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Identification
NameApomorphine
Accession NumberDB00714  (APRD00531)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionA derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. [PubChem]
Structure
Thumb
Synonyms
(-)-10,11-Dihydroxyaporphine
(−)-10,11-dihydroxyaporphine
(6AR)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol
(R)-5,6,6a,7-Tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol
Apomorphin
R-(-)-Apomorphine
R-(−)-apomorphine
External Identifiers
  • APL-130277
  • VR-040
  • VR-400
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ApokynInjection30 mg/3mLSubcutaneousTercica, Inc.2004-07-02Not applicableUs
ApokynInjection30 mg/3mLSubcutaneousUs World Meds, Llc2004-07-02Not applicableUs
MovapoSolution10 mgSubcutaneousPaladin Labs IncNot applicableNot applicableCanada
MovapoSolution10 mgSubcutaneousPaladin Labs IncNot applicableNot applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
IxenseTakeda (discontinued)
SpontaneNot Available
UprimaAbbott (discontinued)
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Apomorphine hydrochloride
41372-20-7
Thumb
  • InChI Key: CXWQXGNFZLHLHQ-DPFCLETOSA-N
  • Monoisotopic Mass: 624.2157777
  • Average Mass: 625.59
DBSALT000818
Categories
UNIIN21FAR7B4S
CAS number58-00-4
WeightAverage: 267.3224
Monoisotopic: 267.125928793
Chemical FormulaC17H17NO2
InChI KeyVMWNQDUVQKEIOC-CYBMUJFWSA-N
InChI
InChI=1S/C17H17NO2/c1-18-8-7-10-3-2-4-12-15(10)13(18)9-11-5-6-14(19)17(20)16(11)12/h2-6,13,19-20H,7-9H2,1H3/t13-/m1/s1
IUPAC Name
(9R)-10-methyl-10-azatetracyclo[7.7.1.0²,⁷.0¹³,¹⁷]heptadeca-1(16),2(7),3,5,13(17),14-hexaene-3,4-diol
SMILES
[H][C@]12CC3=C(C(O)=C(O)C=C3)C3=CC=CC(CCN1C)=C23
Pharmacology
IndicationFor the acute, intermittent treatment of hypomobility, off episodes (end-of-dose wearing off and unpredictable on/off episodes) associated with advanced Parkinson's disease.
Structured Indications
PharmacodynamicsApomorphine is a type of dopaminergic agonist, a morphine derivative which primarily affects the hypothalamic region of the brain. Drugs containing this substance are sometimes used in the treatment of Parkinson's disease or erectile dysfunction. In higher doses it is a highly effective emetic.
Mechanism of actionThe precise mechanism of action of apomorphine as a treatment for Parkinson's disease is unknown, although it is believed to be due to stimulation of post-synaptic dopamine D2-type receptors within the brain. Apomorphine has been shown to improve motor function in an animal model of Parkinson's disease. In particular, apomorphine attenuates the motor deficits induced by lesions in the ascending nigrostriatal dopaminergic pathway with the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in primates.
TargetKindPharmacological actionActionsOrganismUniProt ID
D(3) dopamine receptorProteinyes
agonist
HumanP35462 details
D(4) dopamine receptorProteinyes
agonist
HumanP21917 details
D(2) dopamine receptorProteinyes
agonist
HumanP14416 details
Alpha-2C adrenergic receptorProteinunknown
agonist
HumanP18825 details
Alpha-2B adrenergic receptorProteinunknown
agonist
HumanP18089 details
5-hydroxytryptamine receptor 2CProteinunknown
agonist
HumanP28335 details
D(1B) dopamine receptorProteinunknown
agonist
HumanP21918 details
5-hydroxytryptamine receptor 1AProteinunknown
agonist
HumanP08908 details
5-hydroxytryptamine receptor 2AProteinunknown
agonist
HumanP28223 details
5-hydroxytryptamine receptor 2BProteinunknown
agonist
HumanP41595 details
Alpha-2A adrenergic receptorProteinunknown
agonist
HumanP08913 details
D(1A) dopamine receptorProteinunknown
agonist
HumanP21728 details
5-hydroxytryptamine receptor 1DProteinunknown
agonist
HumanP28221 details
5-hydroxytryptamine receptor 1BProteinunknown
agonist
HumanP28222 details
Neuron-specific vesicular protein calcyonProteinunknown
agonist
HumanQ9NYX4 details
Related Articles
Absorption100% following subcutaneous administration
Volume of distribution
  • 123 to 404 L
Protein binding~50%-albumin
Metabolism

Hepatic

Route of eliminationNot Available
Half life40 minutes (range 30 - 60 minutes)
Clearance
  • 223 L/hr
ToxicityLD50=0.6 mmoles/kg (mice, intraperitoneal)
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINEThe metabolism of Apomorphine can be decreased when combined with 7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE.Experimental
AcebutololApomorphine may increase the atrioventricular blocking (AV block) activities of Acebutolol.Approved
AcetazolamideThe risk or severity of adverse effects can be increased when Apomorphine is combined with Acetazolamide.Approved, Vet Approved
AldesleukinThe risk or severity of adverse effects can be increased when Aldesleukin is combined with Apomorphine.Approved
AliskirenThe risk or severity of adverse effects can be increased when Aliskiren is combined with Apomorphine.Approved, Investigational
AlprenololApomorphine may increase the atrioventricular blocking (AV block) activities of Alprenolol.Approved, Withdrawn
AmifostineThe risk or severity of adverse effects can be increased when Amifostine is combined with Apomorphine.Approved, Investigational
AmilorideThe risk or severity of adverse effects can be increased when Amiloride is combined with Apomorphine.Approved
AmineptineAmineptine may decrease the antihypertensive activities of Apomorphine.Illicit, Withdrawn
AmiodaroneApomorphine may increase the QTc-prolonging activities of Amiodarone.Approved, Investigational
AmisulprideThe therapeutic efficacy of Amisulpride can be decreased when used in combination with Apomorphine.Approved, Investigational
AmitriptylineAmitriptyline may decrease the antihypertensive activities of Apomorphine.Approved
AmlodipineThe risk or severity of adverse effects can be increased when Amlodipine is combined with Apomorphine.Approved
AmobarbitalAmobarbital may increase the hypotensive activities of Apomorphine.Approved, Illicit
Amphotericin BThe risk or severity of adverse effects can be increased when Amphotericin B is combined with Apomorphine.Approved, Investigational
