Page last updated: 2024-11-04

procaterol

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Description

Procaterol is a selective beta2-adrenergic receptor agonist that is used as a bronchodilator for the treatment of asthma and chronic obstructive pulmonary disease (COPD). It was first synthesized in 1976 and has been studied extensively for its pharmacological properties. Procaterol acts by stimulating the beta2-adrenergic receptors in the smooth muscle of the bronchi, leading to relaxation and bronchodilation. This effect helps to improve airflow and reduce symptoms of asthma and COPD. Procaterol is generally well-tolerated, although it can cause side effects such as tremor, headache, and tachycardia. It is important to note that procaterol is not currently marketed in the United States, but it is available in other countries. The research on procaterol continues to explore its potential benefits and risks in the management of respiratory diseases.'

Procaterol: A long-acting beta-2-adrenergic receptor agonist. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4916
CHEMBL ID160519
CHEBI ID91585
SCHEMBL ID4632
MeSH IDM0026203
PubMed CID688561
CHEMBL ID1478530
SCHEMBL ID4633
MeSH IDM0026203

Synonyms (62)

Synonym
AC-13705
pro-air
AKOS005564627
BRD-A22684332-003-02-3
60443-17-6
nsc308904
nsc-308904
BSPBIO_003239
procaterol
KBIO3_002739
SPECTRUM3_001770
SPECTRUM2_001550
SPBIO_001400
gtpl3464
8-hydroxy-5-[1-hydroxy-2-(propan-2-ylamino)butyl]-1h-quinolin-2-one
L023776
72332-33-3
procaterol (inn)
D08424
CHEMBL160519
STK632659
5-[1-hydroxy-2-(propan-2-ylamino)butyl]quinoline-2,8-diol
NCGC00018291-02
NCGC00024381-02
procaterolo
2(1h)-quinolinone, 8-hydroxy-5-(1-hydroxy-2-((1-methylethyl)amino)butyl)-
nsc 308904
8-hydroxy-5-(1-hydroxy-2-((1-methylethyl)amino)butyl)-2(1h)-quinolinone
AKOS015961460
SCHEMBL4632
FKNXQNWAXFXVNW-UHFFFAOYSA-N
5-(1-hydroxy-2-isopropylaminobutyl)-8-hydroxycarbostyril
CHEBI:91585
(r*,s*)-(-)-8-hydroxy-5-(1-hydroxy-2-((1-methylethyl)amino)butyl)-2(1h)-quinolinone
Q27088451
bdbm50493310
BRD-A22684332-003-03-1
8-hydroxy-5-{1-hydroxy-2-[(propan-2-yl)amino]butyl}quinolin-2(1h)-one
DTXSID50860939
AB01275430-01
tocris-1102
NCGC00024999-01
DB01366
NCGC00024999-02
NCGC00018291-01
HMS2089I17
NCGC00024999-03
CHEMBL1478530 ,
cas-72332-33-3
dtxsid5045673 ,
tox21_110941
dtxcid3025673
SCHEMBL4633
tox21_110941_1
NCGC00018291-03
8-hydroxy-5-[(1r,2s)-1-hydroxy-2-[(propan-2-yl)amino]butyl]-1,2-dihydroquinolin-2-one
bdbm50167071
8-hydroxy-5-((1r,2s)-1-hydroxy-2-(isopropylamino)butyl)quinolin-2(1h)-one
Q7247120
procaterol free base
2675401-90-6
EN300-18588546

Research Excerpts

Overview

Procaterol (PCR) is a beta-2-adrenergic bronchodilator widely used in Japanese racehorses for treating lower respiratory disease. Procaterol hydrochloride is a relatively new beta 2-selective agonist with a unique carbostyril nucleus.

