Identification

Name
Dipyridamole
Accession Number
DB00975
Description

A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752)

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 504.6256
Monoisotopic: 504.317251808
Chemical Formula
C24H40N8O4
Synonyms
  • Dipiridamol
  • Dipyridamine
  • Dipyridamole
  • Dipyridamolum
  • Dipyudamine
  • Dypyridamol
External IDs
  • NSC-515776
  • USAF GE-12

Pharmacology

Indication

For as an adjunct to coumarin anticoagulants in the prevention of postoperative thromboembolic complications of cardiac valve replacement and also used in prevention of angina.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

Dipyridamole, a non-nitrate coronary vasodilator that also inhibits platelet aggregation, is combined with other anticoagulant drugs, such as warfarin, to prevent thrombosis in patients with valvular or vascular disorders. Dipyridamole is also used in myocardial perfusion imaging, as an antiplatelet agent, and in combination with aspirin for stroke prophylaxis.

Mechanism of action

Dipyridamole likely inhibits both adenosine deaminase and phosphodiesterase, preventing the degradation of cAMP, an inhibitor of platelet function. This elevation in cAMP blocks the release of arachidonic acid from membrane phospholipids and reduces thromboxane A2 activity. Dipyridamole also directly stimulates the release of prostacyclin, which induces adenylate cyclase activity, thereby raising the intraplatelet concentration of cAMP and further inhibiting platelet aggregation.

TargetActionsOrganism
AcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
inhibitor
Humans
AAdenosine deaminase
inhibitor
Humans
AcGMP-specific 3',5'-cyclic phosphodiesterase
inhibitor
Humans
AcAMP-specific 3',5'-cyclic phosphodiesterase 4A
inhibitor
Humans
UCalcipressin-1Not AvailableHumans
UAlpha-1-acid glycoprotein 1Not AvailableHumans
Absorption

70%

Volume of distribution
  • 1 to 2.5 L/kg
Protein binding

99%

Metabolism

hepatic

Route of elimination

Dipyridamole is metabolized in the liver to the glucuronic acid conjugate and excreted with the bile.

Half-life

40 minutes

Clearance
  • 2.3-3.5 mL/min/kg
Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

Hypotension, if it occurs, is likely to be of short duration, but a vasopressor drug may be used if necessary. The oral LD50 in rats is greater than 6,000 mg/kg while in the dogs, the oral LD50 is approximately 400 mg/kg. LD50=8.4g/kg (orally in rat)

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Dipyridamole (Antiplatelet) Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Dipyridamole.
AcebutololDipyridamole may increase the bradycardic activities of Acebutolol.
AceclofenacThe risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Dipyridamole.
AcemetacinThe risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Dipyridamole.
AcenocoumarolThe risk or severity of bleeding can be increased when Dipyridamole is combined with Acenocoumarol.
AdenosineThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Adenosine.
Albutrepenonacog alfaThe therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Dipyridamole.
AlclofenacThe risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Dipyridamole.
AldesleukinThe risk or severity of bleeding can be increased when Dipyridamole is combined with Aldesleukin.
AlemtuzumabThe risk or severity of bleeding can be increased when Dipyridamole is combined with Alemtuzumab.
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    Severity
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    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level
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Food Interactions
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • Avoid xanthines. Xanthines, found in coffee and tea, can reduce the effectiveness of this medication.
  • Take with or without food. Taking dipyridamole extrended release capusels with a high-fat meal minimally reduces it's AUC and Cmax.

