Identification

Name
Lisuride
Accession Number
DB00589  (APRD00636)
Type
Small Molecule
Groups
Approved, Investigational
Description

An 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 IDs
MIP 2204 / SH 31072 B
Product Ingredients
IngredientUNIICASInChI Key
Lysuride MaleateUV1635N8XW19875-60-6CVQFAMQDTWVJSV-BAXNFHPCSA-N
International/Other Brands
Arolac (Lisapharm) / Dipergon (Bayer) / Dopergin (Bayer) / Dopergine (Bayer Santé) / Proclacam / Revanil
Categories
UNII
E0QN3D755O
CAS number
18016-80-3
Weight
Average: 338.4466
Monoisotopic: 338.210661474
Chemical Formula
C20H26N4O
InChI Key
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][[email protected]@]12CC3=CNC4=CC=CC(=C34)C1=C[[email protected]@H](CN2C)NC(=O)N(CC)CC

Pharmacology

Indication

For the management of Parkinson's Disease

Structured Indications
Not Available
Pharmacodynamics
Not Available
Mechanism of action

Lisuride 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.

TargetActionsOrganism
AD(2) dopamine receptor
agonist
Human
AD(3) dopamine receptor
agonist
Human
AD(4) dopamine receptor
agonist
Human
UD(1A) dopamine receptor
antagonist
Human
UD(1B) dopamine receptor
antagonist
Human
U5-hydroxytryptamine receptor 1A
agonist
Human
U5-hydroxytryptamine receptor 1D
agonist
Human
U5-hydroxytryptamine receptor 2B
antagonist
Human
A5-hydroxytryptamine receptor 2A
agonist
Human
A5-hydroxytryptamine receptor 2C
agonist
Human
U5-hydroxytryptamine receptor 1B
agonist
Human
UAlpha-2A adrenergic receptor
other/unknown
Human
UAlpha-2B adrenergic receptor
other/unknown
Human
UAlpha-2C adrenergic receptor
other/unknown
Human
U5-hydroxytryptamine receptor 7Not AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding

