Page last updated: 2024-12-05

bretylium tosylate

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

Description

Bretylium Tosylate: An agent that blocks the release of adrenergic transmitters and may have other actions. It was formerly used as an antihypertensive agent, but is now proposed as an anti-arrhythmic. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

bretylium tosylate : The tosylate salt of bretylium. It blocks noradrenaline release from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation. [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]

Cross-References

ID SourceID
PubMed CID6100
CHEMBL ID1095292
CHEBI ID3173
SCHEMBL ID40898
MeSH IDM0002920

Synonyms (103)

Synonym
benzenemethanaminium,n-dimethyl-, salt with 4-methylbenzenesulfonic acid (1:1)
wln: er b1k2&1&1 &oswr d1
nsc-62164
bretylii tosilas
chebi:3173 ,
(2-bromobenzyl)ethyldimethylammonium tosylate
tosilato de bretilio
tosilate de bretylium
(2-bromobenzyl)ethyldimethylammonium toluene-4-sulfonate
benzenemethanaminium, 2-bromo-n-ethyl-n,n-dimethyl-, salt with 4-methylbenzenesulfonic acid
dimethylethyl-o-bromobenzylammonium-p-toluenesulphonate
einecs 200-516-8
bretylii tosilas [inn-latin]
bretylium tosilate
2-bromo-n-ethyl-n,n-dimethylbenzenemethanaminium 4-methylbenzenesulfonate
ammonium, (o-bromobenzyl)ethyldimethyl-, p-toluenesulfonate
bretylium tosylate in plastic container
bretilio tosilato [dcit]
bretylium tosylate in dextrose 5% in plastic container
n-ethyl-n-o-bromobenzyl-n,n-dimethylammonium tosylate
tosilate de bretylium [inn-french]
nsc 62164
tosilato de bretilio [inn-spanish]
bretylium tosylate in dextrose 5%
c18h24brno3s
AKOS015842525
MLS000028635 ,
smr000058647
n-[(2-bromophenyl)methyl]-n,n-dimethylethanaminium 4-methylbenzenesulfonate
EU-0100224
cas-61-75-6
NCGC00016119-01
NCGC00016119-02
lopac-b-8406
bretylium tosylate
darentin
bretylol
nsc62164
darenthin
benzenemethanaminium, 2-bromo-n-ethyl-n,n-dimethyl-, salt with 4-methylbenzenesulfonic acid (1:1)
(o-bromobenzyl)ethyldimethylammonium p-toluenesulfonate
61-75-6
asl-603
ornid
bretylium p-toluenesulfonate
bretylate
D00645
bretylol (tn)
bretylium tosilate (inn)
bretylium tosylate (usp)
NCGC00024457-02
NCGC00016119-04
2-bromo-n-ethyl-n,n-dimethylbenzenemethanaminium 4-methyl-benzenesulfontate
B 8406
n-(2-bromobenzyl)-n,n-dimethylethanaminium 4-methylbenzenesulfonate
HMS1570N06
CHEMBL1095292
HMS2097N06
dtxsid1022685 ,
tox21_110308
dtxcid802685
CCG-204319
HMS2235I21
NCGC00016119-03
unii-78zp3yr353
bretilio tosilato
bretylium tosilate [inn]
bretylium tosylate [usan:usp]
78zp3yr353 ,
FT-0603258
(o-bromobenzyl)ethyldimethylammonium p-toluenesulphonate
bretylium tosylate [usp monograph]
bretylium tosylate [orange book]
bretylium tosylate [usan]
bretylium tosylate [usp-rs]
bretylium tosilate [mart.]
bretylium tosilate [who-dd]
bretylium tosylate [mi]
bretylium tosylate [vandf]
SCHEMBL40898
bretyliume tosylate
OPERA_ID_1513
bretylium tosylate, >99% (tlc), powder
mfcd00038731
CS-5728
HY-12961A
bretylium (tosylate)
sr-01000000254
SR-01000000254-2
bretylium tosylate, united states pharmacopeia (usp) reference standard
SR-01000000254-5
HMS3714N06
n-(2-bromobenzyl)-n,n-dimethylethanaminium4-methylbenzenesulfonate
Q27105972
EN300-399743
(2-bromophenyl)methyl-ethyl-dimethylazanium;4-methylbenzenesulfonate
[(2-bromophenyl)methyl](ethyl)dimethylazanium 4-methylbenzene-1-sulfonate
AS-56957
bratylium (cation)
bretylium tosylate (usp monograph)
bretylium tosilate (mart.)
c01bd02
bretylium tosylate (usp-rs)

Research Excerpts

Overview

Bretylium tosylate is a quaternary amine with unique antifibrillatory properties and appears to have a significant role in the management of arrhylmias.

