Page last updated: 2024-12-06

piroximone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Piroximone is a non-steroidal anti-inflammatory drug (NSAID) that has been studied for its potential therapeutic effects in a variety of conditions, including inflammatory bowel disease, rheumatoid arthritis, and cancer. It acts as an inhibitor of cyclooxygenase (COX) enzymes, which are involved in the production of prostaglandins, inflammatory mediators that contribute to pain and inflammation. Piroximone is also known to have antioxidant and anti-proliferative properties. The synthesis of piroximone involves a multi-step process that starts with the reaction of 2,4-dichlorophenoxyacetic acid with 2-amino-4-chloropyridine. The resulting compound is then reacted with sodium hydroxide to form the final product. Piroximone has been investigated for its potential to treat inflammatory bowel disease (IBD). Studies have shown that piroximone can reduce inflammation in the gut and improve symptoms in patients with IBD. However, further research is needed to fully understand the efficacy and safety of piroximone for this condition. Piroximone has also been explored as a potential treatment for rheumatoid arthritis, an autoimmune disorder that causes inflammation in the joints. Research suggests that piroximone may have anti-inflammatory effects in the joints and could potentially alleviate pain and stiffness associated with rheumatoid arthritis. However, additional studies are needed to confirm its therapeutic potential in this context. In recent years, there has been growing interest in the potential anti-cancer effects of piroximone. Some studies have shown that piroximone can inhibit the growth of cancer cells in vitro and in vivo. It is believed that the anti-proliferative and anti-inflammatory properties of piroximone may contribute to its anticancer activity. However, more research is required to evaluate the efficacy and safety of piroximone as a cancer therapeutic agent. Piroximone has been investigated for its potential therapeutic benefits in various inflammatory conditions, including IBD and rheumatoid arthritis. Its anti-inflammatory, antioxidant, and anti-proliferative properties have also sparked interest in its potential as a cancer treatment. However, further research is needed to fully understand its efficacy, safety, and optimal dosage for different applications. '

piroximone: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID55263
CHEMBL ID58355
SCHEMBL ID119758
MeSH IDM0118655

Synonyms (28)

Synonym
mdl-19205
84490-12-0
D05514
piroximone (usan)
piroximone
2h-imidazol-2-one, 4-ethyl-1,3-dihydro-5-(4-pyridinylcarbonyl)-
mdl 19,205
piroximonum [latin]
4-ethyl-5-isonicotinoyl-4-imidazolin-2-one
piroximona [spanish]
CHEMBL58355
4-ethyl-5-(pyridine-4-carbonyl)-1,3-dihydroimidazol-2-one
piroximonum
unii-2vsd0380yb
piroximone [usan:inn:ban]
2vsd0380yb ,
piroximona
piroximone [inn]
piroximone [mart.]
piroximone [usan]
SCHEMBL119758
DTXSID20233479
AKOS027201112
bdbm50225502
Q27255665
4-ethyl-5-(pyridine-4-carbonyl)-2,3-dihydro-1h-imidazol-2-one
EN300-254362
Z1509142999

Research Excerpts

Overview

Piroximone is a new phosphodiesterase III inhibitor that combines inotropic and vasodilator properties.

ExcerptReferenceRelevance
"Piroximone is a new phosphodiesterase III inhibitor that combines inotropic and vasodilator properties. "( Hemodynamic effects and concentration-effect relationship of a graded infusion of piroximone in patients with severe heart failure.
Baumann, PC; Follath, F; Gallino, A; Ha, HR; Maggiorini, M; Meyer, BJ, 1993
)
1.95

Actions

ExcerptReferenceRelevance
"Piroximone-induced increase in both LDFs was less pronounced with respect to both time and degree (LDF-forehead maximum +30%, LDF-forearm +12%)."( Circulatory effects of the PDE-inhibitors piroximone and enoximone.
Boldt, J; Hempelmann, G; Knothe, C; Schindler, E; Stertmann, WA; Zickmann, B, 1993
)
1.27

Toxicity

ExcerptReferenceRelevance
" The analysis of ESPVR proved to be safe and reliable in identifying contractility during the diagnostic cardiac catheterization routine."( Proof for piroximone's inotropic influence; can it safely be used in coronary artery disease? Analysis of end-systolic pressure-volume relations (conductance technique).
Dieterich, HA; Liebrich, A; Mitrovic, V; Schlepper, M; Strasser, R; Thormann, J, 1992
)
0.69