about 15%

Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
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.Experimental
AbirateroneThe serum concentration of Lisuride can be increased when it is combined with Abiraterone.Approved
AcetaminophenThe risk or severity of adverse effects can be increased when Lisuride is combined with Acetaminophen.Approved
AcetazolamideThe risk or severity of adverse effects can be increased when Lisuride is combined with Acetazolamide.Approved, Vet Approved
AldesleukinThe risk or severity of adverse effects can be increased when Lisuride is combined with Aldesleukin.Approved
AlprazolamThe risk or severity of adverse effects can be increased when Lisuride is combined with Alprazolam.Approved, Illicit, Investigational
AmbroxolThe risk or severity of adverse effects can be increased when Lisuride is combined with Ambroxol.Approved, Investigational
AmiodaroneThe metabolism of Lisuride can be decreased when combined with Amiodarone.Approved, Investigational
AmlodipineThe risk or severity of adverse effects can be increased when Lisuride is combined with Amlodipine.Approved
AmphetamineThe metabolism of Lisuride can be decreased when combined with Amphetamine.Approved, Illicit
AmprenavirThe risk or severity of adverse effects can be increased when Lisuride is combined with Amprenavir.Approved
AnastrozoleThe risk or severity of adverse effects can be increased when Lisuride is combined with Anastrozole.Approved, Investigational
AntipyrineThe risk or severity of adverse effects can be increased when Lisuride is combined with Antipyrine.Approved
AprepitantThe serum concentration of Lisuride can be increased when it is combined with Aprepitant.Approved, Investigational
Arsenic trioxideThe risk or severity of adverse effects can be increased when Lisuride is combined with Arsenic trioxide.Approved, Investigational
ArtemetherThe metabolism of Lisuride can be decreased when combined with Artemether.Approved
AstemizoleThe risk or severity of adverse effects can be increased when Lisuride is combined with Astemizole.Approved, Withdrawn
AtazanavirThe metabolism of Lisuride can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Lisuride can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Lisuride is combined with Atorvastatin.Approved
AzelastineThe risk or severity of adverse effects can be increased when Lisuride is combined with Azelastine.Approved
AzithromycinThe risk or severity of adverse effects can be increased when Lisuride is combined with Azithromycin.Approved
BenmoxinThe metabolism of Lisuride can be decreased when combined with Benmoxin.Withdrawn
BetamethasoneThe risk or severity of adverse effects can be increased when Lisuride is combined with Betamethasone.Approved, Vet Approved
BetaxololThe metabolism of Lisuride can be decreased when combined with Betaxolol.Approved
BicalutamideThe risk or severity of adverse effects can be increased when Lisuride is combined with Bicalutamide.Approved
BifonazoleThe risk or severity of adverse effects can be increased when Lisuride is combined with Bifonazole.Approved, Investigational
BoceprevirThe metabolism of Lisuride can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Lisuride can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Lisuride can be decreased when it is combined with Bosentan.Approved, Investigational
Brentuximab vedotinThe risk or severity of adverse effects can be increased when Lisuride is combined with Brentuximab vedotin.Approved
BrofaromineThe metabolism of Lisuride can be decreased when combined with Brofaromine.Experimental
BromocriptineBromocriptine may increase the vasoconstricting activities of Lisuride.Approved, Investigational
BuprenorphineThe risk or severity of adverse effects can be increased when Lisuride is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Lisuride can be decreased when combined with Bupropion.Approved
CabergolineCabergoline may increase the vasoconstricting activities of Lisuride.Approved
CaffeineThe risk or severity of adverse effects can be increased when Lisuride is combined with Caffeine.Approved
CapsaicinThe risk or severity of adverse effects can be increased when Lisuride is combined with Capsaicin.Approved
CarbamazepineThe metabolism of Lisuride can be increased when combined with Carbamazepine.Approved, Investigational
CaroxazoneThe metabolism of Lisuride can be decreased when combined with Caroxazone.Withdrawn
CaspofunginThe risk or severity of adverse effects can be increased when Lisuride is combined with Caspofungin.Approved
CelecoxibThe metabolism of Lisuride can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Lisuride can be increased when it is combined with Ceritinib.Approved
CerivastatinThe risk or severity of adverse effects can be increased when Lisuride is combined with Cerivastatin.Withdrawn
ChloramphenicolThe risk or severity of adverse effects can be increased when Lisuride is combined with Chloramphenicol.Approved, Vet Approved
ChloroquineThe metabolism of Lisuride can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe metabolism of Lisuride can be decreased when combined with Chlorpromazine.Approved, Vet Approved
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Lisuride is combined with Chlorzoxazone.Approved
CholecalciferolThe metabolism of Lisuride can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CilostazolThe risk or severity of adverse effects can be increased when Lisuride is combined with Cilostazol.Approved
CimetidineThe metabolism of Lisuride can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Lisuride can be decreased when combined with Cinacalcet.Approved
CiprofloxacinThe risk or severity of adverse effects can be increased when Lisuride is combined with Ciprofloxacin.Approved, Investigational
CisaprideThe risk or severity of adverse effects can be increased when Lisuride is combined with Cisapride.Approved, Investigational, Withdrawn
