Compounds > fidarestat
Page last updated: 2024-11-07

fidarestat

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Description

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

Cross-References

ID SourceID
PubMed CID160024
CHEMBL ID84446
SCHEMBL ID48827
MeSH IDM0357013

Synonyms (47)

Synonym
sk 860
spiro(4h-1-benzopyran-4,4'-imidazolidine)-2-carboxamide, 6-fluoro-2,3-dihydro-2',5'-dioxo-, (2s-cis)-
(+)-(2s,4s)-6-fluoro-2',5'-dioxospiro(chroman-4,4'-imidazolidine)-2-carboxamide
spiro(4h-1-benzopyran-4,4'-imidazolidine)-2-carboxamide, 2,3-dihydro-2',5'-dioxo-6-fluoro-, (2s-cis)-
(2s,4s)-6-fluoro-2',5'-dioxospiro(3,4-dihydro-2h-1-benzopyran-4,4'-imidazolidine)-2-carboxamide
aldos
snk-860
FID ,
(2s,4s)-2-aminoformyl-6-fluoro-spiro[chroman-4,4'-imidazolidine]-2',5'-dione
fidarestat
DB02021
(s,s)-fidarestat
snk 860
D01842
fidarestat (jan/inn)
aldos (tn)
136087-85-9
NCGC00167477-01
bdbm16512
(2s,4s)-6-fluoro-2'',5''-dioxo-2,3-dihydrospiro[1-benzopyran-4,4''-imidazolidine]-2-carboxamide
chembl84446 ,
(2s,4s)-6-fluoro-2',5'-dioxospiro[2,3-dihydrochromene-4,4'-imidazolidine]-2-carboxamide
dtxcid2026654
dtxsid4046654 ,
tox21_112481
cas-136087-85-9
fidarestat [inn]
unii-8sh8t1164u
8sh8t1164u ,
AKOS016011245
spiro[4h-1-benzopyran-4,4'-imidazolidine]-2-carboxamide,6-fluoro-2,3-dihydro-2',5'-dioxo-, (2s,4s)-
fidarestat [mi]
fidarestat [jan]
SCHEMBL48827
(2s,4s)-6-fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide
J-521366
(2s,4s)-6-fluoro-2',5'-dioxo-2,3-dihydrospiro[chromene-4,4'-imidazolidine]-2-carboxamide
HY-105185
CS-0025231
BCP07501
snk860
((2s,4s)-6-fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide
Q15633938
D86149
(2s,4s)-6-fluoro-2',5'-dioxospiro[chromane-4,4'-imidazolidine]-2-carboxamide
BS160360
AS-84120

Research Excerpts

Overview

Fidarestat is an aldose reductase inhibitor being co-developed by Sanwa Kagaku, NC Curex (a joint venture company created by Japan Energy and Kaken) and Sankyo. It is being developed for the potential treatment of diabetic neuropathy.

ExcerptReferenceRelevance
"Fidarestat is an aldose reductase inhibitor being co-developed by Sanwa Kagaku, NC Curex (a joint venture company created by Japan Energy and Kaken) and Sankyo, for the potential treatment of diabetic neuropathy."( Fidarestat. Sanwa Kagaku/NC Curex/Sankyo.
Giannoukakis, N, 2003)		3.2

Actions

Fidarestat did not cause direct inhibition of PARP activity in a cell-free system containing PARP and NAD(+) but did counteract high-glucose-induced PARP activation in Schwann cells. Fidarest at inhibited the increase with an IC50 value of 18 nmol/l.

ExcerptReferenceRelevance
"Fidarestat did not cause direct inhibition of PARP activity in a cell-free system containing PARP and NAD(+) but did counteract high-glucose-induced PARP activation in Schwann cells."( Aldose reductase inhibition counteracts oxidative-nitrosative stress and poly(ADP-ribose) polymerase activation in tissue sites for diabetes complications.
Hirooka, H; Obrosova, IG; Pacher, P; Stevens, MJ; Szabó, C; Yorek, MA; Zsengeller, Z, 2005)		1.05
"Fidarestat inhibited the increase with an IC50 value of 18 nmol/l."( Pharmacological properties of fidarestat, a potent aldose reductase inhibitor, clarified by using sorbitol in human and rat erythrocytes.
Aoki, T; Makino, M; Mizuno, K; Sassa, H; Sobajima, H; Suzuki, T; Taniko, K, 2001)		1.32

Treatment

Fidarestat pre-treatment to HUVECs restored the Dox-induced decrease in the Nitric Oxide (NO)-levels and eNOS expression. Treatment did not affect diabetes-induced increase in glucose concentrations, but normalized sorbitol and fructose concentrations in sciatic nerve and spinal cord.

