Identification

Name
Pramipexole
Accession Number
DB00413  (APRD00156)
Type
Small Molecule
Groups
Approved, Investigational
Description

Pramipexole is a medication indicated for treating Parkinson's disease and restless legs syndrome (RLS). It is also sometimes used off-label as a treatment for cluster headache or to counteract the problems with low libido experienced by some users of SSRI antidepressant drugs. Pramipexole has shown robust effects on pilot studies in bipolar disorder. Pramipexole is classified as a non-ergoline dopamine agonist.

Structure
Thumb
Synonyms
  • (-)-Pramipexole
  • (S)-N  6-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine
  • 2,6-Benzothiazolediamine, 4,5,6,7-tetrahydro-N(sup 6)-propyl-, (S)-
  • Pramipexol
  • Pramipexole
  • Pramipexolum
External IDs
PNU 98528 / SND 919 Cl 2Y / SUD 919 CL 24 / U 98528 E
Product Ingredients
IngredientUNIICASInChI Key
Pramipexole dihydrochloride monohydrate3D867NP06J191217-81-9APVQOOKHDZVJEX-QTPLPEIMSA-N
Pramipexole hydrochloride4R2HD0M28N104632-25-9QMNWXHSYPXQFSK-KLXURFKVSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act PramipexoleTablet1 mgOralActavis Pharma Company2009-04-15Not applicableCanada
Act PramipexoleTablet0.25 mgOralActavis Pharma Company2009-04-15Not applicableCanada
Act PramipexoleTablet1.5 mgOralActavis Pharma Company2009-04-15Not applicableCanada
Act PramipexoleTablet0.5 mgOralActavis Pharma Company2009-04-15Not applicableCanada
MirapexTablet0.5 mgOralBoehringer Ingelheim (Canada) Ltd Ltee2000-03-17Not applicableCanada
MirapexTablet0.250 mg/1OralPhysicians Total Care, Inc.2007-03-23Not applicableUs
MirapexTablet0.25 mgOralBoehringer Ingelheim (Canada) Ltd Ltee1998-02-26Not applicableCanada
MirapexTablet0.500 mg/1OralRebel Distributors2004-01-01Not applicableUs
MirapexTablet1 mg/1OralBoehringer Ingelheim2004-01-01Not applicableUs
MirapexTablet.250 mg/1OralBoehringer Ingelheim2004-01-01Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-pramipexoleTablet1.5 mgOralApotex Corporation2007-02-26Not applicableCanada
Apo-pramipexoleTablet0.25 mgOralApotex Corporation2007-02-26Not applicableCanada
Apo-pramipexoleTablet0.75 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-pramipexoleTablet1.0 mgOralApotex Corporation2007-02-26Not applicableCanada
Apo-pramipexoleTablet0.125 mgOralApotex CorporationNot applicableNot applicableCanada
Apo-pramipexoleTablet0.5 mgOralApotex Corporation2007-02-26Not applicableCanada
Auro-pramipexoleTablet1 mgOralAuro Pharma Inc2014-04-29Not applicableCanada
Auro-pramipexoleTablet0.125 mgOralAuro Pharma Inc2014-04-29Not applicableCanada
Auro-pramipexoleTablet0.5 mgOralAuro Pharma Inc2014-04-29Not applicableCanada
Auro-pramipexoleTablet1.5 mgOralAuro Pharma Inc2014-04-29Not applicableCanada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Mirapex ERPramipexole dihydrochloride monohydrate (0.375 mg/1) + Pramipexole dihydrochloride monohydrate (0.75 mg/1) + Pramipexole dihydrochloride monohydrate (1.5 mg/1)KitBoehringer Ingelheim Pharmaceuticals, Inc.2010-02-222010-11-03Us
Mirapex ERPramipexole dihydrochloride monohydrate (0.375 mg/1) + Pramipexole dihydrochloride monohydrate (0.75 mg/1) + Pramipexole dihydrochloride monohydrate (1.5 mg/1)KitBoehringer Ingelheim Pharmaceuticals, Inc.2010-02-222010-11-03Us
Mirapex ERPramipexole dihydrochloride monohydrate (0.375 mg/1) + Pramipexole dihydrochloride monohydrate (0.75 mg/1) + Pramipexole dihydrochloride monohydrate (1.5 mg/1)KitBoehringer Ingelheim Pharmaceuticals, Inc.2010-02-222010-11-03Us
International/Other Brands
Glepark (Glenmark) / Medopexol (Medochemie) / Miramel (Clonmel) / Miraper (Specifar) / Mirapexin (Boehringer Ingelheim) / Pexola (Boehringer Ingelheim) / Sifrol (Boehringer Ingelheim) / Sifrol ER (Boehringer Ingelheim)
Categories
UNII
83619PEU5T
CAS number
104632-26-0
Weight
Average: 211.327
Monoisotopic: 211.114318249
Chemical Formula
C10H17N3S
InChI Key
FASDKYOPVNHBLU-ZETCQYMHSA-N
InChI
InChI=1S/C10H17N3S/c1-2-5-12-7-3-4-8-9(6-7)14-10(11)13-8/h7,12H,2-6H2,1H3,(H2,11,13)/t7-/m0/s1
IUPAC Name
(6S)-N6-propyl-4,5,6,7-tetrahydro-1,3-benzothiazole-2,6-diamine
SMILES
CCCN[C@H]1CCC2=C(C1)SC(N)=N2

