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Identification
NameCabergoline
Accession NumberDB00248  (APRD00836)
TypeSmall Molecule
GroupsApproved
DescriptionCabergoline, 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
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Cabergolinetablet0.5 mgoralActavis Pharma Company2007-11-06Not applicableCanada
Cabergolinetablet.5 mg/1oralGreenstone LLC2014-09-22Not applicableUs
Cabergolinetablet0.5 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Dostinextablet0.5 mgoralPfizer Canada Inc2000-06-30Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-cabergolinetablet0.5 mgoralApotex IncNot applicableNot applicableCanada
Cabergolinetablet.5 mg/1oralTeva Pharmaceuticals USA Inc2007-03-07Not applicableUs
Cabergolinetablet.5 mg/1oralApotex Corp.2013-03-08Not applicableUs
Cabergolinetablet.5 mg/1oralMylan Pharmaceuticals Inc.2013-12-02Not applicableUs
Cabergolinetablet.5 mg/1oralAvera Mc Kennan Hospital2015-04-14Not applicableUs
Cabergolinetablet.5 mg/1oralCobalt Laboratories2008-04-21Not applicableUs
Cabergolinetablet.5 mg/1oralPar Pharmaceutical, Inc.2005-12-29Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not 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[[email protected]](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.
Related Articles
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
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

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:12721865 ]
  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:15341508 ]
  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:15330687 ]
  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:8951172 ]
External Links
ATC CodesN04BC06G02CB03
AHFS Codes
  • 28:36.20.04
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
1,10-PhenanthrolineThe serum concentration of Cabergoline can be increased when it is combined with 1,10-Phenanthroline.
3,4-DichloroisocoumarinThe serum concentration of Cabergoline can be increased when it is combined with 3,4-Dichloroisocoumarin.
4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDEThe serum concentration of Cabergoline can be increased when it is combined with 4-(2-AMINOETHYL)BENZENESULFONYL FLUORIDE.
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINEThe metabolism of Cabergoline can be decreased when combined with 7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE.
AcebutololAcebutolol may increase the vasoconstricting activities of Cabergoline.
AcepromazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Acepromazine.
AceprometazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Aceprometazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Acetophenazine.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Cabergoline.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Cabergoline.
AlmotriptanCabergoline may increase the vasoconstricting activities of Almotriptan.
AlogliptinThe serum concentration of Cabergoline can be increased when it is combined with Alogliptin.
Alpha-1-proteinase inhibitorThe serum concentration of Cabergoline can be increased when it is combined with Alpha-1-proteinase inhibitor.
AlprenololAlprenolol may increase the vasoconstricting activities of Cabergoline.
AmiodaroneThe metabolism of Cabergoline can be decreased when combined with Amiodarone.
AmisulprideThe therapeutic efficacy of Amisulpride can be decreased when used in combination with Cabergoline.
AmitriptylineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Amitriptyline.
AmoxapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Amoxapine.
AmperozideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Amperozide.
AmprenavirThe serum concentration of Cabergoline can be increased when it is combined with Amprenavir.
Antithrombin III humanThe serum concentration of Cabergoline can be increased when it is combined with Antithrombin III human.
ApixabanThe serum concentration of Cabergoline can be increased when it is combined with Apixaban.
ApomorphineCabergoline may increase the vasoconstricting activities of Apomorphine.
AprepitantThe serum concentration of Cabergoline can be increased when it is combined with Aprepitant.
AprotininThe serum concentration of Cabergoline can be increased when it is combined with Aprotinin.
ArgatrobanThe serum concentration of Cabergoline can be increased when it is combined with Argatroban.
AripiprazoleThe risk or severity of adverse effects can be increased when Cabergoline is combined with Aripiprazole.
ArotinololArotinolol may increase the vasoconstricting activities of Cabergoline.
AsenapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Asenapine.
AsunaprevirThe serum concentration of Cabergoline can be increased when it is combined with Asunaprevir.
AtazanavirThe serum concentration of Cabergoline can be increased when it is combined with Atazanavir.
AtenololAtenolol may increase the vasoconstricting activities of Cabergoline.
AtomoxetineThe metabolism of Cabergoline can be decreased when combined with Atomoxetine.
AzaperoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Azaperone.
BatimastatThe serum concentration of Cabergoline can be increased when it is combined with Batimastat.
BefunololBefunolol may increase the vasoconstricting activities of Cabergoline.
BenazeprilThe serum concentration of Cabergoline can be increased when it is combined with Benazepril.
BenmoxinThe metabolism of Cabergoline can be decreased when combined with Benmoxin.
BenzamidineThe serum concentration of Cabergoline can be increased when it is combined with Benzamidine.
BetaxololBetaxolol may increase the vasoconstricting activities of Cabergoline.
BevacizumabBevacizumab may increase the cardiotoxic activities of Cabergoline.
BevantololBevantolol may increase the vasoconstricting activities of Cabergoline.
BexaroteneThe serum concentration of Cabergoline can be decreased when it is combined with Bexarotene.
BifeprunoxThe risk or severity of adverse effects can be increased when Cabergoline is combined with Bifeprunox.
BisoprololBisoprolol may increase the vasoconstricting activities of Cabergoline.
BivalirudinThe serum concentration of Cabergoline can be increased when it is combined with Bivalirudin.
BoceprevirThe serum concentration of Cabergoline can be increased when it is combined with Boceprevir.
BopindololBopindolol may increase the vasoconstricting activities of Cabergoline.
BortezomibThe metabolism of Cabergoline can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Cabergoline can be decreased when it is combined with Bosentan.
BrexpiprazoleThe risk or severity of adverse effects can be increased when Cabergoline is combined with Brexpiprazole.
BromocriptineCabergoline may increase the vasoconstricting activities of Bromocriptine.
BufuralolBufuralol may increase the vasoconstricting activities of Cabergoline.
BupranololBupranolol may increase the vasoconstricting activities of Cabergoline.
BuspironeThe risk or severity of adverse effects can be increased when Cabergoline is combined with Buspirone.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Cabergoline.
CandoxatrilThe serum concentration of Cabergoline can be increased when it is combined with Candoxatril.
CaptoprilThe serum concentration of Cabergoline can be increased when it is combined with Captopril.
CarbamazepineThe metabolism of Cabergoline can be increased when combined with Carbamazepine.
CariprazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Cariprazine.
CaroxazoneThe metabolism of Cabergoline can be decreased when combined with Caroxazone.
CarteololCarteolol may increase the vasoconstricting activities of Cabergoline.
CarvedilolCarvedilol may increase the vasoconstricting activities of Cabergoline.
CeliprololCeliprolol may increase the vasoconstricting activities of Cabergoline.
CeritinibThe serum concentration of Cabergoline can be increased when it is combined with Ceritinib.
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.
ChymostatinThe serum concentration of Cabergoline can be increased when it is combined with Chymostatin.
CilastatinThe serum concentration of Cabergoline can be increased when it is combined with Cilastatin.
CilazaprilThe serum concentration of Cabergoline can be increased when it is combined with Cilazapril.
CirazolineCabergoline may increase the hypertensive activities of Cirazoline.
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Cabergoline.
ClarithromycinThe serum concentration of Cabergoline can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Cabergoline can be decreased when combined with Clemastine.
ClomipramineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Clomipramine.
ClotrimazoleThe metabolism of Cabergoline can be decreased when combined with Clotrimazole.
ClozapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Clozapine.
CobicistatThe metabolism of Cabergoline can be decreased when combined with Cobicistat.
ConivaptanThe serum concentration of Cabergoline can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Cabergoline can be decreased when combined with Crizotinib.
CyamemazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Cyamemazine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Cyclobenzaprine.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Cabergoline.
CyclosporineThe metabolism of Cabergoline can be decreased when combined with Cyclosporine.
Dabigatran etexilateThe serum concentration of Cabergoline can be increased when it is combined with Dabigatran etexilate.
DabrafenibThe serum concentration of Cabergoline can be decreased when it is combined with Dabrafenib.
DapiprazoleThe risk or severity of adverse effects can be increased when Cabergoline is combined with Dapiprazole.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Cabergoline.
DarunavirThe serum concentration of Cabergoline can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Cabergoline can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Cabergoline can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Cabergoline can be decreased when combined with Delavirdine.
DesipramineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Desipramine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Cabergoline.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Desvenlafaxine.
DexamethasoneThe serum concentration of Cabergoline can be decreased when it is combined with Dexamethasone.
DextromethorphanThe risk or severity of adverse effects can be increased when Cabergoline is combined with Dextromethorphan.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Cabergoline.
DigoxinDigoxin may decrease the cardiotoxic activities of Cabergoline.
DihydroergotamineCabergoline may increase the vasoconstricting activities of Dihydroergotamine.
DiltiazemThe metabolism of Cabergoline can be decreased when combined with Diltiazem.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Cabergoline.
DolasetronDolasetron may increase the serotonergic activities of Cabergoline.
DoxepinThe risk or severity of adverse effects can be increased when Cabergoline is combined with Doxepin.
DoxycyclineThe metabolism of Cabergoline can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Cabergoline can be decreased when combined with Dronedarone.
DroperidolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Droperidol.
DroxidopaCabergoline may increase the hypertensive activities of Droxidopa.
DuloxetineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Duloxetine.
EcabetThe serum concentration of Cabergoline can be increased when it is combined with Ecabet.
EdoxabanThe serum concentration of Cabergoline can be increased when it is combined with Edoxaban.
EfavirenzThe serum concentration of Cabergoline can be decreased when it is combined with Efavirenz.
ElafinThe serum concentration of Cabergoline can be increased when it is combined with Elafin.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Cabergoline.
EletriptanCabergoline may increase the vasoconstricting activities of Eletriptan.
EnalaprilThe serum concentration of Cabergoline can be increased when it is combined with Enalapril.
EnalaprilatThe serum concentration of Cabergoline can be increased when it is combined with Enalaprilat.
EnalkirenThe serum concentration of Cabergoline can be increased when it is combined with Enalkiren.
EnzalutamideThe serum concentration of Cabergoline can be decreased when it is combined with Enzalutamide.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Cabergoline is combined with Ergoloid mesylate.
Ergoloid mesylateErgoloid mesylate may increase the vasoconstricting activities of Cabergoline.
ErgonovineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Ergonovine.
ErgonovineErgonovine may increase the vasoconstricting activities of Cabergoline.
ErgotamineCabergoline may increase the hypertensive activities of Ergotamine.
ErgotamineErgotamine may increase the vasoconstricting activities of Cabergoline.
ErythromycinThe metabolism of Cabergoline can be decreased when combined with Erythromycin.
EscitalopramThe risk or severity of adverse effects can be increased when Cabergoline is combined with Escitalopram.
Eslicarbazepine acetateThe serum concentration of Cabergoline can be decreased when it is combined with Eslicarbazepine acetate.
EsmololEsmolol may increase the vasoconstricting activities of Cabergoline.
EtravirineThe serum concentration of Cabergoline can be decreased when it is combined with Etravirine.
FencamfamineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fencamfamine.
FentanylThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fentanyl.
FluconazoleThe metabolism of Cabergoline can be decreased when combined with Fluconazole.
FluoxetineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fluoxetine.
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 metabolism of Cabergoline can be decreased when combined with Fluvoxamine.
FluvoxamineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Fluvoxamine.
FosamprenavirThe serum concentration of Cabergoline can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Cabergoline can be increased when it is combined with Fosaprepitant.
FosinoprilThe serum concentration of Cabergoline can be increased when it is combined with Fosinopril.
FosphenytoinThe metabolism of Cabergoline can be increased when combined with Fosphenytoin.
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Cabergoline.
FrovatriptanCabergoline may increase the vasoconstricting activities of Frovatriptan.
FurazolidoneThe metabolism of Cabergoline can be decreased when combined with Furazolidone.
Fusidic AcidThe serum concentration of Cabergoline can be increased when it is combined with Fusidic Acid.
GeldanamycinThe serum concentration of Cabergoline can be increased when it is combined with Geldanamycin.
GM6001The serum concentration of Cabergoline can be increased when it is combined with GM6001.
GranisetronGranisetron may increase the serotonergic activities of Cabergoline.
HaloperidolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Haloperidol.
HirulogThe serum concentration of Cabergoline can be increased when it is combined with Hirulog.
