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Identification
NameLisuride
Accession NumberDB00589  (APRD00636)
TypeSmall Molecule
GroupsApproved
DescriptionAn ergot derivative that acts as an agonist at dopamine D2 receptors (dopamine agonists). It may also act as an antagonist at dopamine D1 receptors, and as an agonist at some serotonin receptors (serotonin agonists). [PubChem]
Structure
Thumb
Synonyms
Lisurid
Lisurida
Lisuride
Lisuridum
N'-((8alpha)-9,10-didehydro-6-methylergolin-8-yl)-N,N-diethylurea
External Identifiers
  • MIP 2204
  • SH 31072 B
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ArolacLisapharm
DipergonBayer
DoperginBayer
DopergineBayer Santé
ProclacamNot Available
RevanilNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Lysuride Maleate
ThumbNot applicableDBSALT001034
Categories
UNIIE0QN3D755O
CAS number18016-80-3
WeightAverage: 338.4466
Monoisotopic: 338.210661474
Chemical FormulaC20H26N4O
InChI KeyInChIKey=BKRGVLQUQGGVSM-KBXCAEBGSA-N
InChI
InChI=1S/C20H26N4O/c1-4-24(5-2)20(25)22-14-10-16-15-7-6-8-17-19(15)13(11-21-17)9-18(16)23(3)12-14/h6-8,10-11,14,18,21H,4-5,9,12H2,1-3H3,(H,22,25)/t14-,18+/m0/s1
IUPAC Name
3,3-diethyl-1-[(4S,7R)-6-methyl-6,11-diazatetracyclo[7.6.1.0²,⁷.0¹²,¹⁶]hexadeca-1(16),2,9,12,14-pentaen-4-yl]urea
SMILES
[H][C@@]12CC3=CNC4=CC=CC(=C34)C1=C[C@@H](CN2C)NC(=O)N(CC)CC
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as indoloquinolines. These are polycyclic aromatic compounds containing an indole fused to a quinoline.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassQuinolines and derivatives
Sub ClassIndoloquinolines
Direct ParentIndoloquinolines
Alternative Parents
Substituents
  • Indoloquinoline
  • Ergoline skeleton
  • Benzoquinoline
  • Pyrroloquinoline
  • Alkaloid or derivatives
  • Isoindole or derivatives
  • Indole or derivatives
  • Indole
  • Aralkylamine
  • Tetrahydropyridine
  • Benzenoid
  • Heteroaromatic compound
  • Pyrrole
  • Urea
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the management of Parkinson's Disease
PharmacodynamicsNot Available
Mechanism of actionLisuride is an anti-Parkinson drug chemically related to the dopaminergic ergoline Parkinson's drugs. Lisuride binds to the 5-HT(1A) and 5-HT(2A/2C) receptors. It is also thought to bind to the dopamine receptor and to act as a dopamine agonist. Evidence has also emerged that Lisuride also binds to the Histamine H1 receptor. Lisuride is also used to lower prolactin and, in low doses, to prevent migraine attacks.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingabout 15%
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
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+1.0
Blood Brain Barrier+0.9382
Caco-2 permeable-0.6106
P-glycoprotein substrateSubstrate0.9135
P-glycoprotein inhibitor IInhibitor0.7002
P-glycoprotein inhibitor IIInhibitor0.7091
Renal organic cation transporterNon-inhibitor0.6231
CYP450 2C9 substrateNon-substrate0.8394
CYP450 2D6 substrateSubstrate0.8919
CYP450 3A4 substrateSubstrate0.7279
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorInhibitor0.7959
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5131
Ames testNon AMES toxic0.5
CarcinogenicityNon-carcinogens0.9156
BiodegradationNot ready biodegradable0.9797
Rat acute toxicity3.1801 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.572
hERG inhibition (predictor II)Inhibitor0.617
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP2.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.14 mg/mLALOGPS
logP2.37ALOGPS
logP2.17ChemAxon
logS-3.4ALOGPS
pKa (Strongest Acidic)15.36ChemAxon
pKa (Strongest Basic)6.88ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area51.37 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity101.81 m3·mol-1ChemAxon
Polarizability38.81 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesG02CB02N02CA07
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINEThe metabolism of Lisuride can be decreased when combined with 7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE.
AbirateroneThe metabolism of Lisuride can be decreased when combined with Abiraterone.
AmiodaroneThe metabolism of Lisuride can be decreased when combined with Amiodarone.
AprepitantThe serum concentration of Lisuride can be increased when it is combined with Aprepitant.
ArtemetherThe metabolism of Lisuride can be decreased when combined with Artemether.
AtazanavirThe metabolism of Lisuride can be decreased when combined with Atazanavir.
