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Description

Fenoterol: A synthetic adrenergic beta-2 agonist that is used as a bronchodilator and tocolytic. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

fenoterol : A member of the class resorcinols that is 5-(1-hydroxyethyl)benzene-1,3-diol in which one of the methyl hydrogens is replaced by a 1-(4-hydroxyphenyl)propan-2-amino group. A beta2-adrenergic agonist, it is used (as the hydrobromide salt) as a bronchodilator in the management of reversible airway obstruction. [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 CID3343
CHEMBL ID32800
CHEMBL ID537445
CHEBI ID149226
SCHEMBL ID5009
MeSH IDM0008336

Synonyms (94)

Synonym
AC-13630
STL356034
BRD-A97104540-004-04-4
gtpl557
KBIO1_000405
DIVK1C_000405
5-(1-hydroxy-2-{[2-(4-hydroxyphenyl)-1-methylethyl]amino}ethyl)benzene-1,3-diol
fenoterol
brn 2157041
th 1165a
partusisten
fenoterolum [inn-latin]
th 1165
benzyl alcohol, 3,5-dihydroxy-alpha-(((p-hydroxy-alpha-methylphenethyl)amino)methyl)-
berotec
SPECTRUM_001246
PRESTWICK2_000282
PRESTWICK3_000282
IDI1_000405
13392-18-2
fenoterol (usan/inn)
D04157
BSPBIO_000184
SPECTRUM5_001572
BPBIO1_000204
AB00053590
5-{1-hydroxy-2-[2-(4-hydroxy-phenyl)-1-methyl-ethylamino]-ethyl}-benzene-1,3-diol
1-(3,5-dihydroxyphenyl)-1-hydroxy-2-((4-hydroxyphenyl)isopropylamino)ethane
1-(p-hydroxyphenyl)-2-((beta-hydroxy-beta-(3',5'-dihydroxyphenyl))ethyl)aminopropane
3,5-dihydroxy-alpha-(((p-hydroxy-alpha-methylphenethyl)amino)methyl)benzyl alcohol
DB01288
phenoterol
KBIO2_001726
KBIOGR_001507
KBIO3_001890
KBIO2_006862
KBIOSS_001726
KBIO2_004294
SPBIO_001376
SPECTRUM4_001014
PRESTWICK1_000282
NINDS_000405
SPBIO_002403
SPECTRUM3_000915
SPECTRUM2_001388
PRESTWICK0_000282
LOPAC0_000544
NCGC00162181-01
NCGC00015430-03
bdbm50131281
5-(1-hydroxy-2-(1-(4-hydroxyphenyl)propan-2-ylamino)ethyl)benzene-1,3-diol
CHEMBL32800 ,
th 1165a [as hydrobromide salt]
th 1165a free base
th-1165a free base
nsc-757811
L000255
fenoterol hbr
rac-(2s)-n-[(2r)-2-(3,5-dihydroxyphenyl)-2-hydroxyethyl]-1-(4-hydroxyphenyl)propan-2-amonium bromide
CHEMBL537445 ,
bdbm50221768
5-[1-hydroxy-2-[1-(4-hydroxyphenyl)propan-2-ylamino]ethyl]benzene-1,3-diol
CHEBI:149226 ,
fenoterolum
5-(1-hydroxy-2-{[1-(4-hydroxyphenyl)propan-2-yl]amino}ethyl)benzene-1,3-diol
nsc 757811
fenoterol [usan:inn:ban]
CCG-204634
AKOS015964608
NCGC00015430-02
S5769
BBL023034
SCHEMBL5009
CS-4466
391234-95-0
HY-B0976
5-[1-hydroxy-2-[[2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-1,3-benzenediol
partusisten (salt/mix)
berotec (salt/mix)
benzyl alcohol, 3,5-dihydroxy-.alpha.-(((p-hydroxy-.alpha.-methylphenethyl)amino)methyl)-
1-(p-hydroxyphenyl)-2-((.beta.-hydroxy-.beta.-(3',5'-dihydroxyphenyl))ethyl)aminopropane
AB00053590_10
DTXSID4023046
SBI-0050527.P003
Q420188
th-1165;phenoterol
BRD-A97104540-004-08-5
BCP29485
th-1165;th 1165;th1165; phenoterol;partusisten
SDCCGSBI-0050527.P004
NCGC00015430-11
HMS3886D03
EN300-18530961
1,3-benzenediol,5-[(1s)-1-hydroxy-2-[[(1r)-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" None have done this during a time when prescribers have been just made aware of potential serious adverse events that might be caused by a commonly prescribed medication."( The effect of a warning about putative adverse events on drug prescribing in general practice.
Barham, PM; Thomson, AN, 1993
)
0.29
" This study does not exclude the possibility that adverse cardiac events could occur with severe hypoxemia."( Cardiovascular safety of high doses of inhaled fenoterol and albuterol in acute severe asthma.
Abboud, RT; Bowie, DM; Chapman, KR; Hodder, RV; McCallum, AL; Mesic-Fuchs, H; Molfino, NA; Newhouse, MT; Paré, PD, 1996
)
0.29
" The overall incidence of adverse events was comparable between both groups."( Comparison of the safety of drug delivery via HFA- and CFC-metered dose inhalers in CAO.
Cannizzaro, G; Hofbauer, P; Huchon, G; Iacono, P; Wald, F, 2000
)
0.31
" The overall incidence of adverse events (AEs) was similar in both groups (29."( Fenoterol hydrobromide delivered via HFA-MDI or CFC-MDI in patients with asthma: a safety and efficacy comparison.
Böhning, W; Freund, E; Goldberg, J; Schmidt, P, 2000
)
0.31
" Outcome parameters were (1) the effects on fetal and maternal heart frequency (FHF/MHF) and blood pressure, and (2) subjective experiences of adverse effects assessed by utilising a questionnaire."( Maternal and fetal side effects of tocolysis using transdermal nitroglycerin or intravenous fenoterol combined with magnesium sulfate.
Gross, W; Kähler, C; Möller, A; Möller, U; Richter, S; Schleussner, E; Seewald, HJ, 2003
)
0.32
"Transdermal nitroglycerin appears to be a safe therapy for the mother and fetus and is a promising new option for the treatment of preterm labour."( Maternal and fetal side effects of tocolysis using transdermal nitroglycerin or intravenous fenoterol combined with magnesium sulfate.
Gross, W; Kähler, C; Möller, A; Möller, U; Richter, S; Schleussner, E; Seewald, HJ, 2003
)
0.32
" In conclusion, IB/FEN delivered via Respimat SMI is at least as effective as, and is as safe as, when delivered via CFC-MDI plus Aerochamber in children with asthma."( Efficacy and safety of ipratropium bromide plus fenoterol inhaled via Respimat Soft Mist Inhaler vs. a conventional metered dose inhaler plus spacer in children with asthma.
Gerken, F; Jeena, PM; Razzouk, H; Schmidt, P; Soemantri, PA; Vertruyen, A; von Berg, A, 2004
)
0.32
" Tocolysis was terminated as a result of maternal adverse effects in the fenoterol group (9%)."( [Effectiveness and safety of atosiban vs. pulsatile administration of fenoterol in the treatment of preterm labour].
Dudenhausen, J; Hopp, H; Nonnenmacher, A, 2009
)
0.35
"The adverse effects in the pulsatile administration of fenoterol for short duration were only dependent on the initial dosage for the arrest of preterm labour."( [Effectiveness and safety of atosiban vs. pulsatile administration of fenoterol in the treatment of preterm labour].
Dudenhausen, J; Hopp, H; Nonnenmacher, A, 2009
)
0.35
"Atosiban was comparable in clinical effectiveness and was associated with fewer maternal and fetal adverse effects, so that fenoterol cannot be recommended."( [Effectiveness and safety of atosiban vs. pulsatile administration of fenoterol in the treatment of preterm labour].
Dudenhausen, J; Hopp, H; Nonnenmacher, A, 2009
)
0.35

