Dipyridamole

Identification

Summary

Dipyridamole is a phosphodiesterase inhibitor used to prevent postoperative thromboembolic events.

Brand Names

Aggrenox, Persantine

Generic Name

Dipyridamole

DrugBank Accession Number

DB00975

Background

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

Similar Structures

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.

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Associated Conditions

Associated Therapies

Anti-platelet Therapy

Contraindications & Blackbox Warnings

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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.

Target	Actions	Organism
AcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	inhibitor	Humans
AcGMP-specific 3',5'-cyclic phosphodiesterase	inhibitor	Humans
AcAMP-specific 3',5'-cyclic phosphodiesterase 4A	inhibitor	Humans
AAdenosine deaminase	inhibitor	Humans
UCalcipressin-1	Not Available	Humans
UAlpha-1-acid glycoprotein 1	Not Available	Humans

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

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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)

Pathways

Pathway	Category
Dipyridamole (Antiplatelet) Action Pathway	Drug 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.

Drug	Interaction
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Abaloparatide	The risk or severity of adverse effects can be increased when Dipyridamole is combined with Abaloparatide.
Abciximab	The risk or severity of bleeding can be increased when Abciximab is combined with Dipyridamole.
Abrocitinib	The risk or severity of bleeding and thrombocytopenia can be increased when Dipyridamole is combined with Abrocitinib.
Acebutolol	Dipyridamole may increase the bradycardic activities of Acebutolol.
Aceclofenac	The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Dipyridamole.
Acemetacin	The risk or severity of bleeding and hemorrhage can be increased when Dipyridamole is combined with Acemetacin.
Acenocoumarol	The risk or severity of bleeding can be increased when Dipyridamole is combined with Acenocoumarol.
Adenosine	The risk or severity of adverse effects can be increased when Dipyridamole is combined with Adenosine.
Albutrepenonacog alfa	The therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Dipyridamole.
Alclofenac	The risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Dipyridamole.

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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

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Dipyridamole	Injection, solution	5 mg/1mL	Intravenous	Hospira, Inc.	2006-04-07	Not applicable
Dipyridamole	Solution	5 mg/1mL	Intravenous	Anazao Health Corporation	2012-05-23	Not applicable
Dipyridamole	Injection, solution	5 mg/1mL	Intravenous	Hospira, Inc.	2006-04-07	Not applicable
Dipyridamole 25 Tab 25mg	Tablet	25 mg	Oral	Pro Doc Limitee	1983-12-31	2002-08-02
Dipyridamole 50 Tab 50mg	Tablet	50 mg	Oral	Pro Doc Limitee	1983-12-31	2002-08-02
Dipyridamole 75 Tab	Tablet	75 mg	Oral	Pro Doc Limitee	1984-12-31	2002-08-02
Dipyridamole for Injection	Solution	5 mg / mL	Intravenous	Novopharm Limited	2002-04-30	2018-05-07
Dipyridamole Injection, USP	Liquid	5 mg / mL	Intravenous	Fresenius Kabi	2002-04-23	Not applicable
Dipyridamole-25	Tablet	25 mg	Oral	Pro Doc Limitee	1998-08-28	2010-07-13
Dipyridamole-50	Tablet	50 mg	Oral	Pro Doc Limitee	1998-08-28	2010-07-13

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Apo-dipyridamole	Tablet	25 mg	Oral	Apotex Corporation	1990-12-31	Not applicable
Apo-dipyridamole	Tablet	100 mg	Oral	Apotex Corporation	Not applicable	Not applicable
Apo-dipyridamole	Tablet	75 mg	Oral	Apotex Corporation	1990-12-31	Not applicable
Apo-dipyridamole	Tablet	50 mg	Oral	Apotex Corporation	1990-12-31	Not applicable
Apo-dipyridamole-SC Tab 25mg	Tablet	25 mg	Oral	Apotex Corporation	1982-12-31	Not applicable
Apo-dipyridamole-SC Tab 50mg	Tablet	50 mg	Oral	Apotex Corporation	1982-12-31	Not applicable
Apo-dipyridamole-SC Tab 75mg	Tablet	75 mg	Oral	Apotex Corporation	1984-12-31	Not applicable
Dipyridamole	Tablet, film coated	25 mg/1	Oral	Proficient Rx LP	2007-08-05	Not applicable
Dipyridamole	Tablet, film coated	25 mg/1	Oral	Rising Pharmaceuticals, Inc.	2007-08-05	Not applicable
Dipyridamole	Tablet, film coated	25 mg/1	Oral	ANI Pharmaceuticals, Inc.	2021-11-22	2024-03-31

