You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameRotigotine
Accession NumberDB05271
TypeSmall Molecule
GroupsApproved
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 Identifiers
  • N-0923
  • SPM 962
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Neupropatch2 mgtransdermalUcb Canada Inc2013-06-27Not applicableCanada
Neupropatch, extended release1 mg/24htransdermalUCB, Inc.2012-04-02Not applicableUs
Neupropatch1 mgtransdermalUcb Canada Inc2013-12-19Not applicableCanada
NeuprokitUCB, Inc.2012-04-02Not applicableUs
Neupropatch, extended release8 mg/24htransdermalUCB, Inc.2012-04-02Not applicableUs
Neupropatch8 mgtransdermalUcb Canada Inc2013-06-27Not applicableCanada
Neupropatch, extended release6 mg/24htransdermalUCB, Inc.2012-04-02Not applicableUs
Neupropatch6 mgtransdermalUcb Canada Inc2013-06-27Not applicableCanada
Neupropatch, extended release4 mg/24htransdermalUCB, Inc.2012-04-02Not applicableUs
Neupropatch4 mgtransdermalUcb Canada Inc2013-06-27Not applicableCanada
Neupropatch, extended release3 mg/24htransdermalUCB, Inc.2012-04-02Not applicableUs
Neupropatch3 mgtransdermalUcb Canada Inc2013-12-19Not applicableCanada
Neupropatch, extended release2 mg/24htransdermalUCB, Inc.2012-04-02Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Rotigotine hydrochloride
125572-93-2
Thumb
  • InChI Key: CEXBONHIOKGWNU-NTISSMGPSA-N
  • Monoisotopic Mass: 351.142362856
  • Average Mass: 351.934
DBSALT000155
Categories
UNII87T4T8BO2E
CAS number99755-59-6
WeightAverage: 315.48
Monoisotopic: 315.165685603
Chemical FormulaC19H25NOS
InChI KeyKFQYTPMOWPVWEJ-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)[[email protected]]1CCC2=C(O)C=CC=C2C1
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassBenzenoids
ClassTetralins
Sub ClassNot Available
Direct ParentTetralins
Alternative Parents
Substituents
  • Tetralin
  • Phenol
  • 1-hydroxy-4-unsubstituted benzenoid
  • 1-hydroxy-2-unsubstituted benzenoid
  • Aralkylamine
  • Thiophene
  • Heteroaromatic compound
  • Tertiary amine
  • Tertiary aliphatic amine
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Organic oxygen compound
  • Amine
  • Organic nitrogen compound
  • Organooxygen compound
  • Organonitrogen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor use/treatment in neurologic disorders and parkinson's disease as well as moderate-to-severe primary Restless Legs Syndrome.
PharmacodynamicsRotigotine 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 actionRotigotine, 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
Related Articles
AbsorptionBioavailability 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 binding92% 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.

SubstrateEnzymesProduct
Rotigotine
Not Available
N-despropyl-rotigotineDetails
Rotigotine
Not Available
N-desthienylethyl-rotigotineDetails
Route of eliminationUrine (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 lifeAfter 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.
ClearanceNot Available
ToxicityThe 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot 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
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6699498 No2000-11-272020-11-27Us
US6884434 No2001-03-302021-03-30Us
US7413747 No1999-03-182019-03-18Us
US8246979 No2007-09-012027-09-01Us
US8246980 No2005-11-272025-11-27Us
US8617591 No2003-07-222023-07-22Us
Properties
StateSolid
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
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
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
ATC CodesN04BC09
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (1.34 MB)
MSDSDownload (29.9 KB)
Interactions
Drug Interactions
Drug
AlfentanilAlfentanil may increase the sedative activities of Rotigotine.
AlprazolamAlprazolam may increase the sedative activities of Rotigotine.
AmisulprideThe therapeutic efficacy of Amisulpride can be decreased when used in combination with Rotigotine.
AmitriptylineAmitriptyline may increase the sedative activities of Rotigotine.
AmobarbitalAmobarbital may increase the sedative activities of Rotigotine.
AmoxapineAmoxapine may increase the sedative activities of Rotigotine.
AzelastineAzelastine may increase the sedative activities of Rotigotine.
BaclofenBaclofen may increase the sedative activities of Rotigotine.
BrimonidineBrimonidine may increase the sedative activities of Rotigotine.
BromazepamBromazepam may increase the sedative activities of Rotigotine.
BrompheniramineBrompheniramine may increase the sedative activities of Rotigotine.
BuprenorphineBuprenorphine may increase the sedative activities of Rotigotine.
BupropionThe risk or severity of adverse effects can be increased when Rotigotine is combined with Bupropion.
BuspironeBuspirone may increase the sedative activities of Rotigotine.
ButabarbitalButabarbital may increase the sedative activities of Rotigotine.
ButorphanolButorphanol may increase the sedative activities of Rotigotine.
CarbamazepineCarbamazepine may increase the sedative activities of Rotigotine.
CarbinoxamineCarbinoxamine may increase the sedative activities of Rotigotine.
