Page last updated: 2024-12-04

buflomedil

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

Description

buflomedil: RN given refers to parent cpd; synonym LL 1656 refers to HCl; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2467
CHEMBL ID188921
CHEBI ID94538
SCHEMBL ID150905
MeSH IDM0056294

Synonyms (49)

Synonym
BRD-K19462402-003-03-0
1-butanone, 4-(1-pyrrolidinyl)-1-(2,4,6-trimethoxyphenyl)-
buflomedil
4-pyrrolidin-1-yl-1-[2,4,6-tris(methyloxy)phenyl]butan-1-one
55837-25-7
einecs 259-851-3
buflomedilum [inn-latin]
2',4',6'-trimethoxy-4-(1-pyrrolidinyl)butyrophenone
4-(1-pyrrolidinyl)-1-(2,4,6-trimethoxyphenyl)-1-butanone
buflomedil [inn:ban:dcf]
NCGC00016831-01
cas-35543-24-9
PRESTWICK3_000426
PRESTWICK2_000426
D07176
buflomedil (inn)
BPBIO1_000454
BSPBIO_000412
NCGC00164382-01
PRESTWICK1_000426
SPBIO_002351
PRESTWICK0_000426
AC-11046
CHEMBL188921 ,
bdbm50170664
4-pyrrolidin-1-yl-1-(2,4,6-trimethoxy-phenyl)-butan-1-one
4-pyrrolidin-1-yl-1-(2,4,6-trimethoxyphenyl)butan-1-one
v7i71dq432 ,
unii-v7i71dq432
buflomedilum
AKOS015967520
NCGC00016831-02
FT-0623280
NCGC00016831-04
buflomedil [mi]
buflomedil [who-dd]
buflomedil [inn]
SCHEMBL150905
W-105544
4-(1-pyrrolidinyl)-1-(2,4,6-trimethoxyphenyl)-1-butanone #
OWYLAEYXIQKAOL-UHFFFAOYSA-N
DTXSID5022697
CHEBI:94538
SBI-0207020.P001
4-(pyrrolidin-1-yl)-1-(2,4,6-trimethoxyphenyl)butan-1-one
Q417862
DB13510
BRD-K19462402-003-13-9
E79447

Research Excerpts

Overview

Buflomedil is a rheological agent largely used as a vasodilator in some European countries. It seems to be an antagonist of both alpha 1- and alpha 2-vascular adrenoceptors.

ExcerptReferenceRelevance
"Buflomedil is a vasoactive agent used to treat peripheral vascular disease."( Buflomedil for intermittent claudication.
de Backer, TL; Vander Stichele, R, 2013
)
2.55
"Buflomedil is a vasoactive agent that has been used for peripheral arterial diseases."( Buflomedil for acute ischaemic stroke.
He, S; Lin, S; Liu, M; Wu, B; Wu, S; Yang, J; Zeng, Q, 2015
)
2.58
"buflomedil is an effective and safe drug for treating diabetic peripheral neuropathy patients."( [Clinical study of the effect of buflomedil on peripheral neuropathy in diabetic patients].
Lei, MX; Zhou, M, 2001
)
2.03
"Buflomedil is a vasoactive agent used to treat peripheral vascular disease."( Buflomedil for intermittent claudication.
Bogaert, M; de Backer, TL; Vander Stichele, R, 2007
)
2.5
"Buflomedil is a vasoactive agent used to treat peripheral vascular disease."( Buflomedil for intermittent claudication.
Bogaert, M; de Backer, TL; Vander Stichele, R, 2008
)
2.51
"Buflomedil is a rheological agent largely used as a vasodilator in some European countries."( Acute buflomedil intoxication: a life-threatening condition.
Alberti, A; Del Monte, D; Gallo, F; Petolillo, M; Valenti, S, 1994
)
1.49
"Buflomedil is a vasoactive agent claimed to have beneficial effects on the microcirculation."( Buflomedil for intermittent claudication.
Bogaert, MG; De Backer, TL; Vander Stichele, RH, 2001
)
2.47
"Buflomedil is a vasoactive drug used in the treatment of peripheral vascular disease, and seems to be an antagonist of both alpha 1- and alpha 2-vascular adrenoceptors. "( Effects of buflomedil and its two derivatives, CRL40634 and CRL40598, on pancreatic exocrine secretion in the rat.
Chariot, J; Nagain, C; Rozé, C; Vaille, C, 1990
)
2.11
"Buflomedil is a vasoactive agent widely used in the treatment of peripheral arterial disease. "( [Comparison of the effectiveness of intra-arterial and intravenous administration of buflomedil in patients with intermittent claudication].
Diehm, C; Eckstein, M; Hübsch-Müller, C, 1989
)
1.94
"Buflomedil chlorhydrate is a newly synthesized molecule with a notable effect of vasodilatation even on cerebral blood vessels. "( [Whole blood filterability in chronic cerebrovascular disorders: effects of the use of buflomedil hydrochloride].
Ciuffetti, G; Lombardini, R; Mercuri, M; Palazzetti, D; Parnetti, L; Rizzo, MT, 1989
)
1.94
"Buflomedil hydrochloride is a vasoactive drug with a variety of pharmacodynamic properties. "( Buflomedil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in peripheral and cerebral vascular diseases.
Clissold, SP; Lynch, S; Sorkin, EM, 1987
)
3.16

