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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
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 KeyInChIKey=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][C@]12CC3=C(C(O)=C(O)C=C3)C3=CC=CC(CCN1C)=C23
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
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.
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.
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
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
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
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)
Interactions
Drug Interactions
Drug
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.
AcebutololApomorphine may increase the atrioventricular blocking (AV block) activities of Acebutolol.
AlprenololApomorphine may increase the atrioventricular blocking (AV block) activities of Alprenolol.
AmineptineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Amineptine.
AmiodaroneApomorphine may increase the QTc-prolonging activities of Amiodarone.
AmitriptylineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Amitriptyline.
AnagrelideApomorphine may increase the QTc-prolonging activities of Anagrelide.
ArotinololApomorphine may increase the atrioventricular blocking (AV block) activities of Arotinolol.
Arsenic trioxideApomorphine may increase the QTc-prolonging activities of Arsenic trioxide.
ArtemetherApomorphine may increase the QTc-prolonging activities of Artemether.
AsenapineApomorphine may increase the QTc-prolonging activities of Asenapine.
AtenololApomorphine may increase the atrioventricular blocking (AV block) activities of Atenolol.
AzithromycinApomorphine may increase the QTc-prolonging activities of Azithromycin.
BedaquilineApomorphine may increase the QTc-prolonging activities of Bedaquiline.
BefunololApomorphine may increase the atrioventricular blocking (AV block) activities of Befunolol.
BenmoxinThe metabolism of Apomorphine can be decreased when combined with Benmoxin.
BetaxololApomorphine may increase the atrioventricular blocking (AV block) activities of Betaxolol.
BevantololApomorphine may increase the atrioventricular blocking (AV block) activities of Bevantolol.
BisoprololApomorphine may increase the atrioventricular blocking (AV block) activities of Bisoprolol.
BopindololApomorphine may increase the atrioventricular blocking (AV block) activities of Bopindolol.
BromocriptineBromocriptine may increase the vasoconstricting activities of Apomorphine.
BufuralolApomorphine may increase the atrioventricular blocking (AV block) activities of Bufuralol.
BupranololApomorphine may increase the atrioventricular blocking (AV block) activities of Bupranolol.
CabergolineCabergoline may increase the vasoconstricting activities of Apomorphine.
CaroxazoneThe metabolism of Apomorphine can be decreased when combined with Caroxazone.
CarteololApomorphine may increase the atrioventricular blocking (AV block) activities of Carteolol.
CarvedilolApomorphine may increase the atrioventricular blocking (AV block) activities of Carvedilol.
CeliprololApomorphine may increase the atrioventricular blocking (AV block) activities of Celiprolol.
CeritinibApomorphine may increase the QTc-prolonging activities of Ceritinib.
ChloroquineApomorphine may increase the QTc-prolonging activities of Chloroquine.
ChlorpromazineApomorphine may increase the QTc-prolonging activities of Chlorpromazine.
CiprofloxacinApomorphine may increase the QTc-prolonging activities of Ciprofloxacin.
CisaprideApomorphine may increase the QTc-prolonging activities of Cisapride.
CitalopramApomorphine may increase the QTc-prolonging activities of Citalopram.
ClarithromycinApomorphine may increase the QTc-prolonging activities of Clarithromycin.
ClomipramineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Clomipramine.
ClozapineApomorphine may increase the QTc-prolonging activities of Clozapine.
CrizotinibApomorphine may increase the QTc-prolonging activities of Crizotinib.
CyclobenzaprineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Cyclobenzaprine.
DesipramineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Desipramine.
DesvenlafaxineDesvenlafaxine may decrease the antihypertensive activities of Apomorphine.
DihydroergotamineDihydroergotamine may increase the vasoconstricting activities of Apomorphine.
DisopyramideApomorphine may increase the QTc-prolonging activities of Disopyramide.
DofetilideApomorphine may increase the QTc-prolonging activities of Dofetilide.
DolasetronDolasetron may increase the hypotensive activities of Apomorphine.
DolasetronApomorphine may increase the QTc-prolonging activities of Dolasetron.
DomperidoneApomorphine may increase the QTc-prolonging activities of Domperidone.
DosulepinThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Dosulepin.
DoxepinThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Doxepin.
DronedaroneApomorphine may increase the QTc-prolonging activities of Dronedarone.