ExcerptReferenceRelevance
"Fidarestat pretreatment prevents HG (25 mM)-induced Thp1 monocyte viability."( Aldose Reductase Inhibitor Protects against Hyperglycemic Stress by Activating Nrf2-Dependent Antioxidant Proteins.
Pal, PB; Ramana, KV; Shukla, K; Sonowal, H; Srivastava, SK, 2017)		1.18
"Fidarestat pre-treatment to HUVECs restored the Dox-induced decrease in the Nitric Oxide (NO)-levels and eNOS expression."( Aldose reductase inhibitor, fidarestat prevents doxorubicin-induced endothelial cell death and dysfunction.
Pal, P; Ramana, KV; Saxena, A; Shukla, K; Sonowal, H; Srivastava, SK, 2018)		1.5
"Fidarestat treatment significantly decreased concentrations of sorbitol and fructose in the retinas of STZ-induced diabetic rats. "( Aldose reductase inhibitor fidarestat attenuates leukocyte-endothelial interactions in experimental diabetic rat retina in vivo.
Hattori, T; Matsubara, A; Ogura, Y; Taniguchi, K, 2010)		2.1
"Fidarestat pre-treatment of rats subjected to IR reduced retinal sorbitol concentration to the levels in non-ischemic controls."( Evaluation of the aldose reductase inhibitor fidarestat on ischemia-reperfusion injury in rat retina.
Agardh, CD; Agardh, E; El-Remessy, AB; Maksimchyk, Y; Obrosova, IG; Pacher, P; Smith, ML, 2010)		1.34
"Fidarestat treatment did not affect diabetes-induced increase in glucose concentrations, but normalized sorbitol and fructose concentrations (enzymatic spectrofluorometric assays) as well as 12(S)-hydroxyeicosatetraenoic concentration (ELISA), a measure of 12/15-lipoxygenase activity, in the sciatic nerve and spinal cord."( Interplay of sorbitol pathway of glucose metabolism, 12/15-lipoxygenase, and mitogen-activated protein kinases in the pathogenesis of diabetic peripheral neuropathy.
Hirooka, H; Nadler, JL; Obrosova, IG; Shevalye, H; Stavniichuk, R, 2012)		1.1
"Fidarestat treatment prevented diabetic cataract formation and counteracted retinal nitrosative stress, and poly(ADP-ribose) polymerase activation, as well as glial activation."( Aldose reductase inhibitor fidarestat counteracts diabetes-associated cataract formation, retinal oxidative-nitrosative stress, glial activation, and apoptosis.
Ali, TK; Drel, VR; El-Remessy, AB; Julius, U; Obrosova, IG; Pacher, P; Shin, J, 2008)		1.36
"Treatment with fidarestat significantly prevented the EAU-induced ocular inflammatory changes."( Amelioration of experimental autoimmune uveoretinitis by aldose reductase inhibition in Lewis rats.
Ramana, KV; Shoeb, M; Srivastava, SK; Yadav, UC, 2011)		0.71

Pharmacokinetics

ExcerptReferenceRelevance
"5% of free form of fidarestat may be pharmacologically active and the Cmax for free fidarestat was found to be 80."( Plasma protein binding, pharmacokinetics, tissue distribution and CYP450 biotransformation studies of fidarestat by ultra high performance liquid chromatography-high resolution mass spectrometry.
Banerjee, SK; Bhandi, MM; Borkar, RM; Dubey, AP; Nandekar, PP; Sangamwar, AT; Srinivas, R, 2015)		0.96

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
" In the present study, we investigated the dose-response effect of an aldose reductase (AR) inhibitor, fidarestat, on retinal vascular changes in the retinas of streptozotocin (STZ)-induced diabetic rats."( Long-term treatment with fidarestat suppresses the development of diabetic retinopathy in STZ-induced diabetic rats.
Jomori, T; Kato, N; Nakayama, Y; Suzuki, T; Yashima, S, )		0.65
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[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)
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC50 (µMol)0.03300.00041.877310.0000AID241371; AID34973; AID595556
Aldo-keto reductase family 1 member A1Homo sapiens (human)IC50 (µMol)1.20000.00502.78569.9000AID242590; AID34177
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC50 (µMol)0.01940.00101.191310.0000AID241413; AID242471; AID254820; AID309933; AID322413; AID34655; AID35131
Aldo-keto reductase family 1 member A1Sus scrofa (pig)IC50 (µMol)2.50000.00051.66804.0000AID242609
Aldo-keto reductase family 1 member B1Sus scrofa (pig)IC50 (µMol)2.50000.01500.61352.5000AID254832
[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)
Aldo-keto reductase family 1 member B1Homo sapiens (human)Kd0.01600.00550.01080.0160AID1802839
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (21)