CitalopramThe metabolism of Lisuride can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Lisuride can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Lisuride can be decreased when combined with Clemastine.Approved
ClindamycinThe risk or severity of adverse effects can be increased when Lisuride is combined with Clindamycin.Approved, Vet Approved
ClobazamThe metabolism of Lisuride can be decreased when combined with Clobazam.Approved, Illicit
ClofazimineThe risk or severity of adverse effects can be increased when Lisuride is combined with Clofazimine.Approved, Investigational
ClomifeneThe risk or severity of adverse effects can be increased when Lisuride is combined with Clomifene.Approved, Investigational
ClomipramineThe metabolism of Lisuride can be decreased when combined with Clomipramine.Approved, Vet Approved
ClotiazepamThe risk or severity of adverse effects can be increased when Lisuride is combined with Clotiazepam.Approved, Illicit
ClotrimazoleThe metabolism of Lisuride can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Lisuride can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Lisuride can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Lisuride can be decreased when combined with Cocaine.Approved, Illicit
ColchicineThe risk or severity of adverse effects can be increased when Lisuride is combined with Colchicine.Approved
ConivaptanThe serum concentration of Lisuride can be increased when it is combined with Conivaptan.Approved, Investigational
Cortisone acetateThe risk or severity of adverse effects can be increased when Lisuride is combined with Cortisone acetate.Approved
CrizotinibThe metabolism of Lisuride can be decreased when combined with Crizotinib.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Lisuride is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe metabolism of Lisuride can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Lisuride can be decreased when it is combined with Dabrafenib.Approved
DalfopristinThe risk or severity of adverse effects can be increased when Lisuride is combined with Dalfopristin.Approved
DanazolThe risk or severity of adverse effects can be increased when Lisuride is combined with Danazol.Approved
DarifenacinThe metabolism of Lisuride can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Lisuride can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Lisuride can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe risk or severity of adverse effects can be increased when Lisuride is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Lisuride can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Lisuride can be decreased when combined with Delavirdine.Approved
DesipramineThe metabolism of Lisuride can be decreased when combined with Desipramine.Approved
DexamethasoneThe risk or severity of adverse effects can be increased when Lisuride is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextropropoxypheneThe risk or severity of adverse effects can be increased when Lisuride is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DiazepamThe risk or severity of adverse effects can be increased when Lisuride is combined with Diazepam.Approved, Illicit, Vet Approved
DiethylstilbestrolThe risk or severity of adverse effects can be increased when Lisuride is combined with Diethylstilbestrol.Approved, Investigational
DihydroergotamineThe metabolism of Lisuride can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Lisuride can be decreased when combined with Diltiazem.Approved
Dimethyl sulfoxideThe risk or severity of adverse effects can be increased when Lisuride is combined with Dimethyl sulfoxide.Approved, Vet Approved
DiphenhydramineThe metabolism of Lisuride can be decreased when combined with Diphenhydramine.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Lisuride is combined with Docetaxel.Approved, Investigational
DosulepinThe metabolism of Lisuride can be decreased when combined with Dosulepin.Approved
DoxorubicinThe risk or severity of adverse effects can be increased when Lisuride is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Lisuride can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Lisuride can be decreased when combined with Dronedarone.Approved
DroxidopaLisuride may increase the hypertensive activities of Droxidopa.Approved, Investigational
DuloxetineThe metabolism of Lisuride can be decreased when combined with Duloxetine.Approved
EconazoleThe risk or severity of adverse effects can be increased when Lisuride is combined with Econazole.Approved
EfavirenzThe risk or severity of adverse effects can be increased when Lisuride is combined with Efavirenz.Approved, Investigational
ElbasvirThe risk or severity of adverse effects can be increased when Lisuride is combined with Elbasvir.Approved
EliglustatThe metabolism of Lisuride can be decreased when combined with Eliglustat.Approved
EnasidenibThe risk or severity of adverse effects can be increased when Lisuride is combined with Enasidenib.Approved
EnzalutamideThe serum concentration of Lisuride can be decreased when it is combined with Enzalutamide.Approved
EpinephrineThe risk or severity of adverse effects can be increased when Lisuride is combined with Epinephrine.Approved, Vet Approved
Ergoloid mesylateErgoloid mesylate may increase the vasoconstricting activities of Lisuride.Approved
ErgonovineErgonovine may increase the vasoconstricting activities of Lisuride.Approved
ErgotamineErgotamine may increase the vasoconstricting activities of Lisuride.Approved
ErythromycinThe metabolism of Lisuride can be decreased when combined with Erythromycin.Approved, Vet Approved
EthanolThe risk or severity of adverse effects can be increased when Lisuride is combined with Ethanol.Approved
EtoposideThe risk or severity of adverse effects can be increased when Lisuride is combined with Etoposide.Approved
EtoricoxibThe risk or severity of adverse effects can be increased when Lisuride is combined with Etoricoxib.Approved, Investigational
