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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyAmrinone
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
Structure for DB01427 (Amrinone)
- Synonyms
- Amcoral
- Amrinona
- Amrinonum
- Inamrinone
- External IDs
- C01CE01 / WIN 40680 / WIN-40680
- Product Ingredients
Ingredient UNII CAS InChI Key Amrinone lactate I229274Y5B 75898-90-7 DOSIONJFGDSKCQ-UHFFFAOYSA-N - 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 
- International/Other Brands
- Amcoral / Inocor
- Categories
- Amines
- Aminopyridines
- Calcium Channel Blockers
- Cardiac Stimulants Excl. Cardiac Glycosides
- Cardiac Therapy
- Cardiotonic Agents
- Cardiovascular Agents
- Cardiovascular System
- Enzyme Inhibitors
- Membrane Transport Modulators
- Phosphodiesterase 3 Inhibitors
- Phosphodiesterase Inhibitors
- Protective Agents
- Pyridines
- Vasodilator Agents
- 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 Actions Organism UcAMP-specific 3',5'-cyclic phosphodiesterase 4B inhibitorHuman UTumor necrosis factor inhibitorHuman AcGMP-inhibited 3',5'-cyclic phosphodiesterase A inhibitorHuman UcAMP-specific 3',5'-cyclic phosphodiesterase 3 Not Available Human - 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 Atorvastatin The risk or severity of adverse effects can be increased when Amrinone is combined with Atorvastatin. 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 Brefeldin A The risk or severity of adverse effects can be increased when 1,6,7,8,9,11A,12,13,14,14A-DECAHYDRO-1,13-DIHYDROXY-6-METHYL-4H-CYCLOPENT[F]OXACYCLOTRIDECIN-4-ONE is combined with Amrinone. Experimental Bucindolol Bucindolol may increase the hypotensive activities of Amrinone. Investigational Bunazosin Bunazosin 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 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 Calcium lactate The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium lactate. Approved, Experimental, Vet Approved Calcium lactate gluconate The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium lactate gluconate. Experimental Calcium laevulate The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium laevulate. Experimental Calcium pangamate The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium pangamate. Experimental Calcium Phosphate The therapeutic efficacy of Amrinone can be decreased when used in combination with Calcium Phosphate. 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 Capric 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 Casein The therapeutic efficacy of Amrinone can be decreased when used in combination with Casein. Approved Caspofungin The risk or severity of adverse effects can be increased when Caspofungin is combined with Amrinone. Approved Cerivastatin The risk or severity of adverse effects can be increased when Amrinone is combined with Cerivastatin. Withdrawn 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 Dichlorophene The risk or severity of adverse effects can be increased when Dichlorophene is combined with Amrinone. Vet Approved 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 Fenticonazole The risk or severity of adverse effects can be increased when Fenticonazole is combined with Amrinone. Experimental 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 Flutrimazole The risk or severity of adverse effects can be increased when Flutrimazole is combined with Amrinone. Experimental Fluvastatin The risk or severity of adverse effects can be increased when Amrinone is combined with Fluvastatin. 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 Hachimycin The risk or severity of adverse effects can be increased when Hachimycin is combined with Amrinone. Experimental 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 Lovastatin The risk or severity of adverse effects can be increased when Amrinone is combined with Lovastatin. Approved, Investigational 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 Mepartricin The risk or severity of adverse effects can be increased when Mepartricin is combined with Amrinone. Experimental 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 Nifuratel The risk or severity of adverse effects can be increased when Nifuratel is combined with Amrinone. Experimental Nikkomycin Z The risk or severity of adverse effects can be increased when Nikkomycin Z is combined with Amrinone. Investigational 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 Omoconazole The risk or severity of adverse effects can be increased when Omoconazole is combined with Amrinone. Experimental 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 Pitavastatin The risk or severity of adverse effects can be increased when Amrinone is combined with Pitavastatin. Approved Posaconazole The risk or severity of adverse effects can be increased when Posaconazole is combined with Amrinone. Approved, Investigational, Vet Approved Pravastatin The risk or severity of adverse effects can be increased when Amrinone is combined with Pravastatin. 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 Pyrrolnitrin The risk or severity of adverse effects can be increased when Pyrrolnitrin is combined with Amrinone. Experimental 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 Rosuvastatin The risk or severity of adverse effects can be increased when Amrinone is combined with Rosuvastatin. 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 Simvastatin The risk or severity of adverse effects can be increased when Amrinone is combined with Simvastatin. 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 Tolciclate The risk or severity of adverse effects can be increased when Tolciclate is combined with Amrinone. Experimental 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 Ubidecarenone The risk or severity of adverse effects can be increased when Amrinone is combined with Ubidecarenone. Experimental Urapidil Urapidil may increase the hypotensive activities of Amrinone. Investigational 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
- ATC Codes
- C01CE01 — Amrinone
- AHFS Codes
- Not Available
- PDB Entries
- Not Available
- FDA label
- Not Available
- MSDS
- Not Available
Clinical Trials
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
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 MS/MS Spectrum - , positive LC-MS/MS splash10-00lr-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
- 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]
- 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
- 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]
- 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
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 October 02, 2017 04:58