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Identification
NameCabergoline
Accession NumberDB00248  (APRD00836)
TypeSmall Molecule
GroupsApproved
Description

Cabergoline, an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor. It is used to treat hyperprolactinemic disorders and Parkinsonian Syndrome. Cabergoline possesses potent agonist activity on dopamine D2 receptors.

Structure
Thumb
Synonyms
(8beta)-N-[3-(dimethylamino)Propyl]-N-[(ethylamino)carbonyl]-6-(2-propenyl)-ergoline-8-carboxamide
(8R)-6-Allyl-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)ergoline-8-carboxamide
1-((6-Allylergolin-8beta-yl)carbonyl)-1-(3-(dimethylamino)propyl)-3-ethylurea
1-[(6-Allylergoline-8beta-yl)carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea
1-Ethyl-3-(3'-dimethylamionpropyl)-2-(6'-allylergoline-8'beta-carbonyl)urea
Cabergolina
Cabergoline
Cabergolinum
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Cabergolinetablet0.5 mgoralActavis Pharma Company2007-11-06Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Cabergolinetablet.5 mg/1oralGreenstone LLC2014-09-22Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cabergolinetablet0.5 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Dostinextablet0.5 mgoralPfizer Canada Inc2000-06-30Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cabergolinetablet.5 mg/1oralTeva Pharmaceuticals USA Inc2007-03-07Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cabergolinetablet.5 mg/1oralAvera Mc Kennan Hospital2015-04-14Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cabergolinetablet.5 mg/1oralApotex Corp.2013-03-08Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cabergolinetablet.5 mg/1oralPar Pharmaceutical, Inc.2005-12-29Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cabergolinetablet.5 mg/1oralCobalt Laboratories2008-04-21Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Cabergolinetablet.5 mg/1oralMylan Pharmaceuticals Inc.2013-12-02Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International Brands
NameCompany
CabaserPfizer
Brand mixturesNot Available
SaltsNot Available
Categories
UNIILL60K9J05T
CAS number81409-90-7
WeightAverage: 451.6043
Monoisotopic: 451.294725453
Chemical FormulaC26H37N5O2
InChI KeyInChIKey=KORNTPPJEAJQIU-KJXAQDMKSA-N
InChI
InChI=1S/C26H37N5O2/c1-5-11-30-17-19(25(32)31(26(33)27-6-2)13-8-12-29(3)4)14-21-20-9-7-10-22-24(20)18(16-28-22)15-23(21)30/h5,7,9-10,16,19,21,23,28H,1,6,8,11-15,17H2,2-4H3,(H,27,33)/t19-,21-,23-/m1/s1
IUPAC Name
1-[3-(dimethylamino)propyl]-3-ethyl-1-[(2R,4R,7R)-6-(prop-2-en-1-yl)-6,11-diazatetracyclo[7.6.1.0²,⁷.0¹²,¹⁶]hexadeca-1(16),9,12,14-tetraene-4-carbonyl]urea
SMILES
[H][C@@]12CC3=CNC4=CC=CC(=C34)[C@@]1([H])C[C@H](CN2CC=C)C(=O)N(CCCN(C)C)C(=O)NCC
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as lysergic acids and derivatives. These are alkaloids with a structure based on the lysergic acid skeleton.
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassErgoline and derivatives
Sub ClassLysergic acids and derivatives
Direct ParentLysergic acids and derivatives
Alternative Parents
Substituents
  • Lysergic acid or derivatives
  • Indoloquinoline
  • Benzoquinoline
  • Quinoline-3-carboxamide
  • Pyrroloquinoline
  • Quinoline
  • Piperidinecarboxylic acid
  • Piperidinecarboxamide
  • 3-piperidinecarboxamide
  • Isoindole or derivatives
  • Indole or derivatives
  • Indole
  • Aralkylamine
  • Ureide
  • Benzenoid
  • Piperidine
  • Heteroaromatic compound
  • Pyrrole
  • Urea
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of hyperprolactinemic disorders, either idiopathic or due to prolactinoma (prolactin-secreting adenomas). May also be used to manage symptoms of Parkinsonian Syndrome as monotherapy during initial symptomatic management or as an adjunct to levodopa therapy during advanced stages of disease.
