Page last updated: 2024-11-04

aprindine

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

Description

Aprindine: A class Ib anti-arrhythmia agent used to manage ventricular and supraventricular arrhythmias. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2218
CHEMBL ID1213033
CHEBI ID135370
SCHEMBL ID34545
MeSH IDM0001626

Synonyms (46)

Synonym
CHEMBL1213033
compound 99170
1,3-propanediamine, n-(2,3-dihydro-1h-inden-2-yl)-n',n'-diethyl-n-phenyl-
aprindine
n-(2,3-dihydro-1h-inden-2-yl)-n',n'-diethyl-n-phenylpropane-1,3-diamine
37640-71-4
D02969
aprindine (usan/inn)
n,3-propanediamine monohydrochloride
nsc284614
fibocil
1, n-(2,3-dihydro-1h-inden-2-yl)-n',n'-diethyl-n-phenyl-, monohydrochloride
aprindin
n,n-diethyl-n'-2-indanyl-n'-phenyl-1,3-propanediamine
n-(3-(diethylamino)propyl)-n-phenyl-2-indanamine
ac 1802
aprindina [inn-spanish]
aprindinum [inn-latin]
n-(2,3-dihydro-1h-inden-2-yl)-n',n'-diethyl-n-phenyl-1,3-propanediamine
aprinidine
DB01429
NCGC00186042-01
n'-(2,3-dihydro-1h-inden-2-yl)-n,n-diethyl-n'-phenylpropane-1,3-diamine
5y48085p9q ,
aprindina
aprindinum
aprindine [usan:inn:ban]
unii-5y48085p9q
SCHEMBL34545
aprindine [who-dd]
compound-99170
aprindine [mi]
aprindine [inn]
aprindine [usan]
NZLBHDRPUJLHCE-UHFFFAOYSA-N
compd 99170
lilly 99170
DTXSID3022615
{3-[(2,3-dihydro-1h-inden-2-yl)(phenyl)amino]propyl}diethylamine
CHEBI:135370
Q263612
SDCCGSBI-0633804.P001
aprinidine; compd 99170; lilly 99170
n/'-(2,3-dihydro-1h-inden-2-yl)-n,n-diethyl-n/'-phenylpropane-1,3-diamine
n-(2,3-dihydro-1h-inden-2-yl)-n',n'-diethyl-n-phenyl-1,3-propaned iamine
n-(2,3-dihydro-1,5-dimethyl-3-oxo-2-phenyl-1h-pyrazol-4-yl)-2-(dimethylamino)propionamide,compound with 4-butyl-1,2-diphenylpyrazolidine-3,5-dione (1:1)

Research Excerpts

Overview

Aprindine hydrochloride is an antiarrhythmic agent presently undergoing clinical trials in the United States. Moxaprindine deserves further assessment in long term studies. Aprindine is a useful agent in refractory ventricular tachycardia.

