Identification

Name
Apomorphine
Accession Number
DB00714
Description

Apomorphine is a non-ergoline dopamine D2 agonist indicated to treat hypomobility associated with Parkinson's. It was first synthesized in 1845 and first used in Parkinson's disease in 1884.10 Apomorphine has also been investigated as an emetic, a sedative, a treatment for alcoholism, and a treatment of other movement disorders.9,10

Apomorphine was granted FDA approval on 20 April 2004.11

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 267.3224
Monoisotopic: 267.125928793
Chemical Formula
C17H17NO2
Synonyms
  • (−)-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
  • Apomorfina
  • Apomorphin
  • Apomorphine
  • R-(−)-apomorphine
External IDs
  • APL-130277
  • VR-040
  • VR-400
  • VR040

Pharmacology

Indication

Apomorphine is indicated to treat acute, intermittent treatment of hypomobility, off episodes associated with advanced Parkinson's disease.11,12

Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Apomorphine is a dopaminergic agonist that may stimulate regions of the brain involved in motor control.8,11,12 It has a short duration of action and a wide therapeutic index as large overdoses are necessary for significant toxicity.11,12 Patients should be counselled regarding the risk of nausea, vomiting, daytime somnolence, hypotension, oral mucosal irritation, falls, hallucinations, psychotic-like behaviour, impulsive behaviour, withdrawal hyperpyrexia, and prolongation of the QT interval.p11,12

Mechanism of action

Apomorphine is a non-ergoline dopamine agonist with high binding affinity to dopamine D2, D3, and D5 receptors.11,12 Stimulation of D2 receptors in the caudate-putamen, a region of the brain responsible for locomotor control, may be responsible for apomorphine's action.8 However, the means by which the cellular effects of apomorphine treat hypomobility of Parkinson's remain unknown.11,12

TargetActionsOrganism
ADopamine D4 receptor
agonist
Humans
ADopamine D2 receptor
agonist
Humans
ADopamine D3 receptor
agonist
Humans
UDopamine D5 receptor
agonist
Humans
UDopamine D1 receptor
agonist
Humans
UAlpha-2C adrenergic receptor
agonist
Humans
UAlpha-2B adrenergic receptor
agonist
Humans
U5-hydroxytryptamine receptor 1A
agonist
Humans
U5-hydroxytryptamine receptor 2A
agonist
Humans
U5-hydroxytryptamine receptor 2B
agonist
Humans
U5-hydroxytryptamine receptor 2C
agonist
Humans
UAlpha-2A adrenergic receptor
agonist
Humans
U5-hydroxytryptamine receptor 1D
agonist
Humans
U5-hydroxytryptamine receptor 1B
agonist
Humans
Absorption

Apomorphine has a plasma Tmax of 10-20 minutes and a cerebrospinal fluid Tmax.4 The Cmax and AUC of apomorphine vary significantly between patients, with 5- to 10-fold differences being reported.4,6

Volume of distribution

The apparent volume of distribution of subcutaneous apomorphine is 123-404L with an average of 218L.11 The apparent volume of distribution of sublingual apomorphine is 3630L.12

Protein binding

Apomorphine is expected to be 99.9% bound to human serum albumin, as no unbound apomorphine is detected.3,6

Metabolism

Apomorphine is N-demethylated by CYP2B6, 2C8, 3A4, and 3A5.11 It can be glucuronidated by various UGTs,11 or sulfated by SULTs 1A1, 1A2, 1A3, 1E1, and 1B1.2 Approximately 60% of sublingual apomorphine is eliminated as a sulfate conjugate, though the structure of these sulfate conjugates are not readily available.2,11 The remainder of an apomorphine dose is eliminated as apomorphine glucuronide and norapomorphine glucuronide.11 Only 0.3% of subcutaneous apomorphine is recovered as the unchanged parent drug.5

Hover over products below to view reaction partners

Route of elimination

Data regarding apomorphine's route of elimination is not readily available.11,12 A study in rats has shown apomorphine is predominantly eliminated in the urine.7

Half-life

The terminal elimination half life of a 15mg sublingual dose of apomorphine is 1.7h,11 while the terminal elimination half life of an intravenous dose is 50 minutes.12

Clearance

The clearance of a 15mg sublingual dose of apomorphine is 1440L/h,11 while the clearance of an intravenous dose is 223L/h.12

Adverse Effects
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Toxicity

Patients experiencing an overdose of apomorphine may present with nausea, hypotension, and loss of consciousness.11 Treat patients with symptomatic and supportive measures.