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Aggrenox	Dipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)	Capsule	Oral	Physicians Total Care, Inc.	2004-08-24	Not applicable
Aggrenox	Dipyridamole (200 mg) + Acetylsalicylic acid (25 mg)	Capsule, extended release	Oral	Boehringer Ingelheim (Canada) Ltd Ltee	2000-04-17	2020-02-24
Aggrenox	Dipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)	Capsule	Oral	Rebel Distributors	1999-12-19	Not applicable
Aggrenox	Dipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)	Capsule, extended release	Oral	Carilion Materials Management	1999-12-19	Not applicable
Aggrenox	Dipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)	Capsule, extended release	Oral	Boehringer Ingelheim Pharmaceuticals Inc.	1999-12-19	Not applicable
Asasantine Cap	Dipyridamole (75 mg) + Acetylsalicylic acid (330 mg)	Capsule	Oral	Boehringer Ingelheim (Canada) Ltd Ltee	1983-12-31	2000-07-31
Aspirin and Dipyridamole	Dipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)	Capsule, extended release	Oral	Teva Pharmaceuticals USA, Inc.	2019-06-10	2021-10-31
Aspirin and Dipyridamole	Dipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)	Capsule, extended release	Oral	Dr. Reddy's Laboratories Inc	2018-10-10	Not applicable
Aspirin and Dipyridamole	Dipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)	Capsule	Oral	West-Ward Pharmaceuticals Corp.	2015-06-24	2020-07-01
Aspirin and Dipyridamole	Dipyridamole (200 mg/1) + Acetylsalicylic acid (25 mg/1)	Capsule, extended release	Oral	Impax Generics	2017-01-18	2017-01-18

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
Dipyridamole	Dipyridamole (5 mg/1mL)	Solution	Intravenous	Anazao Health Corporation	2012-05-23	Not applicable

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

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. [Article]

External Links

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
PDBe Ligand: H9F
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Dipyridamole

PDB Entries

7dmc / 8i4a / 8t6u

FDA label

Download (48.7 KB)

MSDS

Download (73.3 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Not Available	Diabetes	1
4	Completed	Prevention	Angioplasty, Transluminal, Percutaneous Coronary / Atherosclerosis / Coronary Heart Disease (CHD)	1
4	Completed	Prevention	Arteriosclerosis / Cerebral Ischemia / Transient Ischemic Attack	1
4	Completed	Prevention	Cardiovascular Disease (CVD) / Ischemic Heart Disease	1
4	Completed	Prevention	Cirrhosis of the Liver / Portal Hypertension / Status;Splenectomy / Venous Thrombosis (Disorder)	1
4	Completed	Prevention	Endotoxaemia	1
4	Completed	Prevention	Stroke	1
4	Completed	Treatment	Atherosclerosis / Ischemia Reperfusion Injury	1
4	Completed	Treatment	Cardiovascular Disease (CVD) / Ischemia Reperfusion Injury	1
4	Completed	Treatment	Cirrhosis of the Liver / Hypertension / Status;Splenectomy / Venous Thrombosis (Disorder)	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

Form	Route	Strength
Capsule	Oral
Capsule	Oral	25.000 MG
Capsule, extended release	Oral
Tablet	Oral	50 mg
Capsule, delayed release	Oral
Tablet	Oral
Tablet, coated	Oral	100 mg
Tablet	Oral	75 mg
Tablet	Oral	100 mg
Solution	Intravenous	10 mg
Injection	Intravenous	5 mg/1mL
Injection, solution	Intravenous	5 mg/1mL
Solution	Intravenous	5 mg/1mL
Tablet	Oral	25 mg/1
Tablet	Oral	50 mg/1
Tablet	Oral	75 mg/1
Tablet, film coated	Oral	25 mg/1
Tablet, film coated	Oral	50 mg/1
Tablet, film coated	Oral	75 mg/1
Liquid	Intravenous	5 mg / mL
Solution	Parenteral	5 mg
Tablet, film coated	Oral
Tablet, delayed release	Oral
Pill
Tablet, sugar coated	Oral	25 mg
Tablet, sugar coated	Oral	75 mg
Capsule		200 MG
Injection, solution	Intravenous	10 MG/2ML
Pill		75 MG
Solution	Parenteral	10.000 mg
Tablet	Oral	75.000 mg
Tablet, coated	Oral
Solution	Intravenous; Parenteral	10 mg
Tablet, delayed release	Oral	75 mg
Injection	Intramuscular; Intravenous	10 mg/2ml
Solution	Intravenous	5 mg / mL
Tablet, coated	Oral	25 mg/1
Tablet, coated	Oral	50 mg/1
Tablet, coated	Oral	75 mg/1
Tablet	Oral	25 mg
Tablet, film coated	Oral	75 mg
Tablet, coated	Oral	75 mg
Tablet, coated	Oral	25 mg