ExcerptReferenceRelevance
"Bretylium tosylate is a quaternary amine with unique antifibrillatory properties and appears to have a significant role in the management of these arrhylmias."( Quinidine syncope. A report of successful treatment with bretylium tosylate.
Kahn, DR; Reynolds, EW; Tullett, G; VanderArk, CR, 1976
)
1.22
"Bretylium tosylate is an antiarrhythmic agent. "( Bretylium tosylate binds preferentially to muscarinic receptors labelled with [3H]oxotremorine M (SH or 'high affinity' receptors) in rat heart and brain cortex.
Brunner, F; Christophe, J; Gillard, M; Svoboda, M; Waelbroeck, M, 1989
)
3.16

Effects

Bretylium tosylate has been shown effective in the treatment of ventricular fibrillation and in the prevention of its recurrence. It has antiarrhythmic action and also interacts with amiloride-sensitive sodium ion transport sites.

ExcerptReferenceRelevance
"Bretylium tosylate (Bretylol) has recently been approved for parenteral use against resistant ventricular arrhythmias. "( Bretylium tosylate: a newly available antiarrhythmic drug for ventricular arrhythmias.
Bigger, JT; Heissenbuttel, RH, 1979
)
3.15
"Bretylium tosylate has been shown effective in the treatment of ventricular fibrillation and in the prevention of its recurrence. "( Bretylium tosylate versus lidocaine in experimental cardiac arrest.
Blecic, S; Contempré, B; Reuse, C; Vachiery, JL; Vincent, JL, 1990
)
3.16
"Bretylium tosylate has antiarrhythmic action and also interacts with amiloride-sensitive sodium ion transport sites."( Inactivation of acetylcholinesterase with a bretylium tosylate photoaffinity probe.
Branchini, BR; Lajiness, EJ, 1986
)
1.25

Actions

ExcerptReferenceRelevance
"Bretylium tosylate did not increase GTP hydrolysis in HL-60 membranes or with Gi/G(o) proteins."( The class III antiarrhythmic drug amiodarone directly activates pertussis toxin-sensitive G proteins.
Grünbaum, L; Hagelüken, A; Harhammer, R; Nürnberg, B; Schunack, W; Seifert, R, 1995
)
1.01

Treatment

Treatment with bretylium tosylate reduced wavelet amplitude associated with neural activity during baseline in the forearm and leg. Pretreatment completely abolished the depressor response without affecting the baseline level of arterial pressure.

ExcerptReferenceRelevance
"Treatment with bretylium tosylate reduced wavelet amplitude associated with neural activity during baseline in the forearm (d=1.6, P<.05) and leg (d=0.9, P<.05)."( Effect of sympathetic nerve blockade on low-frequency oscillations of forearm and leg skin blood flow in healthy humans.
Del Pozzi, AT; Hodges, GJ; Mallette, MM; Martin, ZT, 2017
)
0.79
"Pretreatment with bretylium tosylate completely abolished the depressor response without affecting the baseline level of arterial pressure."( Neural reflex hypotension induced by very small dose of hypertonic NaCl solution in rats.
Dai, S; Fu, L; Gong, D; Peng, Y; Sato, T; Sun, Y; Wang, D; Wu, Q; Xu, H; Zhang, D, 2009
)
0.68

Toxicity

ExcerptReferenceRelevance
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32