EzetimibeThe risk or severity of adverse effects can be increased when Lisuride is combined with Ezetimibe.Approved
FelodipineThe risk or severity of adverse effects can be increased when Lisuride is combined with Felodipine.Approved, Investigational
FentanylThe risk or severity of adverse effects can be increased when Lisuride is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FluconazoleThe metabolism of Lisuride can be decreased when combined with Fluconazole.Approved
FluoxetineThe metabolism of Lisuride can be decreased when combined with Fluoxetine.Approved, Vet Approved
Fluticasone propionateThe risk or severity of adverse effects can be increased when Lisuride is combined with Fluticasone propionate.Approved
FluvastatinThe risk or severity of adverse effects can be increased when Lisuride is combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Lisuride can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Lisuride can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Lisuride can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Lisuride can be increased when combined with Fosphenytoin.Approved
FurazolidoneThe metabolism of Lisuride can be decreased when combined with Furazolidone.Approved, Investigational, Vet Approved
Fusidic AcidThe serum concentration of Lisuride can be increased when it is combined with Fusidic Acid.Approved
GemfibrozilThe risk or severity of adverse effects can be increased when Lisuride is combined with Gemfibrozil.Approved
GlyburideThe risk or severity of adverse effects can be increased when Lisuride is combined with Glyburide.Approved
Glycerol PhenylbutyrateThe risk or severity of adverse effects can be increased when Lisuride is combined with Glycerol Phenylbutyrate.Approved
HaloperidolThe metabolism of Lisuride can be decreased when combined with Haloperidol.Approved
HarmalineThe metabolism of Lisuride can be decreased when combined with Harmaline.Experimental
HistamineThe risk or severity of adverse effects can be increased when Lisuride is combined with Histamine.Approved, Investigational
HydracarbazineThe metabolism of Lisuride can be decreased when combined with Hydracarbazine.Experimental
HydralazineThe risk or severity of adverse effects can be increased when Lisuride is combined with Hydralazine.Approved
HydrocortisoneThe risk or severity of adverse effects can be increased when Lisuride is combined with Hydrocortisone.Approved, Vet Approved
IdelalisibThe serum concentration of Lisuride can be increased when it is combined with Idelalisib.Approved
IfosfamideThe risk or severity of adverse effects can be increased when Lisuride is combined with Ifosfamide.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Lisuride is combined with Iloperidone.Approved
ImatinibThe metabolism of Lisuride can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Lisuride can be decreased when combined with Imipramine.Approved
IndinavirThe metabolism of Lisuride can be decreased when combined with Indinavir.Approved
indisulamThe risk or severity of adverse effects can be increased when Lisuride is combined with indisulam.Investigational
IproclozideThe metabolism of Lisuride can be decreased when combined with Iproclozide.Withdrawn
IproniazidThe metabolism of Lisuride can be decreased when combined with Iproniazid.Withdrawn
IrbesartanThe risk or severity of adverse effects can be increased when Lisuride is combined with Irbesartan.Approved, Investigational
IrinotecanThe risk or severity of adverse effects can be increased when Lisuride is combined with Irinotecan.Approved, Investigational
IsavuconazoniumThe metabolism of Lisuride can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidThe metabolism of Lisuride can be decreased when combined with Isocarboxazid.Approved
IsoniazidThe metabolism of Lisuride can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Lisuride can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Lisuride can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Lisuride can be increased when it is combined with Ivacaftor.Approved
JosamycinThe risk or severity of adverse effects can be increased when Lisuride is combined with Josamycin.Approved, Investigational
KetazolamThe risk or severity of adverse effects can be increased when Lisuride is combined with Ketazolam.Approved
KetoconazoleThe metabolism of Lisuride can be decreased when combined with Ketoconazole.Approved, Investigational
LansoprazoleThe risk or severity of adverse effects can be increased when Lisuride is combined with Lansoprazole.Approved, Investigational
LapatinibThe risk or severity of adverse effects can be increased when Lisuride is combined with Lapatinib.Approved, Investigational
LercanidipineThe risk or severity of adverse effects can be increased when Lisuride is combined with Lercanidipine.Approved, Investigational
LevofloxacinThe risk or severity of adverse effects can be increased when Lisuride is combined with Levofloxacin.Approved, Investigational
LevosalbutamolThe risk or severity of adverse effects can be increased when Lisuride is combined with Levosalbutamol.Approved
LidocaineThe risk or severity of adverse effects can be increased when Lisuride is combined with Lidocaine.Approved, Vet Approved
LinagliptinThe risk or severity of adverse effects can be increased when Lisuride is combined with Linagliptin.Approved
LomitapideThe risk or severity of adverse effects can be increased when Lisuride is combined with Lomitapide.Approved
LomustineThe risk or severity of adverse effects can be increased when Lisuride is combined with Lomustine.Approved
LopinavirThe metabolism of Lisuride can be decreased when combined with Lopinavir.Approved
LoratadineThe risk or severity of adverse effects can be increased when Lisuride is combined with Loratadine.Approved
LorcaserinThe metabolism of Lisuride can be decreased when combined with Lorcaserin.Approved