ExcerptReferenceRelevance
"Procaterol is a selective and full β"( β
D'Alessandro-Gabazza, CN; Fujimoto, H; Fujisawa, T; Gabazza, EC; Hosoki, K; Kainuma, K; Kobayashi, T; Kuwabara, Y; Nagao, M; Nishihama, K; Toda, M; Yasuma, T, 2017
)
1.18
"Procaterol is a potent β2-agonist frequently used for the management of asthma and chronic obstructive pulmonary disease. "( UGT1A1*28 is associated with greater decrease in serum K⁺ levels following oral intake of procaterol.
Baba, K; Gosho, M; Nishimura, M; Okada, S; Takahashi, A; Tanaka, H; Yamaguchi, E; Yokoe, N, 2015
)
2.08
"Procaterol (PCR) is a beta-2-adrenergic bronchodilator widely used in Japanese racehorses for treating lower respiratory disease. "( Pharmacokinetics of procaterol in thoroughbred horses.
Ishikawa, Y; Kusano, K; Minamijima, Y; Nagata, S; Nomura, M; Toju, K; Yamashita, S, 2016
)
2.2
"Procaterol is a β2-adrenoceptor agonist used as a bronchodilator for the treatment of asthma; it also possesses an anti-inflammatory property. "( Effect of procaterol on Th2-related chemokines production in human monocyte and bronchial epithelial cells.
Chu, YT; Hua, YM; Huang, CH; Hung, CH; Kuo, CH; Lee, MS; Wang, WL, 2010
)
2.21
"Procaterol is a selective β2 agonist, claimed to be more selective than salbutamol."( The efficacy of nebulized procaterol versus nebulized salbutamol for the treatment of moderate acute asthma: a randomized, double-blind, parallel group study.
Louisa, M; Mangunnegoro, H; Novariska, F; Setiawati, A; Wiyono, WH, 2011
)
1.39
"Procaterol hydrochloride is a relatively new beta 2-selective agonist with a unique carbostyril nucleus. "( Inhibition of interferon-gamma production from lymphocytes stimulated with food antigens by a beta 2-agonist, procaterol, in patients with food-sensitive atopic dermatitis.
Fukao, T; Inoue, R; Kaneko, H; Kondo, N; Shinbara, M; Tashita, H; Teramoto, T,
)
1.79
"Procaterol is a potent, orally active beta 2-agonist bronchodilator useful in the treatment of reversible bronchospastic disease. "( Clinical pharmacokinetics of procaterol: dose proportionality after administration of single oral doses.
Blake, DS; Colburn, WA; Coon, MJ; Eldon, MA; Nordblom, GD; Sedman, AJ, 1992
)
2.02
"Procaterol is a new, potent, long-acting beta-2-adrenergic bronchodilator. "( Inhaled procaterol versus salbutamol in bronchial asthma.
Liippo, K; Silvasti, M; Tukiainen, H, 1991
)
2.16
"6 Procaterol appears to be a particularly useful drug for detecting a functional population of beta 2-adrenoceptors in tissues, whether they are the minor or the predominant receptor sub-type present."( Responses to the beta 2-selective agonist procaterol of vascular and atrial preparations with different functional beta-adrenoceptor populations.
O'Donnell, SR; Wanstall, JC, 1985
)
1.09
"Procaterol was found to be an effective, well-tolerated oral bronchodilator with a long duration of action, especially at 0.10 mg twice daily."( A placebo-controlled trial of procaterol: a new long-acting oral beta 2-agonist in bronchial asthma.
Borgen, LA; Brandon, ML; Katz, RM; Rachelefsky, GS; Siegel, SC, 1985
)
1.28
"Procaterol hydrochloride is a new sympathomimetic amine which is highly selective for beta-2 receptors. "( Procaterol metered-dose inhaler in adults with asthma.
Bodman, SF; Nathan, RA; Storms, WW; Wilson, JM, 1985
)
3.15
"Procaterol was found to be an effective drug with a delayed onset of action when administered with food, but no effect on subsequent efficacy or duration of action."( The effect of diet on the efficacy onset and duration of action of procaterol hydrochloride tablets.
Lutz, CN; Spangler, DL; Tinkelman, D, 1987
)
1.23
"Procaterol is a new and effective beta-adrenergic bronchodilator. "( The effect of procaterol treatment on beta-adrenergic bronchodilation and polymorphonuclear leukocyte responsiveness.
Arbabian, M; Borgen, L; Busse, WW; Ruoho, A; Sharpe, G; Smith, A, 1985
)
2.07

Effects

ExcerptReferenceRelevance
"Procaterol has a small but significant inhibitory effect on wheal formation following the intradermal injection of histamine and PAF by an average of 15% (P < .05) and 18% (P < .05) respectively but not against substance P or bradykinin."( Effect of procaterol, a beta 2-adrenoceptor agonist, on skin whealing response caused by inflammatory mediators in asthmatic children.
Arakawa, H; Maeda, S; Morikawa, A; Tokuyama, K, 1995
)
2.14
"Procaterol has a small but significant inhibitory effect on wheal formation following the intradermal injection of histamine and PAF by an average of 15% (P < .05) and 18% (P < .05) respectively but not against substance P or bradykinin."( Effect of procaterol, a beta 2-adrenoceptor agonist, on skin whealing response caused by inflammatory mediators in asthmatic children.
Arakawa, H; Maeda, S; Morikawa, A; Tokuyama, K, 1995
)
2.14

Actions

ExcerptReferenceRelevance
"Procaterol may inhibit rhinovirus infection by reducing ICAM-1 and acidic endosomes as well as modulate airway inflammation in rhinovirus infection."( Procaterol inhibits rhinovirus infection in primary cultures of human tracheal epithelial cells.
Asada, M; Deng, X; Fujiwara, H; Hatachi, Y; Kubo, H; Nagatomi, R; Nakayama, K; Nishimura, H; Sasaki, T; Yamaya, M; Yasuda, H; Yoshida, M, 2011
)
2.53

Treatment

Procaterol treatment reduced (p less than 0.05) the maximal 125I-CYP binding to PMN membranes but only during the initial 2 wk at low dosage. Pretreatment with procaterol (25 - 200 nM) could reduce these effects in a dose-dependent manner.

