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
  • Cleridium 150
  • Curantyl
  • Dipiridamol
  • Dipyridamine
  • Dipyridamolum
  • Dipyudamine
  • Dypyridamol
  • Persantin
External IDs
B01AC07 / NSC-515776 / USAF GE-12
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DipyridamoleTablet75 mg/1OralAvera Mc Kennan Hospital2015-10-28Not applicableUs
DipyridamoleTablet25 mg/1OralRoxane Laboratories2012-02-15Not applicableUs
DipyridamoleTablet75 mg/1OralRoxane Laboratories2012-02-15Not applicableUs
DipyridamoleTablet50 mg/1OralRoxane Laboratories2012-02-15Not applicableUs
DipyridamoleTablet25 mg/1OralCarilion Materials Management2012-02-15Not 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
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 coated25 mg/1OralAvera Mc Kennan Hospital2015-11-17Not applicableUs
DipyridamoleTablet, film coated75 mg/1OralAv Pak2011-08-052016-01-15Us
DipyridamoleTablet, film coated50 mg/1OralTeva1982-01-01Not applicableUs
DipyridamoleTablet25 mg/1OralGlobal Pharmaceuticals, Division of Impax Laboratories, Inc.2007-07-182017-06-20Us
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DipyridamoleSolution5 mg/mLIntravenousAnazao Health Corporation2012-05-23Not applicableUs
International/Other Brands
Agilease (lsei) / Cardoxin (Rafa) / Cleridium 150 (Millot) / Curantyl (Arzneimittelwerk) / Persantin
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 applicableUs
AggrenoxDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)Capsule, extended releaseOralBoehringer Ingelheim1999-12-19Not applicableUs
AggrenoxDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)Capsule, extended releaseOralCarilion Materials Management1999-12-19Not applicableUs00597 0001 60 nlmimage10 7303b9ed
AggrenoxDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)CapsuleOralRebel Distributors1999-12-19Not applicableUs
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)CapsuleOralRoxane Laboratories2015-06-24Not applicableUs
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)Capsule, extended releaseOralTeva2015-07-01Not applicableUs00093 3040 06 nlmimage10 f343f9ef
Aspirin and Extended - Release Dipyridamole Capsules, 25 mg / 200 mgDipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)CapsuleOralPar Pharmaceutical2017-01-30Not applicableUs
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.

Structured Indications
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
AcGMP-specific 3',5'-cyclic phosphodiesterase
inhibitor
Human
AcAMP-specific 3',5'-cyclic phosphodiesterase 4A
inhibitor
Human
AAdenosine deaminase
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
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of 1,10-Phenanthroline can be decreased when used in combination with Dipyridamole.Experimental
AbciximabDipyridamole may increase the anticoagulant activities of Abciximab.Approved
AcebutololDipyridamole may increase the bradycardic activities of Acebutolol.Approved
AcenocoumarolDipyridamole may increase the anticoagulant activities of Acenocoumarol.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Acetylsalicylic acid.Approved, Vet Approved
AdenosineThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Adenosine.Approved, Investigational
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Dipyridamole.Approved
AloxiprinThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Aloxiprin.Experimental
AlprenololDipyridamole may increase the bradycardic activities of Alprenolol.Approved, Withdrawn
AlprostadilAlprostadil may increase the anticoagulant activities of Dipyridamole.Approved, Investigational
AlteplaseDipyridamole may increase the anticoagulant activities of Alteplase.Approved
AmbenoniumThe therapeutic efficacy of Ambenonium can be decreased when used in combination with Dipyridamole.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Aminosalicylic Acid.Approved
AnagrelideDipyridamole may increase the anticoagulant activities of Anagrelide.Approved
AncrodDipyridamole may increase the anticoagulant activities of Ancrod.Investigational
AndrographolideAndrographolide may increase the anticoagulant activities of Dipyridamole.Investigational
AnistreplaseDipyridamole may increase the anticoagulant activities of Anistreplase.Approved
Antithrombin III humanDipyridamole may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Apixaban.Approved
AprotininThe therapeutic efficacy of Dipyridamole can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinDipyridamole may increase the anticoagulant activities of Ardeparin.Approved, Investigational, Withdrawn
ArgatrobanDipyridamole may increase the anticoagulant activities of Argatroban.Approved, Investigational
ArotinololDipyridamole may increase the bradycardic activities of Arotinolol.Investigational
AstaxanthinDipyridamole may increase the anticoagulant activities of Astaxanthin.Investigational
AtenololDipyridamole may increase the bradycardic activities of Atenolol.Approved
AzelastineAzelastine may increase the anticoagulant activities of Dipyridamole.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Balsalazide.Approved, Investigational
BatroxobinDipyridamole may increase the anticoagulant activities of Batroxobin.Experimental