Processvia Protein(s)Taxonomy
lipid metabolic processAldo-keto reductase family 1 member A1Homo sapiens (human)
glucuronate catabolic process to xylulose 5-phosphateAldo-keto reductase family 1 member A1Homo sapiens (human)
L-ascorbic acid biosynthetic processAldo-keto reductase family 1 member A1Homo sapiens (human)
D-glucuronate catabolic processAldo-keto reductase family 1 member A1Homo sapiens (human)
negative regulation of apoptotic processAldo-keto reductase family 1 member A1Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member A1Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member A1Homo sapiens (human)
aldehyde catabolic processAldo-keto reductase family 1 member A1Homo sapiens (human)
cellular detoxification of aldehydeAldo-keto reductase family 1 member A1Homo sapiens (human)
glutathione derivative biosynthetic processAldo-keto reductase family 1 member A1Homo sapiens (human)
retinoid metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
epithelial cell maturationAldo-keto reductase family 1 member B1Homo sapiens (human)
renal water homeostasisAldo-keto reductase family 1 member B1Homo sapiens (human)
carbohydrate metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
C21-steroid hormone biosynthetic processAldo-keto reductase family 1 member B1Homo sapiens (human)
L-ascorbic acid biosynthetic processAldo-keto reductase family 1 member B1Homo sapiens (human)
regulation of urine volumeAldo-keto reductase family 1 member B1Homo sapiens (human)
retinol metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
negative regulation of apoptotic processAldo-keto reductase family 1 member B1Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
fructose biosynthetic processAldo-keto reductase family 1 member B1Homo sapiens (human)
cellular hyperosmotic salinity responseAldo-keto reductase family 1 member B1Homo sapiens (human)
metanephric collecting duct developmentAldo-keto reductase family 1 member B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
all-trans-retinol dehydrogenase (NAD+) activityAldo-keto reductase family 1 member A1Homo sapiens (human)
aldo-keto reductase (NADPH) activityAldo-keto reductase family 1 member A1Homo sapiens (human)
protein bindingAldo-keto reductase family 1 member A1Homo sapiens (human)
allyl-alcohol dehydrogenase activityAldo-keto reductase family 1 member A1Homo sapiens (human)
L-glucuronate reductase activityAldo-keto reductase family 1 member A1Homo sapiens (human)
glucuronolactone reductase activityAldo-keto reductase family 1 member A1Homo sapiens (human)
glycerol dehydrogenase [NADP+] activityAldo-keto reductase family 1 member A1Homo sapiens (human)
S-nitrosoglutathione reductase (NADH) activityAldo-keto reductase family 1 member A1Homo sapiens (human)
S-nitrosoglutathione reductase (NADPH) activityAldo-keto reductase family 1 member A1Homo sapiens (human)
methylglyoxal reductase (NADPH) (acetol producing) activityAldo-keto reductase family 1 member A1Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member A1Homo sapiens (human)
retinal dehydrogenase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member B1Homo sapiens (human)
protein bindingAldo-keto reductase family 1 member B1Homo sapiens (human)
electron transfer activityAldo-keto reductase family 1 member B1Homo sapiens (human)
prostaglandin H2 endoperoxidase reductase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
glyceraldehyde oxidoreductase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
allyl-alcohol dehydrogenase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
L-glucuronate reductase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
glycerol dehydrogenase [NADP+] activityAldo-keto reductase family 1 member B1Homo sapiens (human)
all-trans-retinol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
extracellular spaceAldo-keto reductase family 1 member A1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member A1Homo sapiens (human)
synapseAldo-keto reductase family 1 member A1Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member A1Homo sapiens (human)
apical plasma membraneAldo-keto reductase family 1 member A1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member A1Homo sapiens (human)
extracellular spaceAldo-keto reductase family 1 member B1Homo sapiens (human)
nucleoplasmAldo-keto reductase family 1 member B1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member B1Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member B1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member B1Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (27)