HydracarbazineThe metabolism of Cabergoline can be decreased when combined with Hydracarbazine.
IdelalisibThe serum concentration of Cabergoline can be increased when it is combined with Idelalisib.
IloperidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Iloperidone.
ImatinibThe metabolism of Cabergoline can be decreased when combined with Imatinib.
ImipramineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Imipramine.
IndenololIndenolol may increase the vasoconstricting activities of Cabergoline.
IndinavirThe serum concentration of Cabergoline can be increased when it is combined with Indinavir.
IproclozideThe metabolism of Cabergoline can be decreased when combined with Iproclozide.
IproniazidThe metabolism of Cabergoline can be decreased when combined with Iproniazid.
IsavuconazoniumThe metabolism of Cabergoline can be decreased when combined with Isavuconazonium.
IsocarboxazidThe risk or severity of adverse effects can be increased when Cabergoline is combined with Isocarboxazid.
IsocarboxazidThe metabolism of Cabergoline can be decreased when combined with Isocarboxazid.
IsoflurophateThe serum concentration of Cabergoline can be increased when it is combined with Isoflurophate.
IsradipineThe metabolism of Cabergoline can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Cabergoline can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Cabergoline can be increased when it is combined with Ivacaftor.
IxazomibThe serum concentration of Cabergoline can be increased when it is combined with Ixazomib.
KetoconazoleThe metabolism of Cabergoline can be decreased when combined with Ketoconazole.
LabetalolLabetalol may increase the vasoconstricting activities of Cabergoline.
LepirudinThe serum concentration of Cabergoline can be increased when it is combined with Lepirudin.
LevobunololLevobunolol may increase the vasoconstricting activities of Cabergoline.
LevomilnacipranThe risk or severity of adverse effects can be increased when Cabergoline is combined with Levomilnacipran.
LinagliptinThe serum concentration of Cabergoline can be increased when it is combined with Linagliptin.
LinezolidThe risk or severity of adverse effects can be increased when Cabergoline is combined with Linezolid.
LisinoprilThe serum concentration of Cabergoline can be increased when it is combined with Lisinopril.
LisurideCabergoline may increase the vasoconstricting activities of Lisuride.
LithiumThe risk or severity of adverse effects can be increased when Cabergoline is combined with Lithium.
LopinavirThe serum concentration of Cabergoline can be increased when it is combined with Lopinavir.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Cabergoline.
LovastatinThe metabolism of Cabergoline can be decreased when combined with Lovastatin.
LoxapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Loxapine.
Lu AA21004Cabergoline may increase the vasoconstricting activities of Lu AA21004.
LuliconazoleThe serum concentration of Cabergoline can be increased when it is combined with Luliconazole.
LurasidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Lurasidone.
MaprotilineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Maprotiline.
MebanazineThe metabolism of Cabergoline can be decreased when combined with Mebanazine.
MelperoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Melperone.
MephentermineCabergoline may increase the hypertensive activities of Mephentermine.
MesoridazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Mesoridazine.
MetaraminolCabergoline may increase the hypertensive activities of Metaraminol.
MethadoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Methadone.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Methotrimeprazine.
MethoxamineCabergoline may increase the hypertensive activities of Methoxamine.
Methylene blueThe metabolism of Cabergoline can be decreased when combined with Methylene blue.
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.
MifepristoneThe metabolism of Cabergoline can be decreased when combined with Mifepristone.
MilnacipranThe risk or severity of adverse effects can be increased when Cabergoline is combined with Milnacipran.
MinaprineThe metabolism of Cabergoline can be decreased when combined with Minaprine.
MirtazapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Mirtazapine.
MitotaneThe serum concentration of Cabergoline can be decreased when it is combined with Mitotane.
MoclobemideThe risk or severity of adverse effects can be increased when Cabergoline is combined with Moclobemide.
MoclobemideThe metabolism of Cabergoline can be decreased when combined with Moclobemide.
ModafinilThe serum concentration of Cabergoline can be decreased when it is combined with Modafinil.
MoexiprilThe serum concentration of Cabergoline can be increased when it is combined with Moexipril.
MolindoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Molindone.