PharmacodynamicsCabergoline stimulates centrally-located dopaminergic receptors resulting in a number of pharmacologic effects. Five dopamine receptor types from two dopaminergic subfamilies have been identified. The dopaminergic D1 receptor subfamily consists of D1 and D5 subreceptors, which are associated with dyskinesias. The dopaminergic D2 receptor subfamily consists of D2, D3 and D4 subreceptors, which are associated with improvement of symptoms of movement disorders. Thus, agonist activity specific for D2 subfamily receptors, primarily D2 and D3 receptor subtypes, are the primary targets of dopaminergic antiparkinsonian agents. It is thought that postsynaptic D2 stimulation is primarily responsible for the antiparkinsonian effect of dopamine agonists, while presynaptic D2 stimulation confers neuroprotective effects. This semisynthetic ergot derivative exhibits potent agonist activity on dopamine D2- and D3-receptors. It also exhibits: agonist activity (in order of decreasing binding affinities) on 5-hydroxytryptamine (5-HT)2B, 5-HT2A, 5-HT1D, dopamine D4, 5-HT1A, dopamine D1, 5-HT1B and 5-HT2C receptors and antagonist activity on α2B, α2A, and α2C receptors. Parkinsonian Syndrome manifests when approximately 80% of dopaminergic activity in the nigrostriatal pathway of the brain is lost. As this striatum is involved in modulating the intensity of coordinated muscle activity (e.g. movement, balance, walking), loss of activity may result in dystonia (acute muscle contraction), Parkinsonism (including symptoms of bradykinesia, tremor, rigidity, and flattened affect), akathesia (inner restlessness), tardive dyskinesia (involuntary muscle movements usually associated with long-term loss of dopaminergic activity), and neuroleptic malignant syndrome, which manifests when complete blockage of nigrostriatal dopamine occurs. High dopaminergic activity in the mesolimbic pathway of the brain causes hallucinations and delusions; these side effects of dopamine agonists are manifestations seen in patients with schizophrenia who have overractivity in this area of the brain. The hallucinogenic side effects of dopamine agonists may also be due to 5-HT2A agonism. The tuberoinfundibular pathway of the brain originates in the hypothalamus and terminates in the pituitary gland. In this pathway, dopamine inhibits lactotrophs in anterior pituitary from secreting prolactin. Increased dopaminergic activity in the tuberoinfundibular pathway inhibits prolactin secretion.
Mechanism of actionThe dopamine D2 receptor is a 7-transmembrane G-protein coupled receptor associated with Gi proteins. In lactotrophs, stimulation of dopamine D2 causes inhibition of adenylyl cyclase, which decreases intracellular cAMP concentrations and blocks IP3-dependent release of Ca2+ from intracellular stores. Decreases in intracellular calcium levels may also be brought about via inhibition of calcium influx through voltage-gated calcium channels, rather than via inhibition of adenylyl cyclase. Additionally, receptor activation blocks phosphorylation of p42/p44 MAPK and decreases MAPK/ERK kinase phosphorylation. Inhibition of MAPK appears to be mediated by c-Raf and B-Raf-dependent inhibition of MAPK/ERK kinase. Dopamine-stimulated growth hormone release from the pituitary gland is mediated by a decrease in intracellular calcium influx through voltage-gated calcium channels rather than via adenylyl cyclase inhibition. Stimulation of dopamine D2 receptors in the nigrostriatal pathway leads to improvements in coordinated muscle activity in those with movement disorders. Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D2 receptors. Receptor-binding studies indicate that cabergoline has low affinity for dopamine D1, α1,- and α2- adrenergic, and 5-HT1- and 5-HT2-serotonin receptors.
AbsorptionFirst-pass effect is seen, however the absolute bioavailability is unknown.
Volume of distributionNot Available
Protein bindingModerately bound (40% to 42%) to human plasma proteins in a concentration-independent manner.
Metabolism

