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
  • Amcoral
  • 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 risk or severity of adverse effects can be increased when 2-HYDROXY-1,4-NAPHTHOQUINONE is combined with Amrinone.Experimental
2-mercaptobenzothiazoleThe risk or severity of adverse effects can be increased when 2-mercaptobenzothiazole is combined with Amrinone.Vet Approved
AlfuzosinAlfuzosin may increase the hypotensive activities of Amrinone.Approved, Investigational
AmobarbitalThe metabolism of Amrinone can be increased when combined with Amobarbital.Approved, Illicit
AmorolfineThe risk or severity of adverse effects can be increased when Amorolfine is combined with Amrinone.Approved, Investigational
Amphotericin BThe risk or severity of adverse effects can be increased when Amphotericin B is combined with Amrinone.Approved, Investigational
AnidulafunginThe risk or severity of adverse effects can be increased when Anidulafungin is combined with Amrinone.Approved, Investigational
ArtemetherThe risk or severity of adverse effects can be increased when Artemether is combined with Amrinone.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Amrinone is combined with Atorvastatin.Approved
AtosibanThe risk or severity of adverse effects can be increased when Amrinone is combined with Atosiban.Approved, Investigational
Atracurium besylateAmrinone may increase the neuromuscular blocking activities of Atracurium besylate.Approved
Bafilomycin A1The risk or severity of adverse effects can be increased when Bafilomycin A1 is combined 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 risk or severity of adverse effects can be increased when Benzoic Acid is combined with Amrinone.Approved
BifonazoleThe risk or severity of adverse effects can be increased when Bifonazole is combined with Amrinone.Approved, Investigational
Brefeldin AThe risk or severity of adverse effects can be increased when Brefeldin A is combined with Amrinone.Experimental
BucindololBucindolol may increase the hypotensive activities of Amrinone.Investigational
BunazosinBunazosin may increase the hypotensive activities of Amrinone.Investigational
ButenafineThe risk or severity of adverse effects can be increased when Butenafine is combined with Amrinone.Approved
ButoconazoleThe risk or severity of adverse effects can be increased when Butoconazole is combined with Amrinone.Approved
Calcium AcetateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium Acetate.Approved
Calcium CarbonateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium Carbonate.Approved
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 laevulateThe therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium laevulate.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 risk or severity of adverse effects can be increased when Candicidin is combined with Amrinone.Withdrawn
Capric acidThe risk or severity of adverse effects can be increased when Capric acid is combined with Amrinone.Experimental
CarbomycinThe metabolism of Amrinone can be decreased when combined with Carbomycin.Vet Approved
CarvedilolCarvedilol may increase the hypotensive activities of Amrinone.Approved, Investigational
CaseinThe therapeutic efficacy of Amrinone can be decreased when used in combination with Casein.Approved
CaspofunginThe risk or severity of adverse effects can be increased when Caspofungin is combined with Amrinone.Approved
CerivastatinThe risk or severity of adverse effects can be increased when Amrinone is combined with Cerivastatin.Withdrawn
CeruleninThe risk or severity of adverse effects can be increased when Cerulenin is combined with Amrinone.Approved
ChloroxineThe risk or severity of adverse effects can be increased when Chloroxine is combined with Amrinone.Approved
CiclopiroxThe risk or severity of adverse effects can be increased when Ciclopirox is combined with Amrinone.Approved, Investigational
CimetidineThe serum concentration of Amrinone can be increased when it is combined with Cimetidine.Approved
ClarithromycinThe metabolism of Amrinone can be decreased when combined with Clarithromycin.Approved
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Amrinone.Approved, Nutraceutical
ClotrimazoleThe risk or severity of adverse effects can be increased when Clotrimazole is combined with Amrinone.Approved, Vet Approved
CordycepinThe risk or severity of adverse effects can be increased when Cordycepin is combined with Amrinone.Investigational
CyclosporineThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Amrinone.Approved, Investigational, Vet Approved
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Amrinone.Investigational
DichloropheneThe risk or severity of adverse effects can be increased when Dichlorophene is combined with Amrinone.Vet Approved
DoxazosinDoxazosin may increase the hypotensive activities of Amrinone.Approved
EconazoleThe risk or severity of adverse effects can be increased when Econazole is combined with Amrinone.Approved
EfavirenzThe serum concentration of Amrinone can be decreased when it is combined with Efavirenz.Approved, Investigational