BecaplerminDipyridamole may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BefunololDipyridamole may increase the bradycardic activities of Befunolol.Experimental
BemiparinDipyridamole may increase the anticoagulant activities of Bemiparin.Approved, Investigational
BeraprostDipyridamole may increase the anticoagulant activities of Beraprost.Investigational
BetaxololDipyridamole may increase the bradycardic activities of Betaxolol.Approved
BevantololDipyridamole may increase the bradycardic activities of Bevantolol.Approved
BisoprololDipyridamole may increase the bradycardic activities of Bisoprolol.Approved
BivalirudinDipyridamole may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BopindololDipyridamole may increase the bradycardic activities of Bopindolol.Approved
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Dipyridamole.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Dipyridamole.Approved
BrinaseDipyridamole may increase the anticoagulant activities of Brinase.Experimental
BucindololDipyridamole may increase the bradycardic activities of Bucindolol.Investigational
BuflomedilBuflomedil may increase the anticoagulant activities of Dipyridamole.Experimental
BufuralolDipyridamole may increase the bradycardic activities of Bufuralol.Experimental, Investigational
BupranololDipyridamole may increase the bradycardic activities of Bupranolol.Approved
ButylphthalideButylphthalide may increase the anticoagulant activities of Dipyridamole.Investigational
CangrelorDipyridamole may increase the anticoagulant activities of Cangrelor.Approved
CaplacizumabDipyridamole may increase the anticoagulant activities of Caplacizumab.Investigational
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Carbaspirin calcium.Experimental, Investigational
CarteololDipyridamole may increase the bradycardic activities of Carteolol.Approved
CarvedilolDipyridamole may increase the bradycardic activities of Carvedilol.Approved, Investigational
CeliprololDipyridamole may increase the bradycardic activities of Celiprolol.Approved, Investigational
CertoparinDipyridamole may increase the anticoagulant activities of Certoparin.Approved, Investigational
CilostazolDipyridamole may increase the anticoagulant activities of Cilostazol.Approved
Citric AcidDipyridamole may increase the anticoagulant activities of Citric Acid.Approved, Nutraceutical, Vet Approved
ClopidogrelDipyridamole may increase the anticoagulant activities of Clopidogrel.Approved
CloranololDipyridamole may increase the bradycardic activities of Cloranolol.Experimental
CloricromenDipyridamole may increase the anticoagulant activities of Cloricromen.Experimental
ClorindioneDipyridamole may increase the anticoagulant activities of Clorindione.Experimental
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Dipyridamole.Approved
Collagenase clostridium histolyticumThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Collagenase clostridium histolyticum.Approved, Investigational
CoumaphosThe therapeutic efficacy of Coumaphos can be decreased when used in combination with Dipyridamole.Vet Approved
Dabigatran etexilateDipyridamole may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinDipyridamole may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidDipyridamole may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanDipyridamole may increase the anticoagulant activities of Darexaban.Investigational
DasatinibDasatinib may increase the anticoagulant activities of Dipyridamole.Approved, Investigational
DecamethoniumThe therapeutic efficacy of Decamethonium can be decreased when used in combination with Dipyridamole.Approved
DefibrotideDipyridamole may increase the anticoagulant activities of Defibrotide.Approved, Investigational
DemecariumThe therapeutic efficacy of Demecarium can be decreased when used in combination with Dipyridamole.Approved
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Deoxycholic Acid.Approved
DersalazineThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Dersalazine.Investigational
DesirudinDipyridamole may increase the anticoagulant activities of Desirudin.Approved
DesmoteplaseDipyridamole may increase the anticoagulant activities of Desmoteplase.Investigational
DextranDipyridamole may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Dipyridamole may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Dipyridamole may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Dipyridamole may increase the anticoagulant activities of Dextran 75.Approved
DichlorvosThe therapeutic efficacy of Dichlorvos can be decreased when used in combination with Dipyridamole.Vet Approved
DicoumarolDipyridamole may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Diflunisal.Approved
DiphenadioneDipyridamole may increase the anticoagulant activities of Diphenadione.Experimental
DistigmineThe therapeutic efficacy of Distigmine can be decreased when used in combination with Dipyridamole.Experimental
DitazoleDipyridamole may increase the anticoagulant activities of Ditazole.Approved, Withdrawn
DonepezilThe therapeutic efficacy of Donepezil can be decreased when used in combination with Dipyridamole.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Dipyridamole.Approved, Investigational