Amyl NitriteThe risk or severity of adverse effects can be increased when Amyl Nitrite is combined with Apomorphine.Approved
AnagrelideApomorphine may increase the QTc-prolonging activities of Anagrelide.Approved
Aop200704Apomorphine may increase the atrioventricular blocking (AV block) activities of Aop200704.Investigational
ApraclonidineThe risk or severity of adverse effects can be increased when Apraclonidine is combined with Apomorphine.Approved
AripiprazoleAripiprazole may increase the hypotensive activities of Apomorphine.Approved, Investigational
ArotinololApomorphine may increase the atrioventricular blocking (AV block) activities of Arotinolol.Approved
Arsenic trioxideApomorphine may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherApomorphine may increase the QTc-prolonging activities of Artemether.Approved
AsenapineApomorphine may increase the QTc-prolonging activities of Asenapine.Approved
AtenololApomorphine may increase the atrioventricular blocking (AV block) activities of Atenolol.Approved
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Apomorphine.Approved
AzithromycinApomorphine may increase the QTc-prolonging activities of Azithromycin.Approved
BarbexacloneBarbexaclone may increase the hypotensive activities of Apomorphine.Experimental
BarbitalBarbital may increase the hypotensive activities of Apomorphine.Illicit
BarnidipineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Barnidipine.Approved
BedaquilineApomorphine may increase the QTc-prolonging activities of Bedaquiline.Approved
BefunololApomorphine may increase the atrioventricular blocking (AV block) activities of Befunolol.Experimental
BenazeprilThe risk or severity of adverse effects can be increased when Benazepril is combined with Apomorphine.Approved, Investigational
BendroflumethiazideThe risk or severity of adverse effects can be increased when Bendroflumethiazide is combined with Apomorphine.Approved
BenmoxinThe metabolism of Apomorphine can be decreased when combined with Benmoxin.Withdrawn
BepridilThe risk or severity of adverse effects can be increased when Apomorphine is combined with Bepridil.Approved, Withdrawn
BetaxololApomorphine may increase the atrioventricular blocking (AV block) activities of Betaxolol.Approved
BevantololApomorphine may increase the atrioventricular blocking (AV block) activities of Bevantolol.Approved
BisoprololApomorphine may increase the atrioventricular blocking (AV block) activities of Bisoprolol.Approved
BlonanserinThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Blonanserin.Approved
BopindololApomorphine may increase the atrioventricular blocking (AV block) activities of Bopindolol.Approved
BortezomibThe risk or severity of adverse effects can be increased when Apomorphine is combined with Bortezomib.Approved, Investigational
BretyliumThe risk or severity of adverse effects can be increased when Bretylium is combined with Apomorphine.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Brimonidine is combined with Apomorphine.Approved
BromocriptineBromocriptine may increase the vasoconstricting activities of Apomorphine.Approved, Investigational
BucindololApomorphine may increase the atrioventricular blocking (AV block) activities of Bucindolol.Investigational
BufuralolApomorphine may increase the atrioventricular blocking (AV block) activities of Bufuralol.Experimental, Investigational
BumetanideThe risk or severity of adverse effects can be increased when Bumetanide is combined with Apomorphine.Approved
BupivacaineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Bupivacaine.Approved, Investigational
BupranololApomorphine may increase the atrioventricular blocking (AV block) activities of Bupranolol.Approved
BupropionThe risk or severity of adverse effects can be increased when Apomorphine is combined with Bupropion.Approved
CabergolineCabergoline may increase the vasoconstricting activities of Apomorphine.Approved
CanagliflozinThe risk or severity of adverse effects can be increased when Canagliflozin is combined with Apomorphine.Approved
CandesartanThe risk or severity of adverse effects can be increased when Candesartan is combined with Apomorphine.Approved
CaptoprilThe risk or severity of adverse effects can be increased when Captopril is combined with Apomorphine.Approved
CarbetocinThe risk or severity of adverse effects can be increased when Apomorphine is combined with Carbetocin.Approved
CariprazineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Cariprazine.Approved
CaroxazoneThe metabolism of Apomorphine can be decreased when combined with Caroxazone.Withdrawn
CarteololApomorphine may increase the atrioventricular blocking (AV block) activities of Carteolol.Approved
CarvedilolApomorphine may increase the atrioventricular blocking (AV block) activities of Carvedilol.Approved, Investigational
CeliprololApomorphine may increase the atrioventricular blocking (AV block) activities of Celiprolol.Approved, Investigational
CeritinibApomorphine may increase the QTc-prolonging activities of Ceritinib.Approved
ChloroquineApomorphine may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChlorothiazideThe risk or severity of adverse effects can be increased when Chlorothiazide is combined with Apomorphine.Approved, Vet Approved
ChlorpromazineThe therapeutic efficacy of Chlorpromazine can be decreased when used in combination with Apomorphine.Approved, Vet Approved
ChlorprothixeneThe therapeutic efficacy of Chlorprothixene can be decreased when used in combination with Apomorphine.Approved, Withdrawn
ChlorthalidoneThe risk or severity of adverse effects can be increased when Chlorthalidone is combined with Apomorphine.Approved
CilazaprilThe risk or severity of adverse effects can be increased when Cilazapril is combined with Apomorphine.Approved
CilnidipineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Cilnidipine.Approved