EfinaconazoleThe risk or severity of adverse effects can be increased when Efinaconazole is combined with Amrinone.Approved
ErythromycinThe metabolism of Amrinone can be decreased when combined with Erythromycin.Approved, Vet Approved
FenticonazoleThe risk or severity of adverse effects can be increased when Fenticonazole is combined with Amrinone.Experimental
FluconazoleThe serum concentration of Amrinone can be increased when it is combined with Fluconazole.Approved
FlucytosineThe risk or severity of adverse effects can be increased when Flucytosine is combined with Amrinone.Approved
FlutrimazoleThe risk or severity of adverse effects can be increased when Flutrimazole is combined with Amrinone.Experimental
FluvastatinThe risk or severity of adverse effects can be increased when Amrinone is combined with Fluvastatin.Approved
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Amrinone.Approved
GlyphosateThe risk or severity of adverse effects can be increased when Glyphosate is combined with Amrinone.Experimental
GriseofulvinThe risk or severity of adverse effects can be increased when Griseofulvin is combined with Amrinone.Approved, Vet Approved
HachimycinThe risk or severity of adverse effects can be increased when Hachimycin is combined with Amrinone.Experimental
HaloproginThe risk or severity of adverse effects can be increased when Haloprogin is combined with Amrinone.Approved, Withdrawn
HexetidineThe risk or severity of adverse effects can be increased when Hexetidine is combined with Amrinone.Approved, Investigational
HexobarbitalThe metabolism of Amrinone can be increased when combined with Hexobarbital.Approved
IndoraminIndoramin may increase the hypotensive activities of Amrinone.Withdrawn
IsoconazoleThe risk or severity of adverse effects can be increased when Isoconazole is combined with Amrinone.Approved
ItraconazoleThe risk or severity of adverse effects can be increased when Itraconazole is combined with Amrinone.Approved, Investigational
JosamycinThe metabolism of Amrinone can be decreased when combined with Josamycin.Approved, Investigational
KetoconazoleThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Amrinone.Approved, Investigational
KitasamycinThe metabolism of Amrinone can be decreased when combined with Kitasamycin.Experimental
LabetalolLabetalol may increase the hypotensive activities of Amrinone.Approved
LovastatinThe risk or severity of adverse effects can be increased when Amrinone is combined with Lovastatin.Approved, Investigational
Magnesium HydroxideThe risk or severity of adverse effects can be increased when Amrinone is combined with Magnesium Hydroxide.Approved
Magnesium oxideThe risk or severity of adverse effects can be increased when Amrinone is combined with Magnesium oxide.Approved
Magnesium salicylateThe risk or severity of adverse effects can be increased when Amrinone is combined with Magnesium salicylate.Approved
Magnesium SulfateThe risk or severity of adverse effects can be increased when Amrinone is combined with Magnesium Sulfate.Approved, Vet Approved
MepartricinThe risk or severity of adverse effects can be increased when Mepartricin is combined 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 risk or severity of adverse effects can be increased when Mevastatin is combined with Amrinone.Experimental
MicafunginThe risk or severity of adverse effects can be increased when Micafungin is combined with Amrinone.Approved, Investigational
MiconazoleThe risk or severity of adverse effects can be increased when Miconazole is combined with Amrinone.Approved, Investigational, Vet Approved
MiltefosineThe risk or severity of adverse effects can be increased when Miltefosine is combined with Amrinone.Approved
MivacuriumAmrinone may increase the neuromuscular blocking activities of Mivacurium.Approved
MonensinThe risk or severity of adverse effects can be increased when Monensin is combined with Amrinone.Vet Approved
MyxothiazolThe risk or severity of adverse effects can be increased when Myxothiazol is combined with Amrinone.Experimental
NafcillinThe metabolism of Amrinone can be increased when combined with Nafcillin.Approved
NaftifineThe risk or severity of adverse effects can be increased when Naftifine is combined with Amrinone.Approved
NatamycinThe risk or severity of adverse effects can be increased when Natamycin is combined with Amrinone.Approved
NifuratelThe risk or severity of adverse effects can be increased when Nifuratel is combined with Amrinone.Experimental
Nikkomycin ZThe risk or severity of adverse effects can be increased when Nikkomycin Z is combined with Amrinone.Investigational
NitroprussideAmrinone may increase the hypotensive activities of Nitroprusside.Approved
NitroxolineThe risk or severity of adverse effects can be increased when Nitroxoline is combined with Amrinone.Approved
NystatinThe risk or severity of adverse effects can be increased when Nystatin is combined with Amrinone.Approved, Vet Approved
OleandomycinThe metabolism of Amrinone can be decreased when combined with Oleandomycin.Vet Approved
OmoconazoleThe risk or severity of adverse effects can be increased when Omoconazole is combined with Amrinone.Experimental