CarisoprodolCarisoprodol may increase the sedative activities of Rotigotine.
CetirizineCetirizine may increase the sedative activities of Rotigotine.
ChlordiazepoxideChlordiazepoxide may increase the sedative activities of Rotigotine.
ChlorphenamineChlorphenamine may increase the sedative activities of Rotigotine.
ChlorzoxazoneChlorzoxazone may increase the sedative activities of Rotigotine.
ClemastineClemastine may increase the sedative activities of Rotigotine.
ClobazamClobazam may increase the sedative activities of Rotigotine.
ClomipramineClomipramine may increase the sedative activities of Rotigotine.
ClonazepamClonazepam may increase the sedative activities of Rotigotine.
ClonidineClonidine may increase the sedative activities of Rotigotine.
ClorazepateClorazepate may increase the sedative activities of Rotigotine.
CyclizineCyclizine may increase the sedative activities of Rotigotine.
CyclobenzaprineCyclobenzaprine may increase the sedative activities of Rotigotine.
CyproheptadineCyproheptadine may increase the sedative activities of Rotigotine.
DantroleneDantrolene may increase the sedative activities of Rotigotine.
DesfluraneDesflurane may increase the sedative activities of Rotigotine.
DesipramineDesipramine may increase the sedative activities of Rotigotine.
DesloratadineDesloratadine may increase the sedative activities of Rotigotine.
Dexchlorpheniramine maleateDexchlorpheniramine maleate may increase the sedative activities of Rotigotine.
DiazepamDiazepam may increase the sedative activities of Rotigotine.
DimenhydrinateDimenhydrinate may increase the sedative activities of Rotigotine.
DiphenhydramineDiphenhydramine may increase the sedative activities of Rotigotine.
DoxepinDoxepin may increase the sedative activities of Rotigotine.
DoxylamineDoxylamine may increase the sedative activities of Rotigotine.
EfavirenzEfavirenz may increase the sedative activities of Rotigotine.
EntacaponeEntacapone may increase the sedative activities of Rotigotine.
EstazolamEstazolam may increase the sedative activities of Rotigotine.
EszopicloneEszopiclone may increase the sedative activities of Rotigotine.
EthanolEthanol may increase the sedative activities of Rotigotine.
EthosuximideEthosuximide may increase the sedative activities of Rotigotine.
EthotoinEthotoin may increase the sedative activities of Rotigotine.
EzogabineEzogabine may increase the sedative activities of Rotigotine.
FelbamateFelbamate may increase the sedative activities of Rotigotine.
FentanylFentanyl may increase the sedative activities of Rotigotine.
FexofenadineFexofenadine may increase the sedative activities of Rotigotine.
FlibanserinFlibanserin may increase the sedative activities of Rotigotine.
FlunarizineFlunarizine may increase the sedative activities of Rotigotine.
FlurazepamFlurazepam may increase the sedative activities of Rotigotine.
FosphenytoinFosphenytoin may increase the sedative activities of Rotigotine.
GabapentinGabapentin may increase the sedative activities of Rotigotine.
gabapentin enacarbilgabapentin enacarbil may increase the sedative activities of Rotigotine.
Gamma Hydroxybutyric AcidGamma Hydroxybutyric Acid may increase the sedative activities of Rotigotine.
GuanfacineGuanfacine may increase the sedative activities of Rotigotine.
HydrocodoneHydrocodone may increase the sedative activities of Rotigotine.
HydromorphoneHydromorphone may increase the sedative activities of Rotigotine.
HydroxyzineHydroxyzine may increase the sedative activities of Rotigotine.
ImipramineImipramine may increase the sedative activities of Rotigotine.
IsofluraneIsoflurane may increase the sedative activities of Rotigotine.
KetamineKetamine may increase the sedative activities of Rotigotine.
LamotrigineLamotrigine may increase the sedative activities of Rotigotine.
LevetiracetamLevetiracetam may increase the sedative activities of Rotigotine.
LevocabastineLevocabastine may increase the sedative activities of Rotigotine.
LevocetirizineLevocetirizine may increase the sedative activities of Rotigotine.
LevorphanolLevorphanol may increase the sedative activities of Rotigotine.
LoratadineLoratadine may increase the sedative activities of Rotigotine.
LorazepamLorazepam may increase the sedative activities of Rotigotine.
LoxapineThe therapeutic efficacy of Loxapine can be decreased when used in combination with Rotigotine.
MaprotilineMaprotiline may increase the sedative activities of Rotigotine.
MeclizineMeclizine may increase the sedative activities of Rotigotine.
MeprobamateMeprobamate may increase the sedative activities of Rotigotine.
MetaxaloneMetaxalone may increase the sedative activities of Rotigotine.
MethadoneMethadone may increase the sedative activities of Rotigotine.
MethocarbamolMethocarbamol may increase the sedative activities of Rotigotine.
MethohexitalMethohexital may increase the sedative activities of Rotigotine.
MethsuximideMethsuximide may increase the sedative activities of Rotigotine.
