Apomorphine
Identification
- Name
- Apomorphine
- Accession Number
- DB00714 (APRD00531, DB05816)
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Description
A 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.
- Structure
- 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 IDs
- APL-130277 / VR-040 / VR-400 / VR040
- Product Ingredients
Ingredient UNII CAS InChI Key Apomorphine hydrochloride F39049Y068 41372-20-7 CXWQXGNFZLHLHQ-DPFCLETOSA-N - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Apokyn Injection 30 mg/3mL Subcutaneous Us World Meds, Llc 2004-07-02 Not applicable US Apokyn Injection 30 mg/3mL Subcutaneous Tercica 2004-07-02 2018-01-06 US Movapo Solution 10 mg Subcutaneous Paladin Labs Inc 2017-09-07 Not applicable Canada Movapo Solution 10 mg Subcutaneous Paladin Labs Inc Not applicable Not applicable Canada - International/Other Brands
- Ixense (Takeda (discontinued)) / Spontane / Uprima (Abbott (discontinued))
- Categories
- Alkaloids
- Alpha2 Agonists
- Anti-Parkinson Agents (Dopamine Agonist)
- Anti-Parkinson Drugs
- Aporphines
- Autonomic Agents
- Benzylisoquinolines
- Central Nervous System Agents
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (weak)
- Cytochrome P-450 Enzyme Inhibitors
- Dopamine Agents
- Dopamine Agonists
- Emetics
- Gastrointestinal Agents
- Hypotensive Agents
- Isoquinolines
- Nervous System
- Neurotransmitter Agents
- Nonergot-derivative Dopamine Receptor Agonists
- Opiate Agonists
- Peripheral Nervous System Agents
- QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying)
- Serotonin 5-HT1 Receptor Agonists
- UNII
- N21FAR7B4S
- CAS number
- 58-00-4
- Weight
- Average: 267.3224
Monoisotopic: 267.125928793 - Chemical Formula
- C17H17NO2
- InChI Key
- VMWNQDUVQKEIOC-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][[email protected]]12CC3=C(C(O)=C(O)C=C3)C3=CC=CC(CCN1C)=C23
Pharmacology
- Indication
For 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
- Pharmacodynamics
Apomorphine 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 action
The 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.
Target Actions Organism AD(3) dopamine receptor agonistHuman AD(4) dopamine receptor agonistHuman AD(2) dopamine receptor agonistHuman UAlpha-2C adrenergic receptor agonistHuman UAlpha-2B adrenergic receptor agonistHuman U5-hydroxytryptamine receptor 2C agonistHuman UD(1B) dopamine receptor agonistHuman U5-hydroxytryptamine receptor 1A agonistHuman U5-hydroxytryptamine receptor 2A agonistHuman U5-hydroxytryptamine receptor 2B agonistHuman UAlpha-2A adrenergic receptor agonistHuman UD(1A) dopamine receptor agonistHuman U5-hydroxytryptamine receptor 1D agonistHuman U5-hydroxytryptamine receptor 1B agonistHuman UNeuron-specific vesicular protein calcyon agonistHuman - Absorption
100% following subcutaneous administration
- Volume of distribution
- 123 to 404 L
- Protein binding
~50%-albumin
- Metabolism
Hepatic
- Route of elimination
- Not Available
- Half life
40 minutes (range 30 - 60 minutes)
- Clearance
- 223 L/hr
- Toxicity
LD50=0.6 mmoles/kg (mice, intraperitoneal)
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Drug group 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline The metabolism of Apomorphine can be decreased when combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline. Experimental Acebutolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Acebutolol. Approved, Investigational Aldesleukin The risk or severity of adverse effects can be increased when Apomorphine is combined with Aldesleukin. Approved Aliskiren The risk or severity of adverse effects can be increased when Apomorphine is combined with Aliskiren. Approved, Investigational Alprenolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Alprenolol. Approved, Withdrawn Amifostine The risk or severity of adverse effects can be increased when Amifostine is combined with Apomorphine. Approved, Investigational Amiloride The risk or severity of adverse effects can be increased when Apomorphine is combined with Amiloride. Approved Amineptine Amineptine may decrease the antihypertensive activities of Apomorphine. Illicit, Withdrawn Amiodarone Apomorphine may increase the QTc-prolonging activities of Amiodarone. Approved, Investigational Amisulpride The therapeutic efficacy of Amisulpride can be decreased when used in combination with Apomorphine. Approved, Investigational Amitriptyline Amitriptyline may decrease the antihypertensive activities of Apomorphine. Approved Amlodipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Amlodipine. Approved Amobarbital Amobarbital may increase the hypotensive activities of Apomorphine. Approved, Illicit Amoxapine Amoxapine may decrease the antihypertensive activities of Apomorphine. Approved Amphetamine The metabolism of Apomorphine can be decreased when combined with Amphetamine. Approved, Illicit, Investigational Amphotericin B The risk or severity of adverse effects can be increased when Amphotericin B is combined with Apomorphine. Approved, Investigational Amyl Nitrite The risk or severity of adverse effects can be increased when Apomorphine is combined with Amyl Nitrite. Approved Anagrelide Apomorphine may increase the QTc-prolonging activities of Anagrelide. Approved Apraclonidine The risk or severity of adverse effects can be increased when Apomorphine is combined with Apraclonidine. Approved Aripiprazole Aripiprazole may increase the hypotensive activities of Apomorphine. Approved, Investigational Arotinolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Arotinolol. Investigational Arsenic trioxide Apomorphine may increase the QTc-prolonging activities of Arsenic trioxide. Approved, Investigational Artemether Apomorphine may increase the QTc-prolonging activities of Artemether. Approved Asenapine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Asenapine. Approved Atenolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Atenolol. Approved Azilsartan medoxomil The risk or severity of adverse effects can be increased when Apomorphine is combined with Azilsartan medoxomil. Approved, Investigational Azithromycin Apomorphine may increase the QTc-prolonging activities of Azithromycin. Approved Barbexaclone Barbexaclone may increase the hypotensive activities of Apomorphine. Experimental Barbital Barbital may increase the hypotensive activities of Apomorphine. Illicit Barnidipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Barnidipine. Approved Bedaquiline Apomorphine may increase the QTc-prolonging activities of Bedaquiline. Approved Befunolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Befunolol. Experimental Benazepril The risk or severity of adverse effects can be increased when Apomorphine is combined with Benazepril. Approved, Investigational Bendroflumethiazide The risk or severity of adverse effects can be increased when Apomorphine is combined with Bendroflumethiazide. Approved Benmoxin The metabolism of Apomorphine can be decreased when combined with Benmoxin. Withdrawn Bepridil The risk or severity of adverse effects can be increased when Apomorphine is combined with Bepridil. Approved, Withdrawn Betaxolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Betaxolol. Approved, Investigational Bevantolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Bevantolol. Approved Bisoprolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Bisoprolol. Approved Blonanserin The therapeutic efficacy of Apomorphine can be decreased when used in combination with Blonanserin. Approved, Investigational Bopindolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Bopindolol. Approved Bortezomib The risk or severity of adverse effects can be increased when Apomorphine is combined with Bortezomib. Approved, Investigational Bretylium The risk or severity of adverse effects can be increased when Apomorphine is combined with Bretylium. Approved Brimonidine The risk or severity of adverse effects can be increased when Apomorphine is combined with Brimonidine. Approved Brofaromine The metabolism of Apomorphine can be decreased when combined with Brofaromine. Experimental Bromocriptine Bromocriptine may increase the vasoconstricting activities of Apomorphine. Approved, Investigational Bucindolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Bucindolol. Investigational Bufuralol Apomorphine may increase the atrioventricular blocking (AV block) activities of Bufuralol. Experimental, Investigational Bumetanide The risk or severity of adverse effects can be increased when Apomorphine is combined with Bumetanide. Approved Bupivacaine The risk or severity of adverse effects can be increased when Apomorphine is combined with Bupivacaine. Approved, Investigational Bupranolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Bupranolol. Approved Bupropion The risk or severity of adverse effects can be increased when Apomorphine is combined with Bupropion. Approved Cabergoline Cabergoline may increase the vasoconstricting activities of Apomorphine. Approved Canagliflozin The risk or severity of adverse effects can be increased when Apomorphine is combined with Canagliflozin. Approved Candesartan cilexetil The risk or severity of adverse effects can be increased when Apomorphine is combined with Candesartan cilexetil. Approved Captopril The risk or severity of adverse effects can be increased when Apomorphine is combined with Captopril. Approved Carbetocin The risk or severity of adverse effects can be increased when Apomorphine is combined with Carbetocin. Approved, Investigational Cariprazine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Cariprazine. Approved, Investigational Caroxazone The metabolism of Apomorphine can be decreased when combined with Caroxazone. Withdrawn Carteolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Carteolol. Approved Carvedilol Apomorphine may increase the atrioventricular blocking (AV block) activities of Carvedilol. Approved, Investigational Celiprolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Celiprolol. Approved, Investigational Ceritinib Apomorphine may increase the QTc-prolonging activities of Ceritinib. Approved Chloroquine Apomorphine may increase the QTc-prolonging activities of Chloroquine. Approved, Investigational, Vet Approved Chlorothiazide The risk or severity of adverse effects can be increased when Apomorphine is combined with Chlorothiazide. Approved, Vet Approved Chlorpromazine The therapeutic efficacy of Chlorpromazine can be decreased when used in combination with Apomorphine. Approved, Investigational, Vet Approved Chlorprothixene The therapeutic efficacy of Chlorprothixene can be decreased when used in combination with Apomorphine. Approved, Investigational, Withdrawn Chlorthalidone The risk or severity of adverse effects can be increased when Apomorphine is combined with Chlorthalidone. Approved Cilazapril The risk or severity of adverse effects can be increased when Apomorphine is combined with Cilazapril. Approved Cilnidipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Cilnidipine. Approved, Investigational Ciprofloxacin Apomorphine may increase the QTc-prolonging activities of Ciprofloxacin. Approved, Investigational Cisapride Apomorphine may increase the QTc-prolonging activities of Cisapride. Approved, Investigational, Withdrawn Citalopram Apomorphine may increase the QTc-prolonging activities of Citalopram. Approved Clarithromycin Apomorphine may increase the QTc-prolonging activities of Clarithromycin. Approved Clevidipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Clevidipine. Approved, Investigational Clofarabine The risk or severity of adverse effects can be increased when Apomorphine is combined with Clofarabine. Approved, Investigational Clomipramine Clomipramine may decrease the antihypertensive activities of Apomorphine. Approved, Investigational, Vet Approved Clonidine The risk or severity of adverse effects can be increased when Apomorphine is combined with Clonidine. Approved Cloranolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Cloranolol. Experimental Clozapine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Clozapine. Approved Conivaptan The risk or severity of adverse effects can be increased when Apomorphine is combined with Conivaptan. Approved, Investigational Crizotinib Apomorphine may increase the QTc-prolonging activities of Crizotinib. Approved Cyclobenzaprine Cyclobenzaprine may decrease the antihypertensive activities of Apomorphine. Approved Dapagliflozin The risk or severity of adverse effects can be increased when Apomorphine is combined with Dapagliflozin. Approved Desflurane The risk or severity of adverse effects can be increased when Apomorphine is combined with Desflurane. Approved Desipramine