DroperidolApomorphine may increase the QTc-prolonging activities of Droperidol.
DroxidopaApomorphine may increase the hypertensive activities of Droxidopa.
DuloxetineDuloxetine may decrease the antihypertensive activities of Apomorphine.
EliglustatApomorphine may increase the QTc-prolonging activities of Eliglustat.
Ergoloid mesylateErgoloid mesylate may increase the vasoconstricting activities of Apomorphine.
ErgonovineErgonovine may increase the vasoconstricting activities of Apomorphine.
ErgotamineErgotamine may increase the vasoconstricting activities of Apomorphine.
ErythromycinApomorphine may increase the QTc-prolonging activities of Erythromycin.
EscitalopramApomorphine may increase the QTc-prolonging activities of Escitalopram.
EsmirtazapineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Esmirtazapine.
EsmololApomorphine may increase the atrioventricular blocking (AV block) activities of Esmolol.
FlecainideApomorphine may increase the QTc-prolonging activities of Flecainide.
FluoxetineApomorphine may increase the QTc-prolonging activities of Fluoxetine.
FlupentixolApomorphine may increase the QTc-prolonging activities of Flupentixol.
FurazolidoneThe metabolism of Apomorphine can be decreased when combined with Furazolidone.
Gadobenic acidApomorphine may increase the QTc-prolonging activities of Gadobenic acid.
GemifloxacinApomorphine may increase the QTc-prolonging activities of Gemifloxacin.
GoserelinApomorphine may increase the QTc-prolonging activities of Goserelin.
GranisetronGranisetron may increase the hypotensive activities of Apomorphine.
GranisetronApomorphine may increase the QTc-prolonging activities of Granisetron.
HaloperidolApomorphine may increase the QTc-prolonging activities of Haloperidol.
HydracarbazineThe metabolism of Apomorphine can be decreased when combined with Hydracarbazine.
IbutilideApomorphine may increase the QTc-prolonging activities of Ibutilide.
IloperidoneApomorphine may increase the QTc-prolonging activities of Iloperidone.
ImipramineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Imipramine.
IndenololApomorphine may increase the atrioventricular blocking (AV block) activities of Indenolol.
IproclozideThe metabolism of Apomorphine can be decreased when combined with Iproclozide.
IproniazidThe metabolism of Apomorphine can be decreased when combined with Iproniazid.
IsocarboxazidThe metabolism of Apomorphine can be decreased when combined with Isocarboxazid.
LabetalolApomorphine may increase the atrioventricular blocking (AV block) activities of Labetalol.
LenvatinibApomorphine may increase the QTc-prolonging activities of Lenvatinib.
LeuprolideApomorphine may increase the QTc-prolonging activities of Leuprolide.
LevofloxacinApomorphine may increase the QTc-prolonging activities of Levofloxacin.
LevomilnacipranLevomilnacipran may decrease the antihypertensive activities of Apomorphine.
LopinavirApomorphine may increase the QTc-prolonging activities of Lopinavir.
LumefantrineApomorphine may increase the QTc-prolonging activities of Lumefantrine.
MebanazineThe metabolism of Apomorphine can be decreased when combined with Mebanazine.
MethadoneApomorphine may increase the QTc-prolonging activities of Methadone.
Methylene blueThe metabolism of Apomorphine can be decreased when combined with Methylene blue.
MetoprololApomorphine may increase the atrioventricular blocking (AV block) activities of Metoprolol.
MianserinThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Mianserin.
MifepristoneMifepristone may increase the QTc-prolonging activities of Apomorphine.
MilnacipranMilnacipran may decrease the antihypertensive activities of Apomorphine.
MinaprineThe metabolism of Apomorphine can be decreased when combined with Minaprine.
MirtazapineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Mirtazapine.
MoclobemideThe metabolism of Apomorphine can be decreased when combined with Moclobemide.
MoxifloxacinApomorphine may increase the QTc-prolonging activities of Moxifloxacin.
NadololApomorphine may increase the atrioventricular blocking (AV block) activities of Nadolol.
NialamideThe metabolism of Apomorphine can be decreased when combined with Nialamide.
NilotinibApomorphine may increase the QTc-prolonging activities of Nilotinib.
NortriptylineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Nortriptyline.
OctamoxinThe metabolism of Apomorphine can be decreased when combined with Octamoxin.