Pharmacokinetics

ExcerptReferenceRelevance
"0515 hr-1 and a corresponding elimination half-life of tiv1/2 = 13."( Clinical pharmacokinetics of intravenous and oral bretylium tosylate in survivors of ventricular tachycardia or fibrillation: clinical application of a new assay for bretylium.
Anderson, JL; Johnson, TA; Lucchesi, BR; Patterson, E; Pitt, B; Wagner, JG,
)
0.38
" Intravenous studies showed a sum of 3 exponentials to characterize plasma level-time studies with a terminal half-life of 535 +/- 32 (S."( Bretylium pharmacokinetics and bioavailabilities in man with various doses and modes of administration.
Bialer, M; Garrett, ER; Green, JR,
)
0.13
" Pharmacokinetics of bretylium in dogs could be characterized by a two-compartment open model with a distribution half-life of 7 min and biological half-life of 15."( Pharmacokinetics of bretylium in dogs and the effect of hemoperfusion on elimination.
Comrie, EB; Gibson, TP; Kamath, BL; Look, ZM; McEntegart, CM; Yacobi, A, 1982
)
0.26
"The pharmacokinetic profile of bretylium was studied in four normal male volunteers using a new sensitive EC-GC procedure for its quantitative in biological fluids."( Pharmacokinetics of bretylium in man after intravenous administration.
Adir, J; Josselson, J; Narang, PK; Sadler, J; Yacobi, A, 1980
)
0.26

Bioavailability

ExcerptReferenceRelevance
" Irradiation apparently does not affect the absorption of drugs that are normally well absorbed or poorly absorbed due to slow transport across the GI mucosa."( GI drug absorption in rats exposed to cobalt-60 gamma-radiation I: Extent of absorption.
Brady, ME; Hayton, WL, 1977
)
0.26
"The rate of absorption of sulfanilamide, bretylium tosylate, sulfisoxazole acetyl, and riboflavin was studied in rats exposed to 850 rad of cobalt-60 gamma-radiation either 1 or 5 days before oral drug administration."( GI drug absorption in rats exposed to cobalt-60 gamma-radiation II: in vivo rate of absorption.
Brady, ME; Hayton, WL, 1977
)
0.52
"" Unlike bretylium, which is poorly absorbed from the gut and limited to parenteral use, oral bethanidine is absorbed rapidly."( Antiarrhythmic, antifibrillatory, and hemodynamic actions of bethanidine sulfate: an orally effective analog of bretylium for suppression of ventricular tachyarrhythmias.
Bacaner, MB; Benditt, DG, 1982
)
0.26
" Unlike bretylium, which is very poorly absorbed from the gut, bethanidine is rapidly and effectively absorbed after oral administration."( Suppression of ventricular fibrillation and positive inotropic action of bethanidine sulfate, a chemical analog of bretylium tosylate that is well absorbed orally.
Bacaner, MB; Hoey, MF; Macres, MG, 1982
)
0.47
"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

The chemistry, pharmacology, pharmacokinetics, clinical uses, adverse effects, drug interactions and dosage of bretylium tosylate, a recently approved antiarrhythmic agent, are reviewed.