Products

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Product Images
International/Other Brands
Agilease (lsei) / Cardoxin (Rafa) / Cleridium 150 (Millot) / Curantyl (Arzneimittelwerk) / Persantin
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
DipyridamoleInjection, solution5 mg/1mLIntravenousHospira, Inc.2006-04-07Not applicableUS flag
DipyridamoleSolution5 mg/1mLIntravenousAnazao Health Corporation2012-05-23Not applicableUS flag
DipyridamoleInjection, solution5 mg/1mLIntravenousHospira, Inc.2006-04-07Not applicableUS flag
Dipyridamole 25 Tab 25mgTabletOralPro Doc Limitee1983-12-312002-08-02Canada flag
Dipyridamole 50 Tab 50mgTabletOralPro Doc Limitee1983-12-312002-08-02Canada flag
Dipyridamole 75 TabTabletOralPro Doc Limitee1984-12-312002-08-02Canada flag
Dipyridamole for InjectionSolutionIntravenousNovopharm Limited2002-04-302018-05-07Canada flag
Dipyridamole Injection, USPLiquidIntravenousFresenius Kabi2002-04-23Not applicableCanada flag
Dipyridamole-25TabletOralPro Doc Limitee1998-08-282010-07-13Canada flag
Dipyridamole-50TabletOralPro Doc Limitee1998-08-282010-07-13Canada flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

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

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  • Product Code
    Product Code
    Available for Purchase

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

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-dipyridamole-FC Tab 25mgTabletOralApotex Corporation1990-12-31Not applicableCanada flag
Apo-dipyridamole-FC Tab 50mgTabletOralApotex Corporation1990-12-31Not applicableCanada flag
Apo-dipyridamole-FC Tab 75mgTabletOralApotex Corporation1990-12-31Not applicableCanada flag
Apo-dipyridamole-SC Tab 25mgTabletOralApotex Corporation1982-12-31Not applicableCanada flag
Apo-dipyridamole-SC Tab 50mgTabletOralApotex Corporation1982-12-31Not applicableCanada flag
Apo-dipyridamole-SC Tab 75mgTabletOralApotex Corporation1984-12-31Not applicableCanada flag
DipyridamoleTablet, film coated50 mg/1OralAvera McKennan Hospital2016-03-292017-05-24US flag
DipyridamoleTablet, film coated75 mg/1OralLannett Company, Inc.2008-04-23Not applicableUS flag
DipyridamoleTablet, film coated25 mg/1OralPhysicians Total Care, Inc.2009-08-072013-06-30US flag
DipyridamoleTablet25 mg/1OralCarilion Materials Management2012-02-15Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

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

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  • Product Code
    Product Code
    Available for Purchase

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
AggrenoxDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)Capsule, extended releaseOralCarilion Materials Management1999-12-19Not applicableUS flag00597 0001 60 nlmimage10 7303b9ed
AggrenoxDipyridamole (200 mg) + Acetylsalicylic acid (25 mg)Capsule, extended releaseOralBoehringer Ingelheim (Canada) Ltd Ltee2000-04-172020-02-24Canada flag
AggrenoxDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)Capsule, extended releaseOralBoehringer Ingelheim Pharmaceuticals, Inc.1999-12-19Not applicableUS flag0597 000120180907 15195 qvauis
AggrenoxDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)CapsuleOralPhysicians Total Care, Inc.2004-08-24Not applicableUS flag54868 514320180907 15195 14ldz57
AggrenoxDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)CapsuleOralRebel Distributors1999-12-19Not applicableUS flag
Asasantine CapDipyridamole (75 mg) + Acetylsalicylic acid (330 mg)CapsuleOralBoehringer Ingelheim (Canada) Ltd Ltee1983-12-312000-07-31Canada flag
Aspirin and DipyridamoleDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)Capsule, extended releaseOralDr. Reddy's Laboratories Inc2018-10-10Not applicableUS flag
Aspirin and DipyridamoleDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)Capsule, extended releaseOralSlate Run Pharmaceuticals, Llc2018-08-23Not applicableUS flag
Aspirin and DipyridamoleDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)Capsule, extended releaseOralTeva Pharmaceuticals USA, Inc.2015-07-012019-09-30US flag00093 3040 06 nlmimage10 f343f9ef
Aspirin and DipyridamoleDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)CapsuleOralSandoz Inc2020-07-24Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
DipyridamoleDipyridamole (5 mg/1mL)SolutionIntravenousAnazao Health Corporation2012-05-23Not applicableUS flag