Assay IDTitleYearJournalArticle
AID256543Binding constant against Leu300Pro mutant of aldose reductase at 37.8 uM2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Factorizing selectivity determinants of inhibitor binding toward aldose and aldehyde reductases: structural and thermodynamic properties of the aldose reductase mutant Leu300Pro-fidarestat complex.
AID322412Inhibition of mouse recombinant AKR1C21 at 125 uM2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors.
AID254820Inhibitory concentration against human aldose reductase2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Factorizing selectivity determinants of inhibitor binding toward aldose and aldehyde reductases: structural and thermodynamic properties of the aldose reductase mutant Leu300Pro-fidarestat complex.
AID241413Inhibitory concentration against human ALR22005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Structure of aldehyde reductase holoenzyme in complex with the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity.
AID242590Inhibitory concentration against human ALR1 Aldehyde reductase using DL-glyceraldehyde2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Structure of aldehyde reductase holoenzyme in complex with the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity.
AID595557Inhibition of Wistar rat kidney aldose reductase 1 at 50 uM by spectrophotometric analysis2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Design and synthesis of potent and selective aldose reductase inhibitors based on pyridylthiadiazine scaffold.
AID309933Inhibition of aldose reductase2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Validation of an automated procedure for the prediction of relative free energies of binding on a set of aldose reductase inhibitors.
AID34973Tested for in vitro inhibition activity against rat Aldose reductase (AR)2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography.
AID242609Inhibitory concentration against porcine ALR1 Aldehyde reductase using DL-glyceraldehyde2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Structure of aldehyde reductase holoenzyme in complex with the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity.
AID34655Tested for in vitro inhibition activity against human Aldose reductase (human AR)2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography.
AID541631Inhibition of ALR2 in 5-day STZ-induced diabetic Wistar rat model assessed as normalization of elevated sorbitol levels in sciatic nerves at 100 mg/kg/day, po for 5 days2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Acetic acid derivatives of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide as a novel class of potent aldose reductase inhibitors.
AID541632Inhibition of ALR2 in 5-day STZ-induced diabetic Wistar rat model assessed as blood glucose levels at 100 mg/kg/day, po for 5 days (Rvb = 22.2 +/- 2.62 mmol/L)2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Acetic acid derivatives of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide as a novel class of potent aldose reductase inhibitors.
AID541628Inhibition of Wistar rat lenses ALR2 by spectrophotometry2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Acetic acid derivatives of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide as a novel class of potent aldose reductase inhibitors.
AID254832Inhibitory concentration against porcine aldose reductase2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Factorizing selectivity determinants of inhibitor binding toward aldose and aldehyde reductases: structural and thermodynamic properties of the aldose reductase mutant Leu300Pro-fidarestat complex.
AID1335662Antidiabetic activity in STZ-induced diabetic Sprague-Dawley rat model assessed as aldose reductase activity at 50 uM//kg, po administered for 8 weeks (Rvb = 44.66 +/- 2.7 U)2016European journal of medicinal chemistry, Nov-29, Volume: 124Design and synthesis of chiral 2H-chromene-N-imidazolo-amino acid conjugates as aldose reductase inhibitors.
AID35131Inhibitory activity against aldose reductase enzyme2003Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
Substituted pyrrol-1-ylacetic acids that combine aldose reductase enzyme inhibitory activity and ability to prevent the nonenzymatic irreversible modification of proteins from monosaccharides.
AID34177Tested for in vitro inhibition activity against human aldehyde reductase (AHR)2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography.
AID322413Inhibition of human recombinant aldose reductase2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors.
AID241371Inhibitory concentration against rat ALR2 aldose reductase2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Structure of aldehyde reductase holoenzyme in complex with the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity.
AID595556Inhibition of Wistar rat lens aldose reductase 2 by spectrophotometric analysis2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Design and synthesis of potent and selective aldose reductase inhibitors based on pyridylthiadiazine scaffold.
AID541627Inhibition of Wistar rat kidney ALR1 by spectrophotometry2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Acetic acid derivatives of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide as a novel class of potent aldose reductase inhibitors.
AID242471Binding affinity for human Aldose reductase 2 expressed in Escherichia coli2004Journal of medicinal chemistry, Aug-26, Volume: 47, Issue:18
High-resolution structures of human aldose reductase holoenzyme in complex with stereoisomers of the potent inhibitor Fidarestat: stereospecific interaction between the enzyme and a cyclic imide type inhibitor.
AID254230Binding constant against wild-type human aldose reductase at 18.9 uM2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Factorizing selectivity determinants of inhibitor binding toward aldose and aldehyde reductases: structural and thermodynamic properties of the aldose reductase mutant Leu300Pro-fidarestat complex.
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.
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.
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.
AID1802839SPR Assay from Article 10.1021/acschembio.7b00062: \\Price for Opening the Transient Specificity Pocket in Human Aldose Reductase upon Ligand Binding: Structural, Thermodynamic, Kinetic, and Computational Analysis.\\2017ACS chemical biology, 05-19, Volume: 12, Issue:5
Price for Opening the Transient Specificity Pocket in Human Aldose Reductase upon Ligand Binding: Structural, Thermodynamic, Kinetic, and Computational Analysis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (88)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's10 (11.36)18.2507
2000's40 (45.45)29.6817
2010's35 (39.77)24.3611
2020's3 (3.41)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.82