Pharmacology

Indication

For the treatment of signs and symptoms of idiopathic Parkinson's disease

Associated Conditions
Pharmacodynamics

Pramipexole is a nonergot dopamine agonist with high relative in vitro specificity and full intrinsic activity at the D2 subfamily of dopamine receptors, binding with higher affinity to D3 than to D2 or D4 receptor subtypes. The relevance of D3 receptor binding in Parkinson's disease is unknown. The precise mechanism of action of Pramipexole as a treatment for Parkinson's disease is unknown, although it is believed to be related to its ability to stimulate dopamine receptors in the striatum. This conclusion is supported by electrophysiologic studies in animals that have demonstrated that Pramipexole influences striatal neuronal firing rates via activation of dopamine receptors in the striatum and the substantia nigra, the site of neurons that send projections to the striatum.

Mechanism of action

The precise mechanism of action of Pramipexole as a treatment for Parkinson's disease is unknown, although it is believed to be related to its ability to stimulate dopamine receptors in the striatum.

TargetActionsOrganism
AD(3) dopamine receptor
agonist
Human
AD(2) dopamine receptor
agonist
Human
AD(4) dopamine receptor
agonist
Human
UAlpha-2B adrenergic receptor
unknown
Human
U5-hydroxytryptamine receptor 1A
unknown
Human
U5-hydroxytryptamine receptor 1D
unknown
Human
UAlpha-2A adrenergic receptor
partial agonist
Human
U5-hydroxytryptamine receptor 1B
unknown
Human
U5-hydroxytryptamine receptor 2A
unknown
Human
U5-hydroxytryptamine receptor 2B
unknown
Human
U5-hydroxytryptamine receptor 2C
unknown
Human
UAlpha-2C adrenergic receptor
unknown
Human
UD(1A) dopamine receptor
unknown
Human
UD(1B) dopamine receptor
unknown
Human
Absorption

Rapid. Absolute bioavailability is greater than 90%, indicating that pramipexole is well absorbed and undergoes little presystemic metabolism. Food does not affect the extent of absorption.

Volume of distribution
  • 500 L
Protein binding

About 15% bound to plasma proteins.

Metabolism

No metabolites have been identified in plasma or urine.

Route of elimination

Urinary excretion is the major route of pramipexole elimination, with 90% of a pramipexole dose recovered in urine, almost all as unchanged drug. Nonrenal routes may contribute to a small extent to pramipexole elimination, although no metabolites have been identified in plasma or urine.