Desipramine may decrease the antihypertensive activities of Apomorphine. Approved, Investigational Desvenlafaxine Desvenlafaxine may decrease the antihypertensive activities of Apomorphine. Approved, Investigational Dexmedetomidine The risk or severity of adverse effects can be increased when Apomorphine is combined with Dexmedetomidine. Approved, Vet Approved Dibenzepin Dibenzepin may decrease the antihypertensive activities of Apomorphine. Experimental Diclofenamide The risk or severity of adverse effects can be increased when Apomorphine is combined with Diclofenamide. Approved, Investigational Dihydroergotamine Dihydroergotamine may increase the vasoconstricting activities of Apomorphine. Approved, Investigational Diltiazem The risk or severity of adverse effects can be increased when Apomorphine is combined with Diltiazem. Approved, Investigational Dinutuximab The risk or severity of adverse effects can be increased when Apomorphine is combined with Dinutuximab. Approved, Investigational Dipyridamole The risk or severity of adverse effects can be increased when Apomorphine is combined with Dipyridamole. Approved Disopyramide Apomorphine may increase the QTc-prolonging activities of Disopyramide. Approved Dofetilide Apomorphine may increase the QTc-prolonging activities of Dofetilide. Approved, Investigational Dolasetron Dolasetron may increase the hypotensive activities of Apomorphine. Approved, Investigational Domperidone Apomorphine may increase the QTc-prolonging activities of Domperidone. Approved, Investigational, Vet Approved Dosulepin Dosulepin may decrease the antihypertensive activities of Apomorphine. Approved Doxazosin The risk or severity of adverse effects can be increased when Apomorphine is combined with Doxazosin. Approved Doxepin Doxepin may decrease the antihypertensive activities of Apomorphine. Approved, Investigational Dronedarone Apomorphine may increase the QTc-prolonging activities of Dronedarone. Approved Droperidol The therapeutic efficacy of Droperidol can be decreased when used in combination with Apomorphine. Approved, Vet Approved Droxidopa Apomorphine may increase the hypertensive activities of Droxidopa. Approved, Investigational Duloxetine Apomorphine may increase the orthostatic hypotensive activities of Duloxetine. Approved Efonidipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Efonidipine. Approved, Investigational Eliglustat Apomorphine may increase the QTc-prolonging activities of Eliglustat. Approved Empagliflozin The risk or severity of adverse effects can be increased when Apomorphine is combined with Empagliflozin. Approved Enalapril The risk or severity of adverse effects can be increased when Apomorphine is combined with Enalapril. Approved, Vet Approved Enalaprilat The risk or severity of adverse effects can be increased when Apomorphine is combined with Enalaprilat. Approved Epanolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Epanolol. Experimental Eplerenone The risk or severity of adverse effects can be increased when Apomorphine is combined with Eplerenone. Approved Epoprostenol The risk or severity of adverse effects can be increased when Apomorphine is combined with Epoprostenol. Approved Eprosartan The risk or severity of adverse effects can be increased when Apomorphine is combined with Eprosartan. Approved Ergoloid mesylate Ergoloid mesylate may increase the vasoconstricting activities of Apomorphine. Approved Ergonovine Ergonovine may increase the vasoconstricting activities of Apomorphine. Approved Ergotamine Ergotamine may increase the vasoconstricting activities of Apomorphine. Approved Erythromycin Apomorphine may increase the QTc-prolonging activities of Erythromycin. Approved, Investigational, Vet Approved Escitalopram Apomorphine may increase the QTc-prolonging activities of Escitalopram. Approved, Investigational Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Apomorphine. Investigational Esmolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Esmolol. Approved Etacrynic acid The risk or severity of adverse effects can be increased when Apomorphine is combined with Etacrynic acid. Approved, Investigational Felodipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Felodipine. Approved, Investigational Fenoldopam The risk or severity of adverse effects can be increased when Apomorphine is combined with Fenoldopam. Approved Fimasartan The risk or severity of adverse effects can be increased when Apomorphine is combined with Fimasartan. Approved, Investigational Flecainide Apomorphine may increase the QTc-prolonging activities of Flecainide. Approved, Withdrawn Fluoxetine Apomorphine may increase the QTc-prolonging activities of Fluoxetine. Approved, Vet Approved Flupentixol The therapeutic efficacy of Flupentixol can be decreased when used in combination with Apomorphine. Approved, Investigational, Withdrawn Fluphenazine The therapeutic efficacy of Fluphenazine can be decreased when used in combination with Apomorphine. Approved Fosinopril The risk or severity of adverse effects can be increased when Apomorphine is combined with Fosinopril. Approved Furazolidone The metabolism of Apomorphine can be decreased when combined with Furazolidone. Approved, Investigational, Vet Approved Furosemide The risk or severity of adverse effects can be increased when Apomorphine is combined with Furosemide. Approved, Vet Approved Gadobenic acid Apomorphine may increase the QTc-prolonging activities of Gadobenic acid. Approved, Investigational Gemifloxacin Apomorphine may increase the QTc-prolonging activities of Gemifloxacin. Approved, Investigational Goserelin Apomorphine may increase the QTc-prolonging activities of Goserelin. Approved Granisetron Granisetron may increase the hypotensive activities of Apomorphine. Approved, Investigational Guanfacine The risk or severity of adverse effects can be increased when Apomorphine is combined with Guanfacine. Approved, Investigational Haloperidol The therapeutic efficacy of Haloperidol can be decreased when used in combination with Apomorphine. Approved Halothane The risk or severity of adverse effects can be increased when Apomorphine is combined with Halothane. Approved, Vet Approved Harmaline The metabolism of Apomorphine can be decreased when combined with Harmaline. Experimental Hexobarbital Hexobarbital may increase the hypotensive activities of