CiprofloxacinApomorphine may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideApomorphine may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CitalopramApomorphine may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinApomorphine may increase the QTc-prolonging activities of Clarithromycin.Approved
ClevidipineThe risk or severity of adverse effects can be increased when Clevidipine is combined with Apomorphine.Approved
ClofarabineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Clofarabine.Approved, Investigational
ClomipramineClomipramine may decrease the antihypertensive activities of Apomorphine.Approved, Vet Approved
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Apomorphine.Approved
ClozapineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Clozapine.Approved
ConivaptanThe risk or severity of adverse effects can be increased when Apomorphine is combined with Conivaptan.Approved, Investigational
CrizotinibApomorphine may increase the QTc-prolonging activities of Crizotinib.Approved
CyclobenzaprineCyclobenzaprine may decrease the antihypertensive activities of Apomorphine.Approved
DapagliflozinThe risk or severity of adverse effects can be increased when Dapagliflozin is combined with Apomorphine.Approved
DesfluraneThe risk or severity of adverse effects can be increased when Apomorphine is combined with Desflurane.Approved
DesipramineDesipramine may decrease the antihypertensive activities of Apomorphine.Approved
DesvenlafaxineDesvenlafaxine may decrease the antihypertensive activities of Apomorphine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Apomorphine.Approved, Vet Approved
DiclofenamideThe risk or severity of adverse effects can be increased when Diclofenamide is combined with Apomorphine.Approved
DihydroergotamineDihydroergotamine may increase the vasoconstricting activities of Apomorphine.Approved
DiltiazemThe risk or severity of adverse effects can be increased when Diltiazem is combined with Apomorphine.Approved
DinutuximabThe risk or severity of adverse effects can be increased when Dinutuximab is combined with Apomorphine.Approved
DipyridamoleThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Apomorphine.Approved
DisopyramideApomorphine may increase the QTc-prolonging activities of Disopyramide.Approved
DofetilideApomorphine may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronDolasetron may increase the hypotensive activities of Apomorphine.Approved
DomperidoneApomorphine may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DosulepinDosulepin may decrease the antihypertensive activities of Apomorphine.Approved
DoxazosinThe risk or severity of adverse effects can be increased when Doxazosin is combined with Apomorphine.Approved
DoxepinDoxepin may decrease the antihypertensive activities of Apomorphine.Approved
DronedaroneApomorphine may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolThe therapeutic efficacy of Droperidol can be decreased when used in combination with Apomorphine.Approved, Vet Approved
DroxidopaApomorphine may increase the hypertensive activities of Droxidopa.Approved, Investigational
DuloxetineApomorphine may increase the orthostatic hypotensive activities of Duloxetine.Approved
EfonidipineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Efonidipine.Approved
EliglustatApomorphine may increase the QTc-prolonging activities of Eliglustat.Approved
EmpagliflozinThe risk or severity of adverse effects can be increased when Empagliflozin is combined with Apomorphine.Approved
EnalaprilThe risk or severity of adverse effects can be increased when Enalapril is combined with Apomorphine.Approved, Vet Approved
EnalaprilatThe risk or severity of adverse effects can be increased when Apomorphine is combined with Enalaprilat.Approved
EplerenoneThe risk or severity of adverse effects can be increased when Eplerenone is combined with Apomorphine.Approved
EpoprostenolThe risk or severity of adverse effects can be increased when Apomorphine is combined with Epoprostenol.Approved
EprosartanThe risk or severity of adverse effects can be increased when Eprosartan is combined with Apomorphine.Approved
Ergoloid mesylateErgoloid mesylate may increase the vasoconstricting activities of Apomorphine.Approved
ErgonovineErgonovine may increase the vasoconstricting activities of Apomorphine.Approved
ErgotamineErgotamine may increase the vasoconstricting activities of Apomorphine.Approved
ErythromycinApomorphine may increase the QTc-prolonging activities of Erythromycin.Approved, Vet Approved
EscitalopramApomorphine may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
EsmirtazapineEsmirtazapine may decrease the antihypertensive activities of Apomorphine.Investigational
EsmololApomorphine may increase the atrioventricular blocking (AV block) activities of Esmolol.Approved
Etacrynic acidThe risk or severity of adverse effects can be increased when Etacrynic acid is combined with Apomorphine.Approved
FelodipineThe risk or severity of adverse effects can be increased when Felodipine is combined with Apomorphine.Approved, Investigational
FenoldopamThe risk or severity of adverse effects can be increased when Apomorphine is combined with Fenoldopam.Approved
FimasartanThe risk or severity of adverse effects can be increased when Apomorphine is combined with Fimasartan.Approved
FlecainideApomorphine may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FluoxetineApomorphine may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolApomorphine may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FluphenazineThe therapeutic efficacy of Fluphenazine can be decreased when used in combination with Apomorphine.Approved
FosinoprilThe risk or severity of adverse effects can be increased when Fosinopril is combined with Apomorphine.Approved
FurazolidoneThe metabolism of Apomorphine can be decreased when combined with Furazolidone.Approved, Vet Approved
FurosemideThe risk or severity of adverse effects can be increased when Furosemide is combined with Apomorphine.Approved, Vet Approved
Gadobenic acidApomorphine may increase the QTc-prolonging activities of Gadobenic acid.Approved