MethylphenidateThe risk or severity of adverse effects can be increased when Methylphenidate is combined with Rotigotine.
MetoclopramideThe therapeutic efficacy of Rotigotine can be decreased when used in combination with Metoclopramide.
MidazolamMidazolam may increase the sedative activities of Rotigotine.
MirtazapineMirtazapine may increase the sedative activities of Rotigotine.
MorphineMorphine may increase the sedative activities of Rotigotine.
NalbuphineNalbuphine may increase the sedative activities of Rotigotine.
NitrazepamNitrazepam may increase the sedative activities of Rotigotine.
Nitrous oxideNitrous oxide may increase the sedative activities of Rotigotine.
NortriptylineNortriptyline may increase the sedative activities of Rotigotine.
OlopatadineOlopatadine may increase the sedative activities of Rotigotine.
OrphenadrineOrphenadrine may increase the sedative activities of Rotigotine.
OxazepamOxazepam may increase the sedative activities of Rotigotine.
OxycodoneOxycodone may increase the sedative activities of Rotigotine.
OxymorphoneOxymorphone may increase the sedative activities of Rotigotine.
ParaldehydeParaldehyde may increase the sedative activities of Rotigotine.
PentazocinePentazocine may increase the sedative activities of Rotigotine.
PentobarbitalPentobarbital may increase the sedative activities of Rotigotine.
PerampanelPerampanel may increase the sedative activities of Rotigotine.
PethidinePethidine may increase the sedative activities of Rotigotine.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Rotigotine.
PhenobarbitalPhenobarbital may increase the sedative activities of Rotigotine.
PhenytoinPhenytoin may increase the sedative activities of Rotigotine.
PipotiazinePipotiazine may increase the sedative activities of Rotigotine.
PizotifenPizotifen may increase the sedative activities of Rotigotine.
PomalidomidePomalidomide may increase the sedative activities of Rotigotine.
PregabalinPregabalin may increase the sedative activities of Rotigotine.
PrimidonePrimidone may increase the sedative activities of Rotigotine.
PromethazinePromethazine may increase the sedative activities of Rotigotine.
PropofolPropofol may increase the sedative activities of Rotigotine.
ProtriptylineProtriptyline may increase the sedative activities of Rotigotine.
QuazepamQuazepam may increase the sedative activities of Rotigotine.
RamelteonRamelteon may increase the sedative activities of Rotigotine.
RemifentanilRemifentanil may increase the sedative activities of Rotigotine.
ReserpineReserpine may increase the sedative activities of Rotigotine.
ScopolamineScopolamine may increase the sedative activities of Rotigotine.
Scopolamine butylbromideScopolamine butylbromide may increase the sedative activities of Rotigotine.
SecobarbitalSecobarbital may increase the sedative activities of Rotigotine.
SevofluraneSevoflurane may increase the sedative activities of Rotigotine.
Sodium oxybateSodium oxybate may increase the sedative activities of Rotigotine.
StiripentolStiripentol may increase the sedative activities of Rotigotine.
SufentanilSufentanil may increase the sedative activities of Rotigotine.
SuvorexantSuvorexant may increase the sedative activities of Rotigotine.
TapentadolTapentadol may increase the sedative activities of Rotigotine.
TasimelteonTasimelteon may increase the sedative activities of Rotigotine.
TemazepamTemazepam may increase the sedative activities of Rotigotine.
TetrabenazineTetrabenazine may increase the sedative activities of Rotigotine.
ThalidomideThalidomide may increase the sedative activities of Rotigotine.
TiagabineTiagabine may increase the sedative activities of Rotigotine.
TizanidineTizanidine may increase the sedative activities of Rotigotine.
TolcaponeTolcapone may increase the sedative activities of Rotigotine.
TopiramateTopiramate may increase the sedative activities of Rotigotine.
TramadolTramadol may increase the sedative activities of Rotigotine.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Rotigotine.
TriazolamTriazolam may increase the sedative activities of Rotigotine.
TrimipramineTrimipramine may increase the sedative activities of Rotigotine.
TriprolidineTriprolidine may increase the sedative activities of Rotigotine.
VigabatrinVigabatrin may increase the sedative activities of Rotigotine.
ZaleplonZaleplon may increase the sedative activities of Rotigotine.
ZiconotideZiconotide may increase the sedative activities of Rotigotine.
ZiprasidoneThe therapeutic efficacy of Rotigotine can be decreased when used in combination with Ziprasidone.
ZolpidemZolpidem may increase the sedative activities of Rotigotine.
ZonisamideZonisamide may increase the sedative activities of Rotigotine.
ZopicloneZopiclone 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.

Targets

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
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 ]
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 which inhibit adenylyl cyclase. Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity).
Gene Name:
DRD4
Uniprot ID:
P21917
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 ]
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
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 ]
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
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:
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
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 signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
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 > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
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 ]
Comments
comments powered by Disqus
Drug created on November 18, 2007 11:23 / Updated on June 26, 2016 01:52