Page last updated: 2024-12-06

bambuterol

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

Description

Bambuterol is a bronchodilator that acts as a beta2-adrenergic receptor agonist. It is used to treat asthma and chronic obstructive pulmonary disease (COPD). Bambuterol is a racemic mixture of two enantiomers, the R-enantiomer being the more potent. Bambuterol is thought to work by relaxing the muscles in the airways of the lungs, making it easier to breathe. It is available in both oral and inhalable forms. Bambuterol is typically well-tolerated, but side effects can include headache, tremor, and insomnia. Bambuterol has been studied for its potential use in the treatment of other conditions, such as premature ejaculation and urinary incontinence, but these studies are ongoing. Bambuterol is a relatively old drug and is not as commonly used as some newer bronchodilators, but it is still an effective treatment option for patients with asthma or COPD.'

bambuterol: selective inhibitor of butyrylcholinesterase & acetylcholinesterase [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

bambuterol : A carbamate ester that is terbutaline in which both of the phenolic hydroxy groups have been protected as the corresponding N,N-dimethylcarbamates. A long acting beta-adrenoceptor agonist used in the treatment of asthma, it is a prodrug for terbutaline. [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 CID54766
CHEMBL ID521589
CHEBI ID553827
SCHEMBL ID4431
MeSH IDM0137788

Synonyms (64)

Synonym
MLS002153785
smr001233168
AKOS005574764
BRD-A17462676-003-03-3
bambec
bambuterolum [latin]
(+-)-5-(2-(tert-butylamino)-1-hydroxyethyl)-m-phenylene bis(dimethylcarbamate)
BSPBIO_000481
PRESTWICK3_000361
NCGC00179546-01
D07377
81732-65-2
bambuterol (inn)
PRESTWICK2_000361
BPBIO1_000531
bambuterol
DB01408
(+/-)-5-(2-(tert-butylamino)-1-hydroxyethyl)-m-phenylene bis(dimethylcarbamate)
PRESTWICK0_000361
PRESTWICK1_000361
SPBIO_002402
HMS2089J18
L004435
CHEMBL521589
terbutaline bisdimethylcarbamate
5-[2-(tert-butylamino)-1-hydroxyethyl]benzene-1,3-diyl bis(dimethylcarbamate)
terbutaline bis(dimethylcarbamate)
CHEBI:553827 ,
bambuterolum
[3-[2-(tert-butylamino)-1-hydroxyethyl]-5-(dimethylcarbamoyloxy)phenyl] n,n-dimethylcarbamate
STK643808
[3-[2-(tert-butylamino)-1-oxidanyl-ethyl]-5-(dimethylcarbamoyloxy)phenyl] n,n-dimethylcarbamate
A840189
n,n-dimethylcarbamic acid [3-[2-(tert-butylamino)-1-hydroxyethyl]-5-[dimethylamino(oxo)methoxy]phenyl] ester
NCGC00179546-02
y1850g1ovc ,
unii-y1850g1ovc
bambuterol [inn:ban]
HMS2230O15
oxeol
FT-0602901
gtpl6601
HMS3373N13
bambuterol [mi]
bambuterol [inn]
bambuterol [who-dd]
CS-3157
HY-17501
SCHEMBL4431
DTXSID5048550
AC-35438
(rs)-5-[2-(tert-butylamino)-1-hydroxyethyl]benzene-1,3-diyl bis(dimethylcarbamate)
ANZXOIAKUNOVQU-UHFFFAOYSA-N
SR-05000001470-1
SBI-0207028.P001
5-(2-(tert-butylamino)-1-hydroxyethyl)-1,3-phenylene bis(dimethylcarbamate)
( inverted exclamation marka)-bambutero
BCP21793
Q3633651
bdbm50235800
(+/-)-bambuterol;kwd-2183
BRD-A17462676-003-06-6
()-bambuterol;kwd-2183
GLXC-25236

Research Excerpts

Overview

Bambuterol is a prodrug of β2-agonist commonly used for the treatment of asthma and chronic obstructive pulmonary disease (COPD) It has undesired cardiac effects and less lipophilicity.