Apomorphine. Approved Hydracarbazine The metabolism of Apomorphine can be decreased when combined with Hydracarbazine. Experimental Hydralazine The risk or severity of adverse effects can be increased when Apomorphine is combined with Hydralazine. Approved Hydrochlorothiazide The risk or severity of adverse effects can be increased when Apomorphine is combined with Hydrochlorothiazide. Approved, Vet Approved Hydroflumethiazide The risk or severity of adverse effects can be increased when Apomorphine is combined with Hydroflumethiazide. Approved, Investigational Ibutilide Apomorphine may increase the QTc-prolonging activities of Ibutilide. Approved Iloperidone The therapeutic efficacy of Apomorphine can be decreased when used in combination with Iloperidone. Approved Iloprost The risk or severity of adverse effects can be increased when Apomorphine is combined with Iloprost. Approved, Investigational Imidapril The risk or severity of adverse effects can be increased when Apomorphine is combined with Imidapril. Investigational Imipramine Imipramine may decrease the antihypertensive activities of Apomorphine. Approved Indapamide The risk or severity of adverse effects can be increased when Apomorphine is combined with Indapamide. Approved Indenolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Indenolol. Withdrawn Indoramin The risk or severity of adverse effects can be increased when Apomorphine is combined with Indoramin. Withdrawn Iobenguane The therapeutic efficacy of Iobenguane can be decreased when used in combination with Apomorphine. Approved, Investigational Iprindole Iprindole may decrease the antihypertensive activities of Apomorphine. Experimental Iproclozide The metabolism of Apomorphine can be decreased when combined with Iproclozide. Withdrawn Iproniazid The metabolism of Apomorphine can be decreased when combined with Iproniazid. Withdrawn Irbesartan The risk or severity of adverse effects can be increased when Apomorphine is combined with Irbesartan. Approved, Investigational Isocarboxazid The metabolism of Apomorphine can be decreased when combined with Isocarboxazid. Approved Isoflurane The risk or severity of adverse effects can be increased when Apomorphine is combined with Isoflurane. Approved, Vet Approved Isosorbide Dinitrate The risk or severity of adverse effects can be increased when Apomorphine is combined with Isosorbide Dinitrate. Approved, Investigational Isosorbide Mononitrate The risk or severity of adverse effects can be increased when Apomorphine is combined with Isosorbide Mononitrate. Approved Isoxsuprine The risk or severity of adverse effects can be increased when Apomorphine is combined with Isoxsuprine. Approved, Withdrawn Isradipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Isradipine. Approved, Investigational Labetalol Apomorphine may increase the atrioventricular blocking (AV block) activities of Labetalol. Approved Lacidipine Apomorphine may increase the hypotensive activities of Lacidipine. Approved, Investigational Landiolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Landiolol. Investigational Lenvatinib Apomorphine may increase the QTc-prolonging activities of Lenvatinib. Approved, Investigational Lercanidipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Lercanidipine. Approved, Investigational Leuprolide Apomorphine may increase the QTc-prolonging activities of Leuprolide. Approved, Investigational Levobunolol The risk or severity of adverse effects can be increased when Apomorphine is combined with Levobunolol. Approved Levobupivacaine The risk or severity of adverse effects can be increased when Apomorphine is combined with Levobupivacaine. Approved, Investigational Levodopa Apomorphine may increase the orthostatic hypotensive activities of Levodopa. Approved Levofloxacin Apomorphine may increase the QTc-prolonging activities of Levofloxacin. Approved, Investigational Levomilnacipran Levomilnacipran may decrease the antihypertensive activities of Apomorphine. Approved, Investigational Levosimendan The risk or severity of adverse effects can be increased when Apomorphine is combined with Levosimendan. Approved, Investigational Lisinopril The risk or severity of adverse effects can be increased when Apomorphine is combined with Lisinopril. Approved, Investigational Lofepramine Lofepramine may decrease the antihypertensive activities of Apomorphine. Experimental Lofexidine The risk or severity of adverse effects can be increased when Apomorphine is combined with Lofexidine. Approved, Investigational Lopinavir Apomorphine may increase the QTc-prolonging activities of Lopinavir. Approved Losartan The risk or severity of adverse effects can be increased when Apomorphine is combined with Losartan. Approved Loxapine The therapeutic efficacy of Loxapine can be decreased when used in combination with Apomorphine. Approved Lumateperone The therapeutic efficacy of Apomorphine can be decreased when used in combination with Lumateperone. Investigational Lumefantrine Apomorphine may increase the QTc-prolonging activities of Lumefantrine. Approved Lurasidone The therapeutic efficacy of Apomorphine can be decreased when used in combination with Lurasidone. Approved, Investigational Mannitol The risk or severity of adverse effects can be increased when Apomorphine is combined with Mannitol. Approved, Investigational Mebanazine The metabolism of Apomorphine can be decreased when combined with Mebanazine. Withdrawn Mecamylamine The risk or severity of adverse effects can be increased when Apomorphine is combined with Mecamylamine. Approved, Investigational Melperone The therapeutic efficacy of Apomorphine can be decreased when used in combination with Melperone. Approved, Investigational Mepindolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Mepindolol. Experimental Mesoridazine The therapeutic efficacy of Mesoridazine can be decreased when used in combination with Apomorphine. Approved, Investigational Methadone Apomorphine may increase the QTc-prolonging activities of Methadone. Approved Methazolamide The risk or severity of adverse effects can be increased when Apomorphine is combined with Methazolamide. Approved Methohexital Methohexital may increase the hypotensive activities of Apomorphine. Approved Methotrimeprazine The therapeutic efficacy of Methotrimeprazine can be decreased when used in combination