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

MetricThis Compound (vs All)
Research Demand Index21.82 (24.57)
Research Supply Index4.62 (2.92)
Research Growth Index4.80 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.82)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (3.09%)5.53%
Reviews10 (10.31%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other84 (86.60%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
2,3-diphosphoglycerate
2,3-Diphosphoglycerate: A highly anionic organic phosphate which is present in human red blood cells at about the same molar ratio as hemoglobin. It binds to deoxyhemoglobin but not the oxygenated form, therefore diminishing the oxygen affinity of hemoglobin. This is essential in enabling hemoglobin to unload oxygen in tissue capillaries. It is also an intermediate in the conversion of 3-phosphoglycerate to 2-phosphoglycerate by phosphoglycerate mutase (EC 5.4.2.1). (From Stryer Biochemistry, 4th ed, p160; Enzyme Nomenclature, 1992, p508). 2,3-bisphosphoglyceric acid : A bisphosphoglyceric acid that is glyceric acid carrying two phospho substituents at positions 2 and 3.		1.9810bisphosphoglyceric acid;
tetronic acid derivative		human metabolite
thioctic acid
Thioctic Acid: An octanoic acid bridged with two sulfurs so that it is sometimes also called a pentanoic acid in some naming schemes. It is biosynthesized by cleavage of LINOLEIC ACID and is a coenzyme of oxoglutarate dehydrogenase (KETOGLUTARATE DEHYDROGENASE COMPLEX). It is used in DIETARY SUPPLEMENTS.		2.1110dithiolanes;
heterocyclic fatty acid;
thia fatty acid		fundamental metabolite;
geroprotector
inositol
Inositol: An isomer of glucose that has traditionally been considered to be a B vitamin although it has an uncertain status as a vitamin and a deficiency syndrome has not been identified in man. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1379) Inositol phospholipids are important in signal transduction.. inositol : Any cyclohexane-1,2,3,4,5,6-hexol.. 1D-chiro-inositol : Belonging to the inositol family of compounds, D-chiro-inositol (DCI) is an isomer of glucose. It is an important secondary messenger in insulin signal transduction.. muco-inositol : An inositol that is cyclohexane-1,2,3,4,5,6-hexol having a (1R,2R,3r,4R,5S,6r)-configuration.		4.2941cyclitol;
hexol
phenylacetic acid
phenylacetic acid : A monocarboxylic acid that is toluene in which one of the hydrogens of the methyl group has been replaced by a carboxy group.		2.0310benzenes;
monocarboxylic acid;
phenylacetic acids		allergen;
Aspergillus metabolite;
auxin;
EC 6.4.1.1 (pyruvate carboxylase) inhibitor;
Escherichia coli metabolite;
human metabolite;
plant growth retardant;
plant metabolite;
Saccharomyces cerevisiae metabolite;
toxin
trimethyloxamine
trimethyloxamine: used in manufacture of quaternary ammonium cpds; insect attractant; warming agent for gas; oxidant; structure. trimethylamine N-oxide : A tertiary amine oxide resulting from the oxidation of the amino group of trimethylamine.		2.610tertiary amine oxideEscherichia coli metabolite;
metabolite;
osmolyte
zopolrestat
zopolrestat: structure given in first source		2.7330
flufenamic acid
Flufenamic Acid: An anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically. (From Martindale, The Extra Pharmacopoeia, 30th ed, p16). flufenamic acid : An aromatic amino acid consisting of anthranilic acid carrying an N-(trifluoromethyl)phenyl substituent. An analgesic and anti-inflammatory, it is used in rheumatic disorders.		2.0810aromatic amino acid;
organofluorine compound		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
losartan
Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position		2.9710biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
sb 239063
SB 239063: structure in first source. SB-239063 : A member of the class of imidazoles carrying 4-hydroxycyclohexyl, 4-fluorophenyl and 2-methoxypyrimidin-4-yl substituents at positions 1, 4 and 5 respectively.		2.0210imidazoles
fenofibrate
[no description available]		2.0310benzochromenone;
delta-lactone;
naphtho-alpha-pyrone		platelet aggregation inhibitor;
Sir2 inhibitor
ponalrestat
[no description available]		2.0310phthalazines
fr 74366
[no description available]		3.5220
sorbitol
D-glucitol : The D-enantiomer of glucitol (also known as D-sorbitol).		11.86151glucitolcathartic;
Escherichia coli metabolite;
food humectant;
human metabolite;
laxative;
metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite;
sweetening agent
thymidine
