Identification

Name
Amrinone
Accession Number
DB01427
Type
Small Molecule
Groups
Approved
Description

Amrinone (or inamrinone) is a type 3 pyridine phosphodiesterase inhibitor. It is used in the treatment of congestive heart failure.

Structure
Thumb
Synonyms
  • Amrinona
  • Amrinonum
  • Inamrinone
External IDs
C01CE01 / WIN 40680 / WIN-40680
Product Ingredients
IngredientUNIICASInChI Key
Amrinone lactateI229274Y5B75898-90-7DOSIONJFGDSKCQ-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Inocor Liq 5mg/mlLiquid5 mgIntravenousSanofi1984-12-312000-07-24Canada
International/Other Brands
Amcoral / Inocor
Categories
UNII
JUT23379TN
CAS number
60719-84-8
Weight
Average: 187.198
Monoisotopic: 187.074561925
Chemical Formula
C10H9N3O
InChI Key
RNLQIBCLLYYYFJ-UHFFFAOYSA-N
InChI
InChI=1S/C10H9N3O/c11-9-5-8(6-13-10(9)14)7-1-3-12-4-2-7/h1-6H,11H2,(H,13,14)
IUPAC Name
3-amino-5-(pyridin-4-yl)-1,2-dihydropyridin-2-one
SMILES
NC1=CC(=CNC1=O)C1=CC=NC=C1

Pharmacology

Indication

Used in the treatment of congestive heart failure.

Structured Indications
Not Available
Pharmacodynamics

Amrinone is a positive inotropic cardiotonic with vasodilator properties, phosphodiesterase inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.

Mechanism of action

Amrinone is a phosphodiesterase inhibitor (PDE3), resulting in increased cAMP and cGMP which leads to an increase in the calcium influx like that caused by beta-agonists resulting in increased inotropic effect.

TargetActionsOrganism
UcAMP-specific 3',5'-cyclic phosphodiesterase 4B
inhibitor
Human
UTumor necrosis factor
inhibitor
Human
AcGMP-inhibited 3',5'-cyclic phosphodiesterase A
inhibitor
Human
UcAMP-specific 3',5'-cyclic phosphodiesterase 3Not AvailableHuman
Absorption
Not Available
Volume of distribution
  • 1.2 L/kg [normal volunteers]
Protein binding

10 to 49%

Metabolism

Hepatic.

Route of elimination

The primary route of excretion in man is via the urine as both inamrinone and several metabolites (N-glycolyl, N-acetate, O-glucuronide and N-glucuronide).