ExcerptReferenceRelevance
"Procaterol treatment reduced (p less than 0.05) the maximal 125I-CYP binding to PMN membranes but only during the initial 2 wk at low dosage."( The effect of procaterol treatment on beta-adrenergic bronchodilation and polymorphonuclear leukocyte responsiveness.
Arbabian, M; Borgen, L; Busse, WW; Ruoho, A; Sharpe, G; Smith, A, 1985
)
1.35
"Pretreatment with procaterol (25 - 200 nM) could reduce these effects in a dose-dependent manner."( Procaterol but not dexamethasone protects 16HBE cells from H₂O₂-induced oxidative stress.
Deng, Z; Pu, XP; Sun, SY; Sun, Y; Zhao, X; Zhou, JJ, 2014
)
2.17
"Pretreatment with procaterol inhibited the adhesion of eosinophils to NHLF in a concentration-dependent manner, and shifted the concentration-response curve of budesonide to the left. "( Procaterol potentiates the anti-inflammatory activity of budesonide on eosinophil adhesion to lung fibroblasts.
Ikezono, K; Kamata, M; Mori, T; Muraguchi, M; Yoshida, N, 2009
)
2.13

Toxicity

ExcerptReferenceRelevance
" We conclude that frequent inhalation of PRC (up to 500 micrograms/day) via a jet nebulizer provides rapid relief from acute asthmatic attacks, and is safe clinically even in aged asthmatics receiving intravenous steroids."( [Clinical study on benefit and safety of frequent inhalation of aerosolized procaterol hydrochloride in aged acute asthmatics].
Ikeda, K; Nakashima, A; Tsukino, M, 1992
)
0.51
" No adverse effects including significant increase of heart rate were found."( Safety and usefulness of a novel eMotion electric mesh nebulizer in children with asthma.
Adachi, Y; Fuchizawa, T; Itazawa, T; Ito, Y; Miyawaki, T; Murakami, G; Nakabayashi, M; Okabe, Y; Saeki Adachi, Y, 2006
)
0.33

Pharmacokinetics

This study describes the pharmacokinetic profiles of procaterol and its metabolites following the oral administration of Procaterol hydrochloride hydrate 50 µg. The plasma concentration ofprocaterol reached a Cmax of 136.

ExcerptReferenceRelevance
" Mean plasma procaterol concentration-time profiles and pharmacokinetic parameters for both formulations were essentially superimposable."( Clinical pharmacokinetics and relative bioavailability of oral procaterol.
Battle, MM; Colburn, WA; Coon, MJ; Eldon, MA; Nordblom, GD; Sedman, AJ, 1993
)
0.89
" Pharmacodynamic equivalence was accessed using AUC (FEV1)/h and peak FEV1 as indices, and the data were analyzed by analysis of variance (ANOVA)."( Pharmacodynamic study of procaterol hydrochloride dry powder inhaler: evaluation of pharmacodynamic equivalence between procaterol hydrochloride dry powder inhaler and procaterol hydrochloride metered-dose inhaler in asthma patients in a randomized, doubl
Hiura, A; Kawai, M; Miyamoto, T; Nakashima, M; Sakai, A; Sakata, N; Takaori, S,
)
0.43
" Pharmacodynamic equivalence was assessed using AUC (FEV1)/h and peak FEV1 as indices, and the data was analyzed by analysis of variance."( Pharmacodynamic equivalence study of CFC-free and CFC-containing procaterol hydrochloride metered-dose inhalers.
Akamatsu, K; Kawai, M; Miyamoto, T; Nakamura, Y; Nakashima, M; Takaori, S, 2005
)
0.57
" However, a recently established analytical method using LC-MS/MS has been refined to enable the determination of the pharmacokinetic profile of procaterol and its metabolites in humans."( Pharmacokinetic study of the oral administration of procaterol hydrochloride hydrate 50 µg in healthy adult Japanese men.
Endo, K; Funaki, T; Kashiyama, E; Kobayashi, H; Koga, N; Masuda, M; Miyamoto, T; Shibutani, T; Yasuda, Y, 2010
)
0.81
"Following the oral administration of procaterol hydrochloride hydrate 50 µg, the plasma concentration of procaterol reached a Cmax of 136."( Pharmacokinetic study of the oral administration of procaterol hydrochloride hydrate 50 µg in healthy adult Japanese men.
Endo, K; Funaki, T; Kashiyama, E; Kobayashi, H; Koga, N; Masuda, M; Miyamoto, T; Shibutani, T; Yasuda, Y, 2010
)
0.88
"This study describes the pharmacokinetic profiles of procaterol and its metabolites following the oral administration of procaterol hydrochloride hydrate 50 µg."( Pharmacokinetic study of the oral administration of procaterol hydrochloride hydrate 50 µg in healthy adult Japanese men.
Endo, K; Funaki, T; Kashiyama, E; Kobayashi, H; Koga, N; Masuda, M; Miyamoto, T; Shibutani, T; Yasuda, Y, 2010
)
0.86
" Ten asthmatic and ten non-asthmatic subjects underwent two pharmacokinetic trials."( Pharmacokinetics of nebulized and oral procaterol in asthmatic and non-asthmatic subjects in relation to doping analysis.
Backer, V; Hemmersbach, P; Hostrup, M; Krogh, N; Rzeppa, S, 2016
)
0.7

Compound-Compound Interactions

Procaterol combined with budesonide was well tolerated and effective at improving cough symptoms and quality of life.