Effects

ExcerptReferenceRelevance
"Buflomedil has been reported to improve microvascular perfusion with a secondary increase in tissue oxygen pressure and may therefore be of interest in the study of diabetic retinopathy."( The effect of buflomedil in diabetic retinopathy estimated by ocular fluorophotometry.
Ditzel, J; Kjaergaard, JJ, 1987
)
1.35

Actions

ExcerptReferenceRelevance
"Buflomedil induced an increase of the same order of magnitude in plasma levels of adenosine and adenine nucleotides."( Increase in plasma levels of adenosine and adenine nucleotides after intravenous infusion of buflomedil in humans.
Capecchi, PL; Chiavetta, M; De Lalla, A; Di Perri, T; Laghi Pasini, F; Sensi, S; Sodi, N; Volpi, L, 1995
)
1.23

Treatment

Treatment with buflomedil attenuated ischemia-induced histological loss and damage of CA1 pyramidal cells. The drug significantly reduced both post-ischemic capillary perfusion failure and leukocyte adherence in venules.

ExcerptReferenceRelevance
"Treatment with buflomedil attenuated ischemia-induced histological loss and damage of CA1 pyramidal cells."( Protective effect of buflomedil in a rat model of moderate cerebral ischemia.
Briguglio, FS; De Pasquale, A; Galluzzo, M; Mondello, MR; Raneri, E; Saija, A; Trombetta, D, 2005
)
0.99
"Treatment with buflomedil significantly reduced both post-ischemic capillary perfusion failure and leukocyte adherence in venules."( Buflomedil hydrochloride attenuates tourniquet-induced microvascular reperfusion injury in striated muscle.
Menger, MD; Messmer, K; Pelikan, S; Steiner, D,
)
1.91
"Treatment with buflomedil (3 mg/kg b.w."( Reduction of postischemic reperfusion injury by the vasoactive drug buflomedil.
Lehr, HA; Messmer, K; Nolte, D; Sack, FU, 1991
)
0.86
"Treatment with buflomedil for 3 months led to a significant improvement in signs and symptoms in all four clinical stages."( [Epidemiologic study of peripheral obstructive arteriopathies: clinical effects of treatment with buflomedil chlorhydrate (Loftyl). Processing of data furnished by a polycenter study].
, 1985
)
0.83

Toxicity

Bflomedil is a vasodilator with the indication for peripheral arterial disease (PAD) marketed in Europe since the 1970s but recently suspended by the European Medicines Agency. According to our results, buflomedill is more effective and safe than naftidrofuryl in the treatment of patients with intermittent claudication.

ExcerptReferenceRelevance
" According to our results, buflomedil is more effective and safe than naftidrofuryl in the treatment of patients with intermittent claudication."( Comparison of safety and efficacy of buflomedil and naftidrofuryl in the treatment of intermittent claudication.
Cerdeyra, C; Lucas, MA; Parano, JR; Rosas, G; Villa, JJ, 1981
)
0.83
" The retrospective case of buflomedil illustrates how these methods may be valuable in postmarketing safety evaluation of potentially toxic drugs."( The value of population pharmacokinetics and simulation for postmarketing safety evaluation of dosing guidelines for drugs with a narrow therapeutic index: buflomedil as a case study.
Bleyzac, N; Bourguignon, L; Ducher, M; Goutelle, S; Maire, P; Matanza, D; Odouard, E; Uhart, M, 2012
)
0.87
"Review all the individualized cases of adverse drug reaction (ADR) potentially related to buflomedil, a vasodilator with the indication for peripheral arterial disease (PAD), marketed in Europe since the 1970s but recently suspended by the European Medicines Agency."( Safety profile assessment of buflomedil: an overview of adverse reactions between 1975 and 2011.
Bucolo, C; Camillieri, G; Drago, F; Longo, L; Salomone, S, 2012
)
0.89
" From toxicity and biodegradability study it was proved that the microspheres were safe for internal use and complied with bio-safety criterion."( Comparative bio-safety and in vivo evaluation of native or modified locust bean gum-PVA IPN microspheres.
Ghosh, A; Kaity, S, 2015
)
0.42