Half life

5 to 8 hours

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2-HYDROXY-1,4-NAPHTHOQUINONEThe therapeutic efficacy of 2-HYDROXY-1,4-NAPHTHOQUINONE can be increased when used in combination with Amrinone.Experimental
2-mercaptobenzothiazoleThe therapeutic efficacy of 2-mercaptobenzothiazole can be increased when used in combination with Amrinone.Vet Approved
AlfuzosinThe risk or severity of hypotension can be increased when Alfuzosin is combined with Amrinone.Approved, Investigational
AmobarbitalThe metabolism of Amrinone can be increased when combined with Amobarbital.Approved, Illicit
AmorolfineThe therapeutic efficacy of Amorolfine can be increased when used in combination with Amrinone.Approved, Investigational
Amphotericin BThe therapeutic efficacy of Amphotericin B can be increased when used in combination with Amrinone.Approved, Investigational
AnidulafunginThe therapeutic efficacy of Anidulafungin can be increased when used in combination with Amrinone.Approved, Investigational
ArotinololThe risk or severity of hypotension, conduction block, and bradycardia can be increased when Arotinolol is combined with Amrinone.Investigational
ArtemetherThe therapeutic efficacy of Artemether can be increased when used in combination with Amrinone.Approved
Bafilomycin A1The therapeutic efficacy of Bafilomycin A1 can be increased when used in combination with Amrinone.Experimental
BarbexacloneThe metabolism of Amrinone can be increased when combined with Barbexaclone.Experimental
BarbitalThe metabolism of Amrinone can be increased when combined with Barbital.Illicit
Benzoic AcidThe therapeutic efficacy of Benzoic Acid can be increased when used in combination with Amrinone.Approved, Investigational
BifonazoleThe therapeutic efficacy of Bifonazole can be increased when used in combination with Amrinone.Approved, Investigational
Brefeldin AThe therapeutic efficacy of Brefeldin A can be increased when used in combination with Amrinone.Experimental
BucindololThe risk or severity of hypotension can be increased when Bucindolol is combined with Amrinone.Investigational
BunazosinThe risk or severity of hypotension can be increased when Bunazosin is combined with Amrinone.Investigational
ButenafineThe therapeutic efficacy of Butenafine can be increased when used in combination with Amrinone.Approved
ButoconazoleThe therapeutic efficacy of Butoconazole can be increased when used in combination with Amrinone.Approved
Calcium AcetateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium Acetate.Approved, Investigational
Calcium ChlorideThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium Chloride.Approved
Calcium CitrateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium Citrate.Approved
Calcium glubionateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium glubionate.Approved
Calcium GluceptateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium Gluceptate.Approved
Calcium gluconateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium gluconate.Approved, Vet Approved
Calcium lactateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium lactate.Approved, Experimental, Investigational, Vet Approved
Calcium lactate gluconateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium lactate gluconate.Experimental
Calcium levulinateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium levulinate.Approved, Experimental
Calcium pangamateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium pangamate.Experimental
Calcium PhosphateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium Phosphate.Approved
CandicidinThe therapeutic efficacy of Candicidin can be increased when used in combination with Amrinone.Withdrawn
Capric acidThe therapeutic efficacy of Capric acid can be increased when used in combination with Amrinone.Experimental
CarvedilolThe risk or severity of hypotension can be increased when Carvedilol is combined with Amrinone.Approved, Investigational
CaseinThe therapeutic efficacy of Amrinone can be decreased when used in combination with Casein.Approved
CaspofunginThe therapeutic efficacy of Caspofungin can be increased when used in combination with Amrinone.Approved
CeruleninThe therapeutic efficacy of Cerulenin can be increased when used in combination with Amrinone.Approved
ChloroxineThe therapeutic efficacy of Chloroxine can be increased when used in combination with Amrinone.Approved
CiclopiroxThe therapeutic efficacy of Ciclopirox can be increased when used in combination with Amrinone.Approved, Investigational
CimetidineThe serum concentration of Amrinone can be increased when it is combined with Cimetidine.Approved, Investigational
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Amrinone.Approved
ClotrimazoleThe therapeutic efficacy of Clotrimazole can be increased when used in combination with Amrinone.Approved, Vet Approved
CordycepinThe therapeutic efficacy of Cordycepin can be increased when used in combination with Amrinone.Investigational