LosartanThe risk or severity of adverse effects can be increased when Lisuride is combined with Losartan.Approved
LovastatinThe metabolism of Lisuride can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Lisuride can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Lisuride can be increased when combined with Lumacaftor.Approved
LumefantrineThe metabolism of Lisuride can be decreased when combined with Lumefantrine.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Lisuride is combined with Lurasidone.Approved
ManidipineThe metabolism of Lisuride can be decreased when combined with Manidipine.Approved, Investigational
MebanazineThe metabolism of Lisuride can be decreased when combined with Mebanazine.Withdrawn
MefloquineThe risk or severity of adverse effects can be increased when Lisuride is combined with Mefloquine.Approved
MequitazineThe risk or severity of adverse effects can be increased when Lisuride is combined with Mequitazine.Approved
MethadoneThe metabolism of Lisuride can be decreased when combined with Methadone.Approved
MethazolamideThe risk or severity of adverse effects can be increased when Lisuride is combined with Methazolamide.Approved
MethimazoleThe risk or severity of adverse effects can be increased when Lisuride is combined with Methimazole.Approved
MethotrimeprazineThe metabolism of Lisuride can be decreased when combined with Methotrimeprazine.Approved
Methylene blueThe metabolism of Lisuride can be decreased when combined with Methylene blue.Approved, Investigational
MethylergometrineThe risk or severity of adverse effects can be increased when Lisuride is combined with Methylergometrine.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Lisuride is combined with Methylprednisolone.Approved, Vet Approved
MetoprololThe metabolism of Lisuride can be decreased when combined with Metoprolol.Approved, Investigational
MetronidazoleThe risk or severity of adverse effects can be increased when Lisuride is combined with Metronidazole.Approved
MetyraponeThe risk or severity of adverse effects can be increased when Lisuride is combined with Metyrapone.Approved
MibefradilThe risk or severity of adverse effects can be increased when Lisuride is combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe risk or severity of adverse effects can be increased when Lisuride is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe risk or severity of adverse effects can be increased when Lisuride is combined with Midazolam.Approved, Illicit
MidostaurinThe metabolism of Lisuride can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Lisuride can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineThe metabolism of Lisuride can be decreased when combined with Minaprine.Approved
MirabegronThe metabolism of Lisuride can be decreased when combined with Mirabegron.Approved
MirtazapineThe risk or severity of adverse effects can be increased when Lisuride is combined with Mirtazapine.Approved
MitotaneThe serum concentration of Lisuride can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe risk or severity of adverse effects can be increased when Lisuride is combined with Mitoxantrone.Approved, Investigational
MoclobemideThe metabolism of Lisuride can be decreased when combined with Moclobemide.Approved
ModafinilThe risk or severity of adverse effects can be increased when Lisuride is combined with Modafinil.Approved, Investigational
NefazodoneThe metabolism of Lisuride can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Lisuride can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Lisuride can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Lisuride can be increased when combined with Nevirapine.Approved
NialamideThe metabolism of Lisuride can be decreased when combined with Nialamide.Withdrawn
NicardipineThe metabolism of Lisuride can be decreased when combined with Nicardipine.Approved
NicotinamideThe risk or severity of adverse effects can be increased when Lisuride is combined with Nicotinamide.Approved
NifedipineThe risk or severity of adverse effects can be increased when Lisuride is combined with Nifedipine.Approved
NilotinibThe metabolism of Lisuride can be decreased when combined with Nilotinib.Approved, Investigational
NilvadipineThe risk or severity of adverse effects can be increased when Lisuride is combined with Nilvadipine.Approved, Investigational
NisoldipineThe risk or severity of adverse effects can be increased when Lisuride is combined with Nisoldipine.Approved
NitrendipineThe risk or severity of adverse effects can be increased when Lisuride is combined with Nitrendipine.Approved, Investigational
Nitric OxideThe risk or severity of adverse effects can be increased when Lisuride is combined with Nitric Oxide.Approved
NorfloxacinThe risk or severity of adverse effects can be increased when Lisuride is combined with Norfloxacin.Approved
NoscapineThe risk or severity of adverse effects can be increased when Lisuride is combined with Noscapine.Investigational
OctamoxinThe metabolism of Lisuride can be decreased when combined with Octamoxin.Withdrawn
OlanzapineThe risk or severity of adverse effects can be increased when Lisuride is combined with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Lisuride can be decreased when combined with Olaparib.Approved
OmeprazoleThe risk or severity of adverse effects can be increased when Lisuride is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Lisuride can be increased when it is combined with Osimertinib.Approved
OxybutyninThe risk or severity of adverse effects can be increased when Lisuride is combined with Oxybutynin.Approved, Investigational
OxymetholoneThe risk or severity of adverse effects can be increased when Lisuride is combined with Oxymetholone.Approved, Illicit
PaclitaxelThe risk or severity of adverse effects can be increased when Lisuride is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Lisuride can be increased when it is combined with Palbociclib.Approved