GemifloxacinApomorphine may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GoserelinApomorphine may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronGranisetron may increase the hypotensive activities of Apomorphine.Approved, Investigational
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Apomorphine.Approved, Investigational
HaloperidolThe therapeutic efficacy of Haloperidol can be decreased when used in combination with Apomorphine.Approved
HalothaneThe risk or severity of adverse effects can be increased when Apomorphine is combined with Halothane.Approved, Vet Approved
HexobarbitalHexobarbital may increase the hypotensive activities of Apomorphine.Approved
HydracarbazineThe metabolism of Apomorphine can be decreased when combined with Hydracarbazine.Approved
HydralazineThe risk or severity of adverse effects can be increased when Hydralazine is combined with Apomorphine.Approved
HydrochlorothiazideThe risk or severity of adverse effects can be increased when Hydrochlorothiazide is combined with Apomorphine.Approved, Vet Approved
HydroflumethiazideThe risk or severity of adverse effects can be increased when Apomorphine is combined with Hydroflumethiazide.Approved
IbutilideApomorphine may increase the QTc-prolonging activities of Ibutilide.Approved
IloperidoneApomorphine may increase the QTc-prolonging activities of Iloperidone.Approved
IloprostThe risk or severity of adverse effects can be increased when Apomorphine is combined with Iloprost.Approved, Investigational
ImidaprilThe risk or severity of adverse effects can be increased when Apomorphine is combined with Imidapril.Investigational
ImipramineImipramine may decrease the antihypertensive activities of Apomorphine.Approved
IndapamideThe risk or severity of adverse effects can be increased when Indapamide is combined with Apomorphine.Approved
IndenololApomorphine may increase the atrioventricular blocking (AV block) activities of Indenolol.Withdrawn
IndoraminThe risk or severity of adverse effects can be increased when Apomorphine is combined with Indoramin.Withdrawn
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Apomorphine.Approved
IproclozideThe metabolism of Apomorphine can be decreased when combined with Iproclozide.Withdrawn
IproniazidThe metabolism of Apomorphine can be decreased when combined with Iproniazid.Withdrawn
IrbesartanThe risk or severity of adverse effects can be increased when Irbesartan is combined with Apomorphine.Approved, Investigational
IsocarboxazidThe metabolism of Apomorphine can be decreased when combined with Isocarboxazid.Approved
IsofluraneThe risk or severity of adverse effects can be increased when Apomorphine is combined with Isoflurane.Approved, Vet Approved
Isosorbide DinitrateThe risk or severity of adverse effects can be increased when Isosorbide Dinitrate is combined with Apomorphine.Approved
Isosorbide MononitrateThe risk or severity of adverse effects can be increased when Isosorbide Mononitrate is combined with Apomorphine.Approved
IsoxsuprineThe risk or severity of adverse effects can be increased when Isoxsuprine is combined with Apomorphine.Approved, Withdrawn
IsradipineThe risk or severity of adverse effects can be increased when Isradipine is combined with Apomorphine.Approved
LabetalolApomorphine may increase the atrioventricular blocking (AV block) activities of Labetalol.Approved
LacidipineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Lacidipine.Approved
LenvatinibApomorphine may increase the QTc-prolonging activities of Lenvatinib.Approved
LercanidipineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Lercanidipine.Approved, Investigational
LeuprolideApomorphine may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevobunololThe risk or severity of adverse effects can be increased when Levobunolol is combined with Apomorphine.Approved
LevobupivacaineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Levobupivacaine.Approved
LevodopaApomorphine may increase the orthostatic hypotensive activities of Levodopa.Approved
LevofloxacinApomorphine may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
LevomilnacipranLevomilnacipran may decrease the antihypertensive activities of Apomorphine.Approved
LevosimendanThe risk or severity of adverse effects can be increased when Apomorphine is combined with Levosimendan.Approved, Investigational
LisinoprilThe risk or severity of adverse effects can be increased when Lisinopril is combined with Apomorphine.Approved, Investigational
LofexidineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Lofexidine.Approved, Investigational
LopinavirApomorphine may increase the QTc-prolonging activities of Lopinavir.Approved
LosartanThe risk or severity of adverse effects can be increased when Losartan is combined with Apomorphine.Approved
LoxapineThe therapeutic efficacy of Loxapine can be decreased when used in combination with Apomorphine.Approved
LumateperoneThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Lumateperone.Investigational
LumefantrineApomorphine may increase the QTc-prolonging activities of Lumefantrine.Approved
LurasidoneThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Lurasidone.Approved
MannitolThe risk or severity of adverse effects can be increased when Mannitol is combined with Apomorphine.Approved, Investigational
MebanazineThe metabolism of Apomorphine can be decreased when combined with Mebanazine.Withdrawn
MecamylamineThe risk or severity of adverse effects can be increased when Mecamylamine is combined with Apomorphine.Approved
MelperoneThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Melperone.Approved
MesoridazineThe therapeutic efficacy of Mesoridazine can be decreased when used in combination with Apomorphine.Approved
MethadoneApomorphine may increase the QTc-prolonging activities of Methadone.Approved
MethazolamideThe risk or severity of adverse effects can be increased when Methazolamide is combined with Apomorphine.Approved
MethohexitalMethohexital may increase the hypotensive activities of Apomorphine.Approved
MethotrimeprazineThe therapeutic efficacy of Methotrimeprazine can be decreased when used in combination with Apomorphine.Approved
