Amrinone - DrugBank

ID Pharmacology Interactions References Trials Economics Properties Spectra Taxonomy

Targets (4)

Targets (4)Biointeractions (3)

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

MOL SDF 3D-SDF PDB SMILES InChI View 3D Structure

Synonyms

Amcoral

Amrinona

Amrinonum

Inamrinone

External IDs

C01CE01 / WIN 40680 / WIN-40680

Product Ingredients

Ingredient	UNII	CAS	InChI Key	Details
Amrinone lactate	I229274Y5B	75898-90-7	DOSIONJFGDSKCQ-UHFFFAOYSA-N	Details

Approved Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Inocor Liq 5mg/ml	Liquid	5 mg	Intravenous	Sanofi	1984-12-31	2000-07-24	Canada

Approved Generic Prescription Products

Not Available

Approved Over the Counter Products

Not Available

Unapproved/Other Products

Not Available

International Brands

Name	Company
Amcoral	Not Available
Inocor	Not Available

Brand mixtures

Not Available

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.

Target	Kind	Pharmacological action	Actions	Organism	UniProt ID
cAMP-specific 3',5'-cyclic phosphodiesterase 4B	Protein	unknown	inhibitor	Human	Q07343	details
Tumor necrosis factor	Protein	unknown	inhibitor	Human	P01375	details
cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Protein	yes	inhibitor	Human	Q14432	details
cAMP-specific 3',5'-cyclic phosphodiesterase 3	Protein	unknown	Not Available	Human	not applicable	details