Pharmacokinetics

ExcerptReferenceRelevance
" Patients with renal failure but not asthmatics show changed pharmacokinetic profiles."( Pharmacokinetic/pharmacodynamic characteristics of the beta-2-agonists terbutaline, salbutamol and fenoterol.
Hochhaus, G; Möllmann, H, 1992
)
0.28
" Its pharmacodynamic effects are similar to those of other selective beta 2-adrenoceptor agonists."( Fenoterol: a beta2-adrenergic agonist for use in asthma. Pharmacology, pharmacokinetics, clinical efficacy and adverse effects.
Svedmyr, N,
)
0.13
" We conclude that there is no need to adjust the dose on pharmacokinetic grounds in the course of pregnancy."( Pharmacokinetics of fenoterol in pregnant and nonpregnant women.
Gundert-Remy, U; Hildebrandt, R; Warnke, K; Weitzel, H, 1993
)
0.29
" 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
" Results from the study suggest that (R,R)-MFen can offer pharmacokinetic and metabolic advantages in comparison to an earlier (R,R)-Fen."( Pharmacokinetics and metabolism of (R,R)-methoxyfenoterol in rat.
Furimsky, AM; Green, CE; Iyer, LV; Kim, HS; Mager, DE; Siluk, D; Ta, A; Wainer, IW; Wang, Y, 2010
)
0.36

Compound-Compound Interactions

ExcerptReferenceRelevance
"Two groups each consisting of twelve healthy students received Fenoterol (0,03 microgram/kg/min) alone or in combination with Verapamil (1,2 micrograms/kg/min) intravenously."( [Cardiac effect of fenoterol alone or combined with Verapamil (author's transl)].
Hofstetter, R; Krebs, W; Lang, D; Schmidt, HP; von Bernuth, G, 1979
)
0.26
" The results showed that a temporary relative hypoglycaemia occured in the newborns in short term as well as long term treatment with Partusisten or Partusisten in combination with Isoptin."( [Behaviour of serum concentrations of glucose, immunoreactive insulin and potassium ions in newborns after long term or crash treatments with Partusisten or Partusisten in combination with Isoptin (author's transl)].
Haller, K; Hiltmann, WD; Mohr, D; Vogel, M; Weidinger, H, 1976
)
0.26
" We conclude that metered-dose ipratropium alone has small and clinically unimportant hemodynamic effects and produces no clinically significant increases in the cardiovascular side effects of the bronchodilator regimen when given with fenoterol."( Hemodynamic effects of inhaled ipratropium bromide, alone and combined with an inhaled beta 2-agonist.
Chapman, KR; Leenen, FH; Rebuck, AS; Smith, DL, 1985
)
0.27
"We describe a successful, prolonged, inhibition of preterm labor using nifedipine combined with terbutaline in a patient undergoing complicated obstetrical problems."( The management of preterm labor with the calcium channel-blocking agent nifedipine combined with the beta-mimetic terbutaline.
Friedman, PA; Frigoletto, FD; Kaul, AF; Osathanondh, R; Safon, LE, 1985
)
0.27
" 17 patients (group I) got fenoterol-monotherapy; in 18 patients (group II) fenoterol was combined with the cardioselective beta-1-blocking agent metoprolol."( [Efficency of tocoylsis by fenoterol and fenoterol in combination with a beta-1-blocking compound (author's transl)].
Bernius, U; Hillemanns, HG; Irmer, M; Pohl, C; Steim, H; Trolp, R, 1980
)
0.26
"To compare the maternal and fetal side effects of transdermal nitroglycerin and intravenous fenoterol combined with magnesium sulfate in a prospective randomised study."( Maternal and fetal side effects of tocolysis using transdermal nitroglycerin or intravenous fenoterol combined with magnesium sulfate.
Gross, W; Kähler, C; Möller, A; Möller, U; Richter, S; Schleussner, E; Seewald, HJ, 2003
)
0.32