ExcerptReferenceRelevance
"Aprindine is a very effective antiarrhythmic agent with a narrow therapeutic-toxic ratio. "( Studies with aprindine.
Elharrar, V; Gilmour, RF; Heger, JJ; Prystowsky, EN; Zipes, DP, 1980
)
2.07
"Aprindine hydrochloride is an antiarrhythmic agent presently undergoing clinical trials in the United States. "( Long-term follow-up of patients receiving aprindine. Safety and efficacy.
Bauernfeind, R; Bauman, J; Coelho, A; Prechel, D; Rosen, KM; Strasberg, B; Swiryn, S, 1983
)
1.97
"Moxaprindine is a powerful antiarrhythmic agent which deserves further assessment in long term studies."( The efficacy of intravenous moxaprindine on ventricular ectopic activity.
Guillaume, D; Kulbertus, H; Mary-Rabine, L; Waleffe, A, 1980
)
1.06
"Moxaprindine is a promising new antiarrhythmic drug for the treatment of ventricular arrhythmias, but its value and safely in the chronic oral treatment of these arrhythmias remain to be established."( Moxaprindine in the acute treatment of ventricular arrhythmias in patients with cardiovascular disease.
Kesteloot, H; Staessen, J, 1981
)
1.4
"Aprindine is a long-acting antiarrhythmic agent, effective when administered orally or intravenously in the treatment of ventricular arrhythmias of varying etiologies. "( Aprindine.
Danilo, P, 1979
)
3.15
"Aprindine hydrochloride is an antiarrhythmic drug now under investigation. "( Agranulocytosis associated with aprindine therapy.
Bodenheimer, HC; Samarel, AM, 1979
)
1.99
"Aprindine is a useful agent in refractory ventricular tachycardia, and the absence of the repetitive ventricular response after its intravenous administration predicts long-term clinical responsiveness to the oral form."( Suppression of the repetitive ventricular response: an index of long-term antiarrhythmic effectiveness of aprindine for ventricular tachycardia in man.
Greene, HL; Reid, PR; Schaeffer, AH, 1978
)
1.19
"Aprindine is an effective antiarrhythmic agent in some experimental cardiac arrhythmias, but the appearance of central nervous system toxicity at therapeutic drug concentrations in conscious animals indicates that it may have a narrow margin of safety."( Antiarrhythmic and antifibrillatory properties of aprindine.
Kroll, DA; Lucchesi, BR, 1975
)
1.23
"Aprindine is a very effective antiarrhythmic agent with a narrow therapeutic ratio. "( Aprindine-induced hepatic granulomata.
Elisaf, M; Masalas, C; Stefanaki-Nikou, S; Tsianos, EV; Voulgarelis, M, 1992
)
3.17
"Aprindine is a class Ib antiarrhythmic agent. "( Aprindine blocks the sodium current in guinea-pig ventricular myocytes.
Hisatome, I; Katori, R; Kotake, H; Mashiba, H; Sasaki, N; Sato, R; Tanaka, Y, 1991
)
3.17
"Aprindine hydrochloride is a potent antiarrhythmic agent against various atrial and ventricular tachyarrhythmias. "( Electrophysiologic actions of aprindine in rabbit atrioventricular node.
Habuchi, Y; Homma, N; Nishimura, M; Tanaka, H; Watanabe, Y, 1990
)
2.01

Effects

Aprindine hydrochloride has been extensively used in Europe for the management of ventricular and supraventricular arrhythmias. Aprindine has hydrophobic properties which may be responsible for the inhibitory effect.

ExcerptReferenceRelevance
"Aprindine has hydrophobic properties which may be responsible for the inhibitory effect."( Aprindine inhibits calmodulin-stimulated phosphodiesterase and Ca-ATPase activities.
Hollier, B; Levine, SN,
)
2.3
"Aprindine hydrochloride has been extensively used in Europe for the management of ventricular and supraventricular arrhythmias. "( Aprindine therapy for refractory ventricular tachycardia.
Carleton, RA; Chown, M; Khan, AH, 1983
)
3.15

Actions

Only aprindine caused an increase in LDH leakage above 2 X 10(-4) M. Aprindine was chosen because of its long half-life and few side effects.

ExcerptReferenceRelevance
"Aprindine was chosen because of its long half-life, few side effects, and antiarrhythmic efficacy."( Prophylactic antiarrhythmic therapy of high-risk survivors of myocardial infarction: lower mortality at 1 month but not at 1 year.
Achuff, SC; Baughman, KL; Becker, L; Chandra, NC; Gerstenblith, G; Gottlieb, SH; Heck, C; Henley, S; Humphries, JO; Mellits, ED, 1987
)
0.99
"Only aprindine caused an increase in LDH leakage above 2 X 10(-4) M."( [Effects of antiarrhythmic drugs on rat erythrocytes, isolated hepatocytes and dipalmitoyl phosphatidyl choline (DPPC)-liposomes].
Kasahara, T; Kawashima, I; Manabe, A; Nakayama, S; Sakamoto, K; Shirasaki, K, 1985
)
0.72

Treatment

ExcerptReferenceRelevance
"Treatment with aprindine or mexiletine was effective in 7 (50%) of the 14 patients who did not respond to procainamide and/or disopyramide."( Analysis of ventricular arrhythmias in patients with dilated cardiomyopathy--relationship between the effects of antiarrhythmic agents and severity of myocardial lesions.
Fukuzaki, H; Takarada, A; Yokota, Y, 1990
)
0.62

Toxicity

ExcerptReferenceRelevance
" The comparison of hemodynamic, electrocardiographic and toxic effects of mexiletine with those produced by other antiarrhythmics showed that mexiletine placed itself among the better tolerated antiarrhythmics during the administration of progressively increasing doses."( Hemodynamic, electrocardiographic and toxic effects of the intravenous administration of increasing doses of mexiletine in the dog. Comparison with similar effects produced by other antiarrhythmics.
Carlier, J, 1980
)
0.26
" Bepridil is effective and safe for terminating long-lasting persistent AF."( Usefulness and safety of bepridil in converting persistent atrial fibrillation to sinus rhythm.
Fujiki, A; Inoue, H; Mizumaki, K; Sugao, M; Tsuneda, T, 2003
)
0.32

Pharmacokinetics

Moxaprindine and aprindine are similar in several of their pharmacokinetic characteristics. The mean elimination half-life of aprindin was 18.