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

Drug	Interaction	Drug group
2-HYDROXY-1,4-NAPHTHOQUINONE	The risk or severity of adverse effects can be increased when 2-HYDROXY-1,4-NAPHTHOQUINONE is combined with Amrinone.	Experimental
2-mercaptobenzothiazole	The risk or severity of adverse effects can be increased when 2-mercaptobenzothiazole is combined with Amrinone.	Vet Approved
Alfuzosin	Alfuzosin may increase the hypotensive activities of Amrinone.	Approved, Investigational
Amobarbital	The metabolism of Amrinone can be increased when combined with Amobarbital.	Approved, Illicit
Amorolfine	The risk or severity of adverse effects can be increased when Amorolfine is combined with Amrinone.	Approved
Amphotericin B	The risk or severity of adverse effects can be increased when Amphotericin B is combined with Amrinone.	Approved, Investigational
Anidulafungin	The risk or severity of adverse effects can be increased when Anidulafungin is combined with Amrinone.	Approved, Investigational
Artemether	The risk or severity of adverse effects can be increased when Artemether is combined with Amrinone.	Approved
Atosiban	The risk or severity of adverse effects can be increased when Amrinone is combined with Atosiban.	Approved
Atracurium besylate	Amrinone may increase the neuromuscular blocking activities of Atracurium besylate.	Approved
Bafilomycin A1	The risk or severity of adverse effects can be increased when Bafilomycin A1 is combined with Amrinone.	Experimental
Barbexaclone	The metabolism of Amrinone can be increased when combined with Barbexaclone.	Experimental
Barbital	The metabolism of Amrinone can be increased when combined with Barbital.	Illicit
Benzoic Acid	The risk or severity of adverse effects can be increased when Benzoic Acid is combined with Amrinone.	Approved
Bifonazole	The risk or severity of adverse effects can be increased when Bifonazole is combined with Amrinone.	Approved
Bucindolol	Bucindolol may increase the hypotensive activities of Amrinone.	Investigational
Butenafine	The risk or severity of adverse effects can be increased when Butenafine is combined with Amrinone.	Approved
Butoconazole	The risk or severity of adverse effects can be increased when Butoconazole is combined with Amrinone.	Approved
Calcium	The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium.	Nutraceutical
Calcium Acetate	The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium Acetate.	Approved
Calcium Carbonate	The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium carbonate.	Approved
Calcium Chloride	The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium Chloride.	Approved
Calcium Citrate	The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium citrate.	Approved
Calcium glubionate	The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium glubionate.	Approved
Calcium Gluceptate	The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium Gluceptate.	Approved
Calcium gluconate	The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium gluconate.	Approved, Vet Approved
Candicidin	The risk or severity of adverse effects can be increased when Candicidin is combined with Amrinone.	Withdrawn
Capric acid	The risk or severity of adverse effects can be increased when Decanoic Acid is combined with Amrinone.	Experimental
Carbomycin	The metabolism of Amrinone can be decreased when combined with Carbomycin.	Vet Approved
Carvedilol	Carvedilol may increase the hypotensive activities of Amrinone.	Approved, Investigational
Caspofungin	The risk or severity of adverse effects can be increased when Caspofungin is combined with Amrinone.	Approved
Cerulenin	The risk or severity of adverse effects can be increased when Cerulenin is combined with Amrinone.	Approved
Chloroxine	The risk or severity of adverse effects can be increased when Chloroxine is combined with Amrinone.	Approved
Ciclopirox	The risk or severity of adverse effects can be increased when Ciclopirox is combined with Amrinone.	Approved, Investigational
Cimetidine	The serum concentration of Amrinone can be increased when it is combined with Cimetidine.	Approved
Clarithromycin	The metabolism of Amrinone can be decreased when combined with Clarithromycin.	Approved
Clopidogrel	The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Amrinone.	Approved, Nutraceutical
Clotrimazole	The risk or severity of adverse effects can be increased when Clotrimazole is combined with Amrinone.	Approved, Vet Approved
Cordycepin	The risk or severity of adverse effects can be increased when Cordycepin is combined with Amrinone.	Investigational
Cyclosporine	The risk or severity of adverse effects can be increased when Cyclosporine is combined with Amrinone.	Approved, Investigational, Vet Approved
Dapoxetine	Dapoxetine may increase the orthostatic hypotensive activities of Amrinone.	Investigational
Doxazosin	Doxazosin may increase the hypotensive activities of Amrinone.	Approved
Econazole	The risk or severity of adverse effects can be increased when Econazole is combined with Amrinone.	Approved
Efavirenz	The serum concentration of Amrinone can be decreased when it is combined with Efavirenz.	Approved, Investigational
Efinaconazole	The risk or severity of adverse effects can be increased when Efinaconazole is combined with Amrinone.	Approved
Erythromycin	The metabolism of Amrinone can be decreased when combined with Erythromycin.	Approved, Vet Approved
Fluconazole	The serum concentration of Amrinone can be increased when it is combined with Fluconazole.	Approved
Flucytosine	The risk or severity of adverse effects can be increased when Flucytosine is combined with Amrinone.	Approved
Fosphenytoin	The serum concentration of Fosphenytoin can be increased when it is combined with Amrinone.	Approved
Glyphosate	The risk or severity of adverse effects can be increased when Glyphosate is combined with Amrinone.	Experimental
Griseofulvin	The risk or severity of adverse effects can be increased when Griseofulvin is combined with Amrinone.	Approved, Vet Approved
Haloprogin	The risk or severity of adverse effects can be increased when Haloprogin is combined with Amrinone.	Approved, Withdrawn
Hexetidine	The risk or severity of adverse effects can be increased when Hexetidine is combined with Amrinone.	Approved
Hexobarbital	The metabolism of Amrinone can be increased when combined with Hexobarbital.	Approved
Indoramin	Indoramin may increase the hypotensive activities of Amrinone.	Withdrawn
Isoconazole	The risk or severity of adverse effects can be increased when Isoconazole is combined with Amrinone.	Approved
Itraconazole	The risk or severity of adverse effects can be increased when Itraconazole is combined with Amrinone.	Approved, Investigational
Josamycin	The metabolism of Amrinone can be decreased when combined with Josamycin.	Approved
Ketoconazole	The risk or severity of adverse effects can be increased when Ketoconazole is combined with Amrinone.	Approved, Investigational