Bioavailability

ExcerptReferenceRelevance
" In these experiments, fenoterol and orciprenaline showed better bioavailability than salbutamol."( Determination of bioavailability on the basis of tachycardia after intravenous and oral administration of fenoterol, orciprenaline and salbutamol in non-anaesthetized rats.
Muacevic, G, 1985
)
0.27
" The absorption rate after inhalation differs individually in a large variability (1-27% of the dosage)."( Pharmacokinetics of beta2-sympathomimetics at the example of fenoterol and conclusion for the administration.
Schmidt, EW, 1998
)
0.3
" The data suggest that the total and regional lung deposition of hydrofluoroalkane-based pressurized aerosol formulations is highly product-specific and that changes in bioavailability can be brought about by varying both the constituents of the formulation and the design of the actuator."( Deposition of fenoterol from pressurized metered dose inhalers containing hydrofluoroalkanes.
Harrison, A; Nagel, J; Newman, S; Pitcairn, G; Steed, K, 1999
)
0.3
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" In conclusion, the results suggest that a formulation developed from a mixture of (R,R')-MF and (S,R')-MF may increase the oral bioavailability of (R,R')-MF."( The stereoselective sulfate conjugation of 4'-methoxyfenoterol stereoisomers by sulfotransferase enzymes.
Catz, P; Furimsky, AM; Green, CE; Iyer, LV; Jozwiak, K; Ramamoorthy, A; Rutkowska, E; Tang, L; Wainer, IW, 2012
)
0.38
" The data suggest that a non-racemic mixture of the Fen enantiomers may provide better bioavailability of the active (R,R')-Fen for use in the treatment of cardiovascular disease."( Development and validation of a sensitive LC-MS/MS method for the determination of fenoterol in human plasma and urine samples.
Moaddel, R; Ramamoorthy, A; Sanghvi, M; Strait, J; Wainer, IW, 2013
)
0.39
"Cell membrane permeability is an important determinant for oral absorption and bioavailability of a drug molecule."( Highly predictive and interpretable models for PAMPA permeability.
Jadhav, A; Kerns, E; Nguyen, K; Shah, P; Sun, H; Xu, X; Yan, Z; Yu, KR, 2017
)
0.46