CyclosporineThe therapeutic efficacy of Cyclosporine can be increased when used in combination with Amrinone.Approved, Investigational, Vet Approved
DichloropheneThe therapeutic efficacy of Dichlorophene can be increased when used in combination with Amrinone.Vet Approved
DoxazosinThe risk or severity of hypotension can be increased when Doxazosin is combined with Amrinone.Approved
EconazoleThe therapeutic efficacy of Econazole can be increased when used in combination with Amrinone.Approved
EfavirenzThe serum concentration of Amrinone can be decreased when it is combined with Efavirenz.Approved, Investigational
EfinaconazoleThe therapeutic efficacy of Efinaconazole can be increased when used in combination with Amrinone.Approved
FenticonazoleThe therapeutic efficacy of Fenticonazole can be increased when used in combination with Amrinone.Experimental
FluconazoleThe therapeutic efficacy of Fluconazole can be increased when used in combination with Amrinone.Approved, Investigational
FlucytosineThe therapeutic efficacy of Flucytosine can be increased when used in combination with Amrinone.Approved, Investigational
FlutrimazoleThe therapeutic efficacy of Flutrimazole can be increased when used in combination with Amrinone.Experimental
GlyphosateThe therapeutic efficacy of Glyphosate can be increased when used in combination with Amrinone.Experimental
GriseofulvinThe therapeutic efficacy of Griseofulvin can be increased when used in combination with Amrinone.Approved, Investigational, Vet Approved
HachimycinThe therapeutic efficacy of Hachimycin can be increased when used in combination with Amrinone.Experimental
HaloproginThe therapeutic efficacy of Haloprogin can be increased when used in combination with Amrinone.Approved, Withdrawn
HexetidineThe therapeutic efficacy of Hexetidine can be increased when used in combination with Amrinone.Approved, Investigational
HexobarbitalThe metabolism of Amrinone can be increased when combined with Hexobarbital.Approved
IndoraminThe risk or severity of hypotension can be increased when Indoramin is combined with Amrinone.Withdrawn
IsoconazoleThe therapeutic efficacy of Isoconazole can be increased when used in combination with Amrinone.Approved
ItraconazoleThe therapeutic efficacy of Itraconazole can be increased when used in combination with Amrinone.Approved, Investigational
KetoconazoleThe therapeutic efficacy of Ketoconazole can be increased when used in combination with Amrinone.Approved, Investigational
LabetalolThe risk or severity of hypotension can be increased when Labetalol is combined with Amrinone.Approved
Magnesium hydroxideThe risk or severity of hypotension and neuromuscular blockade can be increased when Amrinone is combined with Magnesium hydroxide.Approved, Investigational
Magnesium oxideThe risk or severity of hypotension and neuromuscular blockade can be increased when Amrinone is combined with Magnesium oxide.Approved
Magnesium salicylateThe risk or severity of hypotension and neuromuscular blockade can be increased when Amrinone is combined with Magnesium salicylate.Approved
Magnesium sulfateThe risk or severity of hypotension and neuromuscular blockade can be increased when Amrinone is combined with Magnesium sulfate.Approved, Investigational, Vet Approved
MepartricinThe therapeutic efficacy of Mepartricin can be increased when used in combination with Amrinone.Experimental
MethohexitalThe metabolism of Amrinone can be increased when combined with Methohexital.Approved
MethylphenobarbitalThe metabolism of Amrinone can be increased when combined with Methylphenobarbital.Approved
MevastatinThe therapeutic efficacy of Mevastatin can be increased when used in combination with Amrinone.Experimental
MicafunginThe therapeutic efficacy of Micafungin can be increased when used in combination with Amrinone.Approved, Investigational
MiconazoleThe therapeutic efficacy of Miconazole can be increased when used in combination with Amrinone.Approved, Investigational, Vet Approved
MiltefosineThe therapeutic efficacy of Miltefosine can be increased when used in combination with Amrinone.Approved, Investigational
MonensinThe therapeutic efficacy of Monensin can be increased when used in combination with Amrinone.Vet Approved
MyxothiazolThe therapeutic efficacy of Myxothiazol can be increased when used in combination with Amrinone.Experimental
NafcillinThe therapeutic efficacy of Amrinone can be decreased when used in combination with Nafcillin.Approved, Investigational
NaftifineThe therapeutic efficacy of Naftifine can be increased when used in combination with Amrinone.Approved
NatamycinThe therapeutic efficacy of Natamycin can be increased when used in combination with Amrinone.Approved
NifuratelThe therapeutic efficacy of Nifuratel can be increased when used in combination with Amrinone.Experimental
Nikkomycin ZThe therapeutic efficacy of Nikkomycin Z can be increased when used in combination with Amrinone.Investigational