Hepatic. Cabergoline is extensively metabolized, predominately via hydrolysis of the acylurea bond of the urea moiety. Cytochrome P-450 mediated metabolism appears to be minimal. The main metabolite identified in urine is 6-allyl-8b-carboxy-ergoline (4-6% of dose). Three other metabolites were identified urine (less than 3% of dose).

SubstrateEnzymesProduct
Cabergoline
Not Available
6-allyl-8b-carboxy-ergolineDetails
Route of eliminationAfter oral dosing of radioactive cabergoline to five healthy volunteers, approximately 22% and 60% of the dose was excreted within 20 days in the urine and feces, respectively. Less than 4% of the dose was excreted unchanged in the urine.
Half lifeThe elimination half-life is estimated from urinary data of 12 healthy subjects to range between 63 to 69 hours.
Clearance
  • renal cl=0,008 L/min
  • nonrenal cl=3.2 L/min
ToxicityOverdosage might be expected to produce nasal congestion, syncope, or hallucinations.
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+1.0
Blood Brain Barrier+0.9383
Caco-2 permeable-0.6583
P-glycoprotein substrateSubstrate0.7972
P-glycoprotein inhibitor IInhibitor0.8903
P-glycoprotein inhibitor IIInhibitor0.7698
Renal organic cation transporterNon-inhibitor0.5339
CYP450 2C9 substrateNon-substrate0.812
CYP450 2D6 substrateNon-substrate0.7438
CYP450 3A4 substrateSubstrate0.6336
CYP450 1A2 substrateNon-inhibitor0.7733
CYP450 2C9 inhibitorNon-inhibitor0.7396
CYP450 2D6 inhibitorNon-inhibitor0.7124
CYP450 2C19 inhibitorNon-inhibitor0.8341
CYP450 3A4 inhibitorNon-inhibitor0.6476
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8712
Ames testNon AMES toxic0.5619
CarcinogenicityNon-carcinogens0.8542
BiodegradationNot ready biodegradable0.846
Rat acute toxicity2.8786 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6224
hERG inhibition (predictor II)Non-inhibitor0.5309
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Impax laboratories inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Par pharmaceutical inc
  • Watson laboratories inc
  • Pharmacia and upjohn co
Packagers
Dosage forms
FormRouteStrength
Tabletoral.5 mg/1
Tabletoral0.5 mg
Prices
Unit descriptionCostUnit
Cabergoline 0.5 mg tablet37.39USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point102-104 °CNot Available
water solubilityInsolubleNot Available
logP2.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.064 mg/mLALOGPS
logP2.97ALOGPS
logP2.58ChemAxon
logS-3.9ALOGPS
pKa (Strongest Acidic)15.25ChemAxon
pKa (Strongest Basic)9.32ChemAxon
Physiological Charge2ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area71.68 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity133.5 m3·mol-1ChemAxon
Polarizability52.5 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