AtomoxetineThe metabolism of Lisuride can be decreased when combined with Atomoxetine.
BenmoxinThe metabolism of Lisuride can be decreased when combined with Benmoxin.
BetaxololThe metabolism of Lisuride can be decreased when combined with Betaxolol.
BexaroteneThe serum concentration of Lisuride can be decreased when it is combined with Bexarotene.
BoceprevirThe metabolism of Lisuride can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Lisuride can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Lisuride can be decreased when it is combined with Bosentan.
BromocriptineBromocriptine may increase the vasoconstricting activities of Lisuride.
BupropionThe metabolism of Lisuride can be decreased when combined with Bupropion.
CabergolineCabergoline may increase the vasoconstricting activities of Lisuride.
CarbamazepineThe metabolism of Lisuride can be increased when combined with Carbamazepine.
CaroxazoneThe metabolism of Lisuride can be decreased when combined with Caroxazone.
CelecoxibThe metabolism of Lisuride can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Lisuride can be increased when it is combined with Ceritinib.
ChloroquineThe metabolism of Lisuride can be decreased when combined with Chloroquine.
ChlorpromazineThe metabolism of Lisuride can be decreased when combined with Chlorpromazine.
CholecalciferolThe metabolism of Lisuride can be decreased when combined with Cholecalciferol.
CimetidineThe metabolism of Lisuride can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Lisuride can be decreased when combined with Cinacalcet.
CitalopramThe metabolism of Lisuride can be decreased when combined with Citalopram.
ClarithromycinThe metabolism of Lisuride can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Lisuride can be decreased when combined with Clemastine.
ClobazamThe metabolism of Lisuride can be decreased when combined with Clobazam.
ClomipramineThe metabolism of Lisuride can be decreased when combined with Clomipramine.
ClotrimazoleThe metabolism of Lisuride can be decreased when combined with Clotrimazole.
ClozapineThe metabolism of Lisuride can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Lisuride can be increased when it is combined with Cobicistat.
CocaineThe metabolism of Lisuride can be decreased when combined with Cocaine.
ConivaptanThe serum concentration of Lisuride can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Lisuride can be decreased when combined with Crizotinib.
CyclosporineThe metabolism of Lisuride can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Lisuride can be decreased when it is combined with Dabrafenib.
DarifenacinThe metabolism of Lisuride can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Lisuride can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Lisuride can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Lisuride can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Lisuride can be decreased when combined with Delavirdine.
DesipramineThe metabolism of Lisuride can be decreased when combined with Desipramine.
DexamethasoneThe serum concentration of Lisuride can be decreased when it is combined with Dexamethasone.
DihydroergotamineDihydroergotamine may increase the vasoconstricting activities of Lisuride.
DiltiazemThe metabolism of Lisuride can be decreased when combined with Diltiazem.
DiphenhydramineThe metabolism of Lisuride can be decreased when combined with Diphenhydramine.
DoxycyclineThe metabolism of Lisuride can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Lisuride can be decreased when combined with Dronedarone.
DroxidopaLisuride may increase the hypertensive activities of Droxidopa.
DuloxetineThe metabolism of Lisuride can be decreased when combined with Duloxetine.
EfavirenzThe serum concentration of Lisuride can be decreased when it is combined with Efavirenz.
EliglustatThe metabolism of Lisuride can be decreased when combined with Eliglustat.
EnzalutamideThe serum concentration of Lisuride can be decreased when it is combined with Enzalutamide.
Ergoloid mesylateErgoloid mesylate may increase the vasoconstricting activities of Lisuride.
ErgonovineErgonovine may increase the vasoconstricting activities of Lisuride.
ErgotamineErgotamine may increase the vasoconstricting activities of Lisuride.
ErythromycinThe metabolism of Lisuride can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Lisuride can be decreased when it is combined with Eslicarbazepine acetate.
EtravirineThe serum concentration of Lisuride can be decreased when it is combined with Etravirine.
FluconazoleThe metabolism of Lisuride can be decreased when combined with Fluconazole.
FluoxetineThe metabolism of Lisuride can be decreased when combined with Fluoxetine.
FluvoxamineThe metabolism of Lisuride can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Lisuride can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Lisuride can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Lisuride can be increased when combined with Fosphenytoin.
FurazolidoneThe metabolism of Lisuride can be decreased when combined with Furazolidone.
Fusidic AcidThe serum concentration of Lisuride can be increased when it is combined with Fusidic Acid.
HaloperidolThe metabolism of Lisuride can be decreased when combined with Haloperidol.
HydracarbazineThe metabolism of Lisuride can be decreased when combined with Hydracarbazine.
IdelalisibThe serum concentration of Lisuride can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Lisuride can be decreased when combined with Imatinib.