Dosage Studied

ExcerptRelevanceReference
" Increase of dosage did not lead to improved effectiveness."( [Parasympathicolytic drugs in treatment of obstructive lung diseases (author's transl)].
Gonsior, E; Meier-Sydow, J; Schultze-Werninghaus, G, 1979
)
0.26
"Fenoterol-Ipratropiumbromid dosage aerosol (IK 6) showed in acute experiments on patients with chronic obstructive disease optimal bronchodilatation."( [Treatment of obstructive disease with fenoterol-ipratropiumbromid dosage aerosol (IK 6). Short and long-terms results (author's transl)].
Ulmer, WT, 1979
)
0.26
" Dosage should be individualized according to the case and labour advancement, and should be based on topographic evaluation of uterine contraction."( [Inhibition of premature uterine contractions].
Adamowicz, R; Brankowska, J; Chazan, B; Leibschang, J; Troszyński, M, 1979
)
0.26
"Aerosolized fenoterol in a dosage of 400 microgram was compared to isoproterenol 150 microgram in 31 asthmatic subjects during the course of a double-blind parallel 90-day study."( Comparison of the bronchodilator effects of aerosol fenoterol and isoproterenol.
Beall, GN; Kuo, J; Smith, R; Steen, SN; Ziment, I, 1977
)
0.26
" However, in late gestosis, a lower dosage should be administered than in labor inhibition."( [Erythrocyte alteration in long standing labor inhibition with a beta-sympathicomimetic drug (Partusisten) (author's transl)].
Buchholz, FG; Heilmann, L, 1978
)
0.26
"Cumulative dose-response curves for orally administered fenoterol and salbutamol concerning effects of FEV1, heart rate, blood pressure and tremor were constructed."( Cumulative dose-response curves for comparison of oral bronchodilating drugs. A study of salbutamol and fenoterol.
Larsson, S; Svedmyr, N, 1977
)
0.26
" 2ng/ml fenoterol were sufficient to increase frequency both in fetal and maternal preparations; dose-response curves were parallel in both cases."( [In vitro responsiveness of fenoterol in fetal and maternal hearts (author's transl)].
Kords, H, 1975
)
0.25
" Since most authors take as optimal therapeutic level of verapamil in blood the range of 100-200 ng/ml, it seems that dosage regimen of 2 x 80 mg/day can be recommended."( [Pharmacokinetic investigations of verapamil used as a concomitant drug in treatment of premature labor].
Jankowski, A; Kotzbach, R; Skublicki, S; Szymański, W, 1992
)
0.28
" We conclude that fenoterol inhaled at a dosage used in clinical practice significantly reduces Kpl but not Mgpl nor MgIE levels in healthy subjects, indicating a lower sensitivity of Mg++ ions to beta 2-adrenergic stimulation than K+ ions."( Metabolic effects of inhaled fenoterol in normal subjects.
Gorus, F; Musch, W; Noppen, M; Vincken, W, 1992
)
0.28
"Reversed-phase high-performance liquid chromatography (RP-HPLC), isotachophoresis (ITP) and capillary zone electrophoresis (CZE) were applied to the determination of salbutamol, terbutaline sulphate and fenoterol hydrobromide in commercially available pharmaceutical dosage forms."( Comparison of isotachophoresis, capillary zone electrophoresis and high-performance liquid chromatography for the determination of salbutamol, terbutaline sulphate and fenoterol hydrobromide in pharmaceutical dosage forms.
Ackermans, MT; Beckers, JL; Everaerts, FM; Seelen, IG, 1992
)
0.28
"Fenoterol hydrobromide (200 micrograms), ipratropium bromide (40 micrograms) and a combination of the two in the same dosage were administered by metered dose inhaler on 3 separate days to 20 patients with chronic bronchitis and emphysema."( Comparison of bronchodilatation produced by an anticholinergic (ipratropium bromide), a beta-2 adrenergic (fenoterol) and their combination in patients with chronic obstructive airway disease. An open trial.
Behera, D; Guleria, R; Jindal, SK, 1991
)
0.28
" The dose-response curves for these agonists were shifted slightly to the right when the amplitude of the twitch was increased up to twice its original size."( Dissociation constants and relative efficacies estimated from the functional antagonism of beta-adrenoceptor agonists on transmural stimulation in rat vas deferens.
Diaz-Toledo, A; Jurkiewicz, A, 1990
)
0.28
"To investigate the dose-response relationship and the time course of the effects of fenoterol (a selective beta 2-adrenergic agonist) on respiratory function in mechanically ventilated patients with acute respiratory failure due to exacerbation of chronic airflow obstruction (CAO), seven consecutive acutely ill patients were studied within 3 days of the onset of mechanical ventilation."( Dose-response effects and time course of effects of inhaled fenoterol on respiratory mechanics and arterial oxygen tension in mechanically ventilated patients with chronic airflow obstruction.
Bernasconi, M; Brandolese, R; Manzin, E; Poggi, R; Rossi, A, 1990
)
0.28
"In a randomized, double-blind, double-dummy, crossover study consisting of two 1-month periods with a 2-week 'run-in' we compared the effects of a combination of fenoterol with ipratropium bromide (Duovent, Boehringer Ingelheim) and salbutamol administered by standard metered dose inhalers in conventional dosage in young adults with nocturnal asthma."( Comparison of a combination of fenoterol with ipratropium bromide (Duovent) and salbutamol in young adults with nocturnal asthma.
Shettar, SP; Wolstenholme, RJ, 1989
)
0.28
" Ten non-asthmatic subjects aged 21-28 yrs performed dose-response curves to nebulized FMLP on 3 study days after pretreatment with saline, F or IB."( The effect of anticholinergic and beta-agonist pretreatment on bronchoconstriction induced by N-formyl-methionyl-leucyl-phenylalanine.
Berend, N; Breslin, AB; Peters, MJ, 1989
)
0.28
"The beta 2-adrenergic agonists are reviewed in terms of their dose-response characteristics, and two newer agents, fenoterol hydrobromide and bitolterol mesylate aerosols, are reviewed in relation to older agents."( New beta 2-adrenergic agonist aerosols.
Kelly, HW,
)
0.13
" Biotransformations are determined by environmental or genetic factors and by the associated therapy and can change dramatically from one patient to another (interindividual variability) or for the same patient by multiple dosing (intra-individual variability)."( [Metabolism of beta-adrenergic substances. Therapeutic implications].
Brès, J; Bressolle, F; Clauzel, AM; Pistre, MC; Rachmat, H,
)
0.13
" The combination with low dosed fenoterol (Berodual) produced equally good subjective and objective results with less side effects than the high dosed fenoterol."( Clinical experience with a bronchospasmolytic aerosol combination.
Forche, G; Harnoncourt, K, 1986
)
0.27
" A single-blind cross-over design was used in order to obtain cumulative dose-response curves."( Dose-response relationship: fenoterol, ipratropium bromide and their combination.
Ciappi, G; Corbo, GM; Culla, G; Magnini, P; Patalano, F; Toscano, L; Valente, S, 1986
)
0.27
" The three dose-response curves (parallel) show that, in respect of an increase in FEV1, 1 puff of Duovent (100 micrograms fenoterol + 40 micrograms ipratropium bromide) is approximately equal to 2 puffs of fenoterol (200 micrograms) and 4 puffs of ipratropium bromide (160 micrograms)."( Acute controlled study of the dose-response relationship of fenoterol, ipratropium bromide and their combination.
Giacopelli, A; Luciani, G; Serra, C, 1986
)
0.27
" Information was compiled daily by the patients themselves on dyspnoea, cough, peak flow, any increase in dosage over the recommended dose and any side-effects that might have developed."( Controlled clinical study of a long-term treatment of chronic obstructive lung disease using a combination of fenoterol and ipratropium bromide in aerosol form.
Giacopelli, A; Serra, C, 1986
)
0.27
" The dosage of the combination was 1 puff of aerosol per 10 kg body weight, up to a maximum of 4 puffs."( Exercise-induced asthma (EIA): its prevention with the combined use of ipratropium bromide and fenoterol.
Bellía, CA; Bodas, AW; Russo, GH, 1986
)
0.27
" At the day of inclusion, 6 and 12 weeks after start, a dose-response curve was obtained after inhalation of the test medicine used during the previous 6-week period."( Comparison of two aerosols containing both fenoterol and ipratropium in a high (Duovent) and low (Berodual) concentration, respectively.