Kitasamycin	The metabolism of Amrinone can be decreased when combined with Kitasamycin.	Experimental
Labetalol	Labetalol may increase the hypotensive activities of Amrinone.	Approved
Magnesium Hydroxide	The risk or severity of adverse effects can be increased when Amrinone is combined with Magnesium hydroxide.	Approved
Magnesium oxide	The risk or severity of adverse effects can be increased when Amrinone is combined with Magnesium oxide.	Approved
Magnesium salicylate	The risk or severity of adverse effects can be increased when Amrinone is combined with Magnesium salicylate.	Approved
Magnesium Sulfate	The risk or severity of adverse effects can be increased when Amrinone is combined with Magnesium Sulfate.	Approved, Vet Approved
Methohexital	The metabolism of Amrinone can be increased when combined with Methohexital.	Approved
Methylphenobarbital	The metabolism of Amrinone can be increased when combined with Methylphenobarbital.	Approved
Mevastatin	The risk or severity of adverse effects can be increased when Mevastatin is combined with Amrinone.	Experimental
Micafungin	The risk or severity of adverse effects can be increased when Micafungin is combined with Amrinone.	Approved, Investigational
Miconazole	The risk or severity of adverse effects can be increased when Miconazole is combined with Amrinone.	Approved, Investigational, Vet Approved
Miltefosine	The risk or severity of adverse effects can be increased when Miltefosine is combined with Amrinone.	Approved
Mivacurium	Amrinone may increase the neuromuscular blocking activities of Mivacurium.	Approved
Monensin	The risk or severity of adverse effects can be increased when Monensin is combined with Amrinone.	Vet Approved
Myxothiazol	The risk or severity of adverse effects can be increased when Myxothiazol is combined with Amrinone.	Experimental
Nafcillin	The metabolism of Amrinone can be increased when combined with Nafcillin.	Approved
Naftifine	The risk or severity of adverse effects can be increased when Naftifine is combined with Amrinone.	Approved
Natamycin	The risk or severity of adverse effects can be increased when Natamycin is combined with Amrinone.	Approved
Nitroprusside	Amrinone may increase the hypotensive activities of Nitroprusside.	Approved
Nitroxoline	The risk or severity of adverse effects can be increased when Nitroxoline is combined with Amrinone.	Approved
Nystatin	The risk or severity of adverse effects can be increased when Nystatin is combined with Amrinone.	Approved, Vet Approved
Oleandomycin	The metabolism of Amrinone can be decreased when combined with Oleandomycin.	Vet Approved
Oxiconazole	The risk or severity of adverse effects can be increased when Oxiconazole is combined with Amrinone.	Approved
pafuramidine	The risk or severity of adverse effects can be increased when pafuramidine is combined with Amrinone.	Investigational
Pentamidine	The risk or severity of adverse effects can be increased when Pentamidine is combined with Amrinone.	Approved
Pentobarbital	The metabolism of Amrinone can be increased when combined with Pentobarbital.	Approved, Vet Approved
Phenobarbital	The metabolism of Amrinone can be increased when combined with Phenobarbital.	Approved
Phenytoin	The serum concentration of Phenytoin can be increased when it is combined with Amrinone.	Approved, Vet Approved
Posaconazole	The risk or severity of adverse effects can be increased when Posaconazole is combined with Amrinone.	Approved, Investigational, Vet Approved
Prazosin	Prazosin may increase the hypotensive activities of Amrinone.	Approved
Primidone	The metabolism of Amrinone can be increased when combined with Primidone.	Approved, Vet Approved
Radicicol	The risk or severity of adverse effects can be increased when Radicicol is combined with Amrinone.	Experimental
Rapacuronium	Amrinone may increase the neuromuscular blocking activities of Rapacuronium.	Withdrawn
Rifabutin	The serum concentration of Amrinone can be decreased when it is combined with Rifabutin.	Approved
Rifampicin	The serum concentration of Amrinone can be decreased when it is combined with Rifampicin.	Approved
Rifapentine	The serum concentration of Amrinone can be decreased when it is combined with Rifapentine.	Approved
Salicylhydroxamic Acid	The risk or severity of adverse effects can be increased when Salicylhydroxamic Acid is combined with Amrinone.	Experimental
Salicylic acid	The risk or severity of adverse effects can be increased when Salicylic acid is combined with Amrinone.	Approved, Vet Approved
Secobarbital	The metabolism of Amrinone can be increased when combined with Secobarbital.	Approved, Vet Approved
Sertaconazole	The risk or severity of adverse effects can be increased when Sertaconazole is combined with Amrinone.	Approved
Silodosin	Silodosin may increase the hypotensive activities of Amrinone.	Approved
Sinefungin	The risk or severity of adverse effects can be increased when Sinefungin is combined with Amrinone.	Experimental
Sirolimus	The risk or severity of adverse effects can be increased when Sirolimus is combined with Amrinone.	Approved, Investigational
Solithromycin	The metabolism of Amrinone can be decreased when combined with Solithromycin.	Investigational
Sulconazole	The risk or severity of adverse effects can be increased when Sulconazole is combined with Amrinone.	Approved
Tamsulosin	Tamsulosin may increase the hypotensive activities of Amrinone.	Approved, Investigational
Tavaborole	The risk or severity of adverse effects can be increased when Tavaborole is combined with Amrinone.	Approved
Telithromycin	The metabolism of Amrinone can be decreased when combined with Telithromycin.	Approved
Terazosin	Terazosin may increase the hypotensive activities of Amrinone.	Approved
Terbinafine	The risk or severity of adverse effects can be increased when Terbinafine is combined with Amrinone.	Approved, Investigational, Vet Approved
Terconazole	The risk or severity of adverse effects can be increased when Terconazole is combined with Amrinone.	Approved
Thiamylal	The metabolism of Amrinone can be increased when combined with Thiamylal.	Approved, Vet Approved
Thiopental	The metabolism of Amrinone can be increased when combined with Thiopental.	Approved, Vet Approved
Thymol	The risk or severity of adverse effects can be increased when Thymol is combined with Amrinone.	Approved
Tioconazole	The risk or severity of adverse effects can be increased when Tioconazole is combined with Amrinone.	Approved
Tolnaftate	The risk or severity of adverse effects can be increased when Tolnaftate is combined with Amrinone.	Approved, Vet Approved
Trimazosin	Trimazosin may increase the hypotensive activities of Amrinone.	Experimental
Trimetrexate	The risk or severity of adverse effects can be increased when Trimetrexate is combined with Amrinone.	Approved, Investigational
Tylosin	The metabolism of Amrinone can be decreased when combined with Tylosin.	Vet Approved
Voriconazole	The 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