ExcerptReferenceRelevance
"Bambuterol is a known potent inhibitor of butyrylcholinesterase, but it has undesired cardiac effects and less lipophilicity."( Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
Jin, Y; Pistolozzi, M; Roy, G; Tan, W; Tian, Y; Wang, S; Wu, J; Xu, L; Zhou, T, 2017
)
1.43
"Bambuterol is a prodrug of β2-agonist commonly used for the treatment of asthma and chronic obstructive pulmonary disease (COPD) with the advantage of once daily dosing and favorable side effect profile."( The Lipid-lowering Effects of R-bambuterol in Healthy Chinese Volunteers: A Randomized Phase I Clinical Study.
Bu, S; Cheng, Q; Quan, L; Tan, W; Xu, H; Ye, Y; Zeng, J; Zhou, T; Zhu, L; Zou, C, 2015
)
1.42
"Bambuterol is a chiral carbamate and a selective inhibitor of butyrylcholinesterase (BChE, EC 3.1.1.8). "( Stereoselective inhibition of human, mouse, and horse cholinesterases by bambuterol enantiomers.
Bosak, A; Gazić, I; Kovarik, Z; Vinković, V, 2008
)
2.02
"Bambuterol is a chiral carbamate known as selective inhibitor of butyrylcholinesterase (BChE). "( Amino acid residues involved in stereoselective inhibition of cholinesterases with bambuterol.
Bosak, A; Gazić, I; Kovarik, Z; Vinković, V, 2008
)
2.01
"Bambuterol is a new long-acting oral bronchodilator for once daily use in patients with asthma. "( One month treatment with the once daily oral beta 2-agonist bambuterol in asthmatic patients.
Baas, A; Knight, A; Larsen, B; Olsson, H; Persson, G, 1995
)
1.98
"Bambuterol is an inactive prodrug which is enzymatically cleaved by plasma cholinesterase to yield the active compound, terbutaline. "( The influence of 10 mg and 20 mg of bambuterol on the duration of succinylcholine-induced neuromuscular blockade.
Eriksson, LI; Lennmarken, C; Staun, P; Wirén, JE, 1990
)
2
"Bambuterol is a new bronchodilator which is also a reversible inhibitor of plasma cholinesterase. "( The effect of bambuterol on plasma cholinesterase activity and suxamethonium-induced neuromuscular blockade in subjects heterozygous for abnormal plasma cholinesterase.
Bang, U; Viby-Mogensen, J; Wirén, JE, 1990
)
2.08
"Bambuterol is a prodrug, from which terbutaline is slowly generated. "( Comparison between a new once-daily, bronchodilating drug, bambuterol, and terbutaline sustained-release, twice daily.
Anehus, S; Gnosspelius, Y; Persson, G, 1988
)
1.96

Effects

ExcerptReferenceRelevance
"Bambuterol (BMB) has been used clinically to treat asthma due to its bronchodilation activity. "( (RS)-bambuterol and its enantiomers: Potential improvement of (R)-bambuterol in mice with colitis.
Deng, L; Guo, H; Lin, Y; Liu, X; Tan, W; Wang, S; Zhang, R; Zou, X, 2022
)
2.68

Actions

ExcerptReferenceRelevance
"R-bambuterol can lower the plasma levels of LDL-C, and marginally raise the ratio of ApoA1/ApoB (indicator of HDL-C/LDL-C) with both a single dose and multiple doses. "( The Lipid-lowering Effects of R-bambuterol in Healthy Chinese Volunteers: A Randomized Phase I Clinical Study.
Bu, S; Cheng, Q; Quan, L; Tan, W; Xu, H; Ye, Y; Zeng, J; Zhou, T; Zhu, L; Zou, C, 2015
)
1.42

Toxicity

ExcerptReferenceRelevance
" The primary objective was to evaluate safety (pulse rate, blood pressure, adverse events, hematology, and clinical chemistry)."( One-year safety study with bambuterol once daily and terbutaline three times daily in 2-12-year-old children with asthma. The Bambuterol Multicentre Study Group.
Kuusela, AL; Marenk, M; Olsson, H; Persson, B; Sandahl, G; Valovirta, E; Zarkovic, JP, 2000
)
0.6
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36

Pharmacokinetics

The pharmacokinetic properties of bambuterol make it suitable for oral once-daily dosage. The method is shown to be accurate, robust and convenient.