MethyclothiazideThe risk or severity of adverse effects can be increased when Methyclothiazide is combined with Apomorphine.Approved
MethyldopaThe risk or severity of adverse effects can be increased when Methyldopa is combined with Apomorphine.Approved
Methylene blueThe metabolism of Apomorphine can be decreased when combined with Methylene blue.Investigational
MethylphenidateThe risk or severity of adverse effects can be increased when Methylphenidate is combined with Apomorphine.Approved, Investigational
MethylphenobarbitalMethylphenobarbital may increase the hypotensive activities of Apomorphine.Approved
MetipranololThe risk or severity of adverse effects can be increased when Metipranolol is combined with Apomorphine.Approved
MetoclopramideThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Metoclopramide.Approved, Investigational
MetolazoneThe risk or severity of adverse effects can be increased when Metolazone is combined with Apomorphine.Approved
MetoprololApomorphine may increase the atrioventricular blocking (AV block) activities of Metoprolol.Approved, Investigational
MianserinThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Mianserin.Approved
MifepristoneMifepristone may increase the QTc-prolonging activities of Apomorphine.Approved, Investigational
MilnacipranMilnacipran may decrease the antihypertensive activities of Apomorphine.Approved
MinaprineThe metabolism of Apomorphine can be decreased when combined with Minaprine.Approved
MinoxidilThe risk or severity of adverse effects can be increased when Minoxidil is combined with Apomorphine.Approved
MirtazapineMirtazapine may decrease the antihypertensive activities of Apomorphine.Approved
MoclobemideThe metabolism of Apomorphine can be decreased when combined with Moclobemide.Approved
MoexiprilThe risk or severity of adverse effects can be increased when Moexipril is combined with Apomorphine.Approved
MolindoneThe therapeutic efficacy of Molindone can be decreased when used in combination with Apomorphine.Approved
MorphineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Morphine.Approved, Investigational
MoxifloxacinApomorphine may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
MoxonidineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Moxonidine.Approved
NabiloneThe risk or severity of adverse effects can be increased when Apomorphine is combined with Nabilone.Approved, Investigational
NadololApomorphine may increase the atrioventricular blocking (AV block) activities of Nadolol.Approved
NebivololThe risk or severity of adverse effects can be increased when Nebivolol is combined with Apomorphine.Approved, Investigational
NesiritideThe risk or severity of adverse effects can be increased when Nesiritide is combined with Apomorphine.Approved, Investigational
NialamideThe metabolism of Apomorphine can be decreased when combined with Nialamide.Withdrawn
NicardipineThe risk or severity of adverse effects can be increased when Nicardipine is combined with Apomorphine.Approved
NicorandilNicorandil may increase the hypotensive activities of Apomorphine.Approved
NifedipineThe risk or severity of adverse effects can be increased when Nifedipine is combined with Apomorphine.Approved
NilotinibApomorphine may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NilvadipineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Nilvadipine.Approved
NimodipineThe risk or severity of adverse effects can be increased when Nimodipine is combined with Apomorphine.Approved
NisoldipineThe risk or severity of adverse effects can be increased when Nisoldipine is combined with Apomorphine.Approved
NitrendipineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Nitrendipine.Approved
Nitric OxideThe risk or severity of adverse effects can be increased when Apomorphine is combined with Nitric Oxide.Approved
NitroglycerinThe risk or severity of adverse effects can be increased when Nitroglycerin is combined with Apomorphine.Approved, Investigational
NitroprussideThe risk or severity of adverse effects can be increased when Nitroprusside is combined with Apomorphine.Approved
NortriptylineNortriptyline may decrease the antihypertensive activities of Apomorphine.Approved
ObinutuzumabThe risk or severity of adverse effects can be increased when Apomorphine is combined with Obinutuzumab.Approved
OctamoxinThe metabolism of Apomorphine can be decreased when combined with Octamoxin.Withdrawn
OfloxacinApomorphine may increase the QTc-prolonging activities of Ofloxacin.Approved
OlanzapineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Olanzapine.Approved, Investigational
OlmesartanThe risk or severity of adverse effects can be increased when Olmesartan is combined with Apomorphine.Approved, Investigational
OndansetronOndansetron may increase the hypotensive activities of Apomorphine.Approved
OpipramolOpipramol may decrease the antihypertensive activities of Apomorphine.Investigational
OxprenololApomorphine may increase the atrioventricular blocking (AV block) activities of Oxprenolol.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Apomorphine is combined with Paclitaxel.Approved, Vet Approved
PaliperidoneApomorphine may increase the QTc-prolonging activities of Paliperidone.Approved
PalonosetronPalonosetron may increase the hypotensive activities of Apomorphine.Approved, Investigational
PanobinostatApomorphine may increase the QTc-prolonging activities of Panobinostat.Approved, Investigational
PapaverineThe risk or severity of adverse effects can be increased when Papaverine is combined with Apomorphine.Approved
PargylineThe metabolism of Apomorphine can be decreased when combined with Pargyline.Approved
PazopanibApomorphine may increase the QTc-prolonging activities of Pazopanib.Approved
PenbutololApomorphine may increase the atrioventricular blocking (AV block) activities of Penbutolol.Approved, Investigational
PentamidineApomorphine may increase the QTc-prolonging activities of Pentamidine.Approved