Drotrecogin alfaDipyridamole may increase the anticoagulant activities of Drotrecogin alfa.Approved, Investigational, Withdrawn
EchothiophateThe therapeutic efficacy of Echothiophate can be decreased when used in combination with Dipyridamole.Approved
Edetic AcidDipyridamole may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Dipyridamole.Approved
EdrophoniumThe therapeutic efficacy of Edrophonium can be decreased when used in combination with Dipyridamole.Approved
EnoxaparinDipyridamole may increase the anticoagulant activities of Enoxaparin.Approved
EpanololDipyridamole may increase the bradycardic activities of Epanolol.Experimental
EpinastineEpinastine may increase the anticoagulant activities of Dipyridamole.Approved, Investigational
EplivanserinDipyridamole may increase the anticoagulant activities of Eplivanserin.Investigational
eplivanserineDipyridamole may increase the anticoagulant activities of eplivanserine.Investigational
EpoprostenolDipyridamole may increase the anticoagulant activities of Epoprostenol.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Dipyridamole.Approved, Investigational
EsmololDipyridamole may increase the bradycardic activities of Esmolol.Approved
Ethyl biscoumacetateDipyridamole may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Dipyridamole.Approved
FenthionThe therapeutic efficacy of Fenthion can be decreased when used in combination with Dipyridamole.Vet Approved
Ferulic acidDipyridamole may increase the anticoagulant activities of Ferulic acid.Experimental
FibrinolysinDipyridamole may increase the anticoagulant activities of Fibrinolysin.Investigational
FluindioneDipyridamole may increase the anticoagulant activities of Fluindione.Investigational
FondaparinuxDipyridamole may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumDipyridamole may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
GabexateDipyridamole may increase the anticoagulant activities of Gabexate.Investigational
GalantamineThe therapeutic efficacy of Galantamine can be decreased when used in combination with Dipyridamole.Approved
Gallamine TriethiodideThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Dipyridamole.Approved
GlucosamineGlucosamine may increase the antiplatelet activities of Dipyridamole.Approved
GuacetisalThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Guacetisal.Experimental
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Hemoglobin crosfumaril.Experimental
HeparinDipyridamole may increase the anticoagulant activities of Heparin.Approved, Investigational
HigenamineDipyridamole may increase the anticoagulant activities of Higenamine.Investigational
Huperzine AThe therapeutic efficacy of Huperzine A can be decreased when used in combination with Dipyridamole.Investigational
HydroxytyrosolHydroxytyrosol may increase the anticoagulant activities of Dipyridamole.Investigational
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Ibritumomab tiuxetan.Approved
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Dipyridamole.Approved
IbudilastIbudilast may increase the anticoagulant activities of Dipyridamole.Approved, Investigational
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Dipyridamole.Approved, Nutraceutical
IdraparinuxDipyridamole may increase the anticoagulant activities of Idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Dipyridamole.Approved, Investigational, Withdrawn
IfetrobanIfetroban may increase the anticoagulant activities of Dipyridamole.Investigational
IloprostDipyridamole may increase the anticoagulant activities of Iloprost.Approved, Investigational
IndenololDipyridamole may increase the bradycardic activities of Indenolol.Withdrawn
IndobufenDipyridamole may increase the anticoagulant activities of Indobufen.Investigational
IpidacrineThe therapeutic efficacy of Ipidacrine can be decreased when used in combination with Dipyridamole.Experimental
IsoflurophateThe therapeutic efficacy of Isoflurophate can be decreased when used in combination with Dipyridamole.Approved, Investigational, Withdrawn
KetanserinKetanserin may increase the anticoagulant activities of Dipyridamole.Investigational
LabetalolDipyridamole may increase the bradycardic activities of Labetalol.Approved
LandiololDipyridamole may increase the bradycardic activities of Landiolol.Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Dipyridamole.Approved
LepirudinDipyridamole may increase the anticoagulant activities of Lepirudin.Approved
LetaxabanDipyridamole may increase the anticoagulant activities of Letaxaban.Investigational
LevobunololDipyridamole may increase the bradycardic activities of Levobunolol.Approved
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Dipyridamole.Approved, Investigational
LinsidomineLinsidomine may increase the anticoagulant activities of Dipyridamole.Experimental
LumacaftorThe serum concentration of Dipyridamole can be decreased when it is combined with Lumacaftor.Approved
MalathionThe therapeutic efficacy of Malathion can be decreased when used in combination with Dipyridamole.Approved, Investigational