ExcerptReferenceRelevance
" The mean elimination half-life of aprindine was 18."( [Effects of intravenous aprindine on hemodynamics in patients with cardiac dysfunction and its pharmacodynamics in patients with premature ventricular contractions].
Hayasaki, K; Matsumoto, N, 1990
)
0.86
"77 microgram/ml and a mean elimination half-life of 26."( Non-linear pharmacokinetics of aprindine hydrochloride in oral administration.
Enomoto, N; Goto, J; Inagaki, H; Sotobata, I; Takahashi, A; Uematsu, H; Yokota, M, 1987
)
0.56
" Moxaprindine and aprindine are similar in several of their pharmacokinetic characteristics."( Pharmacokinetic study of aprindine and moxaprindine in dogs.
Breekpot, F; de Suray, JM; Lavis, A, 1981
)
1.12

Compound-Compound Interactions

Bepridil alone or in combination with aprindine is effective for termination of persistent AF. In Group I, sinus rhythm was pharmacologically restored in 22 patients after an average of 30 days.

ExcerptReferenceRelevance
" Bepridil alone or in combination with aprindine is effective for termination of persistent AF."( Maintenance of sinus rhythm and recovery of atrial mechanical function after cardioversion with bepridil or in combination with aprindine in long-lasting persistent atrial fibrillation.
Fujiki, A; Hirai, T; Inoue, H; Mizumaki, K; Nakagawa, K; Sakabe, M; Tsuneda, T, 2004
)
0.8
" In Group I, sinus rhythm was pharmacologically restored in 22 patients after an average 30 days (7-49 days) of bepridil administration, either alone (11) or in combination with oral aprindine (11); they were followed up while using the same drugs."( Maintenance of sinus rhythm and recovery of atrial mechanical function after cardioversion with bepridil or in combination with aprindine in long-lasting persistent atrial fibrillation.
Fujiki, A; Hirai, T; Inoue, H; Mizumaki, K; Nakagawa, K; Sakabe, M; Tsuneda, T, 2004
)
0.72
"In patients with long-lasting AF, pharmacological conversion with bepridil alone or in combination with aprindine recovered atrial mechanical function better and maintained sinus rhythm longer than electrical conversion."( Maintenance of sinus rhythm and recovery of atrial mechanical function after cardioversion with bepridil or in combination with aprindine in long-lasting persistent atrial fibrillation.
Fujiki, A; Hirai, T; Inoue, H; Mizumaki, K; Nakagawa, K; Sakabe, M; Tsuneda, T, 2004
)
0.74
"Bepridil alone or in combination with aprindine converted long lasting persistent AF in association with an increase in both FCL and FOI."( Drug-induced changes in fibrillation cycle length and organization index can predict chemical cardioversion of long-lasting atrial fibrillation with bepridil alone or in combination with aprindine.
Fujiki, A; Inoue, H; Iwamoto, J; Mizumaki, K; Nishida, K; Sakabe, M; Sugao, M; Tsuneda, T, 2004
)
0.79

Bioavailability

ExcerptReferenceRelevance
"P-glycoprotein (Pgp or ABCB1) is an ABC transporter protein involved in intestinal absorption, drug metabolism, and brain penetration, and its inhibition can seriously alter a drug's bioavailability and safety."( A novel approach for predicting P-glycoprotein (ABCB1) inhibition using molecular interaction fields.
Broccatelli, F; Carosati, E; Cruciani, G; Frosini, M; Goracci, L; Neri, A; Oprea, TI, 2011
)
0.37

Dosage Studied

Aprindine was administered orally in a dosage of 50 to 75 mg/d. In the other 16 patients with a higher dosage regime, 109 mg Aprindine and 707 mg Quinidine base, there was no significant difference.