PentobarbitalPentobarbital may increase the hypotensive activities of Apomorphine.Approved, Vet Approved
PerflutrenApomorphine may increase the QTc-prolonging activities of Perflutren.Approved
PerindoprilThe risk or severity of adverse effects can be increased when Perindopril is combined with Apomorphine.Approved
PerospironeThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Perospirone.Approved
PerphenazineThe therapeutic efficacy of Perphenazine can be decreased when used in combination with Apomorphine.Approved
PhenelzineThe metabolism of Apomorphine can be decreased when combined with Phenelzine.Approved
PheniprazineThe metabolism of Apomorphine can be decreased when combined with Pheniprazine.Withdrawn
PhenobarbitalPhenobarbital may increase the hypotensive activities of Apomorphine.Approved
PhenoxybenzamineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Phenoxybenzamine.Approved
PhenoxypropazineThe metabolism of Apomorphine can be decreased when combined with Phenoxypropazine.Withdrawn
PhentolamineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Phentolamine.Approved
PimavanserinThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Pimavanserin.Investigational
PimozideApomorphine may increase the QTc-prolonging activities of Pimozide.Approved
PindololApomorphine may increase the atrioventricular blocking (AV block) activities of Pindolol.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Apomorphine is combined with Pipamperone.Approved
PirlindoleThe metabolism of Apomorphine can be decreased when combined with Pirlindole.Approved
PivhydrazineThe metabolism of Apomorphine can be decreased when combined with Pivhydrazine.Withdrawn
PractololApomorphine may increase the atrioventricular blocking (AV block) activities of Practolol.Approved
PramipexoleThe risk or severity of adverse effects can be increased when Apomorphine is combined with Pramipexole.Approved, Investigational
PrazosinThe risk or severity of adverse effects can be increased when Prazosin is combined with Apomorphine.Approved
PrimaquineApomorphine may increase the QTc-prolonging activities of Primaquine.Approved
PrimidonePrimidone may increase the hypotensive activities of Apomorphine.Approved, Vet Approved
ProcainamideApomorphine may increase the QTc-prolonging activities of Procainamide.Approved
ProchlorperazineThe therapeutic efficacy of Prochlorperazine can be decreased when used in combination with Apomorphine.Approved, Vet Approved
PromazineThe therapeutic efficacy of Promazine can be decreased when used in combination with Apomorphine.Approved, Vet Approved
PropafenoneApomorphine may increase the QTc-prolonging activities of Propafenone.Approved
PropericiazineThe therapeutic efficacy of Propericiazine can be decreased when used in combination with Apomorphine.Approved
PropofolThe risk or severity of adverse effects can be increased when Apomorphine is combined with Propofol.Approved, Investigational, Vet Approved
PropranololApomorphine may increase the atrioventricular blocking (AV block) activities of Propranolol.Approved, Investigational
ProtriptylineProtriptyline may decrease the antihypertensive activities of Apomorphine.Approved
QuetiapineApomorphine may increase the QTc-prolonging activities of Quetiapine.Approved
QuinaprilThe risk or severity of adverse effects can be increased when Quinapril is combined with Apomorphine.Approved, Investigational
QuinidineApomorphine may increase the QTc-prolonging activities of Quinidine.Approved
QuinineApomorphine may increase the QTc-prolonging activities of Quinine.Approved
RamiprilThe risk or severity of adverse effects can be increased when Ramipril is combined with Apomorphine.Approved
RasagilineThe metabolism of Apomorphine can be decreased when combined with Rasagiline.Approved
RemifentanilThe risk or severity of adverse effects can be increased when Apomorphine is combined with Remifentanil.Approved
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Apomorphine.Approved
RiociguatThe risk or severity of adverse effects can be increased when Riociguat is combined with Apomorphine.Approved
RisperidoneApomorphine may increase the hypotensive activities of Risperidone.Approved, Investigational
RopiniroleThe risk or severity of adverse effects can be increased when Apomorphine is combined with Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Ropivacaine.Approved
RotigotineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Rotigotine.Approved
RP5063The therapeutic efficacy of Apomorphine can be decreased when used in combination with RP5063.Investigational
SacubitrilThe risk or severity of adverse effects can be increased when Apomorphine is combined with Sacubitril.Approved
SafrazineThe metabolism of Apomorphine can be decreased when combined with Safrazine.Withdrawn
SaquinavirApomorphine may increase the QTc-prolonging activities of Saquinavir.Approved, Investigational
SecobarbitalSecobarbital may increase the hypotensive activities of Apomorphine.Approved, Vet Approved
SelegilineThe metabolism of Apomorphine can be decreased when combined with Selegiline.Approved, Investigational, Vet Approved
SertindoleThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Sertindole.Approved, Withdrawn
SevofluraneThe risk or severity of adverse effects can be increased when Apomorphine is combined with Sevoflurane.Approved, Vet Approved
Sodium NitriteThe risk or severity of adverse effects can be increased when Apomorphine is combined with Sodium Nitrite.Approved
SotalolApomorphine may increase the atrioventricular blocking (AV block) activities of Sotalol.Approved
SpironolactoneThe risk or severity of adverse effects can be increased when Spironolactone is combined with Apomorphine.Approved
StreptokinaseThe risk or severity of adverse effects can be increased when Apomorphine is combined with Streptokinase.Approved
SufentanilThe risk or severity of adverse effects can be increased when Apomorphine is combined with Sufentanil.Approved, Investigational
SulfisoxazoleApomorphine may increase the QTc-prolonging activities of Sulfisoxazole.Approved, Vet Approved