The intraperitoneal LD50 in mice is 145µg/kg.13

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Apomorphine can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Apomorphine can be increased when combined with Abatacept.
AbirateroneThe metabolism of Apomorphine can be decreased when combined with Abiraterone.
AcalabrutinibThe metabolism of Apomorphine can be decreased when combined with Acalabrutinib.
AcebutololThe risk or severity of QTc prolongation can be increased when Apomorphine is combined with Acebutolol.
AcenocoumarolThe risk or severity of adverse effects can be increased when Apomorphine is combined with Acenocoumarol.
AcetazolamideThe risk or severity of adverse effects can be increased when Apomorphine is combined with Acetazolamide.
AcetophenazineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Acetophenazine.
AclidiniumApomorphine may increase the central nervous system depressant (CNS depressant) activities of Aclidinium.
AcrivastineThe risk or severity of QTc prolongation can be increased when Apomorphine is combined with Acrivastine.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
  • Avoid alcohol. Ingesting alcohol may potentiate hypotension caused by apomorphine.

Products

Product Ingredients
IngredientUNIICASInChI Key
Apomorphine hydrochlorideF39049Y06841372-20-7CXWQXGNFZLHLHQ-DPFCLETOSA-N
Product Images
International/Other Brands
Ixense (Takeda (discontinued)) / Spontane / Uprima (Abbott (discontinued))
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ApokynLiquid10 mg/1mLSubcutaneousVernalis Pharmaceuticals Inc2006-09-192006-09-19US flag
ApokynInjection30 mg/3mLSubcutaneousTercica2004-07-022011-10-31US flag
ApokynInjection30 mg/3mLSubcutaneousMDD US Operations, LLC2004-07-02Not applicableUS flag
KynmobiFilm, soluble15 mg/1SublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiFilm, soluble25 mg/1SublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiFilm, soluble30 mgSublingualSunovionNot applicableNot applicableCanada flag
KynmobiFilm, soluble20 mg/1SublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiFilm, soluble15 mgSublingualSunovionNot applicableNot applicableCanada flag
KynmobiFilm, soluble10 mg/1SublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiFilm, soluble10 mgSublingualSunovionNot applicableNot applicableCanada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
KynmobiApomorphine hydrochloride (10 mg/1) + Apomorphine hydrochloride (15 mg/1) + Apomorphine hydrochloride (20 mg/1) + Apomorphine hydrochloride (25 mg/1) + Apomorphine hydrochloride (30 mg/1)KitSublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiApomorphine hydrochloride (10 mg/1) + Apomorphine hydrochloride (15 mg/1) + Apomorphine hydrochloride (20 mg/1) + Apomorphine hydrochloride (25 mg/1) + Apomorphine hydrochloride (30 mg/1)KitSublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiApomorphine hydrochloride (10 mg/1) + Apomorphine hydrochloride (15 mg/1) + Apomorphine hydrochloride (20 mg/1) + Apomorphine hydrochloride (25 mg/1) + Apomorphine hydrochloride (30 mg/1)KitSublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiApomorphine hydrochloride (10 mg/1) + Apomorphine hydrochloride (15 mg/1) + Apomorphine hydrochloride (20 mg/1) + Apomorphine hydrochloride (25 mg/1) + Apomorphine hydrochloride (30 mg/1)KitSublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiApomorphine hydrochloride (10 mg/1) + Apomorphine hydrochloride (15 mg/1) + Apomorphine hydrochloride (20 mg/1) + Apomorphine hydrochloride (25 mg/1) + Apomorphine hydrochloride (30 mg/1)KitSublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiApomorphine hydrochloride (10 mg/1) + Apomorphine hydrochloride (15 mg/1) + Apomorphine hydrochloride (20 mg/1) + Apomorphine hydrochloride (25 mg/1) + Apomorphine hydrochloride (30 mg/1)KitSublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiApomorphine hydrochloride (10 mg/1) + Apomorphine hydrochloride (15 mg/1) + Apomorphine hydrochloride (20 mg/1) + Apomorphine hydrochloride (25 mg/1) + Apomorphine hydrochloride (30 mg/1)KitSublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiApomorphine hydrochloride (10 mg/1) + Apomorphine hydrochloride (15 mg/1) + Apomorphine hydrochloride (20 mg/1) + Apomorphine hydrochloride (25 mg/1) + Apomorphine hydrochloride (30 mg/1)KitSublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiApomorphine hydrochloride (10 mg/1) + Apomorphine hydrochloride (15 mg/1) + Apomorphine hydrochloride (20 mg/1) + Apomorphine hydrochloride (25 mg/1) + Apomorphine hydrochloride (30 mg/1)KitSublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag
KynmobiApomorphine hydrochloride (10 mg/1) + Apomorphine hydrochloride (15 mg/1) + Apomorphine hydrochloride (20 mg/1) + Apomorphine hydrochloride (25 mg/1) + Apomorphine hydrochloride (30 mg/1)KitSublingualSunovion Pharmaceuticals Inc.2020-05-21Not applicableUS flag