OfloxacinApomorphine may increase the QTc-prolonging activities of Ofloxacin.
OndansetronOndansetron may increase the hypotensive activities of Apomorphine.
OndansetronApomorphine may increase the QTc-prolonging activities of Ondansetron.
OxprenololApomorphine may increase the atrioventricular blocking (AV block) activities of Oxprenolol.
PaliperidoneApomorphine may increase the QTc-prolonging activities of Paliperidone.
PalonosetronPalonosetron may increase the hypotensive activities of Apomorphine.
PanobinostatApomorphine may increase the QTc-prolonging activities of Panobinostat.
PargylineThe metabolism of Apomorphine can be decreased when combined with Pargyline.
PazopanibApomorphine may increase the QTc-prolonging activities of Pazopanib.
PenbutololApomorphine may increase the atrioventricular blocking (AV block) activities of Penbutolol.
PentamidineApomorphine may increase the QTc-prolonging activities of Pentamidine.
PerflutrenApomorphine may increase the QTc-prolonging activities of Perflutren.
PhenelzineThe metabolism of Apomorphine can be decreased when combined with Phenelzine.
PheniprazineThe metabolism of Apomorphine can be decreased when combined with Pheniprazine.
PhenoxypropazineThe metabolism of Apomorphine can be decreased when combined with Phenoxypropazine.
PimozideApomorphine may increase the QTc-prolonging activities of Pimozide.
PindololApomorphine may increase the atrioventricular blocking (AV block) activities of Pindolol.
PirlindoleThe metabolism of Apomorphine can be decreased when combined with Pirlindole.
PivhydrazineThe metabolism of Apomorphine can be decreased when combined with Pivhydrazine.
PractololApomorphine may increase the atrioventricular blocking (AV block) activities of Practolol.
PrimaquineApomorphine may increase the QTc-prolonging activities of Primaquine.
ProcainamideApomorphine may increase the QTc-prolonging activities of Procainamide.
PromazineApomorphine may increase the QTc-prolonging activities of Promazine.
PropafenoneApomorphine may increase the QTc-prolonging activities of Propafenone.
PropranololApomorphine may increase the atrioventricular blocking (AV block) activities of Propranolol.
ProtriptylineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Protriptyline.
QuetiapineApomorphine may increase the QTc-prolonging activities of Quetiapine.
QuinidineApomorphine may increase the QTc-prolonging activities of Quinidine.
QuinineApomorphine may increase the QTc-prolonging activities of Quinine.
RasagilineThe metabolism of Apomorphine can be decreased when combined with Rasagiline.
SafrazineThe metabolism of Apomorphine can be decreased when combined with Safrazine.
SaquinavirApomorphine may increase the QTc-prolonging activities of Saquinavir.
SelegilineThe metabolism of Apomorphine can be decreased when combined with Selegiline.
SotalolApomorphine may increase the atrioventricular blocking (AV block) activities of Sotalol.
SulfisoxazoleApomorphine may increase the QTc-prolonging activities of Sulfisoxazole.
TelavancinApomorphine may increase the QTc-prolonging activities of Telavancin.
TelithromycinApomorphine may increase the QTc-prolonging activities of Telithromycin.
TetrabenazineApomorphine may increase the QTc-prolonging activities of Tetrabenazine.
ThioridazineApomorphine may increase the QTc-prolonging activities of Thioridazine.
TianeptineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Tianeptine.
TimololApomorphine may increase the atrioventricular blocking (AV block) activities of Timolol.
ToloxatoneThe metabolism of Apomorphine can be decreased when combined with Toloxatone.
ToremifeneApomorphine may increase the QTc-prolonging activities of Toremifene.
Trans-2-PhenylcyclopropylamineThe metabolism of Apomorphine can be decreased when combined with Trans-2-Phenylcyclopropylamine.
TranylcypromineThe metabolism of Apomorphine can be decreased when combined with Tranylcypromine.
TrimipramineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Trimipramine.
VandetanibApomorphine may increase the QTc-prolonging activities of Vandetanib.
VemurafenibApomorphine may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineVenlafaxine may decrease the antihypertensive activities of Apomorphine.
ZiprasidoneApomorphine may increase the QTc-prolonging activities of Ziprasidone.
ZuclopenthixolApomorphine may increase the QTc-prolonging activities of Zuclopenthixol.
Food InteractionsNot Available

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