ExcerptReferenceRelevance
" We evaluated the efficacy and safety of procaterol combined with budesonide for CVA."( Efficacy of procaterol combined with inhaled budesonide for treatment of cough-variant asthma.
Bao, W; Chen, Q; Chen, Z; Lin, Y; Liu, H; Zhao, G; Zhou, X, 2013
)
1.03
"Procaterol combined with budesonide was well tolerated and effective at improving cough symptoms and quality of life in patients with CVA."( Efficacy of procaterol combined with inhaled budesonide for treatment of cough-variant asthma.
Bao, W; Chen, Q; Chen, Z; Lin, Y; Liu, H; Zhao, G; Zhou, X, 2013
)
2.21

Bioavailability

ExcerptReferenceRelevance
"The pharmacokinetics and relative oral bioavailability of procaterol, an orally active beta 2-adrenergic agonist bronchodilator were evaluated in healthy volunteers."( Clinical pharmacokinetics and relative bioavailability of oral procaterol.
Battle, MM; Colburn, WA; Coon, MJ; Eldon, MA; Nordblom, GD; Sedman, AJ, 1993
)
0.77
" These results suggest that the bioavailability of orally administrated PCR in horses is very poor, and the drug was eliminated from the body slowly based on urinary concentrations."( Pharmacokinetics of procaterol in thoroughbred horses.
Ishikawa, Y; Kusano, K; Minamijima, Y; Nagata, S; Nomura, M; Toju, K; Yamashita, S, 2016
)
0.76
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Both doses of procaterol produced significantly greater improvement in PFTs at one hour and for up to seven hours after dosing compared with placebo (p less than 0.03-1 nmol) injected intra-arterially into the AV node artery. The dose-response curve for the positive dromotropic effect ofprocaterol was shifted markedly to the right by approximately 1.5%.

ExcerptRelevanceReference
" Even though the total dosage of inhaled PRC on the 1st day was 496."( [Clinical study on benefit and safety of frequent inhalation of aerosolized procaterol hydrochloride in aged acute asthmatics].
Ikeda, K; Nakashima, A; Tsukino, M, 1992
)
0.51
" Moreover, these agonists caused a shift of the dose-response curve for phenylephrine to the right in a parallel fashion in non-preconstricted preparations."( Vascular alpha-1 antagonistic and agonistic effects of beta adrenoceptor agonists in rabbit common carotid arteries.
Chiba, S; Fujiwara, T, 1992
)
0.28
" Dose-normalized AUC, Cmax, and amount excreted unchanged in urine (Ae) were also similar across dosage levels."( Clinical pharmacokinetics of procaterol: dose proportionality after administration of single oral doses.
Blake, DS; Colburn, WA; Coon, MJ; Eldon, MA; Nordblom, GD; Sedman, AJ, 1992
)
0.57
" dosage regimen."( Evaluation of procaterol and albuterol (salbutamol) aerosol in the treatment of asthma.
Mazza, JA; Reed, CE; Tashkin, DP, 1992
)
0.64
"5 micrograms/kg dosage may, however, be a good starting dose because it assures a reasonable risk/benefit ratio."( Efficacy and duration of action of oral procaterol in asthmatic children after single administration of different dosages.
Boner, AL; Miglioranzi, P; Piacentini, G; Richelli, C; Sette, L; Zanotto, CE, 1990
)
0.55
" Beta adrenergic agonist dose-response curves were obtained in all tissues in the presence and absence of the beta-2 selective antagonist, ICI 118,551."( Further evidence for a homogeneous population of beta-1-adrenoceptors in bovine coronary artery.
Coulombe, PR; Purdy, RE; Stupecky, GL, 1988
)
0.27
" Bronchodilatation was evident 1/2 hr after dosing and peaked at 2 hr."( A placebo-controlled trial of procaterol: a new long-acting oral beta 2-agonist in bronchial asthma.
Borgen, LA; Brandon, ML; Katz, RM; Rachelefsky, GS; Siegel, SC, 1985
)
0.56
" The characteristics of the oral route are easy usage, precise dosage and assured effects."( Oral beta 2-selective adrenergic bronchodilators.
Daniotti, S; Dottorini, M; Grassi, V; Schiassi, M; Tantucci, C, 1986
)
0.27
" The drug has been previously studied in the oral dosage form and has been found to be an effective bronchodilator with a prolonged duration of action."( Procaterol metered-dose inhaler in adults with asthma.
Bodman, SF; Nathan, RA; Storms, WW; Wilson, JM, 1985
)
1.71
" The two active dosage formulations produced a significant EIB inhibitory effect compared with the placebos."( Prevention of exercise-induced bronchospasm in asthmatic children. Effect of aerosol and oral procaterol hydrochloride.
Morooka, T; Nishima, S; Ota, S, 1987
)
0.49
" Despite this, the duration of the bronchodilator effect of procaterol on a twice daily dosage did not seem to be long enough in all patients."( Comparison between oral procaterol and salbutamol in patients with bronchial asthma.
Jaakkola, J; Terho, EO; Torkko, M; Tukiainen, H, 1988
)
0.82
" At each 7 biweekly evaluations, the patient's cumulative bronchodilator dose-response to inhaled isoproterenol (0."( The effect of procaterol treatment on beta-adrenergic bronchodilation and polymorphonuclear leukocyte responsiveness.
Arbabian, M; Borgen, L; Busse, WW; Ruoho, A; Sharpe, G; Smith, A, 1985
)
0.63
" FEV1, pulse rate, and blood pressure were measured at baseline and every two hours after dosing for 12 hours."( Prolonged bronchodilating effect of formoterol versus procaterol in bronchial asthma.
Chetta, A; Del Donno, M; Maiocchi, G; Moretti, D; Olivieri, D; Pisi, G, 1993
)
0.53
" C or D alone shifted dose-response curves to capsaicin (from 10(-7) M to 10(-3) M) to lower concentrations compared with the control, and C+D further shifted them."( Angiotensin-converting enzyme inhibitor and danazol increase sensitivity of cough reflex in female guinea pigs.
Ebihara, T; Nakazawa, H; Ohrui, T; Sasaki, H; Sekizawa, K, 1996
)
0.29
" 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
)
0.55
"A convenient and reliable method to prepare procaterol HCl oral dosage form at an extremely low dosage (25 microg/cap) is presented in this paper."( Production of an extremly low dose procaterol HCl preparation by fluidized-bed coating method: in vitro and in vivo evaluation.
Chen, RR; Gau, CS; Yu, TW, 2006
)
0.87
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
quinolinesA class of aromatic heterocyclic compounds each of which contains a benzene ring ortho fused to carbons 2 and 3 of a pyridine ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency39.81070.177814.390939.8107AID2147
phosphopantetheinyl transferaseBacillus subtilisPotency79.43280.141337.9142100.0000AID1490
GLI family zinc finger 3Homo sapiens (human)Potency19.24320.000714.592883.7951AID1259369; AID1259392
thyroid stimulating hormone receptorHomo sapiens (human)Potency0.01260.001318.074339.8107AID926; AID938
regulator of G-protein signaling 4Homo sapiens (human)Potency23.77810.531815.435837.6858AID504845
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency38.90180.01237.983543.2770AID1645841
retinoid X nuclear receptor alphaHomo sapiens (human)Potency26.83250.000817.505159.3239AID1159527
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency0.04050.001530.607315,848.9004AID1224841; AID1259401
estrogen nuclear receptor alphaHomo sapiens (human)Potency2.68060.000229.305416,493.5996AID743075
cytochrome P450 2D6Homo sapiens (human)Potency21.87610.00108.379861.1304AID1645840
thyroid stimulating hormone receptorHomo sapiens (human)Potency0.00740.001628.015177.1139AID1224843; AID1224895; AID1259393
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency31.62280.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency12.58930.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency12.58930.00636.904339.8107AID883
lamin isoform A-delta10Homo sapiens (human)Potency0.89130.891312.067628.1838AID1487
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency12.58930.00638.235039.8107AID883
[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)
Beta-2 adrenergic receptorHomo sapiens (human)Ki0.03300.00000.66359.5499AID1298705
D(2) dopamine receptorHomo sapiens (human)Ki86.00000.00000.651810.0000AID1298708
[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)Kd0.07940.00000.62888.9130AID770362
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (125)