Resource	Link
Human Metabolome Database (HMDB)	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
Drug Product Database	13165
Wikipedia	Amrinone

ATC Codes

C01CE01 — Amrinone

AHFS Codes

Not Available

PDB Entries

Not Available

FDA label

Not Available

MSDS

Not Available

Clinical Trials

Not Available

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Bedford Labs
Ben Venue Laboratories Inc.
Taylor Pharmaceuticals

Dosage forms

Form	Route	Strength
Liquid	Intravenous	5 mg

Prices

Not Available

Patents

Not Available

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	294-297	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.

Predicted Properties

Property	Value	Source
Water Solubility	5.6 mg/mL	ALOGPS
logP	0.27	ALOGPS
logP	-0.57	ChemAxon
logS	-1.5	ALOGPS
pKa (Strongest Acidic)	11.01	ChemAxon
pKa (Strongest Basic)	4.87	ChemAxon
Physiological Charge	0	ChemAxon
Hydrogen Acceptor Count	3	ChemAxon
Hydrogen Donor Count	2	ChemAxon
Polar Surface Area	68.01 Å²	ChemAxon
Rotatable Bond Count	1	ChemAxon
Refractivity	53.89 m³·mol^-1	ChemAxon
Polarizability	18.94 Å³	ChemAxon
Number of Rings	2	ChemAxon
Bioavailability	1	ChemAxon
Rule of Five	Yes	ChemAxon
Ghose Filter	No	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET features