[no description available]		2.9310pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
metabolite;
mouse metabolite
galactose
galactopyranose : The pyranose form of galactose.		3.150D-galactose;
galactopyranose		Escherichia coli metabolite;
mouse metabolite
carbostyril
Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.		2.0210monohydroxyquinoline;
quinolone		bacterial xenobiotic metabolite
tyrosine
Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.		2.7230amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
mannitol
[no description available]		1.9810mannitolallergen;
antiglaucoma drug;
compatible osmolytes;
Escherichia coli metabolite;
food anticaking agent;
food bulking agent;
food humectant;
food stabiliser;
food thickening agent;
hapten;
metabolite;
osmotic diuretic;
sweetening agent
tryptophan
Tryptophan: An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.. tryptophan : An alpha-amino acid that is alanine bearing an indol-3-yl substituent at position 3.		2.0810erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan		antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
acrolein
[no description available]		2.0810enalherbicide;
human xenobiotic metabolite;
toxin
hexanoic acid
hexanoic acid : A C6, straight-chain saturated fatty acid.		2.0310medium-chain fatty acid;
straight-chain saturated fatty acid		human metabolite;
plant metabolite
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		3.110azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		3.1210diazine;
pyrazines		Daphnia magna metabolite
hydantoins
Hydantoins: Compounds based on imidazolidine dione. Some derivatives are ANTICONVULSANTS.. imidazolidine-2,4-dione : An imidazolidinone with oxo groups at position 2 and 4.		1.9810imidazolidine-2,4-dione
thiazolidines
Thiazolidines: Reduced (protonated) form of THIAZOLES. They can be oxidized to THIAZOLIDINEDIONES.		6.2861thiazolidine
oleanolic acid
[no description available]		2.0810hydroxy monocarboxylic acid;
pentacyclic triterpenoid		plant metabolite
galactitol
[no description available]		2.0110hexitolEscherichia coli metabolite;
human metabolite;
metabolite;
mouse metabolite
2-hydroxyphenylacetic acid
2-hydroxyphenylacetic acid: structure. (2-hydroxyphenyl)acetic acid : A hydroxy monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is substituted by a 2-hydroxyphenyl group. It is a metabolite of phenylalanine and is excreted in the urine of patients suffering from diseases like phenylketonuria.		2.0310hydroxy monocarboxylic acid;
phenols		human metabolite;
mouse metabolite
tetradecanoylphorbol acetate
Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.		1.9810acetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester		antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator
transferrin
Transferrin: An iron-binding beta1-globulin that is synthesized in the LIVER and secreted into the blood. It plays a central role in the transport of IRON throughout the circulation. A variety of transferrin isoforms exist in humans, including some that are considered markers for specific disease states.		2.0310
glutamic acid
Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.		2.0310glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
azoxymethane
Azoxymethane: A potent carcinogen and neurotoxic compound. It is particularly effective in inducing colon carcinomas.		2.110
substance p
[no description available]		2.0210peptideneurokinin-1 receptor agonist;
neurotransmitter;
vasodilator agent
6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid
[no description available]		2.0110chromanol;
monocarboxylic acid;
phenols		antioxidant;
ferroptosis inhibitor;
neuroprotective agent;
radical scavenger;
Wnt signalling inhibitor
tolrestat
tolrestat: RN & structure given in first source		4.3960naphthalenesEC 1.1.1.21 (aldehyde reductase) inhibitor
acridine orange
Acridine Orange: A cationic cytochemical stain specific for cell nuclei, especially DNA. It is used as a supravital stain and in fluorescence cytochemistry. It may cause mutations in microorganisms.. acridine orange : Fluorescent dye useful for cell cycle determination. It is cell-permeable, and interacts with DNA and RNA by intercalation or electrostatic attractions respectively.. acridine orange free base : A member of the class of aminoacridines that is acridine carrying two dimethylamino substituents at positions 3 and 6. The hydrochloride salt is the fluorescent dye 'acridine orange', used for cell cycle determination.		2.0510aminoacridines;
aromatic amine;