PanobinostatThe serum concentration of Lisuride can be increased when it is combined with Panobinostat.Approved, Investigational
ParamethasoneThe risk or severity of adverse effects can be increased when Lisuride is combined with Paramethasone.Approved
PargylineThe metabolism of Lisuride can be decreased when combined with Pargyline.Approved
ParoxetineThe metabolism of Lisuride can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibThe risk or severity of adverse effects can be increased when Lisuride is combined with Pazopanib.Approved
Peginterferon alfa-2bThe serum concentration of Lisuride can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe metabolism of Lisuride can be increased when combined with Pentobarbital.Approved, Vet Approved
PergolideThe risk or severity of adverse effects can be increased when Lisuride is combined with Pergolide.Approved, Investigational, Vet Approved, Withdrawn
PhenelzineThe metabolism of Lisuride can be decreased when combined with Phenelzine.Approved
PheniprazineThe metabolism of Lisuride can be decreased when combined with Pheniprazine.Withdrawn
PhenobarbitalThe metabolism of Lisuride can be increased when combined with Phenobarbital.Approved
PhenoxypropazineThe metabolism of Lisuride can be decreased when combined with Phenoxypropazine.Withdrawn
PhenytoinThe metabolism of Lisuride can be increased when combined with Phenytoin.Approved, Vet Approved
PilocarpineThe risk or severity of adverse effects can be increased when Lisuride is combined with Pilocarpine.Approved
PimozideThe risk or severity of adverse effects can be increased when Lisuride is combined with Pimozide.Approved
PirlindoleThe metabolism of Lisuride can be decreased when combined with Pirlindole.Approved
PivhydrazineThe metabolism of Lisuride can be decreased when combined with Pivhydrazine.Withdrawn
PosaconazoleThe metabolism of Lisuride can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe risk or severity of adverse effects can be increased when Lisuride is combined with Pravastatin.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Lisuride is combined with Prednisolone.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Lisuride is combined with Prednisone.Approved, Vet Approved
PrimaquineThe risk or severity of adverse effects can be increased when Lisuride is combined with Primaquine.Approved
PrimidoneThe metabolism of Lisuride can be increased when combined with Primidone.Approved, Vet Approved
ProcarbazineThe metabolism of Lisuride can be decreased when combined with Procarbazine.Approved
ProgesteroneThe risk or severity of adverse effects can be increased when Lisuride is combined with Progesterone.Approved, Vet Approved
PromazineThe metabolism of Lisuride can be decreased when combined with Promazine.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Lisuride is combined with Propofol.Approved, Investigational, Vet Approved
QuinidineThe metabolism of Lisuride can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Lisuride can be decreased when combined with Quinine.Approved
QuinupristinThe risk or severity of adverse effects can be increased when Lisuride is combined with Quinupristin.Approved
RabeprazoleThe risk or severity of adverse effects can be increased when Lisuride is combined with Rabeprazole.Approved, Investigational
RaloxifeneThe risk or severity of adverse effects can be increased when Lisuride is combined with Raloxifene.Approved, Investigational
RanitidineThe risk or severity of adverse effects can be increased when Lisuride is combined with Ranitidine.Approved
RanolazineThe metabolism of Lisuride can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineThe metabolism of Lisuride can be decreased when combined with Rasagiline.Approved
RegorafenibThe risk or severity of adverse effects can be increased when Lisuride is combined with Regorafenib.Approved
RepaglinideThe risk or severity of adverse effects can be increased when Lisuride is combined with Repaglinide.Approved, Investigational
ResveratrolThe risk or severity of adverse effects can be increased when Lisuride is combined with Resveratrol.Approved, Experimental, Investigational
RifabutinThe metabolism of Lisuride can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Lisuride can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Lisuride can be increased when combined with Rifapentine.Approved
RilpivirineThe risk or severity of adverse effects can be increased when Lisuride is combined with Rilpivirine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Lisuride is combined with Risperidone.Approved, Investigational
RitonavirThe metabolism of Lisuride can be decreased when combined with Ritonavir.Approved, Investigational
RivastigmineThe risk or severity of adverse effects can be increased when Lisuride is combined with Rivastigmine.Approved, Investigational
RolapitantThe metabolism of Lisuride can be decreased when combined with Rolapitant.Approved
RolitetracyclineThe risk or severity of adverse effects can be increased when Lisuride is combined with Rolitetracycline.Approved
RopiniroleThe metabolism of Lisuride can be decreased when combined with Ropinirole.Approved, Investigational
RosuvastatinThe risk or severity of adverse effects can be increased when Lisuride is combined with Rosuvastatin.Approved
RoxithromycinThe risk or severity of adverse effects can be increased when Lisuride is combined with Roxithromycin.Approved, Investigational, Withdrawn
RutinThe risk or severity of adverse effects can be increased when Lisuride is combined with Rutin.Experimental, Investigational
SafrazineThe metabolism of Lisuride can be decreased when combined with Safrazine.Withdrawn
SalbutamolThe risk or severity of adverse effects can be increased when Lisuride is combined with Salbutamol.Approved, Vet Approved
SaquinavirThe metabolism of Lisuride can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe risk or severity of adverse effects can be increased when Lisuride is combined with Sarilumab.Approved