Categories

ATC Codes
B01AC07 — Dipyridamole
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as dialkylarylamines. These are aliphatic aromatic amines in which the amino group is linked to two aliphatic chains and one aromatic group.
Kingdom
Organic compounds
Super Class
Organic nitrogen compounds
Class
Organonitrogen compounds
Sub Class
Amines
Direct Parent
Dialkylarylamines
Alternative Parents
Aminopyrimidines and derivatives / Piperidines / Imidolactams / Heteroaromatic compounds / Azacyclic compounds / Alkanolamines / Primary alcohols / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Alcohol / Alkanolamine / Aminopyrimidine / Aromatic heteropolycyclic compound / Azacycle / Dialkylarylamine / Heteroaromatic compound / Hydrocarbon derivative / Imidolactam / Organic oxygen compound
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
piperidines, tertiary amino compound, tetrol, pyrimidopyrimidine (CHEBI:4653)

Chemical Identifiers

UNII
64ALC7F90C
CAS number
58-32-2
InChI Key
IZEKFCXSFNUWAM-UHFFFAOYSA-N
InChI
InChI=1S/C24H40N8O4/c33-15-11-31(12-16-34)23-26-20-19(21(27-23)29-7-3-1-4-8-29)25-24(32(13-17-35)14-18-36)28-22(20)30-9-5-2-6-10-30/h33-36H,1-18H2
IUPAC Name
2-({6-[bis(2-hydroxyethyl)amino]-4,8-bis(piperidin-1-yl)-[1,3]diazino[5,4-d]pyrimidin-2-yl}(2-hydroxyethyl)amino)ethan-1-ol
SMILES
OCCN(CCO)C1=NC2=C(N=C(N=C2N2CCCCC2)N(CCO)CCO)C(=N1)N1CCCCC1

References

Synthesis Reference

Minutza Leibovici, Itamar Kanari, Michael Fox, "Dipyridamole extended-release formulations and process for preparing same." U.S. Patent US20070184110, issued August 09, 2007.

US20070184110
General References
  1. Diener HC, Cunha L, Forbes C, Sivenius J, Smets P, Lowenthal A: European Stroke Prevention Study. 2. Dipyridamole and acetylsalicylic acid in the secondary prevention of stroke. J Neurol Sci. 1996 Nov;143(1-2):1-13. [PubMed:8981292]
Human Metabolome Database
HMDB0015110
KEGG Drug
D00302
PubChem Compound
3108
PubChem Substance
46506292
ChemSpider
2997
BindingDB
23620
RxNav
3521
ChEBI
4653
ChEMBL
CHEMBL932
ZINC
ZINC000000643046
Therapeutic Targets Database
DNC001625
PharmGKB
PA449367
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Dipyridamole
AHFS Codes
  • 24:12.92 — Miscellaneous Vasodilatating Agents
FDA label
Download (48.7 KB)
MSDS
Download (73.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableDiabetes1
4CompletedPreventionArteriosclerosis / Ischemia, Brain / Transient Ischemic Attack (TIA)1
4CompletedPreventionAtherosclerosis / Coronary Heart Disease (CHD) / Percutaneous Transluminal Coronary Angioplasty1
4CompletedPreventionCardiovascular Heart Disease / Ischemic Heart Disease1
4CompletedPreventionEndotoxaemia1
4CompletedPreventionStroke1
4CompletedTreatmentAtherosclerosis / Ischemia-Reperfusion Injury1
4CompletedTreatmentCardiovascular Heart Disease / Ischemia-Reperfusion Injury1
4CompletedTreatmentCerebrovascular Accident1
4CompletedTreatmentCoronary Arteriosclerosis1