Processvia Protein(s)Taxonomy
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)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
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)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (32)

Processvia Protein(s)Taxonomy
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)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (53)

Assay IDTitleYearJournalArticle
AID1298708Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells2016Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.
AID1298712Selectivity index, ratio of Ki for human D2S receptor to Ki for human beta2 receptor2016Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.
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.
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.
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.
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.
AID77606Intrinsic activity (n=5) in guinea pig trachea1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
erythro-5-[1-Hydroxy-2-(isopropylamino)butyl]-7-hydroxycarbostyril, a terbutaline-type derivative of the bronchodilator procaterol.
AID1134665Bronchodilatory activity in iv dosed mongrel dog assessed as inhibition of histamine-induced bronchospasm administered 1 min prior to histamine challenge relative to l-isoproterenol1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Isomers of erythro-5-(1-hydroxy-2-isopropylaminobutyl)-8-hydroxycarbostyril, a new bronchodilator.
AID1134666Increase in heart rate in iv dosed anesthetized mongrel dog relative to l-isoproterenol1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Isomers of erythro-5-(1-hydroxy-2-isopropylaminobutyl)-8-hydroxycarbostyril, a new bronchodilator.
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.
AID74042Compound was tested for effective dose required for 25% of maximum response in guinea pig trachea1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
erythro-5-[1-Hydroxy-2-(isopropylamino)butyl]-7-hydroxycarbostyril, a terbutaline-type derivative of the bronchodilator procaterol.
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.
AID1134664Separation ratio of ED25 for increase in heart rate in mongrel dog to ED50 for inhibition of bronchoconstriction in mongrel dog1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Isomers of erythro-5-(1-hydroxy-2-isopropylaminobutyl)-8-hydroxycarbostyril, a new bronchodilator.
AID76656Compound was tested for effective dose required for 50% of maximum response in guinea pig trachea1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
erythro-5-[1-Hydroxy-2-(isopropylamino)butyl]-7-hydroxycarbostyril, a terbutaline-type derivative of the bronchodilator procaterol.
AID1298705Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells2016Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
Structure-guided development of dual β2 adrenergic/dopamine D2 receptor agonists.
AID1134668Increase in heart rate in iv dosed anesthetized mongrel dog1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Isomers of erythro-5-(1-hydroxy-2-isopropylaminobutyl)-8-hydroxycarbostyril, a new bronchodilator.
AID77607Intrinsic activity in guinea pig trachea1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
erythro-5-[1-Hydroxy-2-(isopropylamino)butyl]-7-hydroxycarbostyril, a terbutaline-type derivative of the bronchodilator procaterol.
AID1346250Human beta2-adrenoceptor (Adrenoceptors)2010British journal of pharmacology, Jul, Volume: 160, Issue:5
The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical 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.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (290)