Frølund, L; Madsen, F; Svendsen, UG; Weeke, B, 1986
)
0.27
" In the presence of increasing concentrations of ACh (2 X 10(-4) and 2 X 10(-3) mol/L), dose-response curves of the relaxant effect of F were shifted to the right (0."( Interaction between fenoterol, ipratropium, and acetylcholine on human isolated bronchus.
Advenier, C; Bakdach, H; Matran, R; Naline, E; Toty, L, 1988
)
0.27
" Dosage for an acute attack in children is 1 puff (200 micrograms), repeated within 5 minutes if necessary; in adults 1-3 puffs can be given."( Fenoterol: a beta2-adrenergic agonist for use in asthma. Pharmacology, pharmacokinetics, clinical efficacy and adverse effects.
Svedmyr, N,
)
0.13
"Twenty-four elderly male patients with moderate-to-severe chronic airway obstruction took part in a double-blind, placebo-controlled, randomized dose-response and response-duration comparison of a new inhaled anticholinergic bronchodilator oxitropium bromide and the inhaled beta-agonist bronchodilator fenoterol hydrobromide."( Effects of inhaled oxitropium and fenoterol, alone and in combination, in chronic airflow obstruction.
Atkinson, J; Frith, PA; Jenner, B, 1986
)
0.27
" According to the known dosage curve, the dosage of Verapamil would have to be increased multifold to achieve an effect, which is hardly possible due to the cardiodepression and peripheral circulation drop with hypotension that this would entail."( Does the administration of the calcium-antagonist verapamil in tocolysis with beta-sympathicomimetics still make sense?
Blümel, G; Erhardt, W; Fischbach, F; Krieglsteiner, P; Pfeiffer, U; Strigl, R, 1981
)
0.26
"The development and repairability of "wavy ribs" were studied in offspring from dams of rat strain SD-JCL dosed with fenoterol, a beta-adrenoceptor stimulant."( Repairability of drug-induced "wavy ribs" in rat offspring.
Iizuka, M; Iwaki, S; Kast, A; Nishimura, M, 1982
)
0.26
" This study serves to quantitate the pharmacologic effects of several agents on anti-IgE-mediated histamine release from dispersed human lung mast cells and has further suggested that the dispersed cell system is similar to the standard chopped lung system in dose-response relationships, kinetics, and pharmacologic modulation."( Dispersed human lung mast cells. Pharmacologic aspects and comparison with human lung tissue fragments.
Lichtenstein, LM; MacGlashan, DW; Newball, HH; Peters, SP; Schleimer, RP; Schulman, ES, 1982
)
0.26
" The dose-response inhibition curve is paralleled by a fenoterol-induced increase in the cAMP levels of human leukocyte preparations."( Inhibition of IgE-mediated histamine release from human basophils and mast cells by fenoterol.
Ambrosio, G; Bonaduce, D; Condorelli, M; Genovese, A; Marone, G; Triggiani, M, 1984
)
0.27
"The dose-response relationships of a combination of the selective beta adrenergic agonist, fenoterol, and the synthetic anticholinergic drug, ipratropium bromide, were studied."( A dose-response and duration of action assessment of a combined preparation of fenoterol and ipratropium bromide (Duovent).
Archer, PS; Cayton, RM; Packe, GE, 1984
)
0.27
" This provides a simple, rapid and reproducible way of obtaining linear dose-response curves by plotting times of exposures against absolute or percent increases in sRaw."( Drug effect on bronchial response to PGF2 alpha and water inhalation.
Bianco, S; Damonte, C; Robuschi, M, 1983
)
0.27
"1 mg) produced effective bronchodilatation but there was a significant logarithmic dose-response relationship over the dose range tested (0."( A dose-response study on fenoterol (Berotec) solution by inhalation in asthmatic children.
Blackhall, MI; Macartney, B; O'Donnell, SR, 1983
)
0.27
" It is concluded that pretreatment of exercise-induced asthma with a beta-2-agonist is equally effective whether dosed from a pressurized aerosol as when given as a dry powder."( Double-blind pretreatment of exercise-induced asthma with sequential inhalations of fenoterol from an aerosol and as a powder (second of two parts).
Bundgaard, A; Schmidt, A, 1983
)
0.27
"The purpose of this study was to determine the level of protection afforded by fenoterol (200 microgram), administered by pressurized aerosol, in allergen-induced bronchospasm and to compare its effect with that of the same drug administered at the same dosage in powder form."( Double-blind crossover study on the protective effect of fenoterol--administered by pressurized aerosol and in powder form--in allergen-induced asthma.
Cocco, G; D'Amato, G; Melillo, G; Schiano, M, 1984
)
0.27
" Therefore, the indication and dosage of fenoterol should be subjected to more rigid criteria than so far applied."( [Cardiotoxic effect of the tocolytic agent fenoterol (partusisten) in the neonate (author's transl)].
Dame, WR; Hilgenberg, F; Löser, H; Müller, KM; Pfefferkorn, JR; Steinkamp, U, 1981
)
0.26
" Fenoterol used at the dosage of 100 micrograms per puff (half the standard commercially available dose of 200 micrograms per puff) caused significantly more cardiac effects than terbutaline, as measured by the magnitude and duration of increases in heart rate, and the incidence of reported palpitations."( A comparative double-blind study of the bronchodilator effects and side effects of inhaled fenoterol and terbutaline administered in equipotent doses.
Costello, JF; Frame, MH; Gray, BJ, 1982
)
0.26
"Experimental investigations in the rabbit were aimed at solving the question whether the development of a pulmonary oedema during tocolytic therapy with beta 2-sympathomimetics can be explained by hyperhydration, since myocardial necroses are not likely to be the cause of a pulmonary-oedema at the standard clinical dosage level."( [Occurrence of pulmonary oedemas without myocardial necroses under beta 2-sympathomimetic therapy with fenoterol (experimental investigations in the rabbit (author's transl)].
Fenske, M; Grospietsch, G; Kuhn, W, 1980
)
0.26
" We believe the results obtained are important for a better dosage and time distribution of the therapy with beta2 agonists."( Effects of inhaled fenoterol on the circadian rhythm of expiratory flow in allergic bronchial asthma.
Carpentiere, G; Castello, F; Marino, S, 1983
)
0.27
" The lowest dosage of fenoterol was as effective as the highest but had fewer adverse effects."( Comparison of fenoterol, isoproterenol, and isoetharine with phenylephrine aerosol in asthma.
Epstein, JD; Gruebel, BJ; Rotman, HH; Spellman, GG; Weg, JG,
)
0.13
" A certain dosage of Atenolol could be defined, that does not increase labor activity under Fenoterol medication but does decrease cardiac frequency without influence on mean blood pressure."( [Tokolysis and dose-dependent effects of beta-blocking with atenolol in the rabbit].
Behr, J; Czekelius, P; Steib, L,
)
0.13
" If preterm labour was stopped, the dosage had been reduced."( [Clinical study of the labour inhibiting effects an side effects of acetylsalicylic acid (ASA) (author's transl)].
Berg, R; Bolte, A; Wolff, F, 1981
)
0.26
" After the establishment of these measurements Fenoterol has been given in an increasing dosage up to the upper therapeutical range."( [The cardiac hazard of tocolysis and antagonising possibilities. I. The haemodynamic situation of the patient during tocolysis/Protection of the myocardium by means of cardioselective beta-blockade. Experimental results (author's transl)].
Heimisch, W; Mendler, N; Schroll, A; Weidenbach, A; Wischnik, A, 1982
)
0.26
" The increase in FEV1 was the same after both dosage forms and no side effects occurred indicating that powder inhalation is a safe and effective alternative to aerosol inhalation in the treatment of asthma with sympathomimetics."( A comparison between aerosol and inhaled powder administration of fenoterol in adult asthmatics.
Harris, R; Rothwell, RP, 1981
)
0.26
" Doubling the dosage produced little improvement in efficacy but did increase somewhat the severity of side effects."( Fenoterol hydrobromide (Berotec, Th 1165a) 0.1% solution in the treatment of allergic rhinitis.
Ford, RM, 1980
)
0.26
" In order to establish the most satisfactory dosage for Fenoterol, several doses were administered intravenously to pregnant women during birth and the actions on uterine relaxation and on side effects were examined."( Dose-response study of fenoterol on uterine activity in labor at term.