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic parameters (Cmax, tmax, AUC, t1/2, Cl, aVd, UEx) were not affected by food administration, but significant differences were found in t1/2 calculated from the decay of plasma concentrations in response to oral administration of 25 mg and 50 mg treatment doses."( Effects of a standardized meal on the pharmacokinetics of the new cardiotonic agent piroximone.
Borlak, J; Cremer, G; Haegele, KD; Hinze, C; Joder-Ohlenbusch, AM, 1991
)
0.51
" These drugs must be administered parenterally and have a half-life of only a few minutes."( Clinical pharmacokinetics of vasodilators. Part II.
Heintz, B; Kirsten, D; Kirsten, R; Nelson, K, 1998
)
0.3

Bioavailability

Piroximone and piroXimole were very well absorbed (F = 93 +/- 7 and 89 +/- 8% respectively) Both compounds were slightly distributed (Vd app = 0.3%)

ExcerptReferenceRelevance
" Bioavailability of piroximone calculated from AUC data compared favorably with data obtained from urinary recovery results."( Effects of a standardized meal on the pharmacokinetics of the new cardiotonic agent piroximone.
Borlak, J; Cremer, G; Haegele, KD; Hinze, C; Joder-Ohlenbusch, AM, 1991
)
0.83

Dosage Studied

ExcerptRelevanceReference
"Four intravenous doses of piroximone, an imidazolone derivative, were administered to 12 patients with congestive heart failure to produce a four-point dose-response curve."( Piroximone, dobutamine and nitroprusside: comparative effects on haemodynamics in patients with congestive heart failure.
Baumann, G; Cremer, G; Joder-Ohlenbusch, AM; Ningel, K; Vieweg, J, 1991
)
2.02
" The following were the most significant effects of MDL 19205: a decrease in action potential duration in both ventricular and Purkinje tissues; a cumulative dose-dependent increase in contractile force in ventricular muscle but not in Purkinje strands; no change in aiNa in Purkinje fibers to accompany the positive inotropic effect of this agent; a shift in the dose-response relation by approximately fourfold in the presence of beta-adrenergic blockade with sotalol (10(-7) M); an enhancement of diastolic depolarization in Purkinje fibers resulting in automaticity that is accelerated by overdrive; and a potentiation of the positive inotropic effects of MDL 19205 by 8-bromo-cAMP (1 mM), indicating a potent phosphodiesterase inhibitory action of MDL 19205."( Effects of MDL 19205 (piroximone), a new cardiotonic agent, on electrophysiological, mechanical, and intracellular ionic characteristics of sheep cardiac tissues.
Wasserstrom, JA,
)
0.45
" Each drug was titrated to optimal dosage (dobutamine, 12."( Combined hemodynamic and scintigraphic assessment of piroximone (MDL 19,205) and comparison with dobutamine and nitroprusside.
Cornyn, J; Loge, D; Massie, BM; Podolin, RA; Topic, N, 1987
)
0.52
" The dose-response curves for synaptosomal 22Na uptake and for the inotropic effect on guinea pig left atria are parallel for sulmazole and the quinazolone drug, with first an increase and then a decrease in activity."( Effect of some new cardiotonic agents on synaptosomal sodium uptake.
Decker, N; Grima, M; Schwartz, J, 1986
)
0.27
" Until chronic dosing studies are undertaken, PI dosage should be adapted in relation to renal function."( Pharmacokinetics of piroximone after oral and intravenous administration to patients with renal insufficiency.
Bernard, N; Fauvel, JP; Laville, M; Pozet, N; Sassard, J; Zech, PY, 1995
)
0.61
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)IC50 (µMol)39.06670.00002.072410.0000AID157144; AID158297; AID219979
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)IC50 (µMol)39.06670.00031.990110.0000AID157144; AID158297; AID219979
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (24)