DrugSyn.org

US4526892
General References
  1. Pastor P, Tolosa E: [Cabergoline in the treatment of Parkinson’s disease] Neurologia. 2003 May;18(4):202-9. Pubmed
  2. Curran MP, Perry CM: Cabergoline : a review of its use in the treatment of Parkinson’s disease. Drugs. 2004;64(18):2125-41. Pubmed
  3. Bracco F, Battaglia A, Chouza C, Dupont E, Gershanik O, Marti Masso JF, Montastruc JL: The long-acting dopamine receptor agonist cabergoline in early Parkinson’s disease: final results of a 5-year, double-blind, levodopa-controlled study. CNS Drugs. 2004;18(11):733-46. Pubmed
  4. Miyagi M, Arai N, Taya F, Itoh F, Komatsu Y, Kojima M, Isaji M: Effect of cabergoline, a long-acting dopamine D2 agonist, on reserpine-treated rodents. Biol Pharm Bull. 1996 Nov;19(11):1499-502. Pubmed
External Links
ATC CodesG02CB03N04BC06
AHFS Codes
  • 28:36.20.04
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololAcebutolol may increase the vasoconstricting activities of Cabergoline.
AcepromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Acetophenazine.
AlmotriptanCabergoline may increase the vasoconstricting activities of Almotriptan.
AmisulprideThe therapeutic efficacy of Amisulpride can be decreased when used in combination with Cabergoline.
AripiprazoleThe risk or severity of adverse effects can be increased when Cabergoline is combined with Aripiprazole.
ArticaineCabergoline may increase the hypertensive activities of Articaine.
AtenololAtenolol may increase the vasoconstricting activities of Cabergoline.
BendroflumethiazideBendroflumethiazide may increase the vasoconstricting activities of Cabergoline.
BenzquinamideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Benzquinamide.
BetaxololBetaxolol may increase the vasoconstricting activities of Cabergoline.
BisoprololBisoprolol may increase the vasoconstricting activities of Cabergoline.
CarphenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Carphenazine.
CarteololCarteolol may increase the vasoconstricting activities of Cabergoline.
CarvedilolCarvedilol may increase the vasoconstricting activities of Cabergoline.
ChlormezanoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Chlorprothixene.
ClarithromycinThe serum concentration of Cabergoline can be increased when it is combined with Clarithromycin.
ClozapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Clozapine.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Cabergoline.
DipivefrinCabergoline may increase the hypertensive activities of Dipivefrin.
DopamineCabergoline may increase the hypertensive activities of Dopamine.
DroperidolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Droperidol.
EletriptanCabergoline may increase the vasoconstricting activities of Eletriptan.
EphedrineCabergoline may increase the hypertensive activities of Ephedrine.
EpinephrineCabergoline may increase the hypertensive activities of Epinephrine.
EsmololEsmolol may increase the vasoconstricting activities of Cabergoline.
FencamfamineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fencamfamine.
FlupentixolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fluspirilene.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Cabergoline.
FrovatriptanCabergoline may increase the vasoconstricting activities of Frovatriptan.
GranisetronGranisetron may increase the serotonergic activities of Cabergoline.
HaloperidolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Haloperidol.
LabetalolLabetalol may increase the vasoconstricting activities of Cabergoline.
LevobunololLevobunolol may increase the vasoconstricting activities of Cabergoline.
LevonordefrinCabergoline may increase the hypertensive activities of Levonordefrin.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Cabergoline.
LoxapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Loxapine.
MepivacaineCabergoline may increase the hypertensive activities of Mepivacaine.
MesoridazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Mesoridazine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Methotrimeprazine.
MetipranololMetipranolol may increase the vasoconstricting activities of Cabergoline.
MetoclopramideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Metoclopramide.
MetoprololMetoprolol may increase the vasoconstricting activities of Cabergoline.
MidodrineCabergoline may increase the hypertensive activities of Midodrine.
MolindoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Molindone.
NadololNadolol may increase the vasoconstricting activities of Cabergoline.
NaphazolineCabergoline may increase the hypertensive activities of Naphazoline.
NaratriptanCabergoline may increase the vasoconstricting activities of Naratriptan.
NebivololNebivolol may increase the vasoconstricting activities of Cabergoline.
NitroglycerinCabergoline may decrease the vasodilatory activities of Nitroglycerin.
NorepinephrineCabergoline may increase the hypertensive activities of Norepinephrine.
OlanzapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Cabergoline is combined with Ondansetron.
OxymetazolineCabergoline may increase the hypertensive activities of Oxymetazoline.
PaliperidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Paliperidone.
PenbutololPenbutolol may increase the vasoconstricting activities of Cabergoline.
PerphenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Perphenazine.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Cabergoline.
PheniramineCabergoline may increase the hypertensive activities of Pheniramine.
PhenylephrineCabergoline may increase the hypertensive activities of Phenylephrine.
PimozideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Pimozide.
PindololPindolol may increase the vasoconstricting activities of Cabergoline.
PipamperoneThe therapeutic efficacy of Pipamperone can be decreased when used in combination with Cabergoline.
PiperacetazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Piperacetazine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Promazine.
PropranololPropranolol may increase the vasoconstricting activities of Cabergoline.
PropylhexedrineCabergoline may increase the hypertensive activities of Propylhexedrine.
PseudoephedrineCabergoline may increase the hypertensive activities of Pseudoephedrine.
QuetiapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Quetiapine.
RacepinephrineCabergoline may increase the hypertensive activities of Racepinephrine.
RemoxiprideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Risperidone.
RizatriptanCabergoline may increase the vasoconstricting activities of Rizatriptan.
SertindoleThe risk or severity of adverse effects can be increased when Cabergoline is combined with Sertindole.
SotalolSotalol may increase the vasoconstricting activities of Cabergoline.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Cabergoline.
SumatriptanCabergoline may increase the vasoconstricting activities of Sumatriptan.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Cabergoline.
ThioridazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Thiothixene.
TimololTimolol may increase the vasoconstricting activities of Cabergoline.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Cabergoline.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Cabergoline.
TrifluoperazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Triflupromazine.
TriprolidineCabergoline may increase the hypertensive activities of Triprolidine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Ziprasidone.
ZolmitriptanCabergoline may increase the vasoconstricting activities of Zolmitriptan.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Zuclopenthixol.
Food Interactions
  • Absorption is not affected by food.
  • Take with food to improve tolerance.