TimeframeStudies, This Drug (%)All Drugs %
pre-199077 (26.55)18.7374
1990's85 (29.31)18.2507
2000's56 (19.31)29.6817
2010's61 (21.03)24.3611
2020's11 (3.79)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 67.37

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 Index67.37 (24.57)
Research Supply Index5.89 (2.92)
Research Growth Index4.49 (4.65)
Search Engine Demand Index115.89 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (67.37)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials62 (20.67%)5.53%
Trials0 (0.00%)5.53%
Reviews5 (1.67%)6.00%
Reviews0 (0.00%)6.00%
Case Studies10 (3.33%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other223 (74.33%)84.16%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (15)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Comparative Study on the Efficacy and Safety of Procaterol vs Salbutamol Given Via Metered Dose Inhaler With Spacer in the Management of Acute Asthma Attack in the Emergency Room [NCT01091337]Phase 496 participants (Actual)Interventional2006-05-31Completed
A Multicentered, Double-blinded, Placebo-Controlled Trial to Evaluate the Efficacy and Safety of Procaterol Hydrochloride With Inhaled Glucocorticoid in Treatment Patients With Cough Variant Asthma (CVA) [NCT01170429]Phase 4160 participants (Anticipated)Interventional2010-07-31Not yet recruiting
The Efficacy of Nebulized Procaterol Versus Nebulized Salbutamol for the Treatment of Moderate Acute Asthma: a Randomized, Double-blind, Parallel Group Study [NCT00990847]Phase 3140 participants (Actual)Interventional2007-06-30Completed
[NCT01076322]Phase 317 participants (Anticipated)Interventional2009-03-31Completed
"Randomized, Single-dose, Three-way Crossover Study to Assess the Bioavailability of Using SYN006 HFA MDI (Budesonide/Procaterol 180/10mcg) vs Pulmicort pMDI (Budesonide 200 μg) and Meptin Air (Procaterol 10mcg) in Healthy Volunteer." [NCT02165046]Phase 124 participants (Actual)Interventional2012-02-29Completed
An Open-Label, Randomized, Cross-Over Study to Evaluate the Dose Response of SYN006 HFA MDI in Asthma Patients [NCT02162784]Phase 239 participants (Actual)Interventional2013-02-28Completed
A Randomized, Single-Dose, Double-Blind, Double-Dummy, Four-Period, Four-Sequence, Four-Treatment, Placebo and Active Controlled, Comparative, Multiple-Center, Crossover-Design, Bronchoprovocation Study to Evaluate the Pharmacodynamic Equivalence of Albut [NCT03528577]Phase 3128 participants (Actual)Interventional2018-09-22Completed
"Multiple-dose Pharmacokinetics and Tolerability of SYN006 HFA MDI (Budesonide 180ug + Procaterol Hydrochloride 10ug/Dose HFA MDI) Administered Orally to Healthy Volunteers" [NCT02165033]Phase 116 participants (Actual)Interventional2012-11-30Completed
A Randomized, Single-dose, Double-blind, Double-dummy, Placebo and Active Controlled, Crossover Design Study Using Bronchoprovocation to Evaluate the Pharmacodynamic Equivalence of the Test and Reference Metered Dose Inhalers (MDIs) Containing Albuterol S [NCT04912596]148 participants (Anticipated)Interventional2022-08-15Recruiting
A Double-blind, Randomized, Placebo-controlled, 5-way Crossover, Multicenter, Single-dose, Dose-ranging Study to Compare the Efficacy and Safety of Albuterol Spiromax® and ProAir® HFA in Adult and Adolescent Subjects Ages 12 and Older With Persistent Asth [NCT01058863]Phase 272 participants (Actual)Interventional2010-02-28Completed
A Randomized Crossover Trial Comparing the Efficacy and Safety of Tiotropium + Procaterol vs. Tiotropium + Placebo in Moderate COPD Patients [NCT00394485]Phase 450 participants (Anticipated)Interventional2006-05-31Terminated(stopped due to Difficulty in recruting patients)
Comparison of the Pharmacodynamic Profile of Test and Reference Metered Dose Inhalers (MDIs) Containing Albuterol Sulfate Using Bronchoprovocation in Adult Patients With Stable Mild Asthma [NCT02584257]Phase 3217 participants (Actual)Interventional2016-04-30Completed
Comparison of the Pharmacokinetic and Pharmacodynamic Profiles of Albuterol Spiromax® and ProAir® HFA in Pediatric Patients With Persistent Asthma [NCT01844401]Phase 115 participants (Actual)Interventional2013-04-30Completed
A Single-Dose, Multicenter, Randomized, Double-Blind, Double-Dummy, Placebo-Controlled, Five-Period Crossover, Dose-Ranging Efficacy and Safety Comparison of Albuterol Spiromax® and ProAir® HFA in Pediatric Patients With Persistent Asthma [NCT01899144]Phase 261 participants (Actual)Interventional2013-07-31Completed
Effect of Oral Procaterol on Chronic Persistent Cough Following Upper Respiratory Tract Infection: Double-Blind Randomized Placebo-Controlled Trial [NCT02349919]74 participants (Anticipated)Interventional2015-03-31Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01058863 (3) [back to overview]Baseline-adjusted Forced Expiratory Volume in 1 Second (FEV1) Area Under the Curve (AUC 0-6)
NCT01058863 (3) [back to overview]Baseline-adjusted Percent-Predicted Forced Expiratory Volume in 1 Second (PPFEV1) Area Under the Curve (AUC 0-6)
NCT01058863 (3) [back to overview]Participants With Treatment-Emergent Adverse Events
NCT01899144 (3) [back to overview]Baseline-Adjusted Area-Under-The- Forced Expiratory Volume In 1 Second (FEV1) Versus Time Curve Over 6 Hours Post-Dose (FEV1 AUC0-6)
NCT01899144 (3) [back to overview]Baseline-Adjusted Area-Under-The-Percent-Predicted Forced Expiratory Volume In 1 Second (FEV1) Versus Time Curve Over 6 Hours Post-Dose
NCT01899144 (3) [back to overview]Participants With Treatment-Emergent Adverse Events
NCT02584257 (1) [back to overview]Post-dose PC20 Concentration After Receiving Differing Doses of Test, Reference, or Placebo
NCT03528577 (1) [back to overview]Pharmacodynamic Endpoint Post-dose PC20