ExcerptReferenceRelevance
" Thus, the pharmacokinetic properties of bambuterol make it suitable for oral once-daily dosage."( Pharmacokinetics of bambuterol in healthy subjects.
Jönsson, S; Kennedy, BM; Nilsson, M; Nyberg, L; Rosenborg, J; Weibull, E, 1998
)
0.89
"The pharmacokinetic parameters in the present study were grossly similar to those found in a study of bambuterol in subjects with normal plasma cholinesterase activity (N)."( Pharmacokinetics of bambuterol in subjects homozygous for the atypical gene for plasma cholinesterase.
Bang, U; Nyberg, L; Rosenborg, J; Viby-Mogensen, J, 1998
)
0.84
"The pharmacokinetics of orally administered bambuterol were investigated in healthy adult subjects, with particular regard to time to steady state, pharmacokinetic linearity, intraindividual variability for the parent drug and its active beta2-adrenergic metabolite terbutaline and bioequivalence between tablet and solution."( Pharmacokinetics of bambuterol during oral administration of plain tablets and solution to healthy adults.
Larsson, P; Nyberg, L; Rosenborg, J, 2000
)
0.89
" Mean terminal half-life of terbutaline was 22 h and steady-state was reached within one week of bambuterol treatment."( Pharmacokinetics of bambuterol during oral administration of plain tablets and solution to healthy adults.
Larsson, P; Nyberg, L; Rosenborg, J, 2000
)
0.85
" Pharmacokinetic analysis indicated that absorption of bambuterol was slow and multi-phasic and that slow biotransformation to terbutaline occurred both presystemically and systemically."( Clinical-pharmacokinetic aspects of prolonged effect duration as illustrated by beta2-agonists.
Rosenburg, J, 2002
)
0.56
" After an oral administration of 10 mg bambuterol hydrochloride to 18 healthy Chinese volunteers the main pharmacokinetic parameters of bambuterol were as follows: Tmax was (2."( [Determination of bambuterol in human plasma by liquid chromatography-electrospray tandem mass spectrometry: application to pharmacokinetic study].
Chen, XY; Xu, HY; Yang, HY; Zhang, YF; Zhong, DF, 2001
)
0.91
"The method is shown to be accurate, robust and convenient, and suitable for pharmacokinetic studies of bambuterol."( [Determination of bambuterol in human plasma by liquid chromatography-electrospray tandem mass spectrometry: application to pharmacokinetic study].
Chen, XY; Xu, HY; Yang, HY; Zhang, YF; Zhong, DF, 2001
)
0.86
" 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
" The validated method has been successfully applied to the human pharmacokinetic study of R-bambuterol involving 10 healthy volunteers."( A sensitive LC-MS/MS method for simultaneous determination of R-bambuterol and its active metabolite R-terbutaline in human plasma and urine with application to a clinical pharmacokinetic study.
Cheng, Q; Liu, S; Tan, W; Xu, L; Zhao, T; Zhou, T, 2014
)
0.86
" After single intravenous administration, no significant differences were observed between the two drugs in pharmacokinetic data."( Comparative pharmacokinetics and bile transformation of R-enantiomer and racemic bambuterol after single-dose intravenous, oral administration in rats and beagle dogs.
Chen, JD; Guan, S; He, MY; Hu, CY; Huang, LJ; Tan, W; Tang, YX; Yang, YY, 2015
)
0.64
" For the first time, the validated method was successfully applied to an enantioselective pharmacokinetic study of rac-bambuterol in 8 healthy volunteers."( Chiral analysis of bambuterol, its intermediate and active drug in human plasma by liquid chromatography-tandem mass spectrometry: Application to a pharmacokinetic study.
He, M; Liu, S; Qu, S; Tan, W; Xu, B; Xu, L; Zeng, J; Zhao, T; Zhou, T, 2015
)
0.95