OxiconazoleThe risk or severity of adverse effects can be increased when Oxiconazole is combined with Amrinone.Approved
pafuramidineThe risk or severity of adverse effects can be increased when pafuramidine is combined with Amrinone.Investigational
PentamidineThe risk or severity of adverse effects can be increased when Pentamidine is combined with Amrinone.Approved
PentobarbitalThe metabolism of Amrinone can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe metabolism of Amrinone can be increased when combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Amrinone.Approved, Vet Approved
PitavastatinThe risk or severity of adverse effects can be increased when Amrinone is combined with Pitavastatin.Approved
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Amrinone.Approved, Investigational, Vet Approved
PravastatinThe risk or severity of adverse effects can be increased when Amrinone is combined with Pravastatin.Approved
PrazosinPrazosin may increase the hypotensive activities of Amrinone.Approved
PrimidoneThe metabolism of Amrinone can be increased when combined with Primidone.Approved, Vet Approved
PyrrolnitrinThe risk or severity of adverse effects can be increased when Pyrrolnitrin is combined with Amrinone.Experimental
RadicicolThe risk or severity of adverse effects can be increased when Radicicol is combined with Amrinone.Experimental
RapacuroniumAmrinone may increase the neuromuscular blocking activities of Rapacuronium.Withdrawn
RifabutinThe serum concentration of Amrinone can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Amrinone can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Amrinone can be decreased when it is combined with Rifapentine.Approved
RifaximinThe serum concentration of Amrinone can be decreased when it is combined with Rifaximin.Approved, Investigational
RosuvastatinThe risk or severity of adverse effects can be increased when Amrinone is combined with Rosuvastatin.Approved
Salicylhydroxamic AcidThe risk or severity of adverse effects can be increased when Salicylhydroxamic Acid is combined with Amrinone.Experimental
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Amrinone.Approved, Vet Approved
SecobarbitalThe metabolism of Amrinone can be increased when combined with Secobarbital.Approved, Vet Approved
SertaconazoleThe risk or severity of adverse effects can be increased when Sertaconazole is combined with Amrinone.Approved
SilodosinSilodosin may increase the hypotensive activities of Amrinone.Approved
SimvastatinThe risk or severity of adverse effects can be increased when Amrinone is combined with Simvastatin.Approved
SinefunginThe risk or severity of adverse effects can be increased when Sinefungin is combined with Amrinone.Experimental
SirolimusThe risk or severity of adverse effects can be increased when Sirolimus is combined with Amrinone.Approved, Investigational
SolithromycinThe metabolism of Amrinone can be decreased when combined with Solithromycin.Investigational
SulconazoleThe risk or severity of adverse effects can be increased when Sulconazole is combined with Amrinone.Approved
TamsulosinTamsulosin may increase the hypotensive activities of Amrinone.Approved, Investigational
TavaboroleThe risk or severity of adverse effects can be increased when Tavaborole is combined with Amrinone.Approved
TelithromycinThe metabolism of Amrinone can be decreased when combined with Telithromycin.Approved
TerazosinTerazosin may increase the hypotensive activities of Amrinone.Approved
TerbinafineThe risk or severity of adverse effects can be increased when Terbinafine is combined with Amrinone.Approved, Investigational, Vet Approved
TerconazoleThe risk or severity of adverse effects can be increased when Terconazole is combined 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 risk or severity of adverse effects can be increased when Thymol is combined with Amrinone.Approved
TioconazoleThe risk or severity of adverse effects can be increased when Tioconazole is combined with Amrinone.Approved
TolciclateThe risk or severity of adverse effects can be increased when Tolciclate is combined with Amrinone.Experimental
TolnaftateThe risk or severity of adverse effects can be increased when Tolnaftate is combined with Amrinone.Approved, Vet Approved
TrimazosinTrimazosin may increase the hypotensive activities of Amrinone.Experimental
TrimetrexateThe risk or severity of adverse effects can be increased when Trimetrexate is combined with Amrinone.Approved, Investigational
TylosinThe metabolism of Amrinone can be decreased when combined with Tylosin.Vet Approved
UbidecarenoneThe risk or severity of adverse effects can be increased when Amrinone is combined with Ubidecarenone.Approved, Investigational, Nutraceutical
UrapidilUrapidil may increase the hypotensive activities of Amrinone.Investigational
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined 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
HMDB15496
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
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 December 01, 2017 17:22