Baseline-adjusted Forced Expiratory Volume in 1 Second (FEV1) Area Under the Curve (AUC 0-6)

"FEV1 AUC 0-6 is the area under the effect-time curve from time 0 (pre-dose) up to 6 hours post-dose. The baseline for each study day was the average of the 2 pre-dose FEV1 measurements on that study day.~The first baseline spirometry was obtained between 6-11 AM. The highest FEV1 value from two acceptable values was captured for calculation of the efficacy endpoints. Assessments were obtained at approximately 0.5 hours and immediately before dosing, and 5 minutes, 0.25, 0.50, 0.75, 1, 2, 3, 4, 5 and 6 hours after completion of dosing." (NCT01058863)
Timeframe: Day 1 up to Day 30

InterventionL*hour (Mean)
Albuterol Spiromax® 90 mcg1.21
Albuterol Spiromax® 180 mcg1.39
ProAir® HFA 90 mcg1.12
ProAir® HFA 180 mcg1.33
Placebo Inhaler0.24

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Baseline-adjusted Percent-Predicted Forced Expiratory Volume in 1 Second (PPFEV1) Area Under the Curve (AUC 0-6)

"Percent-predicted FEV1 AUC 0-6 is the area under the effect-time curve from time 0 (pre-dose) up to 6 hours post-dose. Percent-predicted FEV1 is the expected FEV1 taking into account age, height, gender and race, as per the National Health and Nutrition Examination Survey III (NHANES III) reference values.~The first baseline spirometry was obtained between 6-11 AM. The highest FEV1 value from two acceptable values was captured for calculation of the efficacy endpoints. Assessments were obtained at approximately 0.5 hours and immediately before dosing, and 5 minutes, 0.25, 0.50, 0.75, 1, 2, 3, 4, 5 and 6 hours after completion of dosing." (NCT01058863)
Timeframe: Day 1 up to Day 30

Intervention% predicted * hour (Mean)
Albuterol Spiromax® 90 mcg35.31
Albuterol Spiromax® 180 mcg41.05
ProAir® HFA 90 mcg33.19
ProAir® HFA 180 mcg40.68
Placebo Inhaler7.58

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Participants With Treatment-Emergent Adverse Events

Adverse events (AEs) summarized in this table are those that began or worsened after treatment with study drug (treatment-emergent AEs). An adverse event was defined in the protocol as any untoward medical occurrence that develops or worsens in severity during the conduct of a clinical study and does not necessarily have a causal relationship to the study drug. Relation of AE to treatment was determined by the investigator. Serious AEs include death, a life-threatening adverse event, inpatient hospitalization or prolongation of existing hospitalization, persistent or significant disability or incapacity, a congenital anomaly or birth defect, OR an important medical event that jeopardized the patient and required medical intervention to prevent the previously listed serious outcomes. (NCT01058863)
Timeframe: Day 1 up to Day 37

Interventionparticipants (Number)
Any adverse eventTreatment-related AEWithdrawn from study due to AEsAny serious AEsTreatment-related serious AEOnset treatment for AE: Placebo InhalerOnset treatment for AE: Albuterol Spiromax 90mcgOnset treatment for AE: Albuterol Spiromax 180mcgOnset treatment for AE: ProAir HFA 90 mcgOnset treatment for AE: ProAir HFA 180 mcg
All Randomized Participants9000023302