Bioavailability

ExcerptReferenceRelevance
"To study the pharmacokinetics and bioavailability of the prodrug bambuterol and its bronchodilator moiety terbutaline in healthy subjects."( Pharmacokinetics of bambuterol in healthy subjects.
Jönsson, S; Kennedy, BM; Nilsson, M; Nyberg, L; Rosenborg, J; Weibull, E, 1998
)
0.86
" Generated terbutaline had a bioavailability of 36% (28-46) after intravenous and 10."( Pharmacokinetics of bambuterol in healthy subjects.
Jönsson, S; Kennedy, BM; Nilsson, M; Nyberg, L; Rosenborg, J; Weibull, E, 1998
)
0.62
" The bioavailability of R-enantiomer and racemate were comparative and relatively high in beagle dogs."( Comparative pharmacokinetics and bile transformation of R-enantiomer and racemic bambuterol after single-dose intravenous, oral administration in rats and beagle dogs.
Chen, JD; Guan, S; He, MY; Hu, CY; Huang, LJ; Tan, W; Tang, YX; Yang, YY, 2015
)
0.64

Dosage Studied

Bambuterol is a prodrug of β2-agonist commonly used for the treatment of asthma and chronic obstructive pulmonary disease. Dose proportionality for terbutaline makes dosing with bambuterl predictable.

ExcerptRelevanceReference
" The Cmax for evening vs morning dosing was 17."( Bambuterol in the treatment of asthma. A placebo-controlled comparison of once-daily morning vs evening administration.
D'Alonzo, GE; Feldman, S; Gnosspelius, Y; Karlsson, K; Smolensky, MH, 1995
)
1.73
"To investigate dose proportionality, dosing frequency, and ethnic aspects of the pharmacokinetics of bambuterol in asthmatic children, and to discuss the relationship with previous observations in adults."( Pharmacokinetics of bambuterol during oral administration to asthmatic children.
Ahlström, H; Alvero, J; Alvero, R; Espos, R; Fajutrao, L; Herrera, J; Kjellman, B; Kubista, J; Laxmyr, L; Leviste, C; Meyer, P; Nyberg, L; Oldaeus, G; Olsson, H; Rosenborg, J; Siricururat, A; Vichyanond, P; Weibull, E; Wettrell, G; Wong, E, 1999
)
0.84
" Peak plasma concentrations and dosing interval area under curve (AUC) of bambuterol and the active metabolite terbutaline were assessed at steady state."( Pharmacokinetics of bambuterol during oral administration to asthmatic children.
Ahlström, H; Alvero, J; Alvero, R; Espos, R; Fajutrao, L; Herrera, J; Kjellman, B; Kubista, J; Laxmyr, L; Leviste, C; Meyer, P; Nyberg, L; Oldaeus, G; Olsson, H; Rosenborg, J; Siricururat, A; Vichyanond, P; Weibull, E; Wettrell, G; Wong, E, 1999
)
0.86
" Twice-daily dosing (2 x AUC(0,12 h)) could not be shown to differ from once-daily dosing (AUC(0,24 h)) in the preschool Caucasians."( Pharmacokinetics of bambuterol during oral administration to asthmatic children.
Ahlström, H; Alvero, J; Alvero, R; Espos, R; Fajutrao, L; Herrera, J; Kjellman, B; Kubista, J; Laxmyr, L; Leviste, C; Meyer, P; Nyberg, L; Oldaeus, G; Olsson, H; Rosenborg, J; Siricururat, A; Vichyanond, P; Weibull, E; Wettrell, G; Wong, E, 1999
)
0.63
" Dose proportionality for terbutaline makes dosing with bambuterol predictable."( Clinical-pharmacokinetic aspects of prolonged effect duration as illustrated by beta2-agonists.
Rosenburg, J, 2002
)
0.56
"Two simple, rapid, accurate and precise methods have been developed for simultaneous estimation of Montelukast sodium and Bambuterol hydrochloride from tablet dosage form."( Simultaneous estimation of Montelukast sodium and Bambuterol hydrochloride in tablets by spectrophotometry.
Kothapalli, LP; Nanda, RK; Pangarkar, VB; Pawar, AA; Thomas, AB,
)
0.59
" After oral dosing of R-bambuterol, the AUCs of R-enantiomer presented linear correlation."( Comparative pharmacokinetics and bile transformation of R-enantiomer and racemic bambuterol after single-dose intravenous, oral administration in rats and beagle dogs.
Chen, JD; Guan, S; He, MY; Hu, CY; Huang, LJ; Tan, W; Tang, YX; Yang, YY, 2015
)
0.95
" The proposed method has been successfully applied to the analysis of BH in pharmaceutical dosage forms without interference from other dosage form additives and the results have been statistically compared with pharmacopeial method."( Application of a new spectrophotometric method manipulating ratio spectra for determination of bambuterol hydrochloride in the presence of its degradation product terbutaline.
Lamie, NT, 2015
)
0.64
" Bambuterol is a prodrug of β2-agonist commonly used for the treatment of asthma and chronic obstructive pulmonary disease (COPD) with the advantage of once daily dosing and favorable side effect profile."( The Lipid-lowering Effects of R-bambuterol in Healthy Chinese Volunteers: A Randomized Phase I Clinical Study.
Bu, S; Cheng, Q; Quan, L; Tan, W; Xu, H; Ye, Y; Zeng, J; Zhou, T; Zhu, L; Zou, C, 2015
)
1.61
"A novel, simple and sensitive spectrofluorimetric approach for determination of terbutaline sulphate (TER) and its prodrug bambuterol (BAM) in their pure and pharmaceutical dosage forms was developed."( Micelle-enhanced spectrofluorimetric method for the rapid determination of bronchodilator terbutaline and its prodrug bambuterol: application for content uniformity test.
Mohamed, AA; Mohamed, SK; Nour-Eldeen, DA; Omar, MA, 2022
)
1.14
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (7)

