Identification

Name
Dipyridamole
Accession Number
DB00975  (APRD00360)
Type
Small Molecule
Groups
Approved
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)

Structure
Thumb
Synonyms
  • Dipiridamol
  • Dipyridamine
  • Dipyridamole
  • Dipyridamolum
  • Dipyudamine
  • Dypyridamol
External IDs
NSC-515776 / USAF GE-12
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DipyridamoleInjection, solution5 mg/1mLIntravenousHospira, Inc.2006-04-07Not applicableUs
DipyridamoleInjection, solution5 mg/1mLIntravenousHospira, Inc.2006-04-07Not applicableUs
Dipyridamole 25 Tab 25mgTablet25 mgOralPro Doc Limitee1983-12-312002-08-02Canada
Dipyridamole 50 Tab 50mgTablet50 mgOralPro Doc Limitee1983-12-312002-08-02Canada
Dipyridamole 75 TabTablet75 mgOralPro Doc Limitee1984-12-312002-08-02Canada
Dipyridamole for InjectionSolution5 mgIntravenousNovopharm Limited2002-04-30Not applicableCanada
Dipyridamole Injection, USPLiquid5 mgIntravenousFresenius Kabi2002-04-23Not applicableCanada
Dipyridamole-25Tablet25 mgOralPro Doc Limitee1998-08-282010-07-13Canada
Dipyridamole-50Tablet50 mgOralPro Doc Limitee1998-08-282010-07-13Canada
Dipyridamole-75Tablet75 mgOralPro Doc Limitee1998-08-282010-07-13Canada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-dipyridamole-FC Tab 25mgTablet25 mgOralApotex Corporation1990-12-31Not applicableCanada
Apo-dipyridamole-FC Tab 50mgTablet50 mgOralApotex Corporation1990-12-31Not applicableCanada
Apo-dipyridamole-FC Tab 75mgTablet75 mgOralApotex Corporation1990-12-31Not applicableCanada
Apo-dipyridamole-SC Tab 25mgTablet25 mgOralApotex Corporation1982-12-31Not applicableCanada
Apo-dipyridamole-SC Tab 50mgTablet50 mgOralApotex Corporation1982-12-31Not applicableCanada
Apo-dipyridamole-SC Tab 75mgTablet75 mgOralApotex Corporation1984-12-31Not applicableCanada
DipyridamoleTablet, film coated75 mg/1OralCadila Pharnmaceuticals2008-05-22Not applicableUs
DipyridamoleTablet, film coated25 mg/1OralGlenmark Generics, Inc. USA1991-02-052013-02-28Us
DipyridamoleTablet25 mg/1OralCarilion Materials Management2012-02-15Not applicableUs
DipyridamoleTablet25 mg/1OralRoxane Laboratories2012-02-15Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
AggrenoxDipyridamole (200 mg) + Acetylsalicylic acid (25 mg)Capsule; Capsule, extended releaseOralBoehringer Ingelheim (Canada) Ltd Ltee2000-04-17Not applicableCanada
AggrenoxDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)CapsuleOralPhysicians Total Care, Inc.2004-08-24Not applicableUs54868 514320180907 15195 14ldz57
AggrenoxDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)Capsule, extended releaseOralBoehringer Ingelheim Pharmaceuticals, Inc.1999-12-19Not applicableUs0597 000120180907 15195 qvauis
AggrenoxDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)CapsuleOralRebel Distributors1999-12-19Not applicableUs
AggrenoxDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)Capsule, extended releaseOralCarilion Materials Management1999-12-19Not applicableUs00597 0001 60 nlmimage10 7303b9ed
Asasantine CapDipyridamole (75 mg) + Acetylsalicylic acid (330 mg)CapsuleOralBoehringer Ingelheim (Canada) Ltd Ltee1983-12-312000-07-31Canada
Aspirin and DipyridamoleDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)Capsule, extended releaseOralTeva Pharmaceuticals USA, Inc.2015-07-012019-09-30Us00093 3040 06 nlmimage10 f343f9ef
Aspirin and DipyridamoleDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)Capsule, extended releaseOralImpax Generics2016-08-29Not applicableUs
Aspirin and DipyridamoleDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)CapsuleOralWest-Ward Pharmaceuticals Corp.2015-06-242020-07-01Us
Aspirin and DipyridamoleDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)Capsule, extended releaseOralDr. Reddy's Laboratories Inc2018-10-10Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
DipyridamoleDipyridamole (5 mg/1mL)SolutionIntravenousAnazao Health Corporation2012-05-23Not applicableUs
International/Other Brands
Agilease (lsei) / Cardoxin (Rafa) / Cleridium 150 (Millot) / Curantyl (Arzneimittelwerk) / Persantin
Categories
UNII
64ALC7F90C
CAS number
58-32-2
Weight
Average: 504.6256
Monoisotopic: 504.317251808
Chemical Formula
C24H40N8O4
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