Targets

1. D(2) dopamine receptor

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
D(2) dopamine receptor P14416 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Lombardi G, Varsaldi F, Miglio G, Papini MG, Battaglia A, Canonico PL: Cabergoline prevents necrotic neuronal death in an in vitro model of oxidative stress. Eur J Pharmacol. 2002 Dec 20;457(2-3):95-8. Pubmed
  3. Kageyama K, Nigawara T, Kamata Y, Takahashi T, Anzai J, Suzuki S, Osamura YR, Suda T: A case of macroprolactinoma with subclinical growth hormone production. Endocr J. 2002 Feb;49(1):41-7. Pubmed
  4. Pastor P, Tolosa E: [Cabergoline in the treatment of Parkinson’s disease] Neurologia. 2003 May;18(4):202-9. Pubmed
  5. Curran MP, Perry CM: Cabergoline : a review of its use in the treatment of Parkinson’s disease. Drugs. 2004;64(18):2125-41. Pubmed
  6. Miyagi M, Arai N, Taya F, Itoh F, Komatsu Y, Kojima M, Isaji M: Effect of cabergoline, a long-acting dopamine D2 agonist, on reserpine-treated rodents. Biol Pharm Bull. 1996 Nov;19(11):1499-502. Pubmed
  7. Ichikawa K, Kojima M: [Pharmacological effects of cabergoline against parkinsonism] Nippon Yakurigaku Zasshi. 2001 Jun;117(6):395-400. Pubmed
  8. Linazasoro G: Conversion from dopamine agonists to cabergoline: an open-label trial in 128 patients with advanced Parkinson disease. Clin Neuropharmacol. 2008 Jan-Feb;31(1):19-24. Pubmed

2. 5-hydroxytryptamine receptor 2B

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2B P41595 Details

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
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed
  3. Sharif NA: Serotonin-2 receptor agonists as novel ocular hypotensive agents and their cellular and molecular mechanisms of action. Curr Drug Targets. 2010 Aug;11(8):978-93. Pubmed
  4. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. Epub 2008 Nov 1. Pubmed
  5. Huang XP, Setola V, Yadav PN, Allen JA, Rogan SC, Hanson BJ, Revankar C, Robers M, Doucette C, Roth BL: Parallel functional activity profiling reveals valvulopathogens are potent 5-hydroxytryptamine(2B) receptor agonists: implications for drug safety assessment. Mol Pharmacol. 2009 Oct;76(4):710-22. Epub 2009 Jul 1. Pubmed

3. D(3) dopamine receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
D(3) dopamine receptor P35462 Details

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
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed
  3. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. Epub 2008 Nov 1. Pubmed

4. 5-hydroxytryptamine receptor 2A

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2A P28223 Details

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
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed
  3. Sharif NA: Serotonin-2 receptor agonists as novel ocular hypotensive agents and their cellular and molecular mechanisms of action. Curr Drug Targets. 2010 Aug;11(8):978-93. Pubmed
  4. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. Epub 2008 Nov 1. Pubmed

5. Alpha-2B adrenergic receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Alpha-2B adrenergic receptor P18089 Details

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
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed
  3. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. Epub 2008 Nov 1. Pubmed
  4. Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ: Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor. J Pharmacol Exp Ther. 2002 Nov;303(2):805-14. Pubmed

6. 5-hydroxytryptamine receptor 1D

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1D P28221 Details

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
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed

7. D(4) dopamine receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
D(4) dopamine receptor P21917 Details

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
  2. Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ: Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor. J Pharmacol Exp Ther. 2002 Nov;303(2):805-14. Pubmed

8. Alpha-2A adrenergic receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Alpha-2A adrenergic receptor P08913 Details

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
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed
  3. Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ: Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor. J Pharmacol Exp Ther. 2002 Nov;303(2):805-14. Pubmed

9. 5-hydroxytryptamine receptor 1A

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1A P08908 Details

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
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed
  3. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. Epub 2008 Nov 1. Pubmed

10. Alpha-2C adrenergic receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Alpha-2C adrenergic receptor P18825 Details

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
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed
  3. Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ: Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor. J Pharmacol Exp Ther. 2002 Nov;303(2):805-14. Pubmed

11. D(1B) dopamine receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
D(1B) dopamine receptor P21918 Details

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
  2. Kvernmo T, Hartter S, Burger E: A review of the receptor-binding and pharmacokinetic properties of dopamine agonists. Clin Ther. 2006 Aug;28(8):1065-78. Pubmed
  3. Ichikawa K, Kojima M: [Pharmacological effects of cabergoline against parkinsonism] Nippon Yakurigaku Zasshi. 2001 Jun;117(6):395-400. Pubmed