TamsulosinThe risk or severity of adverse effects can be increased when Apomorphine is combined with Tamsulosin.Approved, Investigational
TelavancinApomorphine may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinApomorphine may increase the QTc-prolonging activities of Telithromycin.Approved
TelmisartanThe risk or severity of adverse effects can be increased when Telmisartan is combined with Apomorphine.Approved, Investigational
TerazosinThe risk or severity of adverse effects can be increased when Terazosin is combined with Apomorphine.Approved
TetrabenazineApomorphine may increase the QTc-prolonging activities of Tetrabenazine.Approved
ThalidomideThe risk or severity of adverse effects can be increased when Apomorphine is combined with Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThiamylal may increase the hypotensive activities of Apomorphine.Approved, Vet Approved
ThiopentalThiopental may increase the hypotensive activities of Apomorphine.Approved, Vet Approved
ThioproperazineThe therapeutic efficacy of Thioproperazine can be decreased when used in combination with Apomorphine.Approved
ThioridazineApomorphine may increase the QTc-prolonging activities of Thioridazine.Approved
ThiothixeneThe therapeutic efficacy of Thiothixene can be decreased when used in combination with Apomorphine.Approved
TianeptineTianeptine may decrease the antihypertensive activities of Apomorphine.Approved
TimololApomorphine may increase the atrioventricular blocking (AV block) activities of Timolol.Approved
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Apomorphine.Approved
TolazolineThe risk or severity of adverse effects can be increased when Apomorphine is combined with Tolazoline.Approved, Vet Approved
TolcaponeThe risk or severity of adverse effects can be increased when Apomorphine is combined with Tolcapone.Approved, Withdrawn
ToloxatoneThe metabolism of Apomorphine can be decreased when combined with Toloxatone.Approved
TorasemideThe risk or severity of adverse effects can be increased when Torasemide is combined with Apomorphine.Approved
ToremifeneApomorphine may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TrandolaprilThe risk or severity of adverse effects can be increased when Trandolapril is combined with Apomorphine.Approved
Trans-2-PhenylcyclopropylamineThe metabolism of Apomorphine can be decreased when combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe metabolism of Apomorphine can be decreased when combined with Tranylcypromine.Approved
TretinoinThe risk or severity of adverse effects can be increased when Apomorphine is combined with Tretinoin.Approved, Investigational, Nutraceutical
TriamtereneThe risk or severity of adverse effects can be increased when Triamterene is combined with Apomorphine.Approved
TrifluoperazineThe therapeutic efficacy of Trifluoperazine can be decreased when used in combination with Apomorphine.Approved
TrimipramineTrimipramine may decrease the antihypertensive activities of Apomorphine.Approved
TropisetronTropisetron may increase the hypotensive activities of Apomorphine.Investigational
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Apomorphine.Approved, Investigational
VandetanibApomorphine may increase the QTc-prolonging activities of Vandetanib.Approved
VemurafenibApomorphine may increase the QTc-prolonging activities of Vemurafenib.Approved
VenlafaxineVenlafaxine may decrease the antihypertensive activities of Apomorphine.Approved
VerapamilThe risk or severity of adverse effects can be increased when Verapamil is combined with Apomorphine.Approved
ZiprasidoneApomorphine may increase the QTc-prolonging activities of Ziprasidone.Approved
ZotepineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Zotepine.Approved
ZuclopenthixolApomorphine may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis Reference

Narayanasamy Gurusamy, “Process for Making Apomorphine and Apocodeine.” U.S. Patent US20100228032, issued September 09, 2010.

US20100228032
General References
  1. Matsumoto K, Yoshida M, Andersson KE, Hedlund P: Effects in vitro and in vivo by apomorphine in the rat corpus cavernosum. Br J Pharmacol. 2005 Sep;146(2):259-67. [PubMed:16025145 ]
  2. SCHWAB RS, AMADOR LV, LETTVIN JY: Apomorphine in Parkinson's disease. Trans Am Neurol Assoc. 1951;56:251-3. [PubMed:14913646 ]
  3. Cotzias GC, Papavasiliou PS, Fehling C, Kaufman B, Mena I: Similarities between neurologic effects of L-dipa and of apomorphine. N Engl J Med. 1970 Jan 1;282(1):31-3. [PubMed:4901383 ]
  4. Corsini GU, Del Zompo M, Gessa GL, Mangoni A: Therapeutic efficacy of apomorphine combined with an extracerebral inhibitor of dopamine receptors in Parkinson's disease. Lancet. 1979 May 5;1(8123):954-6. [PubMed:87620 ]
  5. Chaudhuri KR, Clough C: Subcutaneous apomorphine in Parkinson's disease. BMJ. 1998 Feb 28;316(7132):641. [PubMed:9522772 ]
External Links
ATC CodesG04BE07N04BC07
AHFS Codes
  • 28:36.20.08
PDB EntriesNot Available
FDA labelDownload (513 KB)
MSDSDownload (25.8 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9816
Blood Brain Barrier+0.9401
Caco-2 permeable+0.777
P-glycoprotein substrateSubstrate0.8501
P-glycoprotein inhibitor INon-inhibitor0.8781
P-glycoprotein inhibitor IINon-inhibitor0.964
Renal organic cation transporterInhibitor0.6477
CYP450 2C9 substrateNon-substrate0.7577
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7039
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9146
CYP450 2D6 inhibitorNon-inhibitor0.9084
CYP450 2C19 inhibitorNon-inhibitor0.8718
CYP450 3A4 inhibitorNon-inhibitor0.9156
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9262
Ames testAMES toxic0.6775
CarcinogenicityNon-carcinogens0.9736
BiodegradationNot ready biodegradable0.8928
Rat acute toxicity2.6446 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6544
hERG inhibition (predictor II)Inhibitor0.7734
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Ipsen biopharm ltd
Packagers
Dosage forms
FormRouteStrength
InjectionSubcutaneous30 mg/3mL
SolutionSubcutaneous10 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubility1.66E+004 mg/LNot Available