Categories

ATC Codes
G04BE07 — ApomorphineN04BC07 — Apomorphine
Drug Categories
Chemical TaxonomyProvided by Classyfire
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
1-hydroxy-2-unsubstituted benzenoid / 1-hydroxy-4-unsubstituted benzenoid / 1-naphthol / 2-naphthol / Amine / Aporphine / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid
show 14 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
isoquinoline alkaloid, isoquinolines (CHEBI:48538)

Chemical Identifiers

UNII
N21FAR7B4S
CAS number
58-00-4
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

References

Synthesis Reference

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

US20100228032
General References
  1. Borkar N, Mu H, Holm R: Challenges and trends in apomorphine drug delivery systems for the treatment of Parkinson's disease. Asian J Pharm Sci. 2018 Nov;13(6):507-517. doi: 10.1016/j.ajps.2017.11.004. Epub 2017 Dec 6. [PubMed:32104425]
  2. Thomas NL, Coughtrie MW: Sulfation of apomorphine by human sulfotransferases: evidence of a major role for the polymorphic phenol sulfotransferase, SULT1A1. Xenobiotica. 2003 Nov;33(11):1139-48. doi: 10.1080/00498250310001609192. [PubMed:14660177]
  3. Fanali G, Rampoldi V, di Masi A, Bolli A, Lopiano L, Ascenzi P, Fasano M: Binding of anti-Parkinson's disease drugs to human serum albumin is allosterically modulated. IUBMB Life. 2010 May;62(5):371-6. doi: 10.1002/iub.317. [PubMed:20225277]
  4. Jenner P, Katzenschlager R: Apomorphine - pharmacological properties and clinical trials in Parkinson's disease. Parkinsonism Relat Disord. 2016 Dec;33 Suppl 1:S13-S21. doi: 10.1016/j.parkreldis.2016.12.003. Epub 2016 Dec 13. [PubMed:27979722]
  5. LeWitt PA: Subcutaneously administered apomorphine: pharmacokinetics and metabolism. Neurology. 2004 Mar 23;62(6 Suppl 4):S8-11. doi: 10.1212/wnl.62.6_suppl_4.s8. [PubMed:15037665]
  6. van der Geest R, van Laar T, Kruger PP, Gubbens-Stibbe JM, Bodde HE, Roos RA, Danhof M: Pharmacokinetics, enantiomer interconversion, and metabolism of R-apomorphine in patients with idiopathic Parkinson's disease. Clin Neuropharmacol. 1998 May-Jun;21(3):159-68. [PubMed:9617507]
  7. Haberzettl R, Fink H, Bert B: The murine serotonin syndrome - evaluation of responses to 5-HT-enhancing drugs in NMRI mice. Behav Brain Res. 2015 Jan 15;277:204-10. doi: 10.1016/j.bbr.2014.04.033. Epub 2014 Apr 27. [PubMed:24780865]
  8. Costall B, Naylor RJ, Nohria V: Hyperactivity response to apomorphine and amphetamine in the mouse: the importance of the nucleus accumbens and caudate-putamen. J Pharm Pharmacol. 1979 Apr;31(4):259-61. doi: 10.1111/j.2042-7158.1979.tb13494.x. [PubMed:36471]
  9. Riegel F, Boehm R: Investigation into the Action of Apomorphin as an Emetic in Its Physiological and Therapeutic Relations. Glasgow Med J. 1872 May;4(3):362-377. [PubMed:30432919]
  10. Auffret M, Drapier S, Verin M: The Many Faces of Apomorphine: Lessons from the Past and Challenges for the Future. Drugs R D. 2018 Jun;18(2):91-107. doi: 10.1007/s40268-018-0230-3. [PubMed:29546602]
  11. FDA Approved Drug Products: Apomorphine Subcutaneous Injection [Link]
  12. FDA Approved Drug Products: Apomorphine Sublingual Film [Link]
  13. Cayman Chemical: Apomorphine MSDS [Link]
Human Metabolome Database
HMDB0014852
KEGG Drug
D07460
PubChem Compound
6005
PubChem Substance
46508653
ChemSpider
5783
BindingDB
29644
RxNav
1043
ChEBI
48538
ChEMBL
CHEMBL53
ZINC
ZINC000000009073
Therapeutic Targets Database
DAP000281
PharmGKB
PA164781163
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Apomorphine
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
PhaseStatusPurposeConditionsCount
4CompletedTreatmentAkinesia / Delayed Levadopa Onset / Delayed Levodopa Onset / Mobility decreased / Motor Symptoms / Parkinson's Disease (PD)1
4CompletedTreatmentBack Pain Lower Back Chronic1
4RecruitingTreatmentParkinson's Disease (PD)2
4TerminatedSupportive CareMotor Symptoms / Parkinson's Disease (PD)1
3Active Not RecruitingTreatmentIdiopathic Parkinson's Disease1
3CompletedBasic ScienceParkinson's Disease (PD)1
3CompletedTreatmentIdiopathic Parkinson's Disease1
3CompletedTreatmentParkinson Disease, Off Episodes1
3CompletedTreatmentParkinson's Disease (PD)8
3RecruitingTreatmentMotor OFF Episodes Associated With Parkinson's Disease1