Half life

8 hours

Clearance
  • renal cl=400 mL/min
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may increase the sedative activities of Pramipexole.
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may increase the sedative activities of Pramipexole.
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may increase the sedative activities of Pramipexole.
4-Methoxyamphetamine4-Methoxyamphetamine may increase the sedative activities of Pramipexole.
5-methoxy-N,N-dimethyltryptamine5-methoxy-N,N-dimethyltryptamine may increase the sedative activities of Pramipexole.
7-Nitroindazole7-Nitroindazole may increase the sedative activities of Pramipexole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the sedative activities of Pramipexole.
AbacavirPramipexole may decrease the excretion rate of Abacavir which could result in a higher serum level.
AcarboseAcarbose may decrease the excretion rate of Pramipexole which could result in a higher serum level.
AcebutololThe risk or severity of adverse effects can be increased when Pramipexole is combined with Acebutolol.
Food Interactions
  • Take without regard to meals, however if nausea is a problem, taking the product with food may reduce its incidence.

References

Synthesis Reference
US4886812
General References
  1. Mierau J, Schneider FJ, Ensinger HA, Chio CL, Lajiness ME, Huff RM: Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors. Eur J Pharmacol. 1995 Jun 23;290(1):29-36. [PubMed:7664822]
External Links
Human Metabolome Database
HMDB0014557
KEGG Drug
D00559
PubChem Compound
119570
PubChem Substance
46505897
ChemSpider
106770
BindingDB
50116766
ChEBI
8356
ChEMBL
CHEMBL301265
Therapeutic Targets Database
DAP000019
PharmGKB
PA164742949
IUPHAR
953
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Pramipexole
ATC Codes
N04BC05 — Pramipexole
AHFS Codes
  • 28:36.20.08 — Nonergot-derivative Dopamine Receptor Agonists

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingTreatmentExtrapyramidal Syndrome1
1CompletedNot AvailableCocaine Abuse / Dependence, Cocaine / Substance Abuse1
1CompletedNot AvailableHealthy Volunteers2
1CompletedTreatmentHealthy Volunteers5
1CompletedTreatmentObsessive Compulsive Disorder (OCD)1
1CompletedTreatmentParkinson's Disease (PD)1
2CompletedDiagnosticParkinson's Disease (PD) / Parkinsonian Syndromes1
2CompletedTreatmentBipolar Disorder (BD)1
2CompletedTreatmentDepression, Bipolar1
2CompletedTreatmentGilles de la Tourette's Syndrome1
2CompletedTreatmentMajor Depressive Disorder (MDD)1
2CompletedTreatmentRestless Legs Syndrome (RLS)2
2TerminatedTreatmentAdvanced Stage Parkinson's Disease1
2TerminatedTreatmentFibromyalgia1
2Unknown StatusTreatmentParkinson's Disease (PD)1
2, 3CompletedTreatmentParkinson's Disease (PD)1
3CompletedTreatmentEarly Parkinson Disease (Early PD)1
3CompletedTreatmentEarly Stage Parkinson's Disease1
3CompletedTreatmentIdiopathic Parkinson's Disease1
3CompletedTreatmentIdiopathic Restless Legs Syndrome2
3CompletedTreatmentParkinson's Disease (PD)10
3CompletedTreatmentRestless Legs Syndrome (RLS)6
3Not Yet RecruitingTreatmentTremor, Essential1
3RecruitingTreatmentParkinson's Disease (PD)1
3Unknown StatusTreatmentSchizoaffective Disorders / Schizophrenic Disorders1
3WithdrawnTreatmentBinge Eating Disorder (BED)1
4Active Not RecruitingOtherMajor Depressive Disorder (MDD)1
4CompletedNot AvailableDepression / Parkinson's Disease (PD)1
4CompletedNot AvailableParkinson's Disease (PD)1
4CompletedDiagnosticParkinson's Disease (PD)1
4CompletedOtherRestless Legs Syndrome (RLS)1
4CompletedTreatmentBipolar Disorder (BD)1
4CompletedTreatmentDepression2
4CompletedTreatmentDepression / Parkinson's Disease (PD)1
4CompletedTreatmentDepression / Restless Legs Syndrome (RLS)1
4CompletedTreatmentParkinson's Disease (PD)4
4CompletedTreatmentRestless Legs Syndrome (RLS)4
4RecruitingTreatmentBipolar Disorder (BD)1
4RecruitingTreatmentParkinson's Disease (PD)1
4SuspendedTreatmentHealthy Volunteers1
4TerminatedTreatmentEarly-Stage Parkinson's Disease1
4Unknown StatusTreatmentParkinson's Disease (PD)1
Not AvailableCompletedNot AvailableHealthy Volunteers1
Not AvailableCompletedNot AvailableHeart Failure, Unspecified1
Not AvailableCompletedNot AvailableParkinson's Disease (PD)9
Not AvailableCompletedNot AvailableRestless Legs Syndrome (RLS)3
Not AvailableCompletedTreatmentIdiopathic Parkinson's Disease1
Not AvailableRecruitingNot AvailableAtypical Parkinson Disease / Corticobasal Degeneration / Gait, Frontal / Multiple System Atrophy (MSA) / Parkinson's Disease (PD) / Parkinsonian Disorders / Progressive Supranuclear Palsy (PSP)1
Not AvailableRecruitingBasic ScienceDopamine / Emotions / Motivation / Pramipexole / Reward1