Prices

Unit description	Cost	Unit
Dipyridamole powder	5.34USD	g
Aggrenox capsule sa	3.25USD	capsule
Aggrenox 25-200 mg 12 Hour Capsule	3.0USD	capsule
Dipyridamole 5 mg/ml ampul	1.5USD	ml
Persantine 75 mg tablet	1.46USD	tablet
Dipyridamole 5 mg/ml vial	1.32USD	ml
Dipyridamole 75 mg tablet	1.28USD	tablet
Persantine 50 mg tablet	1.09USD	tablet
Dipyridamole 50 mg tablet	0.96USD	tablet
Persantine 25 mg tablet	0.89USD	tablet
Dipyridamole 25 mg tablet	0.58USD	tablet
Apo-Dipyridamole (Fc) 75 mg Tablet	0.46USD	tablet
Apo-Dipyridamole (Fc) 50 mg Tablet	0.31USD	tablet
Apo-Dipyridamole (Fc) 25 mg Tablet	0.28USD	tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US6015577	No	2000-01-18	2017-01-18

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	163 °C	PhysProp
water solubility	Slightly	Not Available
logP	1.5	Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.922 mg/mL	ALOGPS
logP	1.52	ALOGPS
logP	1.81	Chemaxon
logS	-2.7	ALOGPS
pKa (Strongest Acidic)	14.97	Chemaxon
pKa (Strongest Basic)	3.54	Chemaxon
Physiological Charge	0	Chemaxon
Hydrogen Acceptor Count	12	Chemaxon
Hydrogen Donor Count	4	Chemaxon
Polar Surface Area	145.44 Å²	Chemaxon
Rotatable Bond Count	12	Chemaxon
Refractivity	142.78 m³·mol^-1	Chemaxon
Polarizability	56.93 Å³	Chemaxon
Number of Rings	4	Chemaxon
Bioavailability	0	Chemaxon
Rule of Five	No	Chemaxon
Ghose Filter	No	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	Yes	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	0.9917
Blood Brain Barrier	-	0.6246
Caco-2 permeable	-	0.7261
P-glycoprotein substrate	Substrate	0.7696
P-glycoprotein inhibitor I	Non-inhibitor	0.5321
P-glycoprotein inhibitor II	Non-inhibitor	0.8383
Renal organic cation transporter	Non-inhibitor	0.615
CYP450 2C9 substrate	Non-substrate	0.8345
CYP450 2D6 substrate	Non-substrate	0.6825
CYP450 3A4 substrate	Non-substrate	0.6849
CYP450 1A2 substrate	Non-inhibitor	0.9045
CYP450 2C9 inhibitor	Inhibitor	0.8045
CYP450 2D6 inhibitor	Inhibitor	0.7201
CYP450 2C19 inhibitor	Non-inhibitor	0.957
CYP450 3A4 inhibitor	Inhibitor	0.6789
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.7806
Ames test	Non AMES toxic	0.7009
Carcinogenicity	Non-carcinogens	0.8884
Biodegradation	Not ready biodegradable	0.988
Rat acute toxicity	2.1167 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Strong inhibitor	0.5271
hERG inhibition (predictor II)	Non-inhibitor	0.633

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	Not Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	Not Available
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	Not Available
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0udl-0291000000-2fc7956fe6ea13c73317
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0a4i-0001190000-346cf73a19cbefa2dc11
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0a4i-0013490000-839580758bc83767be8f
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0udl-0291000000-caeb14eb3ea863e020a0
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0a4i-1348890000-aa1e3a113b8c2768cb08

Targets

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Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	1000	N/A	N/A	A29072

Details1. cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A

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

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
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. [Article]
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. [Article]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	5.00E+02	7.5	24	A27470

Details2. cGMP-specific 3',5'-cyclic phosphodiesterase

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

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. [Article]
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. [Article]
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. [Article]
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. [Article]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Details3. cAMP-specific 3',5'-cyclic phosphodiesterase 4A

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

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Details4. Adenosine deaminase

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

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Details5. Calcipressin-1

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

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. [Article]

Details6. Alpha-1-acid glycoprotein 1

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

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. [Article]

Transporters

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	2000	N/A	N/A	A16089

Details1. Multidrug resistance-associated protein 4

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

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. [Article]
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. [Article]
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. [Article]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	30000	N/A	N/A	A16089

Details2. Multidrug resistance-associated protein 5

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

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. [Article]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	22700	N/A	N/A	A15813
IC 50 (nM)	23700	N/A	N/A	A15813
IC 50 (nM)	34300	N/A	N/A	A15813

Details3. 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

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. [Article]
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. [Article]

Details4. Solute carrier organic anion transporter family member 1B1

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

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. [Article]

Details5. Solute carrier organic anion transporter family member 1B3

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

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. [Article]

Details6. Solute carrier organic anion transporter family member 2B1

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

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. [Article]

Details7. Bile salt export pump

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

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. [Article]

Drug created at June 13, 2005 13:24 / Updated at October 03, 2023 16:58

Dipyridamole

Identification

Structure for Dipyridamole (DB00975)

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

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Clinical Trials

Pharmacoeconomics

Properties

Spectra

Targets

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Transporters

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