N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-ProlineThe serum concentration of Cabergoline can be increased when it is combined with N-(3-Propylcarbamoyloxirane-2-Carbonyl)-Isoleucyl-Proline.
NadololNadolol may increase the vasoconstricting activities of Cabergoline.
NafcillinThe serum concentration of Cabergoline can be decreased when it is combined with Nafcillin.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Cabergoline.
NaratriptanCabergoline may increase the vasoconstricting activities of Naratriptan.
NCX 4016The serum concentration of Cabergoline can be increased when it is combined with NCX 4016.
NefazodoneThe metabolism of Cabergoline can be decreased when combined with Nefazodone.
NefazodoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Nefazodone.
NelfinavirThe serum concentration of Cabergoline can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Cabergoline can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Cabergoline can be decreased when combined with Nevirapine.
NialamideThe metabolism of Cabergoline can be decreased when combined with Nialamide.
NilotinibThe metabolism of Cabergoline can be decreased when combined with Nilotinib.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Cabergoline.
NitroglycerinCabergoline may decrease the vasodilatory activities of Nitroglycerin.
NortriptylineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Nortriptyline.
OctamoxinThe metabolism of Cabergoline can be decreased when combined with Octamoxin.
OlanzapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Olanzapine.
OlaparibThe metabolism of Cabergoline can be decreased when combined with Olaparib.
OmapatrilatThe serum concentration of Cabergoline can be increased when it is combined with Omapatrilat.
OndansetronThe risk or severity of adverse effects can be increased when Cabergoline is combined with Ondansetron.
OndansetronOndansetron may increase the serotonergic activities of Cabergoline.
OsanetantThe risk or severity of adverse effects can be increased when Cabergoline is combined with Osanetant.
OsimertinibThe serum concentration of Cabergoline can be increased when it is combined with Osimertinib.
OtamixabanThe serum concentration of Cabergoline can be increased when it is combined with Otamixaban.
OuabainOuabain may decrease the cardiotoxic activities of Cabergoline.
OxprenololOxprenolol may increase the vasoconstricting activities of Cabergoline.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Cabergoline.
PalbociclibThe serum concentration of Cabergoline can be increased when it is combined with Palbociclib.
PaliperidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Paliperidone.
PalonosetronPalonosetron may increase the serotonergic activities of Cabergoline.
PargylineThe metabolism of Cabergoline can be decreased when combined with Pargyline.
ParoxetineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Paroxetine.
PenbutololPenbutolol may increase the vasoconstricting activities of Cabergoline.
PentobarbitalThe metabolism of Cabergoline can be increased when combined with Pentobarbital.
PergolideCabergoline may increase the vasoconstricting activities of Pergolide.
PerindoprilThe serum concentration of Cabergoline can be increased when it is combined with Perindopril.
PerospironeThe risk or severity of adverse effects can be increased when Cabergoline is combined with Perospirone.
PerphenazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Perphenazine.
PethidineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Pethidine.
PhenelzineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Phenelzine.
PhenelzineThe metabolism of Cabergoline can be decreased when combined with Phenelzine.
PheniprazineThe metabolism of Cabergoline can be decreased when combined with Pheniprazine.
PhenobarbitalThe metabolism of Cabergoline can be increased when combined with Phenobarbital.
PhenoxypropazineThe metabolism of Cabergoline can be decreased when combined with Phenoxypropazine.
PhenylephrineCabergoline may increase the hypertensive activities of Phenylephrine.
PhenytoinThe metabolism of Cabergoline can be increased when combined with Phenytoin.
PhosphoramidonThe serum concentration of Cabergoline can be increased when it is combined with Phosphoramidon.
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.
PipotiazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Pipotiazine.
PirlindoleThe metabolism of Cabergoline can be decreased when combined with Pirlindole.
PivhydrazineThe metabolism of Cabergoline can be decreased when combined with Pivhydrazine.
PosaconazoleThe metabolism of Cabergoline can be decreased when combined with Posaconazole.
PractololPractolol may increase the vasoconstricting activities of Cabergoline.
PrimidoneThe metabolism of Cabergoline can be increased when combined with Primidone.
PrinomastatThe serum concentration of Cabergoline can be increased when it is combined with Prinomastat.
ProcarbazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Procarbazine.