tertiary amino compound		fluorochrome;
histological dye
deoxyglucose
Deoxyglucose: 2-Deoxy-D-arabino-hexose. An antimetabolite of glucose with antiviral activity.. deoxyglucose : A deoxyhexose comprising glucose having at least one hydroxy group replaced by hydrogen.		2.9310
3-deoxyglucosone
3-deoxyglucosone: RN given refers to (D)-isomer. 3-deoxyglucosone : A deoxyketohexose comprising the open-chain form of D-glucose lacking the -OH group at the 3-position and having the keto group at the 2-position.		2.9310deoxyglucose;
deoxyketohexose
as 3201
ranirestat: an aldose reductase inhibitor; AS-3201 and SX-3202 are the (R-(-))- and (S-(+))-isomers, respectively; structure in first source		3.5320
hydroxyl radical
Hydroxyl Radical: The univalent radical OH. Hydroxyl radical is a potent oxidizing agent.		210oxygen hydride;
oxygen radical;
reactive oxygen species
lidorestat
lidorestat: might prove useful in treating chronic diabetic complications; structure in first source		2.0310
minalrestat
minalrestat: a vasoactive agent		7.9640isoquinolines
3-nitrotyrosine
3-nitrotyrosine: RN given refers to parent cpd without isomeric designation. 3-nitrotyrosine : A nitrotyrosine comprising tyrosine having a nitro group at the 3-position on the phenyl ring.		2.72302-nitrophenols;
C-nitro compound;
nitrotyrosine;
non-proteinogenic alpha-amino acid
sorbinil
sorbinil: aldose reductase inhibitor. sorbinil : An azaspiro compound having a monofluoro-substituted chromane skeleton spiro-linked to an imidazolidinedione ring.		4.83100azaspiro compound;
chromanes;
imidazolidinone;
organofluorine compound;
oxaspiro compound		antioxidant;
EC 1.1.1.21 (aldehyde reductase) inhibitor
leupeptins
Leupeptins: A group of acylated oligopeptides produced by Actinomycetes that function as protease inhibitors. They have been known to inhibit to varying degrees trypsin, plasmin, KALLIKREINS, papain and the cathepsins.		2.0610
epiglucan
epiglucan: a highly side-chain/branched alkali-insoluble cell wall glucan from fungus such as Epicoccum nigrum, Botrytis cinerea, ascomycetes & basidiomycetes; also isolated S-4001 from Lei Wan (polyporus mylitiae), HA-beta-glucan from mushroom Pleutotus ostreatus (Fr.) Quel., and translam from seaweed Laminaria cichorioides; with commercially important functional properties including emulsification and friction reduction.		2.610
resveratrol
trans-resveratrol : A resveratrol in which the double bond has E configuration.		2.110resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
imidazolidines
[no description available]		12.3782azacycloalkane;
imidazolidines;
saturated organic heteromonocyclic parent
benzyloxycarbonylleucyl-leucyl-leucine aldehyde
benzyloxycarbonylleucyl-leucyl-leucine aldehyde: proteasome inhibitor. N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal : A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is protected as its benzyloxycarbonyl derivative.		2.0610amino aldehyde;
carbamate ester;
tripeptide		proteasome inhibitor
stilbenes
Stilbenes: Organic compounds that contain 1,2-diphenylethylene as a functional group.. trans-stilbene : The trans-isomer of stilbene.		2.110stilbene
rhodanine
2-mercaptothiazolinone: metabolite in urine from persons exposed to CS2; structure		6.2861thiazolidinone
epalrestat
epalrestat : A monocarboxylic acid that is 1,3-thiazolidine which is substituted on the nitrogen by a carboxymethyl group, at positions 2 and 4 by thioxo and oxo groups, respectively, and at position 5 by a 2-methyl-3-phenylprop-2-en-1-ylidene group. It is an inhibitor of aldose reductase (which catalyses the conversion of glucose to sorbitol) and is used for the treatment of some diabetic complications, including neuropathy.		6.4171monocarboxylic acid;
thiazolidines		EC 1.1.1.21 (aldehyde reductase) inhibitor
oxazolone
Oxazolone: Immunologic adjuvant and sensitizing agent.		7.610
D-fructopyranose
[no description available]		4.3370cyclic hemiketal;
D-fructose;
fructopyranose		sweetening agent
nadp
[no description available]		7.0810
ovalbumin
Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.		2.0810
idd 594
Idd 594: structure in first source		2.0310
quercetin
[no description available]		2.04107-hydroxyflavonol;
pentahydroxyflavone		antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
dinoprostone
prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.		2.4720prostaglandins Ehuman metabolite;
mouse metabolite;
oxytocic
quercitrin
[no description available]		2.0410alpha-L-rhamnoside;
monosaccharide derivative;
quercetin O-glycoside;