RoleDescription
beta-adrenergic agonistAn agent that selectively binds to and activates beta-adrenergic receptors.
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
bronchodilator agentAn agent that causes an increase in the expansion of a bronchus or bronchial tubes.
anti-asthmatic drugA drug used to treat asthma.
EC 3.1.1.7 (acetylcholinesterase) inhibitorAn EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of enzyme acetylcholinesterase (EC 3.1.1.7), which helps breaking down of acetylcholine into choline and acetic acid.
sympathomimetic agentA drug that mimics the effects of stimulating postganglionic adrenergic sympathetic nerves. Included in this class are drugs that directly stimulate adrenergic receptors and drugs that act indirectly by provoking the release of adrenergic transmitters.
tocolytic agentAny compound used to suppress premature labour and immature birth by suppressing uterine contractions.
[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
carbamate esterAny ester of carbamic acid or its N-substituted derivatives.
phenylethanolaminesAn ethanolamine compound having a phenyl (substituted or unsubstituted) group on the carbon bearing the hydroxy substituent.
[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 (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency5.01190.044717.8581100.0000AID485294
USP1 protein, partialHomo sapiens (human)Potency17.78280.031637.5844354.8130AID743255
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
gemininHomo sapiens (human)Potency0.88380.004611.374133.4983AID624296; AID624297
Guanine nucleotide-binding protein GHomo sapiens (human)Potency7.07951.995325.532750.1187AID624288
[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)
AcetylcholinesteraseElectrophorus electricus (electric eel)IC50 (µMol)100.00000.00000.94539.9400AID1439948
CholinesteraseHomo sapiens (human)IC50 (µMol)0.00330.00001.559910.0000AID1439952; AID1439999; AID1470913; AID1879286
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)2.00000.00002.015110.0000AID625249
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)25.00000.00000.933210.0000AID1439950; AID1439998; AID1470912; AID1879285
AcetylcholinesteraseRattus norvegicus (Norway rat)IC50 (µMol)30.00000.00020.52597.2000AID1916869
CholinesteraseEquus caballus (horse)IC50 (µMol)0.11930.00002.22149.4000AID1439951
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)IC50 (µMol)0.00300.00041.48119.8700AID1916909
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processCholinesteraseHomo sapiens (human)
learningCholinesteraseHomo sapiens (human)
negative regulation of cell population proliferationCholinesteraseHomo sapiens (human)
neuroblast differentiationCholinesteraseHomo sapiens (human)
peptide hormone processingCholinesteraseHomo sapiens (human)
response to alkaloidCholinesteraseHomo sapiens (human)
cocaine metabolic processCholinesteraseHomo sapiens (human)
negative regulation of synaptic transmissionCholinesteraseHomo sapiens (human)
response to glucocorticoidCholinesteraseHomo sapiens (human)
response to folic acidCholinesteraseHomo sapiens (human)
choline metabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic processCholinesteraseHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (25)

