongs to the class of organic compounds known as indolines. These are compounds containing an indole moiety, which consists of pyrrolidine ring fused to benzene to form 2,3-dihydroindole.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Indoles and derivatives
Sub Class
Indolines
Direct Parent
Indolines
Alternative Parents
Phenethylamines / Aralkylamines / Trialkylamines / Secondary carboxylic acid amides / Lactams / Amino acids and derivatives / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives
show 1 more
Substituents
Dihydroindole / Phenethylamine / Aralkylamine / Benzenoid / Amino acid or derivatives / Carboxamide group / Lactam / Secondary carboxylic acid amide / Tertiary aliphatic amine / Tertiary amine
show 12 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
tertiary amine, indolones (CHEBI:8888)

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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. 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]
  3. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988]
Details
2. 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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. de Mey C, Enterling D, Meineke I, Yeulet S: Interactions between domperidone and ropinirole, a novel dopamine D2-receptor agonist. Br J Clin Pharmacol. 1991 Oct;32(4):483-8. [PubMed:1683559]
  3. Iida M, Miyazaki I, Tanaka K, Kabuto H, Iwata-Ichikawa E, Ogawa N: Dopamine D2 receptor-mediated antioxidant and neuroprotective effects of ropinirole, a dopamine agonist. Brain Res. 1999 Aug 14;838(1-2):51-9. [PubMed:10446316]
  4. 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]
  5. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988]
  6. Matsukawa N, Maki M, Yasuhara T, Hara K, Yu G, Xu L, Kim KM, Morgan JC, Sethi KD, Borlongan CV: Overexpression of D2/D3 receptors increases efficacy of ropinirole in chronically 6-OHDA-lesioned Parkinsonian rats. Brain Res. 2007 Jul 30;1160:113-23. Epub 2007 May 26. [PubMed:17573046]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. 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]
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 ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 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 ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation...
Gene Name
HTR2B
Uniprot ID
P41595
Uniprot Name
5-hydroxytryptamine receptor 2B
Molecular Weight
54297.41 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
7. 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]
Details
8. 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]
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 ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 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
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 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, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 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
Thioesterase 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 oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 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
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. 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
Protein homodimerization activity
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name
ADRA2C
Uniprot ID
P18825
Uniprot Name
Alpha-2C adrenergic receptor
Molecular Weight
49521.585 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]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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 oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  3. Wynalda MA, Wienkers LC: Assessment of potential interactions between dopamine receptor agonists and various human cytochrome P450 enzymes using a simple in vitro inhibition screen. Drug Metab Dispos. 1997 Oct;25(10):1211-4. [PubMed:9321526]
  4. Kaye CM, Nicholls B: Clinical pharmacokinetics of ropinirole. Clin Pharmacokinet. 2000 Oct;39(4):243-54. doi: 10.2165/00003088-200039040-00001. [PubMed:11069211]
  5. Ropinrole FDA label [File]
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]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
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]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Drug created on June 13, 2005 07:24 / Updated on December 10, 2018 13:39