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.
PromethazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Promethazine.
PropericiazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Propericiazine.
PropranololPropranolol may increase the vasoconstricting activities of Cabergoline.
ProtriptylineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Protriptyline.
PRX-00023Cabergoline may increase the vasoconstricting activities of PRX-00023.
QuetiapineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Quetiapine.
QuinaprilThe serum concentration of Cabergoline can be increased when it is combined with Quinapril.
RamiprilThe serum concentration of Cabergoline can be increased when it is combined with Ramipril.
RanolazineThe metabolism of Cabergoline can be decreased when combined with Ranolazine.
RasagilineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Rasagiline.
RasagilineThe metabolism of Cabergoline can be decreased when combined with Rasagiline.
RemikirenThe serum concentration of Cabergoline can be increased when it is combined with Remikiren.
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.
RifabutinThe metabolism of Cabergoline can be increased when combined with Rifabutin.
RifampicinThe metabolism of Cabergoline can be increased when combined with Rifampicin.
RifapentineThe metabolism of Cabergoline can be increased when combined with Rifapentine.
RisperidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Risperidone.
RitonavirThe serum concentration of Cabergoline can be increased when it is combined with Ritonavir.
RivaroxabanThe serum concentration of Cabergoline can be increased when it is combined with Rivaroxaban.
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Cabergoline.
RizatriptanCabergoline may increase the vasoconstricting activities of Rizatriptan.
RopiniroleCabergoline may increase the vasoconstricting activities of Ropinirole.
SafrazineThe metabolism of Cabergoline can be decreased when combined with Safrazine.
SaquinavirThe serum concentration of Cabergoline can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Cabergoline can be increased when it is combined with Saxagliptin.
SelegilineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Selegiline.
SelegilineThe metabolism of Cabergoline can be decreased when combined with Selegiline.
SertindoleThe risk or severity of adverse effects can be increased when Cabergoline is combined with Sertindole.
SertralineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Sertraline.
SildenafilThe metabolism of Cabergoline can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Cabergoline can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Cabergoline can be increased when it is combined with Simeprevir.
SitagliptinThe serum concentration of Cabergoline can be increased when it is combined with Sitagliptin.
SotalolSotalol may increase the vasoconstricting activities of Cabergoline.
SpiraprilThe serum concentration of Cabergoline can be increased when it is combined with Spirapril.
St. John's WortThe serum concentration of Cabergoline can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Cabergoline can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Cabergoline can be decreased when combined with Sulfisoxazole.
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Cabergoline.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Cabergoline.
SumatriptanCabergoline may increase the vasoconstricting activities of Sumatriptan.
TapentadolThe risk or severity of adverse effects can be increased when Cabergoline is combined with Tapentadol.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Cabergoline.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Cabergoline is combined with Tedizolid Phosphate.
TelaprevirThe serum concentration of Cabergoline can be increased when it is combined with Telaprevir.
TelithromycinThe metabolism of Cabergoline can be decreased when combined with Telithromycin.
TemocaprilThe serum concentration of Cabergoline can be increased when it is combined with Temocapril.
ThioproperazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Thioproperazine.
ThioridazineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Thioridazine.
ThiorphanThe serum concentration of Cabergoline can be increased when it is combined with Thiorphan.
ThiothixeneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Thiothixene.
TiclopidineThe metabolism of Cabergoline can be decreased when combined with Ticlopidine.
TimololTimolol may increase the vasoconstricting activities of Cabergoline.
TipranavirThe serum concentration of Cabergoline can be increased when it is combined with Tipranavir.
TocilizumabThe serum concentration of Cabergoline can be decreased when it is combined with Tocilizumab.
ToloxatoneThe metabolism of Cabergoline can be decreased when combined with Toloxatone.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Cabergoline.
TrandolaprilThe serum concentration of Cabergoline can be increased when it is combined with Trandolapril.
Trans-2-PhenylcyclopropylamineThe metabolism of Cabergoline can be decreased when combined with Trans-2-Phenylcyclopropylamine.
TranylcypromineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Tranylcypromine.
TranylcypromineThe metabolism of Cabergoline can be decreased when combined with Tranylcypromine.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Cabergoline.
TrazodoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Trazodone.