Processvia Protein(s)Taxonomy
amyloid-beta bindingCholinesteraseHomo sapiens (human)
catalytic activityCholinesteraseHomo sapiens (human)
acetylcholinesterase activityCholinesteraseHomo sapiens (human)
cholinesterase activityCholinesteraseHomo sapiens (human)
protein bindingCholinesteraseHomo sapiens (human)
hydrolase activity, acting on ester bondsCholinesteraseHomo sapiens (human)
enzyme bindingCholinesteraseHomo sapiens (human)
choline bindingCholinesteraseHomo sapiens (human)
identical protein bindingCholinesteraseHomo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo sapiens (human)
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
extracellular regionCholinesteraseHomo sapiens (human)
nuclear envelope lumenCholinesteraseHomo sapiens (human)
endoplasmic reticulum lumenCholinesteraseHomo sapiens (human)
blood microparticleCholinesteraseHomo sapiens (human)
plasma membraneCholinesteraseHomo sapiens (human)
extracellular spaceCholinesteraseHomo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo sapiens (human)
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (124)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID1439959Irreversible inhibition of equine serum BuChE assessed as decarbamylation rate constant at 800 nM using S-butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 5 mins by Ellman's method2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1439950Inhibition of human erythrocytes AChE using S-acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
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.
AID1903433Increase in beta2 adrenoceptor expression in bronchus in ovalbumin-induced asthmatic mouse model at 2.6 mg/kg, po administered once daily for 7 days by Western blot analysis
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID1903425Anti-asthmatic activity against ovalbumin-induced asthmatic mouse model assessed as decrease in IL-4 level in BALF at 2.6 mg/kg, po administered once daily for 7 days by ELISA
AID1903423Anti-asthmatic activity against ovalbumin-induced asthmatic mouse model assessed as decrease in IgE level in serum at 2.6 mg/kg, po administered once daily for 7 days by ELISA
AID1439968Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 7 mins by electrocardiogram (Rvb = -25.9 +/- 22.08 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1439990Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 29 mins by electrocardiogram (Rvb = -47.2 +/- 24.77 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
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.
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.
AID1439999Inhibition of human blood BuChE using butyrylthiocholine as substrate2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439963Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 2 mins by electrocardiogram (Rvb = -16.36 +/- 11.14 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439983Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 22 mins by electrocardiogram (Rvb = -41.94 +/- 12.51 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
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]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
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.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1440000Selectivity ratio of IC50 for human blood AChE to IC50 for human blood BuChE2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439988Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 27 mins by electrocardiogram (Rvb = -44.4 +/- 23.19 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439949Inhibition of human erythrocytes AChE at 1x10'-5M using S-acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method relative to control2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1916910Selectivity index, ratio of IC50 for rat AChE to IC50 for rat BChE2022European journal of medicinal chemistry, Oct-05, Volume: 240Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.
AID1439961Selectivity ratio of decarbamylation rate constant for human plasma BuChE to decarbamylation rate constant for equine serum BuChE2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439994Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 33 mins by electrocardiogram (Rvb = -39.12 +/- 24.73 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1470914Selectivity ratio of IC50 for AChE (unknown origin) to IC50 for BuChE (unknown origin)2017European journal of medicinal chemistry, May-26, Volume: 132Recent progress in the identification of selective butyrylcholinesterase inhibitors for Alzheimer's disease.
AID1439960Irreversible inhibition of human plasma BuChE assessed as decarbamylation rate constant at 100 nM using S-butyrylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition measured after 5 mins by Ellman's method2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439972Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 11 mins by electrocardiogram (Rvb = -35.4 +/- 11.4 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439975Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 14 mins by electrocardiogram (Rvb = -38.12 +/- 19.53 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439976Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 15 mins by electrocardiogram (Rvb = -35.14 +/- 24.5 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439962Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 1 mins by electrocardiogram (Rvb = -4.04 +/- 7.52 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1439979Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 18 mins by electrocardiogram (Rvb = -37.61 +/- 15 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439984Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 23 mins by electrocardiogram (Rvb = -44.9 +/- 14.57 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
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.
AID1439982Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 21 mins by electrocardiogram (Rvb = -40.23 +/- 16.21 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439986Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 25 mins by electrocardiogram (Rvb = -43.17 +/- 15.26 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1903429Anti-asthmatic activity against ovalbumin-induced asthmatic mouse model assessed as decrease in IL-13 level in BALF at 2.6 mg/kg, po administered once daily for 7 days by ELISA
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.
AID1439991Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 30 mins by electrocardiogram (Rvb = -43.78 +/- 22.71 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1903427Anti-asthmatic activity against ovalbumin-induced asthmatic mouse model assessed as decrease in IL-5 level in BALF at 2.6 mg/kg, po administered once daily for 7 days by ELISA
AID1903437Binding affinity to immobilized Halo tag-fused beta2 adrenoceptor (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as retention time by chromatography
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.
AID1439966Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 5 mins by electrocardiogram (Rvb = -14.06 +/- 24.25 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1470913Inhibition of BuChE (unknown origin)2017European journal of medicinal chemistry, May-26, Volume: 132Recent progress in the identification of selective butyrylcholinesterase inhibitors for Alzheimer's disease.
