Page last updated: 2024-12-06

toborinone

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

Description

toborinone: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60790
CHEMBL ID116315
CHEBI ID32236
SCHEMBL ID563955
MeSH IDM0208166

Synonyms (32)

Synonym
2(1h)-quinolinone, 6-(3-(((3,4-dimethoxyphenyl)methyl)amino)-2-hydroxypropoxy)-, (+-)-
(+-)-6-(2-hydroxy-3-(veratrylamino)propoxy)carbostyril
toborinone [inn]
ccris 7932
(+-)-6-(3-(((3,4-dimethoxyphenyl)methyl)amino)-2-hydroxypropoxy)-2(1h)-quinolinone
tobonone
opc-18790
toborinone
143343-83-3
toborinone (jan/usan/inn)
D01198
2(1h)-quinolinone, 6-(3-(((3,4-dimethoxyphenyl)methyl)amino)-2-hydroxypropoxy)-
brn 5455092
6-(3-(((3,4-dimethoxyphenyl)methyl)amino)-2-hydroxypropoxy)-2(1h)-quinolinone
torborinone
6-[3-[(3,4-dimethoxyphenyl)methylamino]-2-hydroxypropoxy]-1h-quinolin-2-one
CHEMBL116315
NCGC00183846-01
unii-1u1n0yxm99
1u1n0yxm99 ,
toborinone [usan:inn]
tox21_113290
dtxcid6028739
cas-143343-83-3
dtxsid3048813 ,
toborinone [who-dd]
toborinone [usan]
toborinone [jan]
SCHEMBL563955
128667-95-8
CHEBI:32236
Q27252883

Research Excerpts

Overview

Toborinone is a potent balanced venous and arterial dilator in experimental acute heart failure.

ExcerptReferenceRelevance
"Toborinone is a potent balanced venous and arterial dilator in experimental acute heart failure. "( Acute effects of toborinone on vascular capacitance and conductance in experimental heart failure.
Belenkie, I; Semeniuk, LM; Tyberg, JV, 1998
)
2.08

Pharmacokinetics

ExcerptReferenceRelevance
" No significant differences were observed in mean toborinone pharmacokinetic parameters among the four study groups."( The pharmacokinetics of toborinone in subjects with congestive heart failure and concomitant renal impairment and/or concomitant hepatic impairment.
Bramer, SL; Kitani, M; Miyamoto, G; Tammara, B; Trang, JM, 2002
)
0.87

Bioavailability

ExcerptReferenceRelevance
"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

ExcerptRelevanceReference
" After intravenous dosing of 10 mg/kg [14C]toborinone, fecal and urinary recoveries of the 14C dose were approximately 70% and 26-30%, respectively, in both rats and dogs."( Biotransformation of the novel inotropic agent toborinone (OPC-18790) in rats and dogs. Evidence for the formation of novel glutathione and two cysteine conjugates.
Kitani, M; Matsubara, J; Miyamoto, G; Nagasawa, M; Odomi, M; Uchida, M; Yamada, T, 1997
)
0.82
[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 (1)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency31.62280.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID57666The inotropic effect tested in vitro by using isolated blood-perfused dog heart preparations1992Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
Novel positive inotropic agents: synthesis and biological activities of 6-(3-amino-2-hydroxypropoxy)-2(1H)-quinolinone derivatives.
AID57664The chronotropic effect tested in vitro by using isolated blood-perfused dog heart preparations1992Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
Novel positive inotropic agents: synthesis and biological activities of 6-(3-amino-2-hydroxypropoxy)-2(1H)-quinolinone derivatives.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (37)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's27 (72.97)18.2507
2000's7 (18.92)29.6817
2010's1 (2.70)24.3611
2020's2 (5.41)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (24.32%)5.53%
Reviews3 (8.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other25 (67.57%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]