ImipramineThe metabolism of Lisuride can be decreased when combined with Imipramine.
IndinavirThe metabolism of Lisuride can be decreased when combined with Indinavir.
IproclozideThe metabolism of Lisuride can be decreased when combined with Iproclozide.
IproniazidThe metabolism of Lisuride can be decreased when combined with Iproniazid.
IsavuconazoniumThe metabolism of Lisuride can be decreased when combined with Isavuconazonium.
IsocarboxazidThe metabolism of Lisuride can be decreased when combined with Isocarboxazid.
IsoniazidThe metabolism of Lisuride can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Lisuride can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Lisuride can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Lisuride can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Lisuride can be decreased when combined with Ketoconazole.
LopinavirThe metabolism of Lisuride can be decreased when combined with Lopinavir.
LorcaserinThe metabolism of Lisuride can be decreased when combined with Lorcaserin.
LovastatinThe metabolism of Lisuride can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Lisuride can be increased when it is combined with Luliconazole.
LumefantrineThe metabolism of Lisuride can be decreased when combined with Lumefantrine.
MebanazineThe metabolism of Lisuride can be decreased when combined with Mebanazine.
MethadoneThe metabolism of Lisuride can be decreased when combined with Methadone.
MethotrimeprazineThe metabolism of Lisuride can be decreased when combined with Methotrimeprazine.
Methylene blueThe metabolism of Lisuride can be decreased when combined with Methylene blue.
MetoprololThe metabolism of Lisuride can be decreased when combined with Metoprolol.
MifepristoneThe metabolism of Lisuride can be decreased when combined with Mifepristone.
MinaprineThe metabolism of Lisuride can be decreased when combined with Minaprine.
MirabegronThe metabolism of Lisuride can be decreased when combined with Mirabegron.
MitotaneThe serum concentration of Lisuride can be decreased when it is combined with Mitotane.
MoclobemideThe metabolism of Lisuride can be decreased when combined with Moclobemide.
ModafinilThe serum concentration of Lisuride can be decreased when it is combined with Modafinil.
NafcillinThe serum concentration of Lisuride can be decreased when it is combined with Nafcillin.
NefazodoneThe metabolism of Lisuride can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Lisuride can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Lisuride can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Lisuride can be decreased when combined with Nevirapine.
NialamideThe metabolism of Lisuride can be decreased when combined with Nialamide.
NicardipineThe metabolism of Lisuride can be decreased when combined with Nicardipine.
NilotinibThe metabolism of Lisuride can be decreased when combined with Nilotinib.
OctamoxinThe metabolism of Lisuride can be decreased when combined with Octamoxin.
OlaparibThe metabolism of Lisuride can be decreased when combined with Olaparib.
OsimertinibThe serum concentration of Lisuride can be increased when it is combined with Osimertinib.
PalbociclibThe serum concentration of Lisuride can be increased when it is combined with Palbociclib.
PanobinostatThe metabolism of Lisuride can be decreased when combined with Panobinostat.
PargylineThe metabolism of Lisuride can be decreased when combined with Pargyline.
ParoxetineThe metabolism of Lisuride can be decreased when combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Lisuride can be decreased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe metabolism of Lisuride can be increased when combined with Pentobarbital.
PhenelzineThe metabolism of Lisuride can be decreased when combined with Phenelzine.
PheniprazineThe metabolism of Lisuride can be decreased when combined with Pheniprazine.
PhenobarbitalThe metabolism of Lisuride can be increased when combined with Phenobarbital.
PhenoxypropazineThe metabolism of Lisuride can be decreased when combined with Phenoxypropazine.
PhenytoinThe metabolism of Lisuride can be increased when combined with Phenytoin.
PirlindoleThe metabolism of Lisuride can be decreased when combined with Pirlindole.
PivhydrazineThe metabolism of Lisuride can be decreased when combined with Pivhydrazine.
PosaconazoleThe metabolism of Lisuride can be decreased when combined with Posaconazole.
PrimidoneThe metabolism of Lisuride can be increased when combined with Primidone.
PromazineThe metabolism of Lisuride can be decreased when combined with Promazine.
QuinidineThe metabolism of Lisuride can be decreased when combined with Quinidine.
QuinineThe metabolism of Lisuride can be decreased when combined with Quinine.
RanolazineThe metabolism of Lisuride can be decreased when combined with Ranolazine.
RasagilineThe metabolism of Lisuride can be decreased when combined with Rasagiline.
RifabutinThe metabolism of Lisuride can be increased when combined with Rifabutin.
RifampicinThe metabolism of Lisuride can be increased when combined with Rifampicin.
RifapentineThe metabolism of Lisuride can be increased when combined with Rifapentine.