NitroprussideAmrinone may increase the hypotensive activities of Nitroprusside.Approved, Investigational
NitroxolineThe therapeutic efficacy of Nitroxoline can be increased when used in combination with Amrinone.Approved
NystatinThe therapeutic efficacy of Nystatin can be increased when used in combination with Amrinone.Approved, Vet Approved
OmoconazoleThe therapeutic efficacy of Omoconazole can be increased when used in combination with Amrinone.Experimental
OxiconazoleThe therapeutic efficacy of Oxiconazole can be increased when used in combination with Amrinone.Approved
PafuramidineThe therapeutic efficacy of Pafuramidine can be increased when used in combination with Amrinone.Investigational
PentamidineThe therapeutic efficacy of Pentamidine can be increased when used in combination with Amrinone.Approved, Investigational
PentobarbitalThe metabolism of Amrinone can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PhenobarbitalThe metabolism of Amrinone can be increased when combined with Phenobarbital.Approved, Investigational
PosaconazoleThe therapeutic efficacy of Posaconazole can be increased when used in combination with Amrinone.Approved, Investigational, Vet Approved
PrazosinThe risk or severity of hypotension can be increased when Prazosin is combined with Amrinone.Approved
PrimidoneThe metabolism of Amrinone can be increased when combined with Primidone.Approved, Vet Approved
PyrrolnitrinThe therapeutic efficacy of Pyrrolnitrin can be increased when used in combination with Amrinone.Experimental
RadicicolThe therapeutic efficacy of Radicicol can be increased when used in combination with Amrinone.Experimental
RifabutinThe risk or severity of hypotension can be increased when Rifabutin is combined with Amrinone.Approved, Investigational
RifampicinThe risk or severity of hypotension can be increased when Rifampicin is combined with Amrinone.Approved
RifapentineThe risk or severity of hypotension can be increased when Rifapentine is combined with Amrinone.Approved, Investigational
RifaximinThe risk or severity of hypotension can be increased when Rifaximin is combined with Amrinone.Approved, Investigational
Salicylhydroxamic AcidThe therapeutic efficacy of Salicylhydroxamic Acid can be increased when used in combination with Amrinone.Experimental
Salicylic acidThe therapeutic efficacy of Salicylic acid can be increased when used in combination with Amrinone.Approved, Investigational, Vet Approved
SecobarbitalThe metabolism of Amrinone can be increased when combined with Secobarbital.Approved, Vet Approved
SertaconazoleThe therapeutic efficacy of Sertaconazole can be increased when used in combination with Amrinone.Approved, Investigational
SilodosinThe risk or severity of hypotension can be increased when Silodosin is combined with Amrinone.Approved
SinefunginThe therapeutic efficacy of Sinefungin can be increased when used in combination with Amrinone.Experimental
SirolimusThe therapeutic efficacy of Sirolimus can be increased when used in combination with Amrinone.Approved, Investigational
SulconazoleThe therapeutic efficacy of Sulconazole can be increased when used in combination with Amrinone.Approved
TamsulosinThe risk or severity of hypotension can be increased when Tamsulosin is combined with Amrinone.Approved, Investigational
TavaboroleThe therapeutic efficacy of Tavaborole can be increased when used in combination with Amrinone.Approved, Investigational
TerazosinThe risk or severity of hypotension can be increased when Terazosin is combined with Amrinone.Approved
TerbinafineThe therapeutic efficacy of Terbinafine can be increased when used in combination with Amrinone.Approved, Investigational, Vet Approved
TerconazoleThe therapeutic efficacy of Terconazole can be increased when used in combination with Amrinone.Approved
ThiamylalThe metabolism of Amrinone can be increased when combined with Thiamylal.Approved, Vet Approved
ThiopentalThe metabolism of Amrinone can be increased when combined with Thiopental.Approved, Vet Approved
ThymolThe therapeutic efficacy of Thymol can be increased when used in combination with Amrinone.Approved
TioconazoleThe therapeutic efficacy of Tioconazole can be increased when used in combination with Amrinone.Approved
TolciclateThe therapeutic efficacy of Tolciclate can be increased when used in combination with Amrinone.Experimental
TolnaftateThe therapeutic efficacy of Tolnaftate can be increased when used in combination with Amrinone.Approved, Investigational, Vet Approved
TrimazosinThe risk or severity of hypotension can be increased when Trimazosin is combined with Amrinone.Experimental
TrimetrexateThe therapeutic efficacy of Trimetrexate can be increased when used in combination with Amrinone.Approved, Investigational
UrapidilThe risk or severity of hypotension can be increased when Urapidil is combined with Amrinone.Investigational
VoriconazoleThe therapeutic efficacy of Voriconazole can be increased when used in combination with Amrinone.Approved, Investigational
Food Interactions
Not Available