Pharmacoeconomics

Manufacturers
  • Boehringer ingelheim
Packagers
  • Barr Pharmaceuticals
  • Boehringer Ingelheim Ltd.
  • Cardinal Health
  • Kaiser Foundation Hospital
  • Murfreesboro Pharmaceutical Nursing Supply
  • Pfizer Inc.
  • Pharmacia Inc.
  • Physicians Total Care Inc.
  • Rebel Distributors Corp.
  • Resource Optimization and Innovation LLC
  • Sandoz
  • Stat Rx Usa
  • Teva Pharmaceutical Industries Ltd.
  • Vangard Labs Inc.
  • Zydus Pharmaceuticals
Dosage forms
FormRouteStrength
TabletOral0.75 mg
TabletOral.250 mg/1
TabletOral.500 mg/1
TabletOral.750 mg/1
TabletOral0.125 mg
TabletOral0.25 mg
TabletOral0.250 mg/1
TabletOral0.5 mg
TabletOral0.500 mg/1
TabletOral1.0 mg
TabletOral1.5 mg
Kit
TabletOral0.088 mg
TabletOral0.18 mg
TabletOral0.35 mg
TabletOral0.7 mg
TabletOral1.1 mg
Tablet, extended releaseOral0.26 mg
Tablet, extended releaseOral0.52 mg
Tablet, extended releaseOral1.05 mg
Tablet, extended releaseOral1.57 mg
Tablet, extended releaseOral2.1 mg
Tablet, extended releaseOral2.62 mg
Tablet, extended releaseOral3.15 mg
TabletOral0.50 mg
TabletOral1 mg
TabletOral0.125 mg/1
TabletOral0.25 mg/1
TabletOral0.5 mg/1
TabletOral0.75 mg/1
TabletOral1 mg/1
TabletOral1.5 mg/1
Tablet, extended releaseOral0.375 mg/1
Tablet, extended releaseOral2.25 mg/1
Tablet, extended releaseOral3.75 mg/1
Tablet, extended releaseOral0.75 mg/1
Tablet, extended releaseOral1.5 mg/1
Tablet, extended releaseOral3 mg/1
Tablet, extended releaseOral4.5 mg/1
Prices
Unit descriptionCostUnit
Mirapex er 0.375 mg tablet9.83USD tablet
Mirapex er 0.75 mg tablet9.83USD tablet
Mirapex er 1.5 mg tablet9.83USD tablet
Mirapex er 3 mg tablet9.83USD tablet
Mirapex er 4.5 mg tablet9.83USD tablet
Mirapex 0.125 mg tablet3.48USD tablet
Mirapex 0.25 mg tablet3.42USD tablet
Mirapex 0.5 mg tablet3.42USD tablet
Mirapex 1 mg tablet3.42USD tablet
Mirapex 1.5 mg tablet3.42USD tablet
Mirapex 0.75 mg tablet3.28USD tablet
Pramipexole Dihydrochloride 0.125 mg tablet3.07USD tablet
Pramipexole Dihydrochloride 0.25 mg tablet3.07USD tablet
Pramipexole Dihydrochloride 0.5 mg tablet3.07USD tablet
Pramipexole Dihydrochloride 1 mg tablet3.07USD tablet
Pramipexole Dihydrochloride 1.5 mg tablet3.07USD tablet
Pramipexole di-hcl 0.125 mg tablet2.95USD tablet
Pramipexole di-hcl 0.25 mg tablet2.95USD tablet
Pramipexole di-hcl 0.5 mg tablet2.95USD tablet
Pramipexole di-hcl 1 mg tablet2.95USD tablet
Pramipexole di-hcl 1.5 mg tablet2.95USD tablet
Mirapex 1 mg Tablet2.2USD tablet
Mirapex 1.5 mg Tablet2.2USD tablet
Apo-Pramipexole 1 mg Tablet1.23USD tablet
Apo-Pramipexole 1.5 mg Tablet1.23USD tablet
Co Pramipexole 1 mg Tablet1.23USD tablet
Co Pramipexole 1.5 mg Tablet1.23USD tablet
Novo-Pramipexole 1 mg Tablet1.23USD tablet