logP3.1Not Available
pKa8.92Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.51 mg/mLALOGPS
logP2.51ALOGPS
logP2.87ChemAxon
logS-2.7ALOGPS
pKa (Strongest Acidic)6.58ChemAxon
pKa (Strongest Basic)13.25ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area43.7 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity79.99 m3·mol-1ChemAxon
Polarizability29.7 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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as aporphines. These are quinoline alkaloids containing the dibenzo[de,g]quinoline ring system or a dehydrogenated derivative thereof.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassAporphines
Sub ClassNot Available
Direct ParentAporphines
Alternative Parents
Substituents
  • Aporphine
  • Benzylisoquinoline
  • Phenanthrene
  • Benzoquinoline
  • 1-naphthol
  • 2-naphthol
  • Tetrahydroisoquinoline
  • Quinoline
  • Naphthalene
  • 1,2-diphenol
  • Aralkylamine
  • Benzenoid
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Organoheterocyclic compound
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name:
DRD3
Uniprot ID:
P35462
Molecular Weight:
44224.335 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
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. Boeckler F, Russig H, Zhang W, Lober S, Schetz J, Hubner H, Ferger B, Gmeiner P, Feldon J: FAUC 213, a highly selective dopamine D4 receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and neurochemical models of schizophrenia. Psychopharmacology (Berl). 2004 Aug;175(1):7-17. Epub 2004 Mar 6. [PubMed:15007532 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  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 ]
  4. Mansbach RS, Brooks EW, Sanner MA, Zorn SH: Selective dopamine D4 receptor antagonists reverse apomorphine-induced blockade of prepulse inhibition. Psychopharmacology (Berl). 1998 Jan;135(2):194-200. [PubMed:9497025 ]
  5. Melis MR, Succu S, Sanna F, Melis T, Mascia MS, Enguehard-Gueiffier C, Hubner H, Gmeiner P, Gueiffier A, Argiolas A: PIP3EA and PD-168077, two selective dopamine D4 receptor agonists, induce penile erection in male rats: site and mechanism of action in the brain. Eur J Neurosci. 2006 Oct;24(7):2021-30. [PubMed:17067298 ]
  6. Sanner MA, Chappie TA, Dunaiskis AR, Fliri AF, Desai KA, Zorn SH, Jackson ER, Johnson CG, Morrone JM, Seymour PA, Majchrzak MJ, Faraci WS, Collins JL, Duignan DB, Prete Di CC, Lee JS, Trozzi A: Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist. Bioorg Med Chem Lett. 1998 Apr 7;8(7):725-30. [PubMed:9871530 ]
  7. Succu S, Sanna F, Melis T, Boi A, Argiolas A, Melis MR: Stimulation of dopamine receptors in the paraventricular nucleus of the hypothalamus of male rats induces penile erection and increases extra-cellular dopamine in the nucleus accumbens: Involvement of central oxytocin. Neuropharmacology. 2007 Mar;52(3):1034-43. Epub 2006 Dec 11. [PubMed:17164075 ]
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. Berlin I, de Brettes B, Aymard G, Diquet B, Arnulf I, Puech AJ: Dopaminergic drug response and the genotype (Taq IA polymorphism) of the dopamine D2 receptor. Int J Neuropsychopharmacol. 2000 Mar;3(1):35-43. [PubMed:11343576 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  3. Kim HJ, Koh PO, Kang SS, Paik WY, Choi WS: The localization of dopamine D2 receptor mRNA in the human placenta and the anti-angiogenic effect of apomorphine in the chorioallantoic membrane. Life Sci. 2001 Jan 19;68(9):1031-40. [PubMed:11212866 ]
  4. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
  5. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  6. Lucht MJ, Kuehn KU, Schroeder W, Armbruster J, Abraham G, Schattenberg A, Gaensicke M, Barnow S, Tretzel H, Herrmann FH, Freyberger HJ: Influence of the dopamine D2 receptor (DRD2) exon 8 genotype on efficacy of tiapride and clinical outcome of alcohol withdrawal. Pharmacogenetics. 2001 Nov;11(8):647-53. [PubMed:11692072 ]
  7. Yamada S: [Disruption of prepulse inhibition of acoustic startle as an animal model for schizophrenia]. Nihon Shinkei Seishin Yakurigaku Zasshi. 2000 Oct;20(4):131-9. [PubMed:11215397 ]
  8. Yamada S, Harano M, Annoh N, Nakamura K, Tanaka M: Involvement of serotonin 2A receptors in phencyclidine-induced disruption of prepulse inhibition of the acoustic startle in rats. Biol Psychiatry. 1999 Sep 15;46(6):832-8. [PubMed:10494453 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
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
Actions
agonist
General Function:
Epinephrine binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > 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
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD5
Uniprot ID:
P21918
Molecular Weight:
52950.5 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Virus receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation 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
unknown
Actions
agonist
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is 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
agonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD1
Uniprot ID:
P21728
Molecular Weight:
49292.765 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Guo H, Tang Z, Yu Y, Xu L, Jin G, Zhou J: Apomorphine induces trophic factors that support fetal rat mesencephalic dopaminergic neurons in cultures. Eur J Neurosci. 2002 Nov;16(10):1861-70. [PubMed:12453049 ]
  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 ]
  4. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
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
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
agonist
General Function:
Clathrin light chain binding
Specific Function:
Interacts with clathrin light chain A and stimulates clathrin self-assembly and clathrin-mediated endocytosis.
Gene Name:
CALY
Uniprot ID:
Q9NYX4
Molecular Weight:
23433.49 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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23