ExcerptRelevanceReference
" It may, therefore, be concluded that in patients with otherwise normal hearts aprindin applied in a dosage sufficient to stop the SVT, does not exhibit noteworthy inotropic side effects."( [Changes in hemodynamics and contractility during supraventricular tachycardias and after electrical or aprindin-induced termination (author's transl)].
Merle, H; Schlepper, M; Weppner, HG, 1976
)
0.26
" 14, 1987, and the dosage was decreased gradually."( [A case of aprindine-induced pneumonitis].
Doutsu, Y; Hara, K; Hayashi, T; Hiratani, K; Hirota, M; Kohno, S; Komori, K; Miyazaki, T; Oda, H; Yamaguchi, K, 1990
)
0.67
" With multiple oral administration in 10 mg and 20 mg doses at intervals of 8 h, plasma concentration reached a steady state in 1-2 weeks with either dosage rate."( Non-linear pharmacokinetics of aprindine hydrochloride in oral administration.
Enomoto, N; Goto, J; Inagaki, H; Sotobata, I; Takahashi, A; Uematsu, H; Yokota, M, 1987
)
0.56
" Serious adverse reactions necessitate a change in antiarrhythmic therapy, as opposed to lowering drug dosage to an ineffective level."( Antiarrhythmic drug therapy. Recent advances and current status.
Somberg, J, 1985
)
0.27
" If side effects intervene that may cause continued therapy to be intolerable, changing the antiarrhythmic agent, as opposed to decreasing the dosage to an ineffective range, may be appropriate."( New directions in antiarrhythmic drug therapy.
Somberg, JC, 1984
)
0.27
"Measurement of drug levels is becoming increasingly popular to optimise the dosage of various drugs."( Reliability of antiarrhythmic drug plasma concentration monitoring.
Follath, F; Ganzinger, U; Schuetz, E,
)
0.13
" Aprindine was administered orally in a dosage of 50 to 75 mg/d."( Cardiac effects of aprindine in patients with or without cardiac dysfunction: echocardiographic and clinical evaluation.
Araki, H; Nakagaki, O; Nakamura, M; Orita, Y; Shimada, R, 1983
)
1.5
" The sinus rate was slowed at every dosage level."( Moxaprindine in the acute treatment of ventricular arrhythmias in patients with cardiovascular disease.
Kesteloot, H; Staessen, J, 1981
)
0.88
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
indanes
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency16.83360.100020.879379.4328AID588456
arylsulfatase AHomo sapiens (human)Potency37.93301.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency28.18380.035520.977089.1251AID504332
D(1A) dopamine receptorHomo sapiens (human)Potency31.62280.02245.944922.3872AID488983
flap endonuclease 1Homo sapiens (human)Potency3.76860.133725.412989.1251AID588795
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency20.88680.00378.618923.2809AID2667; AID2668
D(1A) dopamine receptorSus scrofa (pig)Potency18.49270.00378.108123.2809AID2667
Ataxin-2Homo sapiens (human)Potency11.22020.011912.222168.7989AID588378
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency37.93300.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (6)

Processvia Protein(s)Taxonomy
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (60)

Assay IDTitleYearJournalArticle
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID669781Inhibition of human recombinant MDR1 expressed in mouse L5178Y cells assessed as inhibition of rhodamine-123 efflux at 10'-4 M preincubated for 10 mins measured after 20 mins by FACS analysis2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Ligand Promiscuity between the Efflux Pumps Human P-Glycoprotein and S. aureus NorA.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
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
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]
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1480298Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Computer-Aided Discovery and Characterization of Novel Ebola Virus Inhibitors.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
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]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
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]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID598252Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 at 0.1 mM after 20 mins by FACS analysis relative to 5 mM sodium orthovanadate2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
A novel approach for predicting P-glycoprotein (ABCB1) inhibition using molecular interaction fields.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' 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]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID669779Inhibition of norA-mediated ethidium bromide efflux in Staphylococcus aureus SA-1199B harboring grlA A116E mutant at 50 uM after 5 mins by fluorometric analysis2012ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3
Ligand Promiscuity between the Efflux Pumps Human P-Glycoprotein and S. aureus NorA.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID598251Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 after 20 mins by FACS analysis2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
A novel approach for predicting P-glycoprotein (ABCB1) inhibition using molecular interaction fields.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
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]
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (259)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990183 (70.66)18.7374
1990's45 (17.37)18.2507
2000's15 (5.79)29.6817
2010's10 (3.86)24.3611
2020's6 (2.32)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 26.91

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 Index26.91 (24.57)
Research Supply Index5.76 (2.92)
Research Growth Index4.18 (4.65)
Search Engine Demand Index33.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (26.91)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials26 (8.97%)5.53%
Reviews28 (9.66%)6.00%
Case Studies37 (12.76%)4.05%
Observational0 (0.00%)0.25%
Other199 (68.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]