Property	Value	Probability
Human Intestinal Absorption	+	0.9522
Blood Brain Barrier	+	0.9525
Caco-2 permeable	+	0.8867
P-glycoprotein substrate	Non-substrate	0.6469
P-glycoprotein inhibitor I	Non-inhibitor	0.9338
P-glycoprotein inhibitor II	Non-inhibitor	0.9946
Renal organic cation transporter	Non-inhibitor	0.9258
CYP450 2C9 substrate	Non-substrate	0.8642
CYP450 2D6 substrate	Non-substrate	0.8389
CYP450 3A4 substrate	Non-substrate	0.6443
CYP450 1A2 substrate	Inhibitor	0.9107
CYP450 2C9 inhibitor	Inhibitor	0.5328
CYP450 2D6 inhibitor	Non-inhibitor	0.9651
CYP450 2C19 inhibitor	Inhibitor	0.8994
CYP450 3A4 inhibitor	Non-inhibitor	0.6534
CYP450 inhibitory promiscuity	High CYP Inhibitory Promiscuity	0.5933
Ames test	Non AMES toxic	0.8492
Carcinogenicity	Non-carcinogens	0.9116
Biodegradation	Not ready biodegradable	1.0
Rat acute toxicity	2.9371 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9923
hERG inhibition (predictor II)	Non-inhibitor	0.7418

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

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum Type	Description	Splash Key
Predicted GC-MS	Predicted GC-MS Spectrum - GC-MS	Not Available
LC-MS/MS	LC-MS/MS Spectrum - LC-ESI-qTof , Positive	Not Available
LC-MS/MS	LC-MS/MS Spectrum - , positive	splash10-00lr-3900000000-f6b4ee8cb119f30be206	View in MoNA
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 10V, Positive	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 20V, Positive	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 40V, Positive	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 10V, Negative	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 20V, Negative	Not Available
Predicted LC-MS/MS	Predicted LC-MS/MS Spectrum - 40V, Negative	Not Available

Taxonomy

Description

This compound belongs to the class of chemical entities known as bipyridines and oligopyridines. These are organic compounds containing two pyridine rings linked to each other.

Kingdom

Chemical entities

Super Class

Organic compounds

Class

Organoheterocyclic compounds

Sub Class

Pyridines and derivatives

Direct Parent

Bipyridines and oligopyridines

Alternative Parents

Pyridinones / Dihydropyridines / Aminopyridines and derivatives / Primary aromatic amines / Heteroaromatic compounds / Lactams / Azacyclic compounds / Organopnictogen compounds / Organooxygen compounds / Organic oxides

Substituents

Bipyridine / Aminopyridine / Dihydropyridine / Pyridinone / Hydropyridine / Primary aromatic amine / Heteroaromatic compound / Lactam / Azacycle / Amine

Molecular Framework

Aromatic heteromonocyclic compounds

External Descriptors

Not Available

Targets

Details

1. cAMP-specific 3',5'-cyclic phosphodiesterase 4B

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 from antidepressants to antiasthmatic and anti-inflammatory agents.
Gene Name:: PDE4B
Uniprot ID:: Q07343
Uniprot Name:: cAMP-specific 3',5'-cyclic phosphodiesterase 4B
Molecular Weight:: 83342.695 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. [PubMed:17139284 ]
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 ]

Details

2. Tumor necrosis factor

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 action or by stimulation of interleukin-1 secretion and is implicated in the induction of cachexia, Under certain conditions it can stimulate cell proliferation and induce cell differentiation. Impairs ...
Gene Name:: TNF
Uniprot ID:: P01375
Uniprot Name:: Tumor necrosis factor
Molecular Weight:: 25644.15 Da

References

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 ]
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 ]
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 ]
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 ]
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 ]

Details

3. cGMP-inhibited 3',5'-cyclic phosphodiesterase A

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

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
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 ]
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 ]
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

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 September 01, 2017 10:39

Structure for DB01427 (Amrinone)

Targets

References

References

References

References