Page last updated: 2024-11-12

trantinterol

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

Description

trantinterol: beta(2)-adrenoceptor agonist, structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9997788
CHEMBL ID5192245
SCHEMBL ID3171464
MeSH IDM0537424

Synonyms (12)

Synonym
trantinterol
SCHEMBL3171464
2-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert-butylaminoethanol hydrochloride
2-(4-amino-3-chloro-5-trifluoromethylphenyl)-2-t-butylaminoethanol hydrochloride
CHEMBL5192245
2-(4-amino-3-chloro-5-(trifluoromethyl)phenyl)-2-(tert-butylamino)ethan-1-ol hydrochloride
tranterol hydrochloride
611234-02-7 (hcl)
2-[4-amino-3-chloro-5-(trifluoromethyl)phenyl]-2-(tert-butylamino)ethanol;hydrochloride
611234-02-7
GLXC-25520
AKOS040749669

Research Excerpts

Overview

Trantinterol is a novel β2-adrenoceptor agonist, currently undergoing clinical trials for the treatment of asthma.

ExcerptReferenceRelevance
"Trantinterol is a novel β2-adrenoceptor agonist, currently undergoing clinical trials for the treatment of asthma. "( An LC-MS/MS method for simultaneous determination of trantinterol and its major metabolite in rat plasma and its application to a comparative pharmacokinetic study.
Fu, X; Ma, C; Qin, F; Wang, Y; Xiong, Z, 2015
)
2.11
"Trantinterol is a novel β(2)-adrenoceptor agonist used for the treatment of asthma. "( In vivo and in vitro metabolism of a novel β2-adrenoceptor agonist, trantinterol: metabolites isolation and identification by LC-MS/MS and NMR.
Guo, X; Jing, L; Li, F; Li, K; Qin, F, 2013
)
2.07

Actions

ExcerptReferenceRelevance
"Trantinterol did not inhibit CYP2C19, CYP2D6, and CYP3A4/5 (IC(50)>100 μM)."( Assessment of a novel β2-adrenoceptor agonist, trantinterol, for interference with human liver cytochrome P450 enzymes activities.
Jiang, K; Li, F; Li, K; Lu, X; Qin, F, 2011
)
1.35

Pharmacokinetics

The method described herein was fully validated and successfully applied for the pharmacokinetic study of trantinterol in healthy volunteers after oral administration. Significant changes in Cmax and AUC were seen in the elderly and may be clinically important.

ExcerptReferenceRelevance
"9 hours, while the tmax of 1-carbonyl trantinterol differed slightly."( Pharmacokinetics of trantinterol and its metabolite in healthy elderly and young subjects.
Huang, J; Huang, Z; Liu, G; Lu, Y; Pei, Q; Tan, H; Yang, G; Yuan, H, 2015
)
1.01
" Significant changes in Cmax and AUC of trantinterol and 1-carbony trantinterol were seen in the elderly and may be clinically important."( Pharmacokinetics of trantinterol and its metabolite in healthy elderly and young subjects.
Huang, J; Huang, Z; Liu, G; Lu, Y; Pei, Q; Tan, H; Yang, G; Yuan, H, 2015
)
1.01
" The method described herein was fully validated and successfully applied for the pharmacokinetic study of trantinterol in healthy volunteers after oral administration."( Quantification of trantinterol, its two metabolites and their primary conjugated metabolites in human plasma by ultra-high-performance liquid chromatography-tandem mass spectrometry and its application to a pharmacokinetic study.
Li, F; Li, K; Qin, F; Wang, L; Xiong, Z; Yin, B, 2016
)
0.98

Bioavailability

ExcerptReferenceRelevance
" In summary, trantinterol is a potent noncompetitive P-gp inhibitor which may increase the bioavailability of other P-gp substrate drugs coadministered with it."( Trantinterol, a novel β2-adrenoceptor agonist, noncompetitively inhibits P-glycoprotein function in vitro and in vivo.
Fan, H; Fawcett, JP; Gu, J; Guo, Y; Liu, J; Ma, W; Sun, Y; Wang, T; Yang, J; Yang, Y; Yang, Z, 2015
)
2.23

Dosage Studied

ExcerptRelevanceReference
"The chiral inversion and pharmacokinetics of two enantiomers of trantinterol, a new β2 agonist, were studied in rats dosed (+)- or (-)-trantinterol separately."( Bidirectional chiral inversion of trantinterol enantiomers after separate doses to rats.
Cheng, M; Jing, L; Li, F; Pan, L; Qin, F; Sun, G; Wang, X, 2013
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Beta-2 adrenergic receptorHomo sapiens (human)EC50 (µMol)0.06090.00000.311110.0000AID1906919
Beta-1 adrenergic receptorHomo sapiens (human)EC50 (µMol)100.00000.00010.49146.0000AID1906920
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (37)

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)
positive regulation of heart rate by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineBeta-1 adrenergic receptorHomo sapiens (human)
diet induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
response to coldBeta-1 adrenergic receptorHomo sapiens (human)
heat generationBeta-1 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-1 adrenergic receptorHomo sapiens (human)
fear responseBeta-1 adrenergic receptorHomo sapiens (human)
regulation of circadian sleep/wake cycle, sleepBeta-1 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-1 adrenergic receptorHomo sapiens (human)
regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-1 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-1 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-1 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