MefloquineThe therapeutic efficacy of Mefloquine can be decreased when used in combination with Dipyridamole.Approved
MelagatranDipyridamole may increase the anticoagulant activities of Melagatran.Experimental
MemantineThe therapeutic efficacy of Memantine can be decreased when used in combination with Dipyridamole.Approved, Investigational
MepindololDipyridamole may increase the bradycardic activities of Mepindolol.Experimental
MesalazineThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Mesalazine.Approved
Methanesulfonyl FluorideThe therapeutic efficacy of Methanesulfonyl Fluoride can be decreased when used in combination with Dipyridamole.Investigational
Methyl salicylateThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Methyl salicylate.Approved, Vet Approved
MetipranololDipyridamole may increase the bradycardic activities of Metipranolol.Approved
MetoclopramideThe therapeutic efficacy of Metoclopramide can be decreased when used in combination with Dipyridamole.Approved, Investigational
MetoprololDipyridamole may increase the bradycardic activities of Metoprolol.Approved, Investigational
MilrinoneMilrinone may increase the anticoagulant activities of Dipyridamole.Approved
MinaprineThe therapeutic efficacy of Minaprine can be decreased when used in combination with Dipyridamole.Approved
NadololDipyridamole may increase the bradycardic activities of Nadolol.Approved
NadroparinDipyridamole may increase the anticoagulant activities of Nadroparin.Approved
NafamostatDipyridamole may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NaftopidilNaftopidil may increase the anticoagulant activities of Dipyridamole.Investigational
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Dipyridamole.Approved
NebivololDipyridamole may increase the bradycardic activities of Nebivolol.Approved, Investigational
NeostigmineThe therapeutic efficacy of Neostigmine can be decreased when used in combination with Dipyridamole.Approved, Vet Approved
NimesulideNimesulide may increase the anticoagulant activities of Dipyridamole.Approved, Investigational, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Nitroaspirin.Investigational
ObinutuzumabThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Obinutuzumab.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Olsalazine.Approved
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Dipyridamole.Approved, Nutraceutical
OtamixabanDipyridamole may increase the anticoagulant activities of Otamixaban.Investigational
OxprenololDipyridamole may increase the bradycardic activities of Oxprenolol.Approved
OzagrelDipyridamole may increase the anticoagulant activities of Ozagrel.Investigational
ParaoxonThe therapeutic efficacy of Paraoxon can be decreased when used in combination with Dipyridamole.Experimental
ParnaparinDipyridamole may increase the anticoagulant activities of Parnaparin.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Dipyridamole.Approved
PenbutololDipyridamole may increase the bradycardic activities of Penbutolol.Approved, Investigational
Pentaerythritol TetranitrateDipyridamole may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Approved
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Dipyridamole.Approved
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Dipyridamole.Approved, Investigational
PhenindioneDipyridamole may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenprocoumonDipyridamole may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhysostigmineThe therapeutic efficacy of Physostigmine can be decreased when used in combination with Dipyridamole.Approved
PicotamideDipyridamole may increase the anticoagulant activities of Picotamide.Experimental
PindololDipyridamole may increase the bradycardic activities of Pindolol.Approved
Platelet Activating FactorDipyridamole may increase the bradycardic activities of Platelet Activating Factor.Experimental
PractololDipyridamole may increase the bradycardic activities of Practolol.Approved
PrasugrelDipyridamole may increase the anticoagulant activities of Prasugrel.Approved
PropranololDipyridamole may increase the bradycardic activities of Propranolol.Approved, Investigational
Protein CDipyridamole may increase the anticoagulant activities of Protein C.Approved
Protein S humanDipyridamole may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeDipyridamole may increase the anticoagulant activities of Protocatechualdehyde.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Dipyridamole.Approved
PyridostigmineThe therapeutic efficacy of Pyridostigmine can be decreased when used in combination with Dipyridamole.Approved
RamatrobanRamatroban may increase the anticoagulant activities of Dipyridamole.Investigational
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Dipyridamole.Approved, Investigational
RegadenosonThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Regadenoson.Approved
RelcovaptanRelcovaptan may increase the anticoagulant activities of Dipyridamole.Investigational
ResveratrolResveratrol may increase the anticoagulant activities of Dipyridamole.Approved, Experimental, Investigational
ReteplaseDipyridamole may increase the anticoagulant activities of Reteplase.Approved