Pharmacoeconomics

Manufacturers
  • Ipsen biopharm ltd
Packagers
  • Ipsen Pharmaceuticals Inc.
  • Tercica Inc.
  • Vetter Pharma Fertigung GmbH and Co. KG
Dosage Forms
FormRouteStrength
Injection20 mg/2ml
Injection50 mg/5ml
InjectionSubcutaneous5 mg/ml
Injection, solutionCutaneous; Parenteral30 MG/3ML
Injection, solutionParenteral50 MG/5ML
SolutionSubcutaneous5 mg/mL
SolutionSubcutaneous10 mg
InjectionSubcutaneous30 mg/3mL
LiquidSubcutaneous10 mg/1mL
SolutionSubcutaneous5 mg
Film, solubleSublingual10 mg/1
Film, solubleSublingual10 mg
Film, solubleSublingual15 mg/1
Film, solubleSublingual15 mg
Film, solubleSublingual20 mg
Film, solubleSublingual20 mg/1
Film, solubleSublingual25 mg/1
Film, solubleSublingual25 mg
Film, solubleSublingual30 mg/1
Film, solubleSublingual30 mg
KitSublingual
SolutionSubcutaneous
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8603514No2013-12-102024-04-03US flag
US9855221No2018-01-022022-02-14US flag
US9931305No2018-04-032022-02-14US flag
US8765167No2014-07-012024-02-20US flag
US8414922No2011-12-162031-12-16US flag
US9669021No2010-06-112030-06-11US flag
US9669019No2010-06-112030-06-11US flag
US8846074No2011-12-162031-12-16US flag
US9283219No2010-06-112030-06-11US flag
US10420763No2010-06-112030-06-11US flag
US9326981No2010-06-112030-06-11US flag
US10449146No2016-04-192036-04-19US flag
US8663687No2003-02-022023-02-02US flag
US9044475No2010-06-112030-06-11US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP2.0Borkar et al, 2017
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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-014r-0090000000-29608efdadd8efd375a6
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-000i-0090000000-052772c02bbf103a3ef5
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-00kr-0290000000-1e831a8078d43cfbdb51
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0090000000-49baaafc781fbd1a40ea
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0090000000-b2abd157ce4880c73d0b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0090000000-b747e9bb748f801c3f50
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000i-0090000000-1a55345a571167f3fca6