Novo-Pramipexole 1.5 mg Tablet1.23USD tablet
Pms-Pramipexole 1 mg Tablet1.23USD tablet
Pms-Pramipexole 1.5 mg Tablet1.23USD tablet
Sandoz Pramipexole 1 mg Tablet1.23USD tablet
Sandoz Pramipexole 1.5 mg Tablet1.23USD tablet
Mirapex 0.25 mg Tablet1.1USD tablet
Apo-Pramipexole 0.25 mg Tablet0.62USD tablet
Co Pramipexole 0.25 mg Tablet0.62USD tablet
Novo-Pramipexole 0.25 mg Tablet0.62USD tablet
Pms-Pramipexole 0.25 mg Tablet0.62USD tablet
Sandoz Pramipexole 0.25 mg Tablet0.62USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US4886812No1993-10-082010-10-08Us
CA2275379No2006-11-282018-01-16Canada
US6001861No1998-01-162018-01-16Us
US6194445No1998-01-162018-01-16Us
US8679533No2009-09-082029-09-08Us
US7695734No2008-04-262028-04-26Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP0.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.14 mg/mLALOGPS
logP2.18ALOGPS
logP1.76ChemAxon
logS-3.2ALOGPS
pKa (Strongest Acidic)17.66ChemAxon
pKa (Strongest Basic)10.31ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area50.94 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity59.77 m3·mol-1ChemAxon
Polarizability24.47 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9967
Blood Brain Barrier+0.9631
Caco-2 permeable-0.6419
P-glycoprotein substrateSubstrate0.6384
P-glycoprotein inhibitor INon-inhibitor0.842
P-glycoprotein inhibitor IINon-inhibitor0.7464
Renal organic cation transporterNon-inhibitor0.6788
CYP450 2C9 substrateNon-substrate0.8524
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.7558
CYP450 1A2 substrateInhibitor0.9179
CYP450 2C9 inhibitorNon-inhibitor0.7353
CYP450 2D6 inhibitorInhibitor0.5364
CYP450 2C19 inhibitorInhibitor0.586
CYP450 3A4 inhibitorNon-inhibitor0.6708
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7797
Ames testNon AMES toxic0.8133
CarcinogenicityNon-carcinogens0.915
BiodegradationNot ready biodegradable0.9255
Rat acute toxicity2.8676 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8732
hERG inhibition (predictor II)Non-inhibitor0.8397
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as aralkylamines. These are alkylamines in which the alkyl group is substituted at one carbon atom by an aromatic hydrocarbyl group.
Kingdom
Organic compounds
Super Class
Organic nitrogen compounds
Class
Organonitrogen compounds
Sub Class
Amines
Direct Parent
Aralkylamines
Alternative Parents
Thiazoles / Heteroaromatic compounds / Isothioureas / Dialkylamines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Aralkylamine / Heteroaromatic compound / Thiazole / Azole / Isothiourea / Azacycle / Organoheterocyclic compound / Secondary amine / Secondary aliphatic amine / Organopnictogen compound
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
benzothiazoles, diamine (CHEBI:8356)