RitonavirThe metabolism of Lisuride can be decreased when combined with Ritonavir.
RolapitantThe metabolism of Lisuride can be decreased when combined with Rolapitant.
RopiniroleThe metabolism of Lisuride can be decreased when combined with Ropinirole.
SafrazineThe metabolism of Lisuride can be decreased when combined with Safrazine.
SaquinavirThe metabolism of Lisuride can be decreased when combined with Saquinavir.
SelegilineThe metabolism of Lisuride can be decreased when combined with Selegiline.
SertralineThe metabolism of Lisuride can be decreased when combined with Sertraline.
SildenafilThe metabolism of Lisuride can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Lisuride can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Lisuride can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Lisuride can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Lisuride can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Lisuride can be decreased when combined with Sulfisoxazole.
TelaprevirThe metabolism of Lisuride can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Lisuride can be decreased when combined with Telithromycin.
TerbinafineThe metabolism of Lisuride can be decreased when combined with Terbinafine.
ThioridazineThe metabolism of Lisuride can be decreased when combined with Thioridazine.
TiclopidineThe metabolism of Lisuride can be decreased when combined with Ticlopidine.
TipranavirThe metabolism of Lisuride can be decreased when combined with Tipranavir.
TocilizumabThe serum concentration of Lisuride can be decreased when it is combined with Tocilizumab.
ToloxatoneThe metabolism of Lisuride can be decreased when combined with Toloxatone.
Trans-2-PhenylcyclopropylamineThe metabolism of Lisuride can be decreased when combined with Trans-2-Phenylcyclopropylamine.
TranylcypromineThe metabolism of Lisuride can be decreased when combined with Tranylcypromine.
VenlafaxineThe metabolism of Lisuride can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Lisuride can be decreased when combined with Verapamil.
VoriconazoleThe metabolism of Lisuride can be decreased when combined with Voriconazole.
ZiprasidoneThe metabolism of Lisuride can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Targets

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. 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
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
unknown
Actions
antagonist
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. 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
antagonist
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:
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. Kimura K, Akai T, Nakamura K, Yamaguchi M, Nakagawa H, Oshino N: Dual activation by lisuride of central serotonin 5-HT(1A) and dopamine D(2) receptor sites: drug discrimination and receptor binding studies. Behav Pharmacol. 1991 Apr;2(2):105-112. [PubMed:11224054 ]
  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. Marona-Lewicka D, Kurrasch-Orbaugh DM, Selken JR, Cumbay MG, Lisnicchia JG, Nichols DE: Re-evaluation of lisuride pharmacology: 5-hydroxytryptamine1A receptor-mediated behavioral effects overlap its other properties in rats. Psychopharmacology (Berl). 2002 Oct;164(1):93-107. Epub 2002 Jul 19. [PubMed:12373423 ]
  4. Akai T, Takahashi M, Nakada Y, Ohnishi R, Ikoma Y, Yamaguchi M: [Anxiolytic effects of lisuride and its agonistic action to central 5-HT1A receptors]. Nihon Yakurigaku Zasshi. 1991 Apr;97(4):209-20. [PubMed:1678728 ]
  5. Miyazawa T, Murayama C, Nakagawa H: [Effect of lisuride on experimental cerebral infarction in rats]. Nihon Yakurigaku Zasshi. 1991 Dec;98(6):449-56. [PubMed:1783326 ]
  6. Cunningham KA, Callahan PM, Appel JB: Discriminative stimulus properties of 8-hydroxy-2-(di-n-propylamino)tetralin (8-OHDPAT): implications for understanding the actions of novel anxiolytics. Eur J Pharmacol. 1987 Jun 12;138(1):29-36. [PubMed:2887435 ]
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 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 c...
Gene Name:
HTR1D
Uniprot ID:
P28221
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
antagonist
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 change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins ...
Gene Name:
HTR2B
Uniprot ID:
P41595
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 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
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 ]
  2. Egan CT, Herrick-Davis K, Miller K, Glennon RA, Teitler M: Agonist activity of LSD and lisuride at cloned 5HT2A and 5HT2C receptors. Psychopharmacology (Berl). 1998 Apr;136(4):409-14. [PubMed:9600588 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
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 ]
  2. Egan CT, Herrick-Davis K, Miller K, Glennon RA, Teitler M: Agonist activity of LSD and lisuride at cloned 5HT2A and 5HT2C receptors. Psychopharmacology (Berl). 1998 Apr;136(4):409-14. [PubMed:9600588 ]
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 substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of ...
Gene Name:
HTR1B
Uniprot ID:
P28222
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
other/unknown
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 oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
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
other/unknown
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. 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
other/unknown
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
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:
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 ]
  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
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 ]
  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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23