Pharmacokinetics

Buflomedil hydrochloride is a vasoactive drug with a variety of pharmacodynamic properties. A dose-ranging pharmacokinetic study was carried out in eight subjects. The mean buflomedill half-life was 5.

ExcerptReferenceRelevance
"The pharmacokinetic disposition of buflomedil was compared in humans after oral administration of solution, tablets and film tablets."( Pharmacokinetics of buflomedil after various dosage forms.
Ferrario, P; Fraschini, F; Lepore, AM; Pirola, R; Reina, L; Scaglione, F; Zambotti, F; Zecca, L; Zonta, N, 1989
)
0.88
"Buflomedil hydrochloride is a vasoactive drug with a variety of pharmacodynamic properties."( Buflomedil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in peripheral and cerebral vascular diseases.
Clissold, SP; Lynch, S; Sorkin, EM, 1987
)
3.16
"A dose-ranging pharmacokinetic study of buflomedil was carried out in eight subjects to determine the pharmacokinetic parameters of the drug after oral and intravenous administration."( The clinical pharmacokinetics of buflomedil in normal subjects after intravenous and oral administration.
Aynilian, GH; Chiou, WL; Gundert-Remy, U; Lam, G; Mann, W; Weber, E, 1981
)
0.81
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" Then, the pharmacokinetic model was used to perform a 1000-patient Monte Carlo simulation for the two recommended buflomedil dosage regimens."( The value of population pharmacokinetics and simulation for postmarketing safety evaluation of dosing guidelines for drugs with a narrow therapeutic index: buflomedil as a case study.
Bleyzac, N; Bourguignon, L; Ducher, M; Goutelle, S; Maire, P; Matanza, D; Odouard, E; Uhart, M, 2012
)
0.79

Bioavailability

ExcerptReferenceRelevance
" This level of bioavailability was attributed to the hepatic first-pass effect."( The clinical pharmacokinetics of buflomedil in normal subjects after intravenous and oral administration.
Aynilian, GH; Chiou, WL; Gundert-Remy, U; Lam, G; Mann, W; Weber, E, 1981
)
0.54
" Results showed an overall significant mean difference in absorption rate between the two formulations."( Evaluation of two buflomedil tablet formulations in patients with atherosclerotic disease.
Buggia, I; Graziani, P; Iacona, I; Melzi D'eril, G; Molinaro, M; Raffaghello, S; Regazzi, MB; Specchia, G, 1994
)
0.62
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Buflomedil at a dosage of 50mg/kg weight produces seizures. Risk of overdosing associated with latest dosing recommendations of the French Drug Agency.