ExcerptRelevanceReference
"The chemistry, pharmacology, pharmacokinetics, clinical uses, adverse effects, drug interactions and dosage of bretylium tosylate, a recently approved antiarrhythmic agent, are reviewed."( Bretylium tosylate: a review.
Bryan, CK; Darby, MH, 1979
)
1.91
" 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
" Pharmacokinetic data for drugs administered endotracheally are lacking; therefore, dosage recommendations are empirical."( Endotracheal drug therapy in cardiopulmonary resuscitation.
Raehl, CL, 1986
)
0.27
" In order to minimize the risk of potential toxicity following multiple dosing in such patients, dosage adjustments are necessary."( Nomogram for bretylium dosing in renal impairment.
Adir, J; Josselson, J; Narang, PK, 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
" The strong linear relationships between renal and total clearance, beta, and the creatinine clearance, may be helpful in adjusting dosage regimens for bretylium in patients with renal dysfunction."( Bretylium kinetics in renal insufficiency.
Adir, J; Josselson, J; Narang, PK; Sadler, JH; Yacobi, A, 1983
)
0.27
" These unique effects of bretylium on conduction and excitability in the normal, in the center, and across the border of ischemic myocardium, when a therapeutic dosage of the drug is used, further validate its antiarrhythmic potential and offer an insight into its mechanism of action in the setting of acute myocardial ischemia."( Electrophysiologic effects of bretylium on canine ventricular muscle during acute ischemia and reperfusion.
Fujimoto, T; Hamamoto, H; Mandel, WJ; McCullen, A; Melvin, N; Peter, T, 1983
)
0.27
" In one group (n = 7), a bolus dosage of bretylium tosylate (BT), 6 mg/kg body wt, was administered at 25 degrees C before rewarming."( Effect of bretylium tosylate on ventricular fibrillation threshold during hypothermia in dogs.
Bjørnstad, H; Mortensen, E; Refsum, H; Sager, G, 1994
)
0.96
"To test the hypothesis that cutaneous vasoconstrictor responsiveness to exogenous norepinephrine is reduced in older compared with young subjects, dose-response relations between norepinephrine and skin blood flow were established."( Effect of age on cutaneous vasoconstrictor responses to norepinephrine in humans.
Monahan, KD; Ray, CA; Short, DS; Wilson, TE, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
adrenergic antagonistAn agent that binds to but does not activate adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists.
anti-arrhythmia drugA drug used for the treatment or prevention of cardiac arrhythmias. Anti-arrhythmia drugs may affect the polarisation-repolarisation phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibres.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
[role 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]

Drug Classes (2)

ClassDescription
quaternary ammonium saltDerivatives of ammonium compounds, (NH4(+))Y(-), in which all four of the hydrogens bonded to nitrogen have been replaced with univalent (usually organyl) groups.
organosulfonate saltAny organic salt prepared using an organosulfonic acid as the acid component.
[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 (25)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ThrombopoietinHomo sapiens (human)Potency12.58930.02517.304831.6228AID917; AID918
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.50120.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency31.62280.00207.533739.8107AID891
mitogen-activated protein kinase 1Homo sapiens (human)Potency10.00000.039816.784239.8107AID995
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency1.58490.031610.279239.8107AID884; AID885
M-phase phosphoprotein 8Homo sapiens (human)Potency0.79430.177824.735279.4328AID488949
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency11.22020.251215.843239.8107AID504327
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency11.29470.00106.000935.4813AID943; AID944
lamin isoform A-delta10Homo sapiens (human)Potency0.07080.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency1.58491.000012.224831.6228AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (50)

Assay IDTitleYearJournalArticle
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1124028Inhibition of [3H]dopamine reuptake at DAT in Sprague-Dawley rat brain striatal synaptosomes incubated for 5 mins prior to [3H]dopamine addition measured after 3 mins by scintillation counting analysis1979Journal of medicinal chemistry, Apr, Volume: 22, Issue:4
Inhibition of uptake of catecholamines by benzylamine derivatives.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1124027Inhibition of [3H]norepinephrine reuptake at NET in Sprague-Dawley rat brain cortical synaptosomes incubated for 5 mins prior to [3H]norepinephrine addition measured after 3 mins by scintillation counting analysis1979Journal of medicinal chemistry, Apr, Volume: 22, Issue:4
Inhibition of uptake of catecholamines by benzylamine derivatives.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1124029Selectivity ratio of I50 for [3H]dopamine reuptake at DAT in Sprague-Dawley rat brain striatal synaptosomes to I50 for [3H]norepinephrine reuptake at NET in Sprague-Dawley rat brain cortical synaptosomes1979Journal of medicinal chemistry, Apr, Volume: 22, Issue:4
Inhibition of uptake of catecholamines by benzylamine derivatives.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
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.
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.
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.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
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.
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.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (288)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990210 (72.92)18.7374
1990's40 (13.89)18.2507
2000's20 (6.94)29.6817
2010's15 (5.21)24.3611
2020's3 (1.04)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.32

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 Index29.32 (24.57)
Research Supply Index5.83 (2.92)
Research Growth Index4.10 (4.65)
Search Engine Demand Index42.09 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials20 (6.27%)5.53%
Reviews28 (8.78%)6.00%
Case Studies21 (6.58%)4.05%
Observational0 (0.00%)0.25%
Other250 (78.37%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]