with Apomorphine. Approved, Investigational Methyclothiazide The risk or severity of adverse effects can be increased when Apomorphine is combined with Methyclothiazide. Approved Methyldopa The risk or severity of adverse effects can be increased when Apomorphine is combined with Methyldopa. Approved Methylene blue The metabolism of Apomorphine can be decreased when combined with Methylene blue. Approved, Investigational Methylergometrine Methylergometrine may increase the vasoconstricting activities of Apomorphine. Approved Methylphenidate The risk or severity of adverse effects can be increased when Methylphenidate is combined with Apomorphine. Approved, Investigational Methylphenobarbital Methylphenobarbital may increase the hypotensive activities of Apomorphine. Approved Metipranolol The risk or severity of adverse effects can be increased when Apomorphine is combined with Metipranolol. Approved Metoclopramide The therapeutic efficacy of Apomorphine can be decreased when used in combination with Metoclopramide. Approved, Investigational Metolazone The risk or severity of adverse effects can be increased when Apomorphine is combined with Metolazone. Approved Metoprolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Metoprolol. Approved, Investigational Mianserin The therapeutic efficacy of Apomorphine can be decreased when used in combination with Mianserin. Approved, Investigational Mifepristone Mifepristone may increase the QTc-prolonging activities of Apomorphine. Approved, Investigational Milnacipran Milnacipran may decrease the antihypertensive activities of Apomorphine. Approved, Investigational Minaprine The metabolism of Apomorphine can be decreased when combined with Minaprine. Approved Minoxidil The risk or severity of adverse effects can be increased when Apomorphine is combined with Minoxidil. Approved, Investigational Mirtazapine Mirtazapine may decrease the antihypertensive activities of Apomorphine. Approved Moclobemide The metabolism of Apomorphine can be decreased when combined with Moclobemide. Approved, Investigational Moexipril The risk or severity of adverse effects can be increased when Apomorphine is combined with Moexipril. Approved Molindone The therapeutic efficacy of Molindone can be decreased when used in combination with Apomorphine. Approved Morphine The risk or severity of adverse effects can be increased when Apomorphine is combined with Morphine. Approved, Investigational Moxifloxacin Apomorphine may increase the QTc-prolonging activities of Moxifloxacin. Approved, Investigational Moxonidine The risk or severity of adverse effects can be increased when Apomorphine is combined with Moxonidine. Approved, Investigational Nabilone The risk or severity of adverse effects can be increased when Apomorphine is combined with Nabilone. Approved, Investigational Nadolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Nadolol. Approved Nebivolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Nebivolol. Approved, Investigational Nesiritide The risk or severity of adverse effects can be increased when Apomorphine is combined with Nesiritide. Approved, Investigational Nialamide The metabolism of Apomorphine can be decreased when combined with Nialamide. Withdrawn Nicardipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Nicardipine. Approved, Investigational Nicorandil Nicorandil may increase the hypotensive activities of Apomorphine. Approved, Investigational Nifedipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Nifedipine. Approved Nilotinib Apomorphine may increase the QTc-prolonging activities of Nilotinib. Approved, Investigational Nilvadipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Nilvadipine. Approved, Investigational Nimodipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Nimodipine. Approved, Investigational Nisoldipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Nisoldipine. Approved Nitrendipine The risk or severity of adverse effects can be increased when Apomorphine is combined with Nitrendipine. Approved, Investigational Nitric Oxide The risk or severity of adverse effects can be increased when Apomorphine is combined with Nitric Oxide. Approved Nitroglycerin The risk or severity of adverse effects can be increased when Apomorphine is combined with Nitroglycerin. Approved, Investigational Nitroprusside The risk or severity of adverse effects can be increased when Apomorphine is combined with Nitroprusside. Approved, Investigational Nitrous acid The risk or severity of adverse effects can be increased when Apomorphine is combined with Nitrous acid. Approved, Investigational Nortriptyline Nortriptyline may decrease the antihypertensive activities of Apomorphine. Approved Obinutuzumab The risk or severity of adverse effects can be increased when Apomorphine is combined with Obinutuzumab. Approved, Investigational Octamoxin The metabolism of Apomorphine can be decreased when combined with Octamoxin. Withdrawn Ofloxacin Apomorphine may increase the QTc-prolonging activities of Ofloxacin. Approved Olanzapine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Olanzapine. Approved, Investigational Olmesartan The risk or severity of adverse effects can be increased when Apomorphine is combined with Olmesartan. Approved, Investigational Ondansetron Ondansetron may increase the hypotensive activities of Apomorphine. Approved Opipramol Opipramol may decrease the antihypertensive activities of Apomorphine. Investigational Oxprenolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Oxprenolol. Approved Paclitaxel The risk or severity of adverse effects can be increased when Apomorphine is combined with Paclitaxel. Approved, Vet Approved Paliperidone The therapeutic efficacy of Apomorphine can be decreased when used in combination with Paliperidone. Approved Palonosetron Palonosetron may increase the hypotensive activities of Apomorphine. Approved, Investigational Panobinostat Apomorphine may increase the QTc-prolonging activities of Panobinostat. Approved, Investigational Papaverine The risk or severity of adverse effects can be increased when Apomorphine is combined with Papaverine. Approved, Investigational Pargyline The metabolism of Apomorphine can be decreased when combined with Pargyline. Approved Pazopanib Apomorphine may increase the QTc-prolonging activities of Pazopanib. Approved Penbutolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Penbutolol. Approved, Investigational Pentamidine Apomorphine may increase the QTc-prolonging activities of Pentamidine. Approved, Investigational Pentobarbital Pentobarbital may increase the hypotensive activities of Apomorphine. Approved, Investigational, Vet Approved Perflutren Apomorphine may increase the QTc-prolonging activities of Perflutren. Approved Perindopril The risk or severity of adverse effects can be increased when Apomorphine is combined with Perindopril. Approved Perospirone The therapeutic efficacy of Apomorphine can be decreased when used in combination with Perospirone. Approved Perphenazine The therapeutic efficacy of Perphenazine can be decreased when used in combination with Apomorphine. Approved Phenelzine The metabolism of Apomorphine can be decreased when combined with Phenelzine. Approved Pheniprazine The metabolism of Apomorphine can be decreased when combined with Pheniprazine. Withdrawn Phenobarbital Phenobarbital may increase the hypotensive activities of Apomorphine. Approved, Investigational Phenoxybenzamine The risk or severity of adverse effects can be increased when Apomorphine is combined with Phenoxybenzamine. Approved Phenoxypropazine The metabolism of Apomorphine can be decreased when combined with Phenoxypropazine. Withdrawn Phentolamine The risk or severity of adverse effects can be increased when Apomorphine is combined with Phentolamine. Approved Pimavanserin The therapeutic efficacy of Apomorphine can be decreased when used in combination with Pimavanserin. Approved, Investigational Pimozide The therapeutic efficacy of Pimozide can be decreased when used in combination with Apomorphine. Approved Pindolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Pindolol. Approved, Investigational Pipamperone The risk or severity of adverse effects can be increased when Apomorphine is combined with Pipamperone. Approved, Investigational Pirlindole The metabolism of Apomorphine can be decreased when combined with Pirlindole. Approved Pivhydrazine The metabolism of Apomorphine can be decreased when combined with Pivhydrazine. Withdrawn Platelet Activating Factor Apomorphine may increase the atrioventricular blocking (AV block) activities of Platelet Activating Factor. Experimental Practolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Practolol. Approved Pramipexole The risk or severity of adverse effects can be increased when Apomorphine is combined with Pramipexole. Approved, Investigational Prazosin The risk or severity of adverse effects can be increased when Apomorphine is combined with Prazosin. Approved Primaquine Apomorphine may increase the QTc-prolonging activities of Primaquine. Approved Primidone Primidone may increase the hypotensive activities of Apomorphine. Approved, Vet Approved Procainamide Apomorphine may increase the QTc-prolonging activities of Procainamide. Approved Procarbazine The metabolism of Apomorphine can be decreased when combined with Procarbazine. Approved, Investigational Prochlorperazine The therapeutic efficacy of Prochlorperazine can be decreased when used in combination with Apomorphine. Approved, Vet Approved Promazine The therapeutic efficacy of Promazine can be decreased when used in combination with Apomorphine. Approved, Vet Approved Propafenone Apomorphine may increase the QTc-prolonging activities of Propafenone. Approved Propericiazine The therapeutic efficacy of Propericiazine can be decreased when used in combination with Apomorphine. Approved, Investigational Propofol The risk or severity of adverse effects can be increased when Apomorphine is combined with Propofol. Approved, Investigational, Vet Approved Propranolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Propranolol. Approved, Investigational Protriptyline Protriptyline may decrease the antihypertensive activities of Apomorphine. Approved Quetiapine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Quetiapine. Approved Quinapril The risk or severity of adverse effects can be increased when Apomorphine is combined with Quinapril. Approved, Investigational Quinidine Apomorphine may increase the QTc-prolonging activities of Quinidine. Approved, Investigational Quinine Apomorphine may increase the QTc-prolonging activities of Quinine. Approved Ramipril The risk or severity of adverse effects can be increased when Apomorphine is combined with Ramipril. Approved Rasagiline The metabolism of Apomorphine can be decreased when combined with Rasagiline. Approved Remifentanil The risk or severity of adverse effects can be increased when Apomorphine is combined with Remifentanil. Approved Reserpine The risk or severity of adverse effects can be increased when Apomorphine is combined with Reserpine. Approved, Investigational Riociguat The risk or severity of adverse effects can be increased when Apomorphine is combined with Riociguat. Approved Risperidone Apomorphine may increase the hypotensive activities of Risperidone. Approved, Investigational Ropinirole The risk or severity of adverse effects can be increased when Apomorphine is combined with Ropinirole. Approved, Investigational Ropivacaine The risk or severity of adverse effects can be increased when Apomorphine is combined with Ropivacaine. Approved Rotigotine The risk or severity of adverse effects can be increased when Apomorphine is combined with Rotigotine. Approved RP5063 The therapeutic efficacy of Apomorphine can be decreased when used in combination with RP5063. Investigational Sacubitril The risk or severity of adverse effects can be increased when Apomorphine is combined with Sacubitril. Approved Safrazine The metabolism of Apomorphine can be decreased when combined with Safrazine. Withdrawn Saquinavir Apomorphine may increase the QTc-prolonging activities of Saquinavir. Approved, Investigational Secobarbital Secobarbital may increase the hypotensive activities of Apomorphine. Approved, Vet Approved Selegiline The metabolism of Apomorphine can be decreased when combined with Selegiline. Approved, Investigational, Vet Approved Sertindole The therapeutic efficacy of Apomorphine can be decreased when used in combination with Sertindole. Approved, Investigational, Withdrawn Sevoflurane The risk or severity of adverse effects can be increased when Apomorphine is combined with Sevoflurane. Approved, Vet Approved Sotalol