SelegilineThe metabolism of Lisuride can be decreased when combined with Selegiline.Approved, Investigational, Vet Approved
SertralineThe metabolism of Lisuride can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Lisuride can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Lisuride can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Lisuride can be increased when it is combined with Simeprevir.Approved
SimvastatinThe risk or severity of adverse effects can be increased when Lisuride is combined with Simvastatin.Approved
SirolimusThe risk or severity of adverse effects can be increased when Lisuride is combined with Sirolimus.Approved, Investigational
SitaxentanThe risk or severity of adverse effects can be increased when Lisuride is combined with Sitaxentan.Approved, Investigational, Withdrawn
SorafenibThe risk or severity of adverse effects can be increased when Lisuride is combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Lisuride can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Lisuride can be increased when it is combined with Stiripentol.Approved
SulfamethoxazoleThe risk or severity of adverse effects can be increased when Lisuride is combined with Sulfamethoxazole.Approved
SulfanilamideThe risk or severity of adverse effects can be increased when Lisuride is combined with Sulfanilamide.Approved
SulfinpyrazoneThe risk or severity of adverse effects can be increased when Lisuride is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Lisuride can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusThe risk or severity of adverse effects can be increased when Lisuride is combined with Tacrolimus.Approved, Investigational
TadalafilThe risk or severity of adverse effects can be increased when Lisuride is combined with Tadalafil.Approved, Investigational
TamoxifenThe risk or severity of adverse effects can be increased when Lisuride is combined with Tamoxifen.Approved
TelaprevirThe metabolism of Lisuride can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Lisuride can be decreased when combined with Telithromycin.Approved
TemsirolimusThe risk or severity of adverse effects can be increased when Lisuride is combined with Temsirolimus.Approved
TeniposideThe risk or severity of adverse effects can be increased when Lisuride is combined with Teniposide.Approved
TerbinafineThe metabolism of Lisuride can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerfenadineThe risk or severity of adverse effects can be increased when Lisuride is combined with Terfenadine.Withdrawn
TesmilifeneThe risk or severity of adverse effects can be increased when Lisuride is combined with Tesmilifene.Investigational
TestosteroneThe risk or severity of adverse effects can be increased when Lisuride is combined with Testosterone.Approved, Investigational
TetracyclineThe risk or severity of adverse effects can be increased when Lisuride is combined with Tetracycline.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Lisuride is combined with Thiopental.Approved, Vet Approved
ThioridazineThe metabolism of Lisuride can be decreased when combined with Thioridazine.Approved, Withdrawn
TicagrelorThe risk or severity of adverse effects can be increased when Lisuride is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Lisuride can be decreased when combined with Ticlopidine.Approved
TioconazoleThe risk or severity of adverse effects can be increased when Lisuride is combined with Tioconazole.Approved
TipranavirThe metabolism of Lisuride can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Lisuride can be decreased when it is combined with Tocilizumab.Approved
TofisopamThe risk or severity of adverse effects can be increased when Lisuride is combined with Tofisopam.Approved
ToloxatoneThe metabolism of Lisuride can be decreased when combined with Toloxatone.Approved
TopiroxostatThe risk or severity of adverse effects can be increased when Lisuride is combined with Topiroxostat.Approved, Investigational
TopotecanThe risk or severity of adverse effects can be increased when Lisuride is combined with Topotecan.Approved, Investigational
TramadolThe risk or severity of adverse effects can be increased when Lisuride is combined with Tramadol.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe metabolism of Lisuride can be decreased when combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe metabolism of Lisuride can be decreased when combined with Tranylcypromine.Approved
TroglitazoneThe risk or severity of adverse effects can be increased when Lisuride is combined with Troglitazone.Investigational, Withdrawn
TroleandomycinThe risk or severity of adverse effects can be increased when Lisuride is combined with Troleandomycin.Approved
Valproic AcidThe risk or severity of adverse effects can be increased when Lisuride is combined with Valproic Acid.Approved, Investigational
VenlafaxineThe metabolism of Lisuride can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Lisuride can be decreased when combined with Verapamil.Approved
VinblastineThe risk or severity of adverse effects can be increased when Lisuride is combined with Vinblastine.Approved
VincristineThe risk or severity of adverse effects can be increased when Lisuride is combined with Vincristine.Approved, Investigational
VinorelbineThe risk or severity of adverse effects can be increased when Lisuride is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe metabolism of Lisuride can be decreased when combined with Voriconazole.Approved, Investigational
ZafirlukastThe risk or severity of adverse effects can be increased when Lisuride is combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe metabolism of Lisuride can be decreased when combined with Ziprasidone.Approved
ZucapsaicinThe risk or severity of adverse effects can be increased when Lisuride is combined with Zucapsaicin.Approved
Food Interactions
Not Available