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)
beta-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
beta1-adrenergic receptor activityBeta-1 adrenergic receptorHomo sapiens (human)
protein bindingBeta-1 adrenergic receptorHomo sapiens (human)
PDZ domain bindingBeta-1 adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingBeta-1 adrenergic receptorHomo sapiens (human)
protein heterodimerization activityBeta-1 adrenergic receptorHomo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic membrane potentialBeta-1 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

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)
early endosomeBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
Schaffer collateral - CA1 synapseBeta-1 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-1 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-1 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (69)

Assay IDTitleYearJournalArticle
AID1906924Bronchodilatory activity in rabbit model assessed as inhibition of acetylcholine-induced bronchoconstriction at 3 ug/kg, iv measured after 1 min by Konzett-Roessler methodology relative to control
AID1906983Acute toxicity in ip dosed Kunming mouse assessed as death within 1 hr
AID1906978Acute toxicity in ip dosed Kunming mouse assessed as decrease in activity
AID1906981Acute toxicity in ip dosed Kunming mouse assessed as trembling
AID1906951AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis
AID1906932Antiinflammatory activity in Sprague- Dawley rat model of ovalbumin induced allergic asthma assessed as reduction in histamine release from lung fragments at 10^-2 umol/L administered 5 mins prior to allergen challenge and measured after 10 mins
AID1906921Selectivity ratio of EC50 for beta1 adrenoceptor (unknown orgin) expressed in HEK293 cells to EC50 for human beta2 adrenoceptor (unknown orgin) expressed in HEK293 cells
AID1906984Acute toxicity in Kunming mouse assessed as change in liver morphology
AID1906936Antiinflammatory activity in Sprague- Dawley rat model of ovalbumin induced allergic asthma assessed as reduction in histamine release from lung fragments at 10^-2 umol/L administered 5 mins prior to allergen challenge and measured after 10 mins in presen
AID1906976Acute toxicity in ig dosed Kunming mouse assessed as convulsion after 1 hr
AID1906920Agonist activity at beta1 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
AID1906962Acute toxicity in Kunming mouse assessed as mortality rate at 48 mg/kg, ip
AID1906988Acute toxicity in Kunming mouse assessed as change in kidney morphology
AID1906949Oral bioavailability in Sprague-Dawley rat at 1 mg/kg by LC-MS/MS analysis
AID1906980Acute toxicity in ip dosed Kunming mouse assessed as staggered walking
AID1906968Acute toxicity in Kunming mouse assessed as mortality rate at 35 mg/kg, ip
AID1906961Acute toxicity in Kunming mouse assessed as mortality rate at 56 mg/kg, ip
AID1906982Acute toxicity in ip dosed Kunming mouse assessed as convulsion
AID1906969Acute toxicity in Kunming mouse assessed as mortality rate at 29 mg/kg, ip
AID1906985Acute toxicity in Kunming mouse assessed as change in heart morphology
AID1906943Relaxant activity in guinea pig smooth muscle cells assessed as decrease in intracellular calcium level at 1 umol/L incubated for 5 mins in presence of propranolol by Flura2AM staining based fluorescence assay
AID1906986Acute toxicity in Kunming mouse assessed as change in spleen morphology
AID1906971Acute toxicity in ip dosed Kunming mouse assessed as lethal dose
AID1906931Bronchodilatory activity in rabbit model assessed as inhibition of acetylcholine-induced bronchoconstriction at 1 ug/kg, iv measured after 45 mins by Konzett-Roessler methodology relative to control
AID1906952Half life in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis
AID1906963Acute toxicity in Kunming mouse assessed as mortality rate at 400 mg/kg, po
AID1906941Relaxant activity in guinea pig smooth muscle cells assessed as decrease in intracellular calcium level at 2.5 x 10^-3 umol/L incubated for 5 mins by Flura2AM staining based fluorescence assay
AID1906956AUC (0 to t) in Beagle dog at 0.3 mg/kg, iv by LC-MS/MS analysis
AID1906940Relaxant activity in guinea pig smooth muscle cells assessed as decrease in intracellular calcium level at 5 x 10^-2 umol/L incubated for 5 mins by Flura2AM staining based fluorescence assay
AID1906948Cmax in Sprague-Dawley rat at 1 mg/kg, po by LC-MS/MS analysis
AID1906970Acute toxicity in po dosed Kunming mouse assessed as lethal dose
AID1906933Antiinflammatory activity in Sprague-Dawley rat model of ovalbumin induced allergic asthma assessed as reduction in histamine release from lung fragments at 10^-1 umol/L administered 5 mins prior to allergen challenge and measured after 10 mins
AID1906966Acute toxicity in Kunming mouse assessed as mortality rate at 246 mg/kg, po
AID1906925Bronchodilatory activity in rabbit model assessed as inhibition of acetylcholine-induced bronchoconstriction at 1 ug/kg, iv measured after 1 min by Konzett-Roessler methodology relative to control