Pharmacoeconomics

Manufacturers
  • App pharmaceuticals llc
  • Baxter healthcare corp anesthesia and critical care
  • Bedford laboratories div ben venue laboratories inc
  • Claris lifesciences ltd
  • Hospira inc
  • Teva parenteral medicines inc
  • Boehringer ingelheim pharmaceuticals inc
  • Actavis totowa llc
  • Barr laboratories inc
  • Glenmark generics inc usa
  • Impax laboratories inc
  • Lannett holdings inc
  • Murty pharmaceuticals inc
  • Purepac pharmaceutical co
  • Sandoz inc
  • Watson laboratories inc
  • Zydus pharmaceuticals usa inc
  • Boehringer Ingelheim Pharmaceuticals, Inc
Packagers
  • Amerisource Health Services Corp.
  • Apotex Inc.
  • APP Pharmaceuticals
  • Avkare Incorporated
  • Barr Pharmaceuticals
  • Baxter International Inc.
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Boehringer Ingelheim Ltd.
  • Cadila Healthcare Ltd.
  • Cardinal Health
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • General Injectables and Vaccines Inc.
  • Glenmark Generics Ltd.
  • Global Pharmaceuticals
  • Group Health Cooperative
  • H and H Laboratories
  • Heartland Repack Services LLC
  • Hospira Inc.
  • Impax Laboratories Inc.
  • Kaiser Foundation Hospital
  • Lake Erie Medical and Surgical Supply
  • Lannett Co. Inc.
  • Major Pharmaceuticals
  • Mallinckrodt Inc.
  • Mead Johnson and Co.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Murty Pharmaceuticals Inc.
  • Novex Pharma
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Physicians Total Care Inc.
  • Prepak Systems Inc.
  • Qualitest
  • Rebel Distributors Corp.
  • Resource Optimization and Innovation LLC
  • Rising Pharmaceuticals
  • Sandhills Packaging Inc.
  • Sicor Pharmaceuticals
  • Southwood Pharmaceuticals
  • Spectrum Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
  • UDL Laboratories
  • Vangard Labs Inc.
  • Zydus Pharmaceuticals
Dosage Forms
FormRouteStrength
CapsuleOral
CapsuleOral200 MG
Capsule, extended releaseOral
Capsule, extended releaseOral25 mg
Capsule75 mg
TabletOral
Capsule, delayed releaseOral200 mg
SolutionIntravenous10 mg
InjectionIntravenous5 mg/1mL
Injection, solutionIntravenous5 mg/1mL
SolutionIntravenous5 mg/1mL
TabletOral25 mg/1
TabletOral50 mg/1
TabletOral75 mg/1
Tablet, film coatedOral25 mg/1
Tablet, film coatedOral50 mg/1
Tablet, film coatedOral75 mg/1
SolutionIntravenous
LiquidIntravenous
Tablet, film coatedOral75 mg
TabletOral75 MG
Capsule200 MG
Injection, solutionIntravenous10 MG/2ML
Pill75 MG
Tablet, coatedOral25 MG
Tablet, coatedOral75 MG
SolutionIntravenous; Parenteral10 mg
SolutionIntravenous5 mg
Tablet, coatedOral25 mg/1
Tablet, coatedOral50 mg/1
Tablet, coatedOral75 mg/1
Prices
Unit descriptionCostUnit
Dipyridamole powder5.34USD g
Aggrenox capsule sa3.25USD capsule
Aggrenox 25-200 mg 12 Hour Capsule3.0USD capsule
Dipyridamole 5 mg/ml ampul1.5USD ml
Persantine 75 mg tablet1.46USD tablet
Dipyridamole 5 mg/ml vial1.32USD ml
Dipyridamole 75 mg tablet1.28USD tablet
Persantine 50 mg tablet1.09USD tablet
Dipyridamole 50 mg tablet0.96USD tablet
Persantine 25 mg tablet0.89USD tablet
Dipyridamole 25 mg tablet0.58USD tablet
Apo-Dipyridamole (Fc) 75 mg Tablet0.46USD tablet
Apo-Dipyridamole (Fc) 50 mg Tablet0.31USD tablet
Apo-Dipyridamole (Fc) 25 mg Tablet0.28USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6015577No2000-01-182017-01-18US flag
Additional Data Available
  • Filed On
    Filed On
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Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)163 °CPhysProp
water solubilitySlightlyNot Available
logP1.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.922 mg/mLALOGPS
logP1.52ALOGPS
logP1.81ChemAxon
logS-2.7ALOGPS
pKa (Strongest Acidic)14.97ChemAxon
pKa (Strongest Basic)6.59ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count12ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area145.44 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity142.78 m3·mol-1ChemAxon
Polarizability56.94 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9917
Blood Brain Barrier-0.6246
Caco-2 permeable-0.7261
P-glycoprotein substrateSubstrate0.7696
P-glycoprotein inhibitor INon-inhibitor0.5321
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterNon-inhibitor0.615
CYP450 2C9 substrateNon-substrate0.8345
CYP450 2D6 substrateNon-substrate0.6825
CYP450 3A4 substrateNon-substrate0.6849
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorInhibitor0.8045
CYP450 2D6 inhibitorInhibitor0.7201
CYP450 2C19 inhibitorNon-inhibitor0.957
CYP450 3A4 inhibitorInhibitor0.6789
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7806
Ames testNon AMES toxic0.7009
CarcinogenicityNon-carcinogens0.8884
BiodegradationNot ready biodegradable0.988
Rat acute toxicity2.1167 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.5271
hERG inhibition (predictor II)Non-inhibitor0.633
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udl-0291000000-2fc7956fe6ea13c73317
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0001190000-346cf73a19cbefa2dc11
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-0013490000-839580758bc83767be8f
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udl-0291000000-caeb14eb3ea863e020a0
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4i-1348890000-aa1e3a113b8c2768cb08