Kidess, E; Lippert, TH; Peters, FD, 1980
)
0.26
" A dose-response curve for nebulized ipratropium was determined."( [Use of ipratropium bromide by inhalation in the treatment of acute asthma in children. Clinical experience].
Beck, R, 1995
)
0.29
" Isolated atrial strips showed a right shift of their dose-response curve to isoprenaline in the presence of the highly selective beta 2-AR antagonist ICI 118,551 at concentrations above 1 x 10(-8) mol/L."( The effects of sympathomimetics on the cardiovascular system of sheep.
Allen, R; Alley, MR; Baxter, S; Burgess, C; Crane, J; Dallimore, JA; Davie, PS; Kealey, AS; Lapwood, KR; Pack, RJ, 1994
)
0.29
" Dose-response curves were constructed using cumulative doses of 100 micrograms, 200 micrograms, 400 micrograms, 1000 micrograms, 2000 micrograms, and 4000 micrograms, and airways and systemic responses were measured 20 minutes after each dose with 40 minute increments."( Comparison of the relative airways and systemic potencies of inhaled fenoterol and salbutamol in asthmatic patients.
Clark, RA; Dhillon, DP; Lipworth, BJ; McDevitt, DG; Newnham, DM; Winter, JH, 1995
)
0.29
" However, dosage requirements have not been thoroughly evaluated and comparative dose-response data for these agents are limited."( Comparative dose-response study of three anticholinergic agents and fenoterol using a metered dose inhaler in patients with chronic obstructive pulmonary disease.
Ikeda, A; Izumi, T; Koyama, H; Nishimura, K, 1995
)
0.29
" At 72 h after the last administration of saline, fenoterol, and ovalbumin, the dose-response relationship between pulmonary resistance (RL) and nebulized acetylcholine (ACh) was measured."( Chronic fenoterol exposure increases in vivo and in vitro airway responses in guinea pigs.
Bai, TR; Bramley, AM; McNamara, A; Paré, PD; Wang, ZL, 1994
)
0.29
"The relative bronchodilator (delta FEV1, V25, V50) potency and side effect profile (delta tremor, heart rate, breathlessness, BP) of nebulized salbutamol and fenoterol were evaluated by means of a randomized, double-blind, crossover, cumulative (50 to 2,500 micrograms) dose-response study."( Dose-effect relationship of the beta-agonists fenoterol and salbutamol in patients with asthma.
Dolovich, MB; Kazim, F; Newhouse, MT, 1994
)
0.29
" The cumulative dose-response curve of oxitropium bromide inhaled from a metered-dose inhaler was determined in eleven normal subjects."( Bronchodilator effects of oxitropium bromide, fenoterol, and their combination in normal subjects.
Fujimura, M; Hashimoto, T; Kamio, Y; Matsuda, T, 1993
)
0.29
" One hour after inhaling single doses of placebo, salmeterol 25 micrograms, or formoterol 12 micrograms, dose-response curves to repeated doses of inhaled fenoterol were constructed (cumulative doses of 100-3200 micrograms)."( Effects of prior treatment with salmeterol and formoterol on airway and systemic beta 2 responses to fenoterol.
Grove, A; Lipworth, BJ, 1996
)
0.29
" There were no significant differences in the area under the dose-response curve for any of the parameters during the dose-response curve following treatment with salmeterol or formoterol compared with placebo."( Effects of prior treatment with salmeterol and formoterol on airway and systemic beta 2 responses to fenoterol.
Grove, A; Lipworth, BJ, 1996
)
0.29
"Prior treatment with low doses of salmeterol or formoterol does not significantly alter bronchodilator dose-response curves to repeated doses of fenoterol in stable asthmatic patients."( Effects of prior treatment with salmeterol and formoterol on airway and systemic beta 2 responses to fenoterol.
Grove, A; Lipworth, BJ, 1996
)
0.29
" We emphasise that the accuracy especially of the CRP for early prediction of silent infection in preterm labour does not seem to be impaired by this corticosteroid in a dosage usually administered for prevention of respiratory distress syndrome."( [Does lung maturation therapy with 16-methylene-prednisolone modify maternal infection parameters in threatened premature labor?].
Heyl, W; Rath, W; Reister, F; Winkler, M, 1996
)
0.29
" An appropriate dosing schedule for fenoterol needs to be redefined."( Oral fenoterol versus sustained release theophylline in adult asthmatics.
Almagro, J; Andrade, RJ; Hidalgo Sanchez, R; Lucena, MI; Sanchez de la Cuesta, F, 1997
)
0.3
"The aim of this study was to develop a microspherical dosage form for a highly water-soluble drug, fenoterol HBr, by using the water insoluble, non-biodegradable polymer, ethyl cellulose."( Modification of the initial release of a highly water-soluble drug from ethyl cellulose microspheres.
Lin, WJ; Wu, TL,
)
0.13
"A simple and highly sensitive voltammetric method was developed for the determination of isoxsuprine HCl (I) and fenoterol HBr (II) in dosage forms and biological fluids."( Voltammetric determination of isoxsuprine and fenoterol in dosage forms and biological fluids through nitrosation.
Al-Majed, AA; Al-Malaq, HA; Belal, F, 2000
)
0.31
" The objective of this study was to describe the dose-response relationship of combined doses of fenoterol hydrobromide (F) and ipratropium bromide (I) (F/I) delivered via Respimat, a soft mist inhaler, and to establish the Respimat dose which is as efficacious and as safe as the standard marketed dose of F/I (100/40 microg) which is delivered via a conventional metered dose inhaler (MDI)."( Improved delivery of fenoterol plus ipratropium bromide using Respimat compared with a conventional metered dose inhaler.
Beckers, B; Freund, E; Goldberg, J; Hinzmann, R, 2001
)
0.31
" At 72 h after the last inhalation of PRO, FEN or vehicle, the dose-response relationship between lung resistance (R(L)) and intravenously administered acetylcholine (ACh) was measured."( Airway responsiveness and airway remodeling after chronic exposure to procaterol and fenoterol in guinea pigs in vivo.
Arakawa, H; Kato, M; Mochizuki, H; Morikawa, A; Nishimura, H; Ohki, Y; Sato, A; Tokuyama, K, 2002
)
0.31
" We conducted an extensive dose-response study to determine the most efficacious dose of fenoterol for increasing skeletal muscle mass in adult rats and used this dose in testing the hypothesis that fenoterol may have therapeutic potential for ameliorating age-related muscle wasting and weakness."( Beta 2-agonist administration reverses muscle wasting and improves muscle function in aged rats.
Gregorevic, P; Lynch, GS; Plant, DR; Ryall, JG; Sillence, MN, 2004
)
0.32
" The primary endpoint was the change in forced expiratory volume in 1 second (FEV1) during the first 60 min after dosing (area under the curve from 0-1 h [AUC(0-1 h)]) on day 29."( Efficacy and safety of ipratropium bromide plus fenoterol inhaled via Respimat Soft Mist Inhaler vs. a conventional metered dose inhaler plus spacer in children with asthma.
Gerken, F; Jeena, PM; Razzouk, H; Schmidt, P; Soemantri, PA; Vertruyen, A; von Berg, A, 2004
)
0.32
" Analysis of the primary endpoint (change in forced expiratory volume in 1 s [FEV1] in the first 60 min after dosing [area under the curve; AUC0-1h]) on day 85 showed that the efficacy of Respimat SMI 20/50 (but not Respimat SMI 10/25) was not inferior to that of MDI 40/100."( Improved delivery of ipratropium bromide/fenoterol from Respimat Soft Mist Inhaler in patients with COPD.
Beck, E; Bowen, I; Hesse, Ch; Kilfeather, SA; Lee, A; Ponitz, HH; Schmidt, P, 2004
)
0.32
"The adverse effects in the pulsatile administration of fenoterol for short duration were only dependent on the initial dosage for the arrest of preterm labour."( [Effectiveness and safety of atosiban vs. pulsatile administration of fenoterol in the treatment of preterm labour].
Dudenhausen, J; Hopp, H; Nonnenmacher, A, 2009
)
0.35
" The dose-response relationship was similar within the non-asthma patients."( Beta2-adrenergic agonist use and the risk of multiple sclerosis: a total population-based case-control study.
Lee, CT; Lin, FC; Tsai, CP, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
bronchodilator agentAn agent that causes an increase in the expansion of a bronchus or bronchial tubes.
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.
beta-adrenergic agonistAn agent that selectively binds to and activates beta-adrenergic receptors.
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 (3)