AID1906979Acute toxicity in ip dosed Kunming mouse assessed as slow breathing
AID1906919Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
AID1906937Antiinflammatory activity in Sprague- Dawley rat model of ovalbumin induced allergic asthma assessed as reduction in histamine release from lung fragments at 10^-1 umol/L administered 5 mins prior to allergen challenge and measured after 10 mins in presen
AID1906928Bronchodilatory activity in rabbit model assessed as inhibition of acetylcholine-induced bronchoconstriction at 1 ug/kg, iv measured after 30 mins by Konzett-Roessler methodology relative to control
AID1906934Antiinflammatory activity in Sprague- Dawley rat model of ovalbumin induced allergic asthma assessed as reduction in histamine release from lung fragments at 1 umol/L administered 5 mins prior to allergen challenge and measured after 10 mins
AID1906927Bronchodilatory activity in rabbit model assessed as inhibition of acetylcholine-induced bronchoconstriction at 3 ug/kg, iv measured after 30 mins by Konzett-Roessler methodology relative to control
AID1906944Oral bioavailability in Beagle dog at 0.3 mg/kg by LC-MS/MS analysis
AID1906958Cmax in Beagle dog at 0.3 mg/kg, po by LC-MS/MS analysis
AID1906938Antiinflammatory activity in Sprague- Dawley rat model of ovalbumin induced allergic asthma assessed as reduction in histamine release from lung fragments at 1 umol/L administered 5 mins prior to allergen challenge and measured after 10 mins in presence o
AID1906960Acute toxicity in Kunming mouse assessed as mortality rate at 470 mg/kg, po
AID1906974Acute toxicity in ig dosed Kunming mouse assessed as staggered walking after 1 hr
AID1906939Relaxant activity in guinea pig smooth muscle cells assessed as decrease in intracellular calcium level at 1 umol/L incubated for 5 mins by Flura2AM staining based fluorescence assay
AID1906989Bronchodilatory activity in iv dosed rabbit model assessed as inhibition of acetylcholine-induced bronchoconstriction measured after 1 min by Konzett-Roessler methodology relative to control
AID1906950AUC (0 to t) in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis
AID1906957AUC (0 to infinity) in Beagle dog at 0.3 mg/kg, iv by LC-MS/MS analysis
AID1906922Relaxant activity in Hartley guinea pig tracheal strips model of histamine-induced smooth muscle contraction at 8 x 10^-6 mol/L relative to control
AID1906965Acute toxicity in Kunming mouse assessed as mortality rate at 289 mg/kg, po
AID1906954AUC (0 to infinity) in Beagle dog at 0.3 mg/kg, po by LC-MS/MS analysis
AID1906977Acute toxicity in ig dosed Kunming mouse assessed as death within 2 hrs
AID1906973Acute toxicity in ig dosed Kunming mouse assessed as slow breathing after 1 hr
AID1906964Acute toxicity in Kunming mouse assessed as mortality rate at 340 mg/kg, po
AID1906923Bronchodilatory activity in rabbit model assessed as inhibition of acetylcholine-induced bronchoconstriction at 9 ug/kg, iv measured after 1 min by Konzett-Roessler methodology relative to control
AID1906945AUC (0 to t) in Sprague-Dawley rat at 1 mg/kg, po by LC-MS/MS analysis
AID1906946AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/kg, po by LC-MS/MS analysis
AID1906959Half life in Beagle dog at 0.3 mg/kg, iv by LC-MS/MS analysis
AID1906947Half life in Sprague-Dawley rat at 1 mg/kg, po by LC-MS/MS analysis
AID1906929Bronchodilatory activity in rabbit model assessed as inhibition of acetylcholine-induced bronchoconstriction at 9 ug/kg, iv measured after 45 mins by Konzett-Roessler methodology relative to control
AID1906953AUC (0 to t) in Beagle dog at 0.3 mg/kg, po by LC-MS/MS analysis
AID1906930Bronchodilatory activity in rabbit model assessed as inhibition of acetylcholine-induced bronchoconstriction at 3 ug/kg, iv measured after 45 mins by Konzett-Roessler methodology relative to control
AID1906987Acute toxicity in Kunming mouse assessed as change in lung morphology
AID1906955Half life in Beagle dog at 0.3 mg/kg, po by LC-MS/MS analysis
AID1906926Bronchodilatory activity in rabbit model assessed as inhibition of acetylcholine-induced bronchoconstriction at 9 ug/kg, iv measured after 30 mins by Konzett-Roessler methodology relative to control
AID1906975Acute toxicity in ig dosed Kunming mouse assessed as trembling after 1 hr
AID1906972Acute toxicity in ig dosed Kunming mouse assessed as decrease in activity after 1 hr
AID1906967Acute toxicity in Kunming mouse assessed as mortality rate at 41 mg/kg, ip
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (11.11)29.6817
2010's15 (83.33)24.3611
2020's1 (5.56)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.17

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

MetricThis Compound (vs All)
Research Demand Index12.17 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index5.17 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.17)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (5.56%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (94.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]