AID1439974Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 13 mins by electrocardiogram (Rvb = -37.85 +/- 14.54 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
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.
AID1439987Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 26 mins by electrocardiogram (Rvb = -46.48 +/- 17.52 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1916909Inhibition of rat BChE2022European journal of medicinal chemistry, Oct-05, Volume: 240Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.
AID625294Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in O'Brien data2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1879286Inhibition of BuchE (unknown origin)2022Bioorganic & medicinal chemistry letters, 04-01, Volume: 61Design, synthesis, biological evaluation and molecular modeling of N-isobutyl-N-((2-(p-tolyloxymethyl)thiazol-4yl)methyl)benzo[d][1,3] dioxole-5-carboxamides as selective butyrylcholinesterase inhibitors.
AID1439973Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 12 mins by electrocardiogram (Rvb = -40.39 +/- 20.17 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439954Irreversible inhibition of equine serum BuChE assessed as second order carbamylation rate constant using S-butyrylthiocholine iodide as substrate preincubated up to 45 mins followed by substrate addition measured after 5 mins2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439965Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 4 mins by electrocardiogram (Rvb = -13.79 +/- 13.4 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1439948Inhibition of electric eel AChE using S-acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439997Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 36 mins by electrocardiogram (Rvb = -32.32 +/- 25.52 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1439956Selectivity ratio of Ki for human plasma BuChE assessed as second order carbamylation rate constant to Ki for equine serum BuChE assessed as second order carbamylation rate constant2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
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.
AID1470912Inhibition of AChE (unknown origin)2017European journal of medicinal chemistry, May-26, Volume: 132Recent progress in the identification of selective butyrylcholinesterase inhibitors for Alzheimer's disease.
AID1439964Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 3 mins by electrocardiogram (Rvb = -14.4 +/- 19.94 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439980Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 19 mins by electrocardiogram (Rvb = -38.67 +/- 13.91 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439970Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 9 mins by electrocardiogram (Rvb = -31.96 +/- 17.01 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
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.
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.
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.
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.
AID1439977Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 16 mins by electrocardiogram (Rvb = -38.67 +/- 10.18 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
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.
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.
AID1439996Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 35 mins by electrocardiogram (Rvb = -31.81 +/- 27.31 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
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.
AID1879285Inhibition of AChE (unknown origin)2022Bioorganic & medicinal chemistry letters, 04-01, Volume: 61Design, synthesis, biological evaluation and molecular modeling of N-isobutyl-N-((2-(p-tolyloxymethyl)thiazol-4yl)methyl)benzo[d][1,3] dioxole-5-carboxamides as selective butyrylcholinesterase inhibitors.
AID1439981Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 20 mins by electrocardiogram (Rvb = -40.16 +/- 13.12 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439995Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 34 mins by electrocardiogram (Rvb = -35 +/- 23.88 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
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]
AID1439985Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 24 mins by electrocardiogram (Rvb = -44.48 +/- 12.38 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439978Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 17 mins by electrocardiogram (Rvb = -38.32 +/- 10.76 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1916869Inhibition of rat AChE2022European journal of medicinal chemistry, Oct-05, Volume: 240Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.
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]
AID1439998Inhibition of human blood AChE using acetylthiocholine as substrate2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1439989Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 28 mins by electrocardiogram (Rvb = -49.06 +/- 20.71 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439967Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 6 mins by electrocardiogram (Rvb = -19.47 +/- 22.55 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
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]
AID1903419Anti-asthmatic activity against ovalbumin-induced asthmatic mouse model assessed as infiltration of inflammatory cells in the perivascular and peribronchiolar region of lungs at 2.6 mg/kg, po administered once daily for 7 days by H and E staining based li
AID1439993Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 32 mins by electrocardiogram (Rvb = -43.48 +/- 20.81 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439951Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID625295Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in Pfizer data2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1439992Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 31 mins by electrocardiogram (Rvb = -42.8 +/- 29.79 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439955Irreversible inhibition of human plasma BuChE assessed as second order carbamylation rate constant using S-butyrylthiocholine iodide as substrate preincubated up to 45 mins followed by substrate addition measured after 5 mins2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1439969Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 8 mins by electrocardiogram (Rvb = -27.98 +/- 16.02 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439971Cardiotoxicity in Kunming mouse assessed as change in heart rate at 20 mg/kg, ip measured after 10 mins by electrocardiogram (Rvb = -34.85 +/- 19.78 No_unit)2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1439952Inhibition of human plasma BuChE using S-butyrylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method2017European journal of medicinal chemistry, Jan-27, Volume: 126Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' 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.
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
AID1345972Human butyrylcholinesterase (Hydrolases)2003Neurochemical research, Apr, Volume: 28, Issue:3-4
Cholinesterases: new roles in brain function and in Alzheimer's disease.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (124)