ClassDescription
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
secondary alcoholA secondary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has two other carbon atoms attached to it.
resorcinolsAny benzenediol in which the two hydroxy groups are meta to one another.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glp-1 receptor, partialHomo sapiens (human)Potency18.35640.01846.806014.1254AID624148
thioredoxin reductaseRattus norvegicus (Norway rat)Potency37.68580.100020.879379.4328AID588453
GLS proteinHomo sapiens (human)Potency4.46680.35487.935539.8107AID624146
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency3.98110.035520.977089.1251AID504332
beta-2 adrenergic receptorHomo sapiens (human)Potency5.80480.00586.026332.6427AID485366
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.15100.060110.745337.9330AID485368
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
Beta-2 adrenergic receptorHomo sapiens (human)Ki0.12600.00000.66359.5499AID777624
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.06000.00040.16800.9772AID40848
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Beta-2 adrenergic receptorHomo sapiens (human)Kd0.11950.00000.62888.9130AID770362; AID777628
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)EC50 (µMol)0.01850.00020.88438.2000AID298201; AID298207
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (54)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
diet induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
regulation of sodium ion transportBeta-2 adrenergic receptorHomo sapiens (human)
transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-2 adrenergic receptorHomo sapiens (human)
smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
cell surface receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
endosome to lysosome transportBeta-2 adrenergic receptorHomo sapiens (human)
response to coldBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase A signalingBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of bone mineralizationBeta-2 adrenergic receptorHomo sapiens (human)
heat generationBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-2 adrenergic receptorHomo sapiens (human)
bone resorptionBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of mini excitatory postsynaptic potentialBeta-2 adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of autophagosome maturationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of lipophagyBeta-2 adrenergic receptorHomo sapiens (human)
cellular response to amyloid-betaBeta-2 adrenergic receptorHomo sapiens (human)
response to psychosocial stressBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cAMP-dependent protein kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of AMPA receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-2 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
amyloid-beta bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta2-adrenergic receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase bindingBeta-2 adrenergic receptorHomo sapiens (human)
potassium channel regulator activityBeta-2 adrenergic receptorHomo sapiens (human)
identical protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-2 adrenergic receptorHomo sapiens (human)
protein-containing complex bindingBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-2 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
nucleusBeta-2 adrenergic receptorHomo sapiens (human)
lysosomeBeta-2 adrenergic receptorHomo sapiens (human)
endosomeBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-2 adrenergic receptorHomo sapiens (human)
Golgi apparatusBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
endosome membraneBeta-2 adrenergic receptorHomo sapiens (human)
membraneBeta-2 adrenergic receptorHomo sapiens (human)
apical plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneBeta-2 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-2 adrenergic receptorHomo sapiens (human)
receptor complexBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (107)