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. Can hydrolyze both cAMP and cGMP, but has higher affinity for cAMP and is more efficient wit...
Gene Name
PDE10A
Uniprot ID
Q9Y233
Uniprot Name
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Molecular Weight
88411.71 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Fujishige K, Kotera J, Michibata H, Yuasa K, Takebayashi S, Okumura K, Omori K: Cloning and characterization of a novel human phosphodiesterase that hydrolyzes both cAMP and cGMP (PDE10A). J Biol Chem. 1999 Jun 25;274(26):18438-45. [PubMed:10373451]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Zinc ion binding
Specific Function
Catalyzes the hydrolytic deamination of adenosine and 2-deoxyadenosine. Plays an important role in purine metabolism and in adenosine homeostasis. Modulates signaling by extracellular adenosine, an...
Gene Name
ADA
Uniprot ID
P00813
Uniprot Name
Adenosine deaminase
Molecular Weight
40764.13 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP (PubMed:9714779, ...
Gene Name
PDE5A
Uniprot ID
O76074
Uniprot Name
cGMP-specific 3',5'-cyclic phosphodiesterase
Molecular Weight
99984.14 Da
References
  1. Kulkarni SK, Patil CS: Phosphodiesterase 5 enzyme and its inhibitors: update on pharmacological and therapeutical aspects. Methods Find Exp Clin Pharmacol. 2004 Dec;26(10):789-99. [PubMed:15672122]
  2. Santini F, Casali G, Franchi G, Auriemma S, Lusini M, Barozzi L, Favaro A, Messina A, Mazzucco A: Hemodynamic effects of inhaled nitric oxide and phosphodiesterase inhibitor (dipyridamole) on secondary pulmonary hypertension following heart valve surgery in adults. Int J Cardiol. 2005 Aug 18;103(2):156-63. [PubMed:16080974]
  3. Kruuse C, Lassen LH, Iversen HK, Oestergaard S, Olesen J: Dipyridamole may induce migraine in patients with migraine without aura. Cephalalgia. 2006 Aug;26(8):925-33. [PubMed:16886928]
  4. Jackson EK, Ren J, Zacharia LC, Mi Z: Characterization of renal ecto-phosphodiesterase. J Pharmacol Exp Ther. 2007 May;321(2):810-5. Epub 2007 Feb 16. [PubMed:17308037]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes.
Gene Name
PDE4A
Uniprot ID
P27815
Uniprot Name
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Molecular Weight
98142.155 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Inhibits calcineurin-dependent transcriptional responses by binding to the catalytic domain of calcineurin A. Could play a role during central nervous system development.
Specific Function
Calcium-dependent protein serine/threonine phosphatase regulator activity
Gene Name
RCAN1
Uniprot ID
P53805
Uniprot Name
Calcipressin-1
Molecular Weight
28078.425 Da
References
  1. Mulero MC, Aubareda A, Orzaez M, Messeguer J, Serrano-Candelas E, Martinez-Hoyer S, Messeguer A, Perez-Paya E, Perez-Riba M: Inhibiting the calcineurin-NFAT (nuclear factor of activated T cells) signaling pathway with a regulator of calcineurin-derived peptide without affecting general calcineurin phosphatase activity. J Biol Chem. 2009 Apr 3;284(14):9394-401. doi: 10.1074/jbc.M805889200. Epub 2009 Feb 3. [PubMed:19189965]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