References

General References
Not Available
External Links
Human Metabolome Database
HMDB14727
KEGG Drug
D08132
PubChem Compound
28864
PubChem Substance
46505557
ChemSpider
26847
BindingDB
50056445
ChEBI
51164
ChEMBL
CHEMBL157138
Therapeutic Targets Database
DAP000255
PharmGKB
PA164749019
IUPHAR
227
Guide to Pharmacology
GtP Drug Page
Wikipedia
Lisuride
ATC Codes
G02CB02 — LisurideN02CA07 — Lisuride

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Unknown StatusTreatmentCocaine-Related Disorders1
3CompletedTreatmentIdiopathic Parkinson's Disease1
3CompletedTreatmentRestless Legs Syndrome (RLS)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

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/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as indoloquinolines. These are polycyclic aromatic compounds containing an indole fused to a quinoline.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Quinolines and derivatives
Sub Class
Indoloquinolines
Direct Parent
Indoloquinolines
Alternative Parents
Ergoline and derivatives / Benzoquinolines / Pyrroloquinolines / 3-alkylindoles / Isoindoles and derivatives / Aralkylamines / Benzenoids / Pyrroles / Heteroaromatic compounds / Ureas
show 6 more
Substituents
Ergoline skeleton / Indoloquinoline / Benzoquinoline / Pyrroloquinoline / 3-alkylindole / Indole / Indole or derivatives / Isoindole or derivatives / Alkaloid or derivatives / Aralkylamine
show 18 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
monocarboxylic acid amide (CHEBI:51164)

Targets

Details
1. 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. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
Details
2. D(3) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Sh3 domain binding
Specific Function
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
Molecular Weight
48359.86 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
Details
4. D(1A) dopamine receptor
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
Uniprot Name
D(1A) dopamine receptor
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
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 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. 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 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
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...
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]
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-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]
  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-...
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]
  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 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
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 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
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...
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
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
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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
Molecular Weight
53554.43 Da
References
  1. Knight JA, Smith C, Toohey N, Klein MT, Teitler M: Pharmacological analysis of the novel, rapid, and potent inactivation of the human 5-Hydroxytryptamine7 receptor by risperidone, 9-OH-Risperidone, and other inactivating antagonists. Mol Pharmacol. 2009 Feb;75(2):374-80. doi: 10.1124/mol.108.052084. Epub 2008 Nov 7. [PubMed:18996971]
  2. Toohey N, Klein MT, Knight J, Smith C, Teitler M: Human 5-HT7 receptor-induced inactivation of forskolin-stimulated adenylate cyclase by risperidone, 9-OH-risperidone and other "inactivating antagonists". Mol Pharmacol. 2009 Sep;76(3):552-9. doi: 10.1124/mol.109.056283. Epub 2009 Jun 9. [PubMed:19509219]

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...
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]
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]

Drug created on June 13, 2005 07:24 / Updated on November 07, 2017 01:40