Assay IDTitleYearJournalArticle
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.
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]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
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.
AID624612Specific activity of expressed human recombinant UGT1A92000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID777628Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.
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.
AID298214Partition coefficient, log P of the compound2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Nitric oxide donor beta2-agonists: furoxan derivatives containing the fenoterol moiety and related furazans.
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.
AID624609Specific activity of expressed human recombinant UGT1A62000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID298201Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Nitric oxide donor beta2-agonists: furoxan derivatives containing the fenoterol moiety and related furazans.
AID22293Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID771316Cellular uptake in human HEK293 cells assessed as human OCT2-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
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.
AID1526753Intrinsic clearance in human liver microsomes2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.
AID1772567Apparent permeability of the compound across basolateral side to apical side in dog MDCK-II cells incubated for 150 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-05, Volume: 223Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives.
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
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
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.
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID771314Cellular uptake in human HEK293 cells assessed as human OCT2-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis relative to passive uptake2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID218848Change in Gibb's free energy at Low affinity beta-2-adrenoceptor in the Chang living cells1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Mapping of the beta 2-adrenoceptor on Chang liver cells. Differences between high- and low-affinity receptor states.
AID298212Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction at 100 uM in presence of propranolol2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Nitric oxide donor beta2-agonists: furoxan derivatives containing the fenoterol moiety and related furazans.
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.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' 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]
AID777624Displacement of [3H]-CGP12177 from human recombinant beta2 adrenoceptor expressed in HEK293 cells after 1 hr by scintillation counting analysis2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.
AID1585796Efflux ratio of apparent permeability in human Caco2 cells at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
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]
AID218849Compound was evaluated for change in Gibb's free energy at Low affinity beta2- adrenoceptor in the membranes of bovine skeletal muscle preparation; Not determined1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Mapping of the beta 2-adrenoceptor on Chang liver cells. Differences between high- and low-affinity receptor states.
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.
AID770362Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM2013Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19
β2-Adrenoceptor agonists in the regulation of mitochondrial biogenesis.
AID40848In vitro inhibitory concentration Beta-2 adrenergic receptor in Guinea pig trachea2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Synthesis and preliminary evaluation of (R,R)(S,S) 5-(2-(2-[4-(2-[(18)F]fluoroethoxy)phenyl]-1-methylethylamino)-1-hydroxyethyl)-benzene-1,3-diol ([(18)F]FEFE) for the in vivo visualisation and quantification of the beta2-adrenergic receptor status in lun
AID298211Vasodilating activity against phenylephrine-induced contractions in rat thoracic aorta2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Nitric oxide donor beta2-agonists: furoxan derivatives containing the fenoterol moiety and related furazans.
AID1585792Apparent permeability across apical to basolateral side in human Caco2 cells at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity.
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.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID194554Effect on Oxytocin-Induced contractions of rat uterus at concentrations 50 uM2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
3-Alkylamino-4H-pyrido[2,3-e]-1,2,4-thiadiazine 1,1-dioxides structurally related to diazoxide and pinacidil as potassium channel openers acting on vascular smooth muscle cells: design, synthesis, and pharmacological evaluation.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
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.
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.
AID771317Cellular uptake in human HEK293 cells assessed as human OCT1-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID218847Change in Gibb's free energy at High affinity beta2- adrenoceptor in Chang living cells.1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Mapping of the beta 2-adrenoceptor on Chang liver cells. Differences between high- and low-affinity receptor states.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID624606Specific activity of expressed human recombinant UGT1A12000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID770364Induction of Mitochondrial biogenesis in rabbit RPT cells at 10 to 3000 nM after 24 hrs by FCCP-OCR assay relative to control2013Bioorganic & medicinal chemistry letters, Oct-01, Volume: 23, Issue:19
β2-Adrenoceptor agonists in the regulation of mitochondrial biogenesis.
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.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1772566Apparent permeability of the compound across apical side to basolateral side in dog MDCK-II cells incubated for 150 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-05, Volume: 223Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives.
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.
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.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1585794Apparent permeability across apical to basolateral side in human Caco2 cells assessed as mean drug recovery at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity.
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.
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.
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]
AID298204Antioxidant activity in rat hepatic microsomal membrane2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Nitric oxide donor beta2-agonists: furoxan derivatives containing the fenoterol moiety and related furazans.
AID1585793Apparent permeability across basolateral to apical side in human Caco2 cells at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity.
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1585795Apparent permeability across basolateral to apical side in human Caco2 cells assessed as mean drug recovery at 2 uM after 2 hrs by lucifer yellow dye-based LC-MS/MS analysis2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity.
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]
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.
AID26304Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID771315Cellular uptake in human HEK293 cells assessed as human OCT1-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis relative to passive uptake2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
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.
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.
AID1772568Efflux ratio of apparent permeability in dog MDCK-II cells2021European journal of medicinal chemistry, Nov-05, Volume: 223Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives.
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.
AID194552Effect on Oxytocin-Induced contractions of rat uterus at concentrations 10 uM2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
3-Alkylamino-4H-pyrido[2,3-e]-1,2,4-thiadiazine 1,1-dioxides structurally related to diazoxide and pinacidil as potassium channel openers acting on vascular smooth muscle cells: design, synthesis, and pharmacological evaluation.
AID194553Effect on Oxytocin-Induced contractions of rat uterus at concentrations 100 uM2000Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
3-Alkylamino-4H-pyrido[2,3-e]-1,2,4-thiadiazine 1,1-dioxides structurally related to diazoxide and pinacidil as potassium channel openers acting on vascular smooth muscle cells: design, synthesis, and pharmacological evaluation.
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.
AID298207Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Nitric oxide donor beta2-agonists: furoxan derivatives containing the fenoterol moiety and related furazans.
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.
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]
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.
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.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
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.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID1346250Human beta2-adrenoceptor (Adrenoceptors)2013ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.
AID1508612NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Highly predictive and interpretable models for PAMPA permeability.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,631)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990918 (56.28)18.7374
1990's426 (26.12)18.2507
2000's161 (9.87)29.6817
2010's107 (6.56)24.3611
2020's19 (1.16)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 78.12

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 Index78.12 (24.57)
Research Supply Index7.74 (2.92)
Research Growth Index4.24 (4.65)
Search Engine Demand Index143.25 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (78.12)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials520 (29.12%)5.53%
Reviews60 (3.36%)6.00%
Case Studies61 (3.42%)4.05%
Observational0 (0.00%)0.25%
Other1,145 (64.11%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]