Molecular Weight
23511.38 Da
References
  1. Herve F, Duche JC, d'Athis P, Marche C, Barre J, Tillement JP: Binding of disopyramide, methadone, dipyridamole, chlorpromazine, lignocaine and progesterone to the two main genetic variants of human alpha 1-acid glycoprotein: evidence for drug-binding differences between the variants and for the presence of two separate drug-binding sites on alpha 1-acid glycoprotein. Pharmacogenetics. 1996 Oct;6(5):403-15. [PubMed:8946472]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Atpase activity, coupled to transmembrane movement of substances
Specific Function
May be an organic anion pump relevant to cellular detoxification.
Gene Name
ABCC4
Uniprot ID
O15439
Uniprot Name
Multidrug resistance-associated protein 4
Molecular Weight
149525.33 Da
References
  1. van Aubel RA, Smeets PH, Peters JG, Bindels RJ, Russel FG: The MRP4/ABCC4 gene encodes a novel apical organic anion transporter in human kidney proximal tubules: putative efflux pump for urinary cAMP and cGMP. J Am Soc Nephrol. 2002 Mar;13(3):595-603. [PubMed:11856762]
  2. Reid G, Wielinga P, Zelcer N, De Haas M, Van Deemter L, Wijnholds J, Balzarini J, Borst P: Characterization of the transport of nucleoside analog drugs by the human multidrug resistance proteins MRP4 and MRP5. Mol Pharmacol. 2003 May;63(5):1094-103. [PubMed:12695538]
  3. Rius M, Nies AT, Hummel-Eisenbeiss J, Jedlitschky G, Keppler D: Cotransport of reduced glutathione with bile salts by MRP4 (ABCC4) localized to the basolateral hepatocyte membrane. Hepatology. 2003 Aug;38(2):374-84. [PubMed:12883481]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Organic anion transmembrane transporter activity
Specific Function
Acts as a multispecific organic anion pump which can transport nucleotide analogs.
Gene Name
ABCC5
Uniprot ID
O15440
Uniprot Name
Multidrug resistance-associated protein 5
Molecular Weight
160658.8 Da
References
  1. Reid G, Wielinga P, Zelcer N, De Haas M, Van Deemter L, Wijnholds J, Balzarini J, Borst P: Characterization of the transport of nucleoside analog drugs by the human multidrug resistance proteins MRP4 and MRP5. Mol Pharmacol. 2003 May;63(5):1094-103. [PubMed:12695538]
Details
3. P-glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [PubMed:11602674]
  2. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. [PubMed:11716514]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. [PubMed:22541068]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. [PubMed:22541068]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name
SLCO2B1
Uniprot ID
O94956
Uniprot Name
Solute carrier organic anion transporter family member 2B1
Molecular Weight
76709.98 Da
References
  1. Karlgren M, Vildhede A, Norinder U, Wisniewski JR, Kimoto E, Lai Y, Haglund U, Artursson P: Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63. doi: 10.1021/jm300212s. Epub 2012 May 15. [PubMed:22541068]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [PubMed:24014644]

Drug created on June 13, 2005 07:24 / Updated on November 25, 2020 08:53

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