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
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
Human
AAdenosine deaminase
inhibitor
Human
AcGMP-specific 3',5'-cyclic phosphodiesterase
inhibitor
Human
AcAMP-specific 3',5'-cyclic phosphodiesterase 4A
inhibitor
Human
UCalcipressin-1Not AvailableHuman
UAlpha-1-acid glycoprotein 1Not AvailableHuman
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
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
DrugInteraction
(1,2,6,7-3H)TestosteroneThe therapeutic efficacy of Dipyridamole can be increased when used in combination with (1,2,6,7-3H)Testosterone.
(R)-warfarinThe risk or severity of bleeding can be increased when Dipyridamole is combined with (R)-warfarin.
(S)-WarfarinThe risk or severity of bleeding can be increased when Dipyridamole is combined with (S)-Warfarin.
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic AcidDipyridamole may increase the antihypertensive activities of 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
1-TestosteroneThe therapeutic efficacy of Dipyridamole can be increased when used in combination with 1-Testosterone.
1,10-PhenanthrolineThe therapeutic efficacy of 1,10-Phenanthroline can be decreased when used in combination with Dipyridamole.
18-methyl-19-nortestosteroneThe therapeutic efficacy of Dipyridamole can be increased when used in combination with 18-methyl-19-nortestosterone.
4-hydroxycoumarinThe risk or severity of bleeding can be increased when Dipyridamole is combined with 4-hydroxycoumarin.
4-HydroxytestosteroneThe therapeutic efficacy of Dipyridamole can be increased when used in combination with 4-Hydroxytestosterone.
5beta-dihydrotestosteroneThe therapeutic efficacy of Dipyridamole can be increased when used in combination with 5beta-dihydrotestosterone.
Food Interactions
  • Coffee and tea can decrease the effect of dipyridamole.
  • Take with food to reduce irritation.

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]
External Links
Human Metabolome Database
HMDB0015110
KEGG Drug
D00302
PubChem Compound
3108
PubChem Substance
46506292
ChemSpider
2997
BindingDB
23620
ChEBI
4653
ChEMBL
CHEMBL932
Therapeutic Targets Database
DNC001625
PharmGKB
PA449367
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Dipyridamole
ATC Codes
B01AC07 — 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
0Unknown StatusNot AvailableCoronary Angiography1
1CompletedNot AvailableHealthy Volunteers1
1CompletedTreatmentHealthy Volunteers4
1CompletedTreatmentHigh Blood Pressure (Hypertension)1
1, 2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
1, 2RecruitingTreatmentHenoch-Schönlein Purpura Nephritis1
2CompletedPreventionCardiovascular Disease (CVD) / Carotid Stenosis / Cerebrovascular Disorders / Heart Diseases / Vascular Diseases1
2CompletedTreatmentMalignant Neoplasm of Pancreas1
2CompletedTreatmentRheumatoid Arthritis2
2Not Yet RecruitingTreatmentDry Eye Syndromes / Pterygium1
2RecruitingTreatmentIntracerebral Hemorrhage / Nonvalvular Atrial Fibrillation1
2TerminatedTreatmentMetastatic Breast Cancer (MBC)1
2Unknown StatusNot AvailableIschaemic Heart Diseases1
2Unknown StatusTreatmentCancer of the Ovary1
3CompletedPreventionAngina Pectoris / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia1
3CompletedPreventionCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia1
3CompletedPreventionCerebrovascular Accidents1
3CompletedPreventionRenal Failure1
3CompletedTreatmentCarotid Artery Dissection / Cervical Artery Dissection / Strokes / Vertebral Artery Dissection1
4CompletedNot AvailableDiabetes Mellitus (DM)1
4CompletedPreventionArteriosclerosis / Ischemia, Brain / Transient Ischaemic Attack (TIA)1
4CompletedPreventionAtherosclerosis / Coronary Heart Disease (CHD) / Percutaneous Transluminal Coronary Angioplasty1
4CompletedPreventionCardiovascular Disease (CVD) / Ischaemic Heart Diseases1
4CompletedPreventionEndotoxaemia1
4CompletedPreventionStrokes1
4CompletedTreatmentAtherosclerosis / Ischemia-Reperfusion Injury1
4CompletedTreatmentCardiovascular Disease (CVD) / Ischemia-Reperfusion Injury1
4CompletedTreatmentHealthy Volunteers1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Liver Cirrhosis / Status;Splenectomy / Thrombosis, Venous1
4CompletedTreatmentMania1
4RecruitingPreventionHigh Blood Pressure (Hypertension) / Liver Cirrhosis / Status;Splenectomy / Thrombosis, Venous1
4TerminatedDiagnosticCoronary Artery Disease1
Not AvailableActive Not RecruitingTreatmentStrokes / Transient Ischaemic Attack (TIA)1
Not AvailableCompletedNot AvailableAtherosclerosis / Cardiovascular Disease (CVD) / Carotid Stenosis / Strokes1
Not AvailableCompletedBasic ScienceArterial hypoxia / Hyperemia1
Not AvailableCompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder1
Not AvailableRecruitingNot AvailableIgA Nephropathy / Immunosuppressive Treatment / Proteinuria in Nephrotic Range1
Not AvailableRecruitingTreatmentSystemic Lupus Erythematosus (SLE)1
Not AvailableTerminatedTreatmentPeripheral Arterial Disease (PAD)1

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
Capsule, extended releaseOral
Capsule; capsule, extended releaseOral
TabletOral50 mg
CapsuleOral
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
LiquidIntravenous5 mg
TabletOral100 mg
SolutionIntravenous5 mg
Tablet, coatedOral25 mg/1
Tablet, coatedOral50 mg/1
Tablet, coatedOral75 mg/1
TabletOral25 mg
TabletOral75 mg
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)
US6015577No2000-01-182017-01-18Us

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

Taxonomy

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
Dialkylarylamine / Aminopyrimidine / Piperidine / Pyrimidine / Imidolactam / Heteroaromatic compound / Organoheterocyclic compound / Alkanolamine / Azacycle / Alcohol
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
piperidines, tertiary amino compound, tetrol, pyrimidopyrimidine (CHEBI:4653)

Targets

Kind
Protein
Organism
Human
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
Human
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
Human
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
Human
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
Human
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
Human
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
Human
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
Human
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]
Kind
Protein
Organism
Human
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
Human
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
Human
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
Human
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
Human
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 December 18, 2018 05:46