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.
TrimipramineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Trimipramine.
UbenimexThe serum concentration of Cabergoline can be increased when it is combined with Ubenimex.
VenlafaxineThe metabolism of Cabergoline can be decreased when combined with Venlafaxine.
VenlafaxineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Venlafaxine.
VerapamilThe metabolism of Cabergoline can be decreased when combined with Verapamil.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Cabergoline.
VilazodoneCabergoline may increase the vasoconstricting activities of Vilazodone.
VildagliptinThe serum concentration of Cabergoline can be increased when it is combined with Vildagliptin.
VoriconazoleThe metabolism of Cabergoline can be decreased when combined with Voriconazole.
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Cabergoline.
VortioxetineCabergoline may increase the vasoconstricting activities of Vortioxetine.
XimelagatranThe serum concentration of Cabergoline can be increased when it is combined with Ximelagatran.
ZiprasidoneThe risk or severity of adverse effects can be increased when Cabergoline is combined with Ziprasidone.
ZiprasidoneThe metabolism of Cabergoline can be decreased when combined with Ziprasidone.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Cabergoline.
ZolmitriptanCabergoline may increase the vasoconstricting activities of Zolmitriptan.
ZotepineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Zotepine.
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

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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  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:12464354 ]
  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:12008749 ]
  4. Pastor P, Tolosa E: [Cabergoline in the treatment of Parkinson's disease]. Neurologia. 2003 May;18(4):202-9. [PubMed:12721865 ]
  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:15341508 ]
  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:8951172 ]
  7. Ichikawa K, Kojima M: [Pharmacological effects of cabergoline against parkinsonism]. Nihon Yakurigaku Zasshi. 2001 Jun;117(6):395-400. [PubMed:11436517 ]
  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. doi: 10.1097/wnf.0b013e318067bcc4. [PubMed:18303487 ]
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 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  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:20426763 ]
  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. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
  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. doi: 10.1124/mol.109.058057. Epub 2009 Jul 1. [PubMed:19570945 ]
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 inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name:
DRD3
Uniprot ID:
P35462
Molecular Weight:
44224.335 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. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  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. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
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 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  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:20426763 ]
  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. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
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 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  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. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
  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:12388667 ]
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 ]
  2. 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:
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. 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. 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:12388667 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
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 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  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:12388667 ]
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 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  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. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
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 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  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:12388667 ]
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. 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. 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:16982285 ]
  3. Ichikawa K, Kojima M: [Pharmacological effects of cabergoline against parkinsonism]. Nihon Yakurigaku Zasshi. 2001 Jun;117(6):395-400. [PubMed:11436517 ]
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. 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. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  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:16982285 ]
  4. Ichikawa K, Kojima M: [Pharmacological effects of cabergoline against parkinsonism]. Nihon Yakurigaku Zasshi. 2001 Jun;117(6):395-400. [PubMed:11436517 ]
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 ]
  2. 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 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 ]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988 ]
  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:20426763 ]
  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. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53554.43 Da
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. doi: 10.1016/j.exer.2008.10.003. Epub 2008 Nov 1. [PubMed:18992242 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
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:12388666 ]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Protein heterodimerization activity
Specific Function:
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
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:12388666 ]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Alpha1-adrenergic receptor activity
Specific Function:
This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
Gene Name:
ADRA1D
Uniprot ID:
P25100
Molecular Weight:
60462.205 Da
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:12388666 ]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Receptor signaling protein activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
Gene Name:
ADRB1
Uniprot ID:
P08588
Molecular Weight:
51322.1 Da
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:12388666 ]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Protein homodimerization activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine.
Gene Name:
ADRB2
Uniprot ID:
P07550
Molecular Weight:
46458.32 Da
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:12388666 ]
  2. PDSP Ki Database [Link]
Kind
Protein group
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.
Components:
NameUniProt IDDetails
D(1A) dopamine receptorP21728 Details
D(1B) dopamine receptorP21918 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:12388666 ]
  2. PDSP Ki Database [Link]
22. D(2S) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
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:12388666 ]
  2. PDSP Ki Database [Link]
23. D(2L) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
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:12388666 ]
  2. PDSP Ki Database [Link]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23