12. D(1A) dopamine receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
D(1A) dopamine receptor P21728 Details

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
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed
  3. Kvernmo T, Hartter S, Burger E: A review of the receptor-binding and pharmacokinetic properties of dopamine agonists. Clin Ther. 2006 Aug;28(8):1065-78. Pubmed
  4. Ichikawa K, Kojima M: [Pharmacological effects of cabergoline against parkinsonism] Nippon Yakurigaku Zasshi. 2001 Jun;117(6):395-400. Pubmed

13. 5-hydroxytryptamine receptor 1B

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1B P28222 Details

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
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed

14. 5-hydroxytryptamine receptor 2C

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2C P28335 Details

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
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. Pubmed
  3. Sharif NA: Serotonin-2 receptor agonists as novel ocular hypotensive agents and their cellular and molecular mechanisms of action. Curr Drug Targets. 2010 Aug;11(8):978-93. Pubmed
  4. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. Epub 2008 Nov 1. Pubmed

15. 5-hydroxytryptamine receptor 7

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 7 P34969 Details

References:

  1. Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C: Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes. Exp Eye Res. 2009 Mar;88(3):386-97. Epub 2008 Nov 1. Pubmed

16. Alpha-1A adrenergic receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: binder

Components

Name UniProt ID Details
Alpha-1A adrenergic receptor P35348 Details

References:

  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. Pubmed
  2. National Institute ofMental Health. PDSD Ki Database (Internet) [cited 2013 Jul 24]. ChapelHill (NC): University of North Carolina. 1998-2013. Available from: http://pdsp.med.unc.edu/pdsp.php

17. Alpha-1B adrenergic receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: binder

Components

Name UniProt ID Details
Alpha-1B adrenergic receptor P35368 Details

References:

  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. Pubmed
  2. National Institute ofMental Health. PDSD Ki Database (Internet) [cited 2013 Jul 24]. ChapelHill (NC): University of North Carolina. 1998-2013. Available from: http://pdsp.med.unc.edu/pdsp.php

18. Alpha-1D adrenergic receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: binder

Components

Name UniProt ID Details
Alpha-1D adrenergic receptor P25100 Details

References:

  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. Pubmed
  2. National Institute ofMental Health. PDSD Ki Database (Internet) [cited 2013 Jul 24]. ChapelHill (NC): University of North Carolina. 1998-2013. Available from: http://pdsp.med.unc.edu/pdsp.php

19. Beta-1 adrenergic receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: binder

Components

Name UniProt ID Details
Beta-1 adrenergic receptor P08588 Details

References:

  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. Pubmed
  2. National Institute ofMental Health. PDSD Ki Database (Internet) [cited 2013 Jul 24]. ChapelHill (NC): University of North Carolina. 1998-2013. Available from: http://pdsp.med.unc.edu/pdsp.php

20. Beta-2 adrenergic receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: binder

Components

Name UniProt ID Details
Beta-2 adrenergic receptor P07550 Details

References:

  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. Pubmed
  2. National Institute ofMental Health. PDSD Ki Database (Internet) [cited 2013 Jul 24]. ChapelHill (NC): University of North Carolina. 1998-2013. Available from: http://pdsp.med.unc.edu/pdsp.php

21. D(1) dopamine receptor

Kind: Protein group

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details
D(1A) dopamine receptor P21728 Details
D(1B) dopamine receptor P21918 Details

References:

  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. Pubmed
  2. National Institute ofMental Health. PDSD Ki Database (Internet) [cited 2013 Jul 24]. ChapelHill (NC): University of North Carolina. 1998-2013. Available from: http://pdsp.med.unc.edu/pdsp.php

22. D(2S) dopamine receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details

References:

  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. Pubmed
  2. National Institute ofMental Health. PDSD Ki Database (Internet) [cited 2013 Jul 24]. ChapelHill (NC): University of North Carolina. 1998-2013. Available from: http://pdsp.med.unc.edu/pdsp.php

23. D(2L) dopamine receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: agonist

Components

Name UniProt ID Details

References:

  1. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A: Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther. 2002 Nov;303(2):791-804. Pubmed
  2. National Institute ofMental Health. PDSD Ki Database (Internet) [cited 2013 Jul 24]. ChapelHill (NC): University of North Carolina. 1998-2013. Available from: http://pdsp.med.unc.edu/pdsp.php

Enzymes

1. Cytochrome P450 3A4

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

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

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Drug created on June 13, 2005 07:24 / Updated on October 08, 2013 14:22