Targets

Details
1. Dopamine D4 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Sh3 domain binding
Specific Function
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
Molecular Weight
48359.86 Da
References
  1. 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]
  8. LeWitt PA: Subcutaneously administered apomorphine: pharmacokinetics and metabolism. Neurology. 2004 Mar 23;62(6 Suppl 4):S8-11. doi: 10.1212/wnl.62.6_suppl_4.s8. [PubMed:15037665]
Details
2. Dopamine D2 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. 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]
  9. LeWitt PA: Subcutaneously administered apomorphine: pharmacokinetics and metabolism. Neurology. 2004 Mar 23;62(6 Suppl 4):S8-11. doi: 10.1212/wnl.62.6_suppl_4.s8. [PubMed:15037665]
Details
3. Dopamine D3 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. LeWitt PA: Subcutaneously administered apomorphine: pharmacokinetics and metabolism. Neurology. 2004 Mar 23;62(6 Suppl 4):S8-11. doi: 10.1212/wnl.62.6_suppl_4.s8. [PubMed:15037665]
Details
4. Dopamine D5 receptor
Kind
Protein
Organism
Humans
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
  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]
  3. LeWitt PA: Subcutaneously administered apomorphine: pharmacokinetics and metabolism. Neurology. 2004 Mar 23;62(6 Suppl 4):S8-11. doi: 10.1212/wnl.62.6_suppl_4.s8. [PubMed:15037665]
Details
5. Dopamine D1 receptor
Kind
Protein
Organism
Humans
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
  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]
  5. LeWitt PA: Subcutaneously administered apomorphine: pharmacokinetics and metabolism. Neurology. 2004 Mar 23;62(6 Suppl 4):S8-11. doi: 10.1212/wnl.62.6_suppl_4.s8. [PubMed:15037665]
Kind
Protein
Organism
Humans
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
  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
Humans
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
  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
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  2. LeWitt PA: Subcutaneously administered apomorphine: pharmacokinetics and metabolism. Neurology. 2004 Mar 23;62(6 Suppl 4):S8-11. doi: 10.1212/wnl.62.6_suppl_4.s8. [PubMed:15037665]
Kind
Protein
Organism
Humans
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
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  2. LeWitt PA: Subcutaneously administered apomorphine: pharmacokinetics and metabolism. Neurology. 2004 Mar 23;62(6 Suppl 4):S8-11. doi: 10.1212/wnl.62.6_suppl_4.s8. [PubMed:15037665]
Kind
Protein
Organism
Humans
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
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  2. LeWitt PA: Subcutaneously administered apomorphine: pharmacokinetics and metabolism. Neurology. 2004 Mar 23;62(6 Suppl 4):S8-11. doi: 10.1212/wnl.62.6_suppl_4.s8. [PubMed:15037665]
Kind
Protein
Organism
Humans
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
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  2. LeWitt PA: Subcutaneously administered apomorphine: pharmacokinetics and metabolism. Neurology. 2004 Mar 23;62(6 Suppl 4):S8-11. doi: 10.1212/wnl.62.6_suppl_4.s8. [PubMed:15037665]
Kind
Protein
Organism
Humans
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
  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
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
O-methyltransferase activity
Specific Function
Catalyzes the O-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like L-DOP...
Gene Name
COMT
Uniprot ID
P21964
Uniprot Name
Catechol O-methyltransferase
Molecular Weight
30036.77 Da
References
  1. van der Geest R, van Laar T, Kruger PP, Gubbens-Stibbe JM, Bodde HE, Roos RA, Danhof M: Pharmacokinetics, enantiomer interconversion, and metabolism of R-apomorphine in patients with idiopathic Parkinson's disease. Clin Neuropharmacol. 1998 May-Jun;21(3):159-68. [PubMed:9617507]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sulfotransferase activity
Specific Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of catecholamines, phenolic drugs and neurotransmitters. Has also estroge...
Gene Name
SULT1A1
Uniprot ID
P50225
Uniprot Name
Sulfotransferase 1A1
Molecular Weight
34165.13 Da
References