References

Synthesis Reference

Lesher,G.Y. and Opalka, C.J.; US. Patent 4,004,012; January 18,1977; assigned to Sterling Drug Inc. Lesher, G.Y. and Opalka, C.J.; U.S. Patent 4,107,315; August 15,1978; assigned to Sterling Drug Inc.

General References
Not Available
External Links
Human Metabolome Database
HMDB0015496
KEGG Drug
D00231
KEGG Compound
C13594
PubChem Compound
3698
PubChem Substance
46504647
ChemSpider
3570
BindingDB
34651
ChEBI
2686
ChEMBL
CHEMBL12856
Therapeutic Targets Database
DAP001392
PharmGKB
PA164746803
Wikipedia
Amrinone
ATC Codes
C01CE01 — Amrinone

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Taylor Pharmaceuticals
Dosage forms
FormRouteStrength
LiquidIntravenous5 mg
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)294-297Lesher,G.Y. and Opalka, C.J.; US. Patent 4,004,012; January 18,1977; assigned to Sterling Drug Inc. Lesher, G.Y. and Opalka, C.J.; U.S. Patent 4,107,315; August 15,1978; assigned to Sterling Drug Inc.
Predicted Properties
PropertyValueSource
Water Solubility5.6 mg/mLALOGPS
logP0.27ALOGPS
logP-0.57ChemAxon
logS-1.5ALOGPS
pKa (Strongest Acidic)11.01ChemAxon
pKa (Strongest Basic)4.87ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area68.01 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity53.89 m3·mol-1ChemAxon
Polarizability18.94 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9522
Blood Brain Barrier+0.9525
Caco-2 permeable+0.8867
P-glycoprotein substrateNon-substrate0.6469
P-glycoprotein inhibitor INon-inhibitor0.9338
P-glycoprotein inhibitor IINon-inhibitor0.9946
Renal organic cation transporterNon-inhibitor0.9258
CYP450 2C9 substrateNon-substrate0.8642
CYP450 2D6 substrateNon-substrate0.8389
CYP450 3A4 substrateNon-substrate0.6443
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorInhibitor0.5328
CYP450 2D6 inhibitorNon-inhibitor0.9651
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorNon-inhibitor0.6534
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5933
Ames testNon AMES toxic0.8492
CarcinogenicityNon-carcinogens0.9116
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.9371 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9923
hERG inhibition (predictor II)Non-inhibitor0.7418
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
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00lr-3900000000-f6b4ee8cb119f30be206