ExcerptRelevanceReference
"The pharmacokinetics of a sustained release (SR) formulation of pyridoxal phosphate of buflomedil (Pirxane retard) has been studied after oral administration to healthy volunteers using among else a gaschromatographic dosage method."( Pharmacokinetics of a sustained release formulation of pyridoxal phosphate of buflomedil after single or repeated oral doses in healthy volunteers.
Borgonovo, E; Covini, D; de Bernardi di Valserra, M; Feletti, F; Germogli, R, 1992
)
0.73
" Buflomedil at a dosage of 50 mg/kg weight produces seizures."( Buflomedil intoxication: the little-known risk.
Lara, B; Martínez-Sierra, R; Torres, A, 1992
)
2.64
" Six healthy male volunteers received a single oral dose of the three different dosage formulations."( Pharmacokinetics of buflomedil after various dosage forms.
Ferrario, P; Fraschini, F; Lepore, AM; Pirola, R; Reina, L; Scaglione, F; Zambotti, F; Zecca, L; Zonta, N, 1989
)
0.6
" and then orally, at a dosage of 600 mg/day."( Effects of buflomedil hydrochloride in occlusive arterial disease of the lower limbs stage IV.
Briguglio, E; Briguglio, F; Di Marco, V; Intilisano, A; Materia, G; Swat, M, 1986
)
0.66
" This study suggests to reduce the usual dosage to half its value in the renal disease."( Pharmacokinetics of buflomedil after intravenous administration in patients with chronic renal failure.
d'Athis, P; Fillastre, JP; Olive, G; Rey, E; Richard, MO, 1984
)
0.59
" The no-adverse-effect dosage was considered to be 12 mg/kg/day."( Buflomedil: three month intravenous safety evaluation in rats.
Cusick, PK; Fort, FL; Heyman, IA; Kesterson, JW; Lewkowski, JP; Tekeli, S, 1982
)
1.71
" Therefore, the no-toxic-effect dosage was 400 mg/kg/day which is 40 times the maximum clinical dosage."( Buflomedil: one-year oral safety evaluation in rats.
Fort, FL; Gregson, RL; Patterson, DR; Ruckman, SA, 1993
)
1.73
" The dosage of dioxin was 32 microg/ml of blood and 32 ng/ml of blood."( Rheological and biochemical examination of red blood cells after treatment with different pharmacological and toxic substances.
Dabrowski, Z; Nowak, E; Smolenski, O; Spodaryk, K; Wyrwicz, G, 2002
)
0.31
" We retrospectively assessed the risk of buflomedil overdosing associated with the latest dosing recommendations of the French Drug Agency (AFSSAPS)."( The value of population pharmacokinetics and simulation for postmarketing safety evaluation of dosing guidelines for drugs with a narrow therapeutic index: buflomedil as a case study.
Bleyzac, N; Bourguignon, L; Ducher, M; Goutelle, S; Maire, P; Matanza, D; Odouard, E; Uhart, M, 2012
)
0.84
" From an initial cumulative number of 1054 case reports, there were 401 cases of intentional overdose (IOD) of which 63 were fatal, and 137 cases of accidental overdose, with two fatalities, and 516 case reports of ADRs under normal conditions of use of the product at normal therapeutic dosage with 11 fatalities."( Safety profile assessment of buflomedil: an overview of adverse reactions between 1975 and 2011.
Bucolo, C; Camillieri, G; Drago, F; Longo, L; Salomone, S, 2012
)
0.67
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
[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 (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency4.94870.035520.977089.1251AID504332; AID588344
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency7.94330.00207.533739.8107AID891
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency3.16230.010039.53711,122.0200AID588547
lamin isoform A-delta10Homo sapiens (human)Potency0.31620.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
C-8 sterol isomeraseSaccharomyces cerevisiae S288CKi7.15000.00000.90487.1500AID239296
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)Ki0.06000.00040.54906.7000AID239597
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)2.17050.00030.70285.3660AID625223
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki1.10110.00000.490110.0000AID239347; AID625223
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (11)

Processvia Protein(s)Taxonomy
cholesterol biosynthetic process3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cholesterol metabolic process3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
hemopoiesis3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cholesterol biosynthetic process via desmosterol3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cholesterol biosynthetic process via lathosterol3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
ossification involved in bone maturation3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
C-8 sterol isomerase activity3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
steroid delta-isomerase activity3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
protein binding3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
identical protein binding3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cholestenol delta-isomerase activity3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
nuclear envelope3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
endoplasmic reticulum3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
endoplasmic reticulum membrane3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
cytoplasmic vesicle3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
nuclear membrane3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
endoplasmic reticulum3-beta-hydroxysteroid-Delta(8),Delta(7)-isomeraseHomo sapiens (human)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (55)

Assay IDTitleYearJournalArticle
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
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.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1774075Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli assessed as ANS saturation ratio at 400 uM incubated for 1 hr in presence of 7.5 uM ANS by fluorescence method (Rvb = 56 +/- 2.3%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID239597Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
AID1774076Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli at 400 uM incubated for 1 hr in presence of 75 uM ANS by fluorescence method (Rvb = 91 +/- 0.92%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1774078Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 4 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID239347Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1774079Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 10 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID239296Affinity for ERG2 of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine radioligand2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (274)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990122 (44.53)18.7374
1990's80 (29.20)18.2507
2000's42 (15.33)29.6817
2010's22 (8.03)24.3611
2020's8 (2.92)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 41.24

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index41.24 (24.57)
Research Supply Index5.90 (2.92)
Research Growth Index4.26 (4.65)
Search Engine Demand Index65.76 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (41.24)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials65 (21.67%)5.53%
Reviews22 (7.33%)6.00%
Case Studies32 (10.67%)4.05%
Observational0 (0.00%)0.25%
Other181 (60.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]