Apomorphine may increase the atrioventricular blocking (AV block) activities of Sotalol. Approved Spironolactone The risk or severity of adverse effects can be increased when Apomorphine is combined with Spironolactone. Approved Streptokinase The risk or severity of adverse effects can be increased when Apomorphine is combined with Streptokinase. Approved, Investigational Sufentanil The risk or severity of adverse effects can be increased when Apomorphine is combined with Sufentanil. Approved, Investigational Sulfisoxazole Apomorphine may increase the QTc-prolonging activities of Sulfisoxazole. Approved, Vet Approved Talinolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Talinolol. Investigational Tamsulosin The risk or severity of adverse effects can be increased when Apomorphine is combined with Tamsulosin. Approved, Investigational Telavancin Apomorphine may increase the QTc-prolonging activities of Telavancin. Approved Telithromycin Apomorphine may increase the QTc-prolonging activities of Telithromycin. Approved Telmisartan The risk or severity of adverse effects can be increased when Apomorphine is combined with Telmisartan. Approved, Investigational Terazosin The risk or severity of adverse effects can be increased when Apomorphine is combined with Terazosin. Approved Tertatolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Tertatolol. Experimental Tetrabenazine Apomorphine may increase the QTc-prolonging activities of Tetrabenazine. Approved, Investigational Thalidomide The risk or severity of adverse effects can be increased when Apomorphine is combined with Thalidomide. Approved, Investigational, Withdrawn Thiamylal Thiamylal may increase the hypotensive activities of Apomorphine. Approved, Vet Approved Thiopental Thiopental may increase the hypotensive activities of Apomorphine. Approved, Vet Approved Thioproperazine The therapeutic efficacy of Thioproperazine can be decreased when used in combination with Apomorphine. Approved Thioridazine The therapeutic efficacy of Thioridazine can be decreased when used in combination with Apomorphine. Approved, Withdrawn Thiothixene The therapeutic efficacy of Thiothixene can be decreased when used in combination with Apomorphine. Approved Tianeptine Tianeptine may decrease the antihypertensive activities of Apomorphine. Approved, Investigational Timolol Apomorphine may increase the atrioventricular blocking (AV block) activities of Timolol. Approved Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Apomorphine. Approved, Investigational Tolazoline The risk or severity of adverse effects can be increased when Apomorphine is combined with Tolazoline. Approved, Vet Approved Tolcapone The risk or severity of adverse effects can be increased when Apomorphine is combined with Tolcapone. Approved, Withdrawn Toloxatone The metabolism of Apomorphine can be decreased when combined with Toloxatone. Approved Torasemide The risk or severity of adverse effects can be increased when Apomorphine is combined with Torasemide. Approved Toremifene Apomorphine may increase the QTc-prolonging activities of Toremifene. Approved, Investigational Trandolapril The risk or severity of adverse effects can be increased when Apomorphine is combined with Trandolapril. Approved Tranylcypromine The metabolism of Apomorphine can be decreased when combined with Tranylcypromine. Approved, Investigational Tretinoin The risk or severity of adverse effects can be increased when Apomorphine is combined with Tretinoin. Approved, Investigational, Nutraceutical Triamterene The risk or severity of adverse effects can be increased when Apomorphine is combined with Triamterene. Approved Trifluoperazine The therapeutic efficacy of Trifluoperazine can be decreased when used in combination with Apomorphine. Approved, Investigational Trimipramine Trimipramine may decrease the antihypertensive activities of Apomorphine. Approved Tropisetron Tropisetron may increase the hypotensive activities of Apomorphine. Approved, Investigational Valsartan The risk or severity of adverse effects can be increased when Apomorphine is combined with Valsartan. Approved, Investigational Vandetanib Apomorphine may increase the QTc-prolonging activities of Vandetanib. Approved Vemurafenib Apomorphine may increase the QTc-prolonging activities of Vemurafenib. Approved Venlafaxine Venlafaxine may decrease the antihypertensive activities of Apomorphine. Approved Verapamil The risk or severity of adverse effects can be increased when Apomorphine is combined with Verapamil. Approved Ziprasidone The therapeutic efficacy of Apomorphine can be decreased when used in combination with Ziprasidone. Approved Zotepine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Zotepine. Approved, Investigational, Withdrawn Zuclopenthixol The therapeutic efficacy of Zuclopenthixol can be decreased when used in combination with Apomorphine. Approved, Investigational - Food Interactions
- Not Available
References
- Synthesis Reference
Narayanasamy Gurusamy, "Process for Making Apomorphine and Apocodeine." U.S. Patent US20100228032, issued September 09, 2010.
US20100228032- General References
- 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]
- SCHWAB RS, AMADOR LV, LETTVIN JY: Apomorphine in Parkinson's disease. Trans Am Neurol Assoc. 1951;56:251-3. [PubMed:14913646]
- 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]
- 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]
- Chaudhuri KR, Clough C: Subcutaneous apomorphine in Parkinson's disease. BMJ. 1998 Feb 28;316(7132):641. [PubMed:9522772]
- External Links
- Human Metabolome Database
- HMDB0014852
- KEGG Drug
- D07460
- PubChem Compound
- 6005
- PubChem Substance
- 46508653
- ChemSpider
- 5783
- BindingDB
- 50001955
- ChEBI
- 48538
- ChEMBL
- CHEMBL53
- Therapeutic Targets Database
- DAP000281
- PharmGKB
- PA164781163
- IUPHAR
- 33
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Apomorphine
- ATC Codes
- G04BE07 — Apomorphine
- G04BE — Drugs used in erectile dysfunction
- G04B — UROLOGICALS
- G04 — UROLOGICALS
- G — GENITO URINARY SYSTEM AND SEX HORMONES
- AHFS Codes
- 28:36.20.08 — Nonergot-derivative Dopamine Receptor Agonists
- 28:08.08 — Opiate Agonists
- FDA label
- Download (513 KB)
- MSDS
- Download (25.8 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Ipsen biopharm ltd
- Packagers
- Ipsen Pharmaceuticals Inc.