ReviparinDipyridamole may increase the anticoagulant activities of Reviparin.Approved, Investigational
RidogrelRidogrel may increase the anticoagulant activities of Dipyridamole.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Dipyridamole.Approved, Investigational
RiociguatDipyridamole may increase the hypotensive activities of Riociguat.Approved
RivaroxabanDipyridamole may increase the anticoagulant activities of Rivaroxaban.Approved
RivastigmineThe therapeutic efficacy of Rivastigmine can be decreased when used in combination with Dipyridamole.Approved, Investigational
RosiglitazoneDipyridamole may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
Salicylic acidThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Salicylic acid.Approved, Vet Approved
SarpogrelateDipyridamole may increase the anticoagulant activities of Sarpogrelate.Investigational
SaruplaseDipyridamole may increase the anticoagulant activities of Saruplase.Experimental
SelexipagDipyridamole may increase the anticoagulant activities of Selexipag.Approved
SevofluraneSevoflurane may increase the anticoagulant activities of Dipyridamole.Approved, Vet Approved
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Dipyridamole.Approved
SotalolDipyridamole may increase the bradycardic activities of Sotalol.Approved
SRT501SRT501 may increase the anticoagulant activities of Dipyridamole.Investigational
StreptokinaseDipyridamole may increase the anticoagulant activities of Streptokinase.Approved, Investigational
SulodexideDipyridamole may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TacrineThe therapeutic efficacy of Tacrine can be decreased when used in combination with Dipyridamole.Investigational, Withdrawn
TalinololDipyridamole may increase the bradycardic activities of Talinolol.Investigational
TenecteplaseDipyridamole may increase the anticoagulant activities of Tenecteplase.Approved
TertatololDipyridamole may increase the bradycardic activities of Tertatolol.Experimental
TesmilifeneTesmilifene may increase the anticoagulant activities of Dipyridamole.Investigational
TicagrelorDipyridamole may increase the anticoagulant activities of Ticagrelor.Approved
TiclopidineTiclopidine may increase the anticoagulant activities of Dipyridamole.Approved
TimololDipyridamole may increase the bradycardic activities of Timolol.Approved
TinzaparinDipyridamole may increase the anticoagulant activities of Tinzaparin.Approved
TioclomarolDipyridamole may increase the anticoagulant activities of Tioclomarol.Experimental
TipranavirTipranavir may increase the antiplatelet activities of Dipyridamole.Approved, Investigational
TirofibanTirofiban may increase the anticoagulant activities of Dipyridamole.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Dipyridamole.Approved, Investigational
TositumomabThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Tositumomab.Approved, Investigational
TranilastTranilast may increase the anticoagulant activities of Dipyridamole.Approved, Investigational
TrapidilTrapidil may increase the anticoagulant activities of Dipyridamole.Approved
TreprostinilDipyridamole may increase the anticoagulant activities of Treprostinil.Approved, Investigational
TrichlorfonThe therapeutic efficacy of Trichlorfon can be decreased when used in combination with Dipyridamole.Vet Approved
TriflusalDipyridamole may increase the anticoagulant activities of Triflusal.Approved, Investigational
Trolamine salicylateThe risk or severity of adverse effects can be increased when Dipyridamole is combined with Trolamine salicylate.Approved
TroxerutinDipyridamole may increase the anticoagulant activities of Troxerutin.Investigational
TubocurarineThe therapeutic efficacy of Tubocurarine can be decreased when used in combination with Dipyridamole.Approved
UrokinaseDipyridamole may increase the anticoagulant activities of Urokinase.Approved, Investigational, Withdrawn
VemurafenibThe serum concentration of Dipyridamole can be increased when it is combined with Vemurafenib.Approved
VincristineThe excretion of Vincristine can be decreased when combined with Dipyridamole.Approved, Investigational
Vitamin EVitamin E may increase the antiplatelet activities of Dipyridamole.Approved, Nutraceutical, Vet Approved
VorapaxarDipyridamole may increase the anticoagulant activities of Vorapaxar.Approved
WarfarinDipyridamole may increase the anticoagulant activities of Warfarin.Approved
XimelagatranDipyridamole may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
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
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 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
Dosage forms
FormRouteStrength
Capsule, extended releaseOral
Capsule; capsule, extended releaseOral
TabletOral50 mg
CapsuleOral
InjectionIntravenous5 mg/mL
SolutionIntravenous5 mg/mL
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)
US6015577No1997-01-182017-01-18Us

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
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
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
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]

Drug created on June 13, 2005 07:24 / Updated on January 19, 2018 10:53