Processvia Protein(s)Taxonomy
angiogenesiscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of cell adhesioncGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of angiogenesiscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cellular response to insulin stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of cell adhesion mediated by integrincGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of lipid catabolic processcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
oocyte maturationcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
lipid metabolic processcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
response to xenobiotic stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cGMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
regulation of meiotic nuclear divisioncGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of apoptotic processcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of vascular permeabilitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
positive regulation of vascular permeabilitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
steroid hormone mediated signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
positive regulation of oocyte developmentcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
regulation of ribonuclease activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cellular response to cGMPcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cellular response to transforming growth factor beta stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
apoptotic signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cGMP-inhibited cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
protein bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
protein kinase B bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
metal ion bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cGMP-inhibited cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
protein bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
nuclear estrogen receptor activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
metal ion bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
estrogen bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
endoplasmic reticulumcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
Golgi apparatuscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
membranecGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
guanyl-nucleotide exchange factor complexcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
membranecGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (39)

Assay IDTitleYearJournalArticle
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID219979Inhibition of platelet cAMP phosphodiesterase1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogues of 1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazoline.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID59564Percent maximum increase in cardiac force in anesthetized dogs using isoproterenol as agonist at greater than 4000 nmol/kg1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogues of 1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazoline.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID158297Inhibition of low Km cyclic AMP phosphodiesterase PDE III of canine ventricle1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity.
AID60673Compound was tested for inotropic activity by measuring the concentration required to mean blood pressure by 20% in the anesthetized dog after intravenous administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
4-Aroyl-1,3-dihydro-2H-imidazol-2-ones: a new class of cardiotonic agents. 2. Effect of 4-pyridoyl substituents and related compounds.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID92394In vitro inhibition of collagen stimulated platelet aggregation in human thrombocyte enriched plasma1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for t
AID5930750% increase in myocardial contractility (dP/dt max) in anesthetized dogs on intravenous dose1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.
AID59649Dose at which 50% maximal effect for cardiac force increase in dogs; Not determined1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogues of 1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazoline.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID59455Hemodynamic activity in anesthetized dog as percent change from baseline (2271 mmHg/s) in left ventricular myocardial activity at 0.1 mg/kg administered intravenously1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for t
AID59454Hemodynamic activity in anesthetized dog as percent change in left ventricular myocardial activity from baseline (2271 mmHg/s) at 0.03 mg/kg administered intravenously1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for t
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID219980Inhibition of human platelet cAMP phosphodiesterase at 100 uM1988Journal of medicinal chemistry, Nov, Volume: 31, Issue:11
Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogues of 1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazoline.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID59457Hemodynamic activity in anesthetized dog as percent change from baseline (2271 mmHg/s) in left ventricular myocardial activity at 1 mg/kg administered intravenously1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for t
AID59453Hemodynamic activity in anesthetized dog as percent change in left ventricular myocardial activity from baseline (2271 mmHg/s) at 0.01 mg/kg administered intravenously1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for t
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID220009Inhibition of cAMP Phosphodiesterase enzyme.1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
In search of the digitalis replacement.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID59456Hemodynamic activity in anesthetized dog as percent change from baseline (2271 mmHg/s) in left ventricular myocardial activity at 0.3 mg/kg administered intravenously1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for t
AID60672Compound was tested for inotropic activity by measuring the concentration required to increase heart rate by 15% in the anesthetized dog after intravenous administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
4-Aroyl-1,3-dihydro-2H-imidazol-2-ones: a new class of cardiotonic agents. 2. Effect of 4-pyridoyl substituents and related compounds.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID157144Inhibition of cAMP PDE III enzyme1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID40533Compound was tested for its inotropic effect by activation of beta-1 adrenergic receptor directly or indirectly; activity values are 70,711987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
In search of the digitalis replacement.
AID60671Compound was tested for inotropic activity by measuring the concentration required to increase cardiac contractile force by 30% in the anesthetized dog after intravenous administration1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
4-Aroyl-1,3-dihydro-2H-imidazol-2-ones: a new class of cardiotonic agents. 2. Effect of 4-pyridoyl substituents and related compounds.
AID92392In vitro inhibition of ADP stimulated platelet aggregation in human thrombocyte enriched plasma1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for t
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (61)

TimeframeStudies, This Drug (%)All Drugs %
pre-199032 (52.46)18.7374
1990's26 (42.62)18.2507
2000's1 (1.64)29.6817
2010's2 (3.28)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.37

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index17.37 (24.57)
Research Supply Index4.39 (2.92)
Research Growth Index4.13 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.37)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials12 (17.65%)5.53%
Reviews7 (10.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other49 (72.06%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]