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Baseline-Adjusted Area-Under-The- Forced Expiratory Volume In 1 Second (FEV1) Versus Time Curve Over 6 Hours Post-Dose (FEV1 AUC0-6)

FEV1 AUC0-6 was calculated using the linear trapezoidal rule, and baseline adjustment was made by subtracting the average of the 2 pre-dose FEV1 values from each post-dose FEV1 determination. (NCT01899144)
Timeframe: Treatment visits 1-5 (approximately days 1, 6, 11, 16, and 21); -35 and -5 minutes prior to dosing and 5 (±2), 15 (±5), 30 (±5), 45 (±5), 60 (±5), 120 (±5), 180 (±5), 240 (±5), 300 (±5), and 360 (±5) minutes after the completion of study drug administrati

InterventionL*hour (Mean)
Albuterol Spiromax 90 mcg0.88
Albuterol Spiromax 180 mcg0.93
ProAir HFA 90 mcg0.74
ProAir HFA 180 mcg0.93
Placebo0.48

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Baseline-Adjusted Area-Under-The-Percent-Predicted Forced Expiratory Volume In 1 Second (FEV1) Versus Time Curve Over 6 Hours Post-Dose

"Percent predicted FEV1: measured FEV1 as a percent of the predicted values for the patients of similar characteristics. Predicted FEV1 values were computed and adjusted for age, height, and gender for patients aged 4-5 years (Eigen et al 2001) and for patients aged 6-11 years (Quanjer et al 1995) using ATS/European Thoracic Society (ERS) criteria applicable to pediatric patients (ATS/ERS 2007).~The percent predicted FEV1 (PPFEV1) area under the curve (AUC)0-6 was calculated using the linear trapezoidal rule, and baseline adjustment was made by subtracting the average of the 2 pre-dose PPFEV1 values from each post-dose PPFEV1 determination." (NCT01899144)
Timeframe: Treatment visits 1-5 (approximately days 1, 6, 11, 16, and 21); -35 and -5 minutes prior to dosing and 5 (±2), 15 (±5), 30 (±5), 45 (±5), 60 (±5), 120 (±5), 180 (±5), 240 (±5), 300 (±5), and 360 (±5) minutes after the completion of study drug administrati

Intervention%predicted FEV1*hour (Mean)
Albuterol Spiromax 90 mcg46.6
Albuterol Spiromax 180 mcg48.0
ProAir HFA 90 mcg37.9
ProAir HFA 180 mcg49.1
Placebo25.4

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Participants With Treatment-Emergent Adverse Events

"Adverse events (AEs) summarized in this table are those that began or worsened after treatment with study drug (treatment-emergent AEs). An adverse event was defined in the protocol as any untoward medical occurrence that develops or worsens in severity during the conduct of a clinical study and does not necessarily have a causal relationship to the study drug. Severity was rated by the investigator as mild (no limitation of usual activities), moderate, or severe (inability to carry out usual activities).~Relation of AE to treatment was determined by the investigator. Serious AEs include death, a life-threatening adverse event, inpatient hospitalization or prolongation of existing hospitalization, persistent or significant disability or incapacity, a congenital anomaly or birth defect, OR an important medical event that jeopardized the patient and required medical intervention to prevent the previously listed serious outcomes." (NCT01899144)
Timeframe: Day 1 up to Day 35

,,,,
Interventionparticipants (Number)
Treatment-related AESevere TEAERelated TEAEDeathSerious AETEAE leading to withdrawal
Albuterol Spiromax 180 mcg200000
Albuterol Spiromax 90 mcg000000
Placebo100000
ProAir HFA 180 mcg100000
ProAir HFA 90 mcg500000

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Post-dose PC20 Concentration After Receiving Differing Doses of Test, Reference, or Placebo

The primary efficacy endpoint was the postdose PC20 following administration of differing doses of albuterol (or placebo) by inhalation. The 20% reduction in FEV1 was determined relative to the saline stage FEV1 measured before albuterol or placebo administration. Additionally, an analysis of superiority to placebo was performed for the T and R products prior to the BE determination. In this study the ITT and PP populations were identical. (NCT02584257)
Timeframe: Post-dose at Visits 2-6 of the study, a total of approximately 4 weeks.

Interventionlog(mg/mL) (Least Squares Mean)
Placebo Dose0.608
90 mcg ProAir HFA3.779
180 mcg ProAir HFA4.432
90 mcg Lupin Albuterol HFA MDI3.928
180 mcg Lupin Albuterol HFA MDI4.481

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Pharmacodynamic Endpoint Post-dose PC20

"The primary pharmacodynamic endpoint is the post-dose PC20, which is the provocative concentration of methacholine challenge agent required to reduce the forced expiry volume in one second (FEV1) by 20%, following the administration of different doses of albuterol (or placebo) by inhalation.~Primary analysis group -pharmacodynamic population." (NCT03528577)
Timeframe: Approximately 15 minutes after last inhalation of study product

Interventionmg/mL (Mean)
Primary Analysis Group114

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