- Tercica Inc.
- Vetter Pharma Fertigung GmbH and Co. KG
- Dosage forms
Form Route Strength Injection Subcutaneous 30 mg/3mL Solution Subcutaneous 10 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 1.66E+004 mg/L Not Available logP 3.1 Not Available pKa 8.92 Not Available - Predicted Properties
Property Value Source Water Solubility 0.51 mg/mL ALOGPS logP 2.51 ALOGPS logP 2.87 ChemAxon logS -2.7 ALOGPS pKa (Strongest Acidic) 6.58 ChemAxon pKa (Strongest Basic) 13.25 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 43.7 Å2 ChemAxon Rotatable Bond Count 0 ChemAxon Refractivity 79.99 m3·mol-1 ChemAxon Polarizability 29.7 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9816 Blood Brain Barrier + 0.9401 Caco-2 permeable + 0.777 P-glycoprotein substrate Substrate 0.8501 P-glycoprotein inhibitor I Non-inhibitor 0.8781 P-glycoprotein inhibitor II Non-inhibitor 0.964 Renal organic cation transporter Inhibitor 0.6477 CYP450 2C9 substrate Non-substrate 0.7577 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.7039 CYP450 1A2 substrate Inhibitor 0.9107 CYP450 2C9 inhibitor Non-inhibitor 0.9146 CYP450 2D6 inhibitor Non-inhibitor 0.9084 CYP450 2C19 inhibitor Non-inhibitor 0.8718 CYP450 3A4 inhibitor Non-inhibitor 0.9156 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9262 Ames test AMES toxic 0.6775 Carcinogenicity Non-carcinogens 0.9736 Biodegradation Not ready biodegradable 0.8928 Rat acute toxicity 2.6446 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6544 hERG inhibition (predictor II) Inhibitor 0.7734
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Taxonomy
- Description
- This 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.
- Kingdom
- Organic compounds
- Super Class
- Alkaloids and derivatives
- Class
- Aporphines
- Sub Class
- Not Available
- Direct Parent
- Aporphines
- Alternative Parents
- Phenanthrenes and derivatives / Benzoquinolines / Naphthols and derivatives / Tetrahydroisoquinolines / Aralkylamines / 1-hydroxy-4-unsubstituted benzenoids / 1-hydroxy-2-unsubstituted benzenoids / Trialkylamines / Azacyclic compounds / Organopnictogen compounds show 2 more
- Substituents
- Aporphine / Benzoquinoline / Phenanthrene / 2-naphthol / 1-naphthol / Naphthalene / Quinoline / Tetrahydroisoquinoline / 1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid show 14 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- isoquinoline alkaloid, isoquinolines (CHEBI:48538)
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
- Uniprot Name
- D(3) dopamine receptor
- Molecular Weight
- 44224.335 Da
References
- 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 ...
- Gene Name
- DRD4
- Uniprot ID
- P21917
- Uniprot Name
- D(4) dopamine receptor
- Molecular Weight
- 48359.86 Da
References
- 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]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- 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]
- 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]
- 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]
- 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]
- 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
- Uniprot Name
- D(2) dopamine receptor
- Molecular Weight
- 50618.91 Da
References
- 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]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- 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]
- 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]
- Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988]
- 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]
- 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]
- 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
- Uniprot Name
- Alpha-2C adrenergic receptor
- Molecular Weight
- 49521.585 Da
References
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Epinephrine binding
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
- Gene Name
- ADRA2B
- Uniprot ID
- P18089
- Uniprot Name
- Alpha-2B adrenergic receptor
- Molecular Weight
- 49565.8 Da
References
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
- Gene Name
- HTR2C
- Uniprot ID
- P28335
- Uniprot Name
- 5-hydroxytryptamine receptor 2C
- Molecular Weight
- 51820.705 Da
References
- 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
- Uniprot Name
- D(1B) dopamine receptor
- Molecular Weight
- 52950.5 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- 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
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Virus receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
- Gene Name
- HTR2A
- Uniprot ID
- P28223
- Uniprot Name
- 5-hydroxytryptamine receptor 2A
- Molecular Weight
- 52602.58 Da
References
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation...
- Gene Name
- HTR2B
- Uniprot ID
- P41595
- Uniprot Name
- 5-hydroxytryptamine receptor 2B
- Molecular Weight
- 54297.41 Da
References
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Thioesterase binding
- Specific Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
- Gene Name
- ADRA2A
- Uniprot ID
- P08913
- Uniprot Name
- Alpha-2A adrenergic receptor
- Molecular Weight
- 48956.275 Da
References
- 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
- Uniprot Name
- D(1A) dopamine receptor
- Molecular Weight
- 49292.765 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- 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]
- 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]
- 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 subst...
- Gene Name
- HTR1D
- Uniprot ID
- P28221
- Uniprot Name
- 5-hydroxytryptamine receptor 1D
- Molecular Weight
- 41906.38 Da
References
- Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Serotonin receptor activity
- Specific Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
- Gene Name
- HTR1B
- Uniprot ID
- P28222
- Uniprot Name
- 5-hydroxytryptamine receptor 1B
- Molecular Weight
- 43567.535 Da
References
- 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
- Uniprot Name
- Neuron-specific vesicular protein calcyon
- Molecular Weight
- 23433.49 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Enzymes
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
Drug created on June 13, 2005 07:24 / Updated on April 23, 2018 23:02