  1. Thomas NL, Coughtrie MW: Sulfation of apomorphine by human sulfotransferases: evidence of a major role for the polymorphic phenol sulfotransferase, SULT1A1. Xenobiotica. 2003 Nov;33(11):1139-48. doi: 10.1080/00498250310001609192. [PubMed:14660177]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of catecholamines, phenolic drugs and neurotransmitters. Is also responsible for the sulfonation and activation of minoxidil. Mediates the metabolic activation of carcinogenic N-hydroxyarylamines to DNA binding products and could so participate as modulating factor of cancer risk.
Specific Function
Aryl sulfotransferase activity
Gene Name
SULT1A2
Uniprot ID
P50226
Uniprot Name
Sulfotransferase 1A2
Molecular Weight
34309.49 Da
References
  1. Thomas NL, Coughtrie MW: Sulfation of apomorphine by human sulfotransferases: evidence of a major role for the polymorphic phenol sulfotransferase, SULT1A1. Xenobiotica. 2003 Nov;33(11):1139-48. doi: 10.1080/00498250310001609192. [PubMed:14660177]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of phenolic monoamines (neurotransmitters such as dopamine, norepinephrine and serotonin) and phenolic and catechol drugs.
Specific Function
Amine sulfotransferase activity
Gene Name
SULT1A3
Uniprot ID
P0DMM9
Uniprot Name
Sulfotransferase 1A3
Molecular Weight
34195.96 Da
References
  1. Thomas NL, Coughtrie MW: Sulfation of apomorphine by human sulfotransferases: evidence of a major role for the polymorphic phenol sulfotransferase, SULT1A1. Xenobiotica. 2003 Nov;33(11):1139-48. doi: 10.1080/00498250310001609192. [PubMed:14660177]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sulfotransferase activity
Specific Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of estradiol and estrone. May play a role in the regulation of estrogen r...
Gene Name
SULT1E1
Uniprot ID
P49888
Uniprot Name
Estrogen sulfotransferase
Molecular Weight
35126.185 Da
References
  1. Thomas NL, Coughtrie MW: Sulfation of apomorphine by human sulfotransferases: evidence of a major role for the polymorphic phenol sulfotransferase, SULT1A1. Xenobiotica. 2003 Nov;33(11):1139-48. doi: 10.1080/00498250310001609192. [PubMed:14660177]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sulfotransferase activity
Specific Function
Sulfotransferase that utilizes 3'-phospho-5'-adenylyl sulfate (PAPS) as sulfonate donor to catalyze the sulfate conjugation of many hormones, neurotransmitters, drugs and xenobiotic compounds. Sulf...
Gene Name
SULT1B1
Uniprot ID
O43704
Uniprot Name
Sulfotransferase family cytosolic 1B member 1
Molecular Weight
34898.955 Da
References
  1. Thomas NL, Coughtrie MW: Sulfation of apomorphine by human sulfotransferases: evidence of a major role for the polymorphic phenol sulfotransferase, SULT1A1. Xenobiotica. 2003 Nov;33(11):1139-48. doi: 10.1080/00498250310001609192. [PubMed:14660177]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. FDA Approved Drug Products: Apomorphine Subcutaneous Injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. FDA Approved Drug Products: Apomorphine Subcutaneous Injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. FDA Approved Drug Products: Apomorphine Subcutaneous Injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
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
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. FDA Approved Drug Products: Apomorphine Subcutaneous Injection [Link]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...

Components:
References
  1. FDA Approved Drug Products: Apomorphine Subcutaneous Injection [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Fanali G, Rampoldi V, di Masi A, Bolli A, Lopiano L, Ascenzi P, Fasano M: Binding of anti-Parkinson's disease drugs to human serum albumin is allosterically modulated. IUBMB Life. 2010 May;62(5):371-6. doi: 10.1002/iub.317. [PubMed:20225277]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Monoamine transmembrane transporter activity
Specific Function
Involved in the ATP-dependent vesicular transport of biogenic amine neurotransmitters. Pumps cytosolic monoamines including dopamine, norepinephrine, serotonin, and histamine into synaptic vesicles...
Gene Name
SLC18A2
Uniprot ID
Q05940
Uniprot Name
Synaptic vesicular amine transporter
Molecular Weight
55712.075 Da
References
  1. Truong JG, Hanson GR, Fleckenstein AE: Apomorphine increases vesicular monoamine transporter-2 function: implications for neurodegeneration. Eur J Pharmacol. 2004 May 25;492(2-3):143-7. doi: 10.1016/j.ejphar.2004.03.060. [PubMed:15178358]

Drug created on June 13, 2005 07:24 / Updated on September 22, 2020 02:11

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