TimeframeStudies, This Drug (%)All Drugs %
pre-199013 (10.48)18.7374
1990's40 (32.26)18.2507
2000's27 (21.77)29.6817
2010's32 (25.81)24.3611
2020's12 (9.68)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 62.55

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

MetricThis Compound (vs All)
Research Demand Index62.55 (24.57)
Research Supply Index5.11 (2.92)
Research Growth Index4.85 (4.65)
Search Engine Demand Index103.43 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (62.55)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials35 (27.13%)5.53%
Reviews7 (5.43%)6.00%
Case Studies1 (0.78%)4.05%
Observational0 (0.00%)0.25%
Other86 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The Safety Evaluation of Theophylline and Bambuterol When Administered Orally Alone and in Combination to Healthy Volunteers [NCT01566565]Phase 120 participants (Actual)Interventional2012-03-31Completed
Randomised, Open-label, Parallel-group Study of the Response to Bronchodilator Treatment in Subjects With Eosinophilic Bronchitis and the Mechanism of Varied Responses to Bronchodilator Treatment. [NCT02002754]Phase 445 participants (Anticipated)Interventional2012-06-30Recruiting
A 12-week, Double-blind, Multicenter, 3-crossover, Placebo Controlled and Randomized Trial to Investigate the Efficacy and Safety of 10mg and 5mg Bambuterol Tablets Once Daily in Patients With Chronic Obstructive Pulmonary Disease (COPD) [NCT01796730]Phase 460 participants (Actual)Interventional2013-02-28Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]