Taxonomy

Description
This compound belongs to the class of organic compounds known as bipyridines and oligopyridines. These are organic compounds containing two pyridine rings linked to each other.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyridines and derivatives
Sub Class
Bipyridines and oligopyridines
Direct Parent
Bipyridines and oligopyridines
Alternative Parents
Pyridinones / Dihydropyridines / Aminopyridines and derivatives / Heteroaromatic compounds / Lactams / Azacyclic compounds / Primary amines / Organopnictogen compounds / Organooxygen compounds / Organic oxides
show 1 more
Substituents
Bipyridine / Aminopyridine / Dihydropyridine / Pyridinone / Hydropyridine / Heteroaromatic compound / Lactam / Azacycle / Amine / Primary amine
show 8 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Hydrolyzes the second messenger cAMP, which is a key regulator of many important physiological processes. May be involved in mediating central nervous system effects of therapeutic agents ranging f...
Gene Name
PDE4B
Uniprot ID
Q07343
Uniprot Name
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
Molecular Weight
83342.695 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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Tumor necrosis factor receptor binding
Specific Function
Cytokine that binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It is mainly secreted by macrophages and can induce cell death of certain tumor cell lines. It is potent pyrogen causing fever by direct ac...
Gene Name
TNF
Uniprot ID
P01375
Uniprot Name
Tumor necrosis factor
Molecular Weight
25644.15 Da
References
  1. Kumar A, Kosuri R, Kandula P, Dimou C, Allen J, Parrillo JE: Effects of epinephrine and amrinone on contractility and cyclic adenosine monophosphate generation of tumor necrosis factor alpha-exposed cardiac myocytes. Crit Care Med. 1999 Feb;27(2):286-92. [PubMed:10075051]
  2. Bergman MR, Kao RH, McCune SA, Holycross BJ: Myocardial tumor necrosis factor-alpha secretion in hypertensive and heart failure-prone rats. Am J Physiol. 1999 Aug;277(2 Pt 2):H543-50. [PubMed:10444479]
  3. Haddad JJ, Land SC, Tarnow-Mordi WO, Zembala M, Kowalczyk D, Lauterbach R: Immunopharmacological potential of selective phosphodiesterase inhibition. I. Differential regulation of lipopolysaccharide-mediated proinflammatory cytokine (interleukin-6 and tumor necrosis factor-alpha) biosynthesis in alveolar epithelial cells. J Pharmacol Exp Ther. 2002 Feb;300(2):559-66. [PubMed:11805217]
  4. Marx D, Tassabehji M, Heer S, Huttenbrink KB, Szelenyi I: Modulation of TNF and GM-CSF release from dispersed human nasal polyp cells and human whole blood by inhibitors of different PDE isoenzymes and glucocorticoids. Pulm Pharmacol Ther. 2002;15(1):7-15. [PubMed:11969359]
  5. Giroir BP, Beutler B: Effect of amrinone on tumor necrosis factor production in endotoxic shock. Circ Shock. 1992 Mar;36(3):200-7. [PubMed:1611705]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Metal ion binding
Specific Function
Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes.
Gene Name
PDE3A
Uniprot ID
Q14432
Uniprot Name
cGMP-inhibited 3',5'-cyclic phosphodiesterase A
Molecular Weight
124978.06 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  2. Kobayashi T, Sugawara Y, Ohkubo T, Imamura H, Makuuchi M: Effects of amrinone on hepatic ischemia-reperfusion injury in rats. J Hepatol. 2002 Jul;37(1):31-8. [PubMed:12076859]
  3. Ko Y, Morita K, Nagahori R, Kinouchi K, Shinohara G, Kagawa H, Hashimoto K: Myocardial cyclic AMP augmentation with high-dose PDEIII inhibitor in terminal warm blood cardioplegia. Ann Thorac Cardiovasc Surg. 2009 Oct;15(5):311-7. [PubMed:19901885]
  4. Kucuk C, Akcan A, Akyyldyz H, Akgun H, Muhtaroglu S, Sozuer E: Effects of amrinone in an experimental model of hepatic ischemia-reperfusion injury. J Surg Res. 2009 Jan;151(1):74-9. doi: 10.1016/j.jss.2008.02.008. Epub 2008 Mar 13. [PubMed:18468627]
4. cAMP-specific 3',5'-cyclic phosphodiesterase 3
Kind
Protein
Organism
Human
Pharmacological action
Unknown
References
  1. Weishaar RE, Kobylarz-Singer DC, Steffen RP, Kaplan HR: Subclasses of cyclic AMP-specific phosphodiesterase in left ventricular muscle and their involvement in regulating myocardial contractility. Circ Res. 1987 Oct;61(4):539-47. [PubMed:2820608]

Drug created on July 24, 2007 06:34 / Updated on March 02, 2018 05:18