Targets

Details
1. D(3) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  3. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988]
Details
2. D(2) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  3. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988]
Details
3. D(4) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Sh3 domain binding
Specific Function
Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins ...
Gene Name
DRD4
Uniprot ID
P21917
Uniprot Name
D(4) dopamine receptor
Molecular Weight
48359.86 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Unknown
General Function
Epinephrine binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  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
Unknown
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  2. 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
Unknown
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1D
Uniprot ID
P28221
Uniprot Name
5-hydroxytryptamine receptor 1D
Molecular Weight
41906.38 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  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
Partial agonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  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
Unknown
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive subst...
Gene Name
HTR1B
Uniprot ID
P28222
Uniprot Name
5-hydroxytryptamine receptor 1B
Molecular Weight
43567.535 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  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
Unknown
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  2. 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
Unknown
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation...
Gene Name
HTR2B
Uniprot ID
P41595
Uniprot Name
5-hydroxytryptamine receptor 2B
Molecular Weight
54297.41 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  2. 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
Unknown
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  2. 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
Unknown
General Function
Protein homodimerization activity
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name
ADRA2C
Uniprot ID
P18825
Uniprot Name
Alpha-2C adrenergic receptor
Molecular Weight
49521.585 Da
References
  1. Kvernmo T, Houben J, Sylte I: Receptor-binding and pharmacokinetic properties of dopaminergic agonists. Curr Top Med Chem. 2008;8(12):1049-67. [PubMed:18691132]
  2. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988]
Details
13. D(1A) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Unknown
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD1
Uniprot ID
P21728
Uniprot Name
D(1A) dopamine receptor
Molecular Weight
49292.765 Da
References
  1. 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
Unknown
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name
DRD5
Uniprot ID
P21918
Uniprot Name
D(1B) dopamine receptor
Molecular Weight
52950.5 Da
References
  1. Lam YW: Clinical pharmacology of dopamine agonists. Pharmacotherapy. 2000 Jan;20(1 Pt 2):17S-25S. [PubMed:10641988]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. Ishiguro N, Saito A, Yokoyama K, Morikawa M, Igarashi T, Tamai I: Transport of the dopamine D2 agonist pramipexole by rat organic cation transporters OCT1 and OCT2 in kidney. Drug Metab Dispos. 2005 Apr;33(4):495-9. Epub 2005 Jan 7. [PubMed:15640376]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Secondary active organic cation transmembrane transporter activity
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. Ishiguro N, Saito A, Yokoyama K, Morikawa M, Igarashi T, Tamai I: Transport of the dopamine D2 agonist pramipexole by rat organic cation transporters OCT1 and OCT2 in kidney. Drug Metab Dispos. 2005 Apr;33(4):495-9. Epub 2005 Jan 7. [PubMed:15640376]

Drug created on June 13, 2005 07:24 / Updated on November 14, 2018 12:41