tetrahydroxyflavone		antileishmanial agent;
antioxidant;
EC 1.1.1.184 [carbonyl reductase (NADPH)] inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.14.18.1 (tyrosinase) inhibitor;
plant metabolite
chrysin
chrysin : A dihydroxyflavone in which the two hydroxy groups are located at positions 5 and 7.		2.04107-hydroxyflavonol;
dihydroxyflavone		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
EC 2.7.11.18 (myosin-light-chain kinase) inhibitor;
hepatoprotective agent;
plant metabolite
myricetin
[no description available]		2.04107-hydroxyflavonol;
hexahydroxyflavone		antineoplastic agent;
antioxidant;
cyclooxygenase 1 inhibitor;
food component;
geroprotector;
hypoglycemic agent;
plant metabolite
neuropeptide y
Neuropeptide Y: A 36-amino acid peptide present in many organs and in many sympathetic noradrenergic neurons. It has vasoconstrictor and natriuretic activity and regulates local blood flow, glandular secretion, and smooth muscle activity. The peptide also stimulates feeding and drinking behavior and influences secretion of pituitary hormones.		2.1110
epidermal growth factor
Epidermal Growth Factor: A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.		2.9310
deoxyguanosine
[no description available]		2.4320purine 2'-deoxyribonucleoside;
purines 2'-deoxy-D-ribonucleoside		Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
8-hydroxy-2'-deoxyguanosine
8-Hydroxy-2'-Deoxyguanosine: Common oxidized form of deoxyguanosine in which C-8 position of guanine base has a carbonyl group.. 8-hydroxy-2'-deoxyguanosine : Guanosine substituted at the purine 8-position by a hydroxy group. It is used as a biomarker of oxidative DNA damage.		2.4320guanosinesbiomarker
ConditionIndicatedRelationship StrengthStudiesTrials
Diabetes Mellitus
A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.		03.6230
Alloxan Diabetes
[description not available]		05.71190
Complications of Diabetes Mellitus
[description not available]		02.4720
Cataract, Membranous
[description not available]		03.4270
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.5880
Cataract
Partial or complete opacity on or in the lens or capsule of one or both eyes, impairing vision or causing blindness. The many kinds of cataract are classified by their morphology (size, shape, location) or etiology (cause and time of occurrence). (Dorland, 27th ed)		08.4270
Colitis Gravis
[description not available]		02.610
Colitis, Ulcerative
Inflammation of the COLON that is predominantly confined to the MUCOSA. Its major symptoms include DIARRHEA, rectal BLEEDING, the passage of MUCUS, and ABDOMINAL PAIN.		02.610
Cardiac Toxicity
[description not available]		02.1510
Cancer of Colon
[description not available]		03.4970
Colonic Neoplasms
Tumors or cancer of the COLON.		03.4970
Cardiotoxicity
Damage to the HEART or its function secondary to exposure to toxic substances such as drugs used in CHEMOTHERAPY; IMMUNOTHERAPY; or RADIATION.		02.1510
Hyperglycemia, Postprandial
Abnormally high BLOOD GLUCOSE level after a meal.		02.5820
Hyperglycemia
Abnormally high BLOOD GLUCOSE level.		02.5820
Intestinal Polyps
Discrete abnormal tissue masses that protrude into the lumen of the INTESTINE. A polyp is attached to the intestinal wall either by a stalk, pedunculus, or by a broad base.		07.1710
Chronic Illness
[description not available]		02.0810
Airway Remodeling
The structural changes in the number, mass, size and/or composition of the airway tissues.		02.0810
Asthma, Bronchial
[description not available]		02.4820
Allergic Reaction
[description not available]		02.0810
Innate Inflammatory Response
[description not available]		02.7730
Metaplasia
A condition in which there is a change of one adult cell type to another similar adult cell type.		02.0810
Asthma
A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).		02.4820
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		02.0810
Hypersensitivity
Altered reactivity to an antigen, which can result in pathologic reactions upon subsequent exposure to that particular antigen.		02.0810
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.7730
Diabetic Glomerulosclerosis
[description not available]		04.7940
Diabetic Nephropathies
KIDNEY injuries associated with diabetes mellitus and affecting KIDNEY GLOMERULUS; ARTERIOLES; KIDNEY TUBULES; and the interstitium. Clinical signs include persistent PROTEINURIA, from microalbuminuria progressing to ALBUMINURIA of greater than 300 mg/24 h, leading to reduced GLOMERULAR FILTRATION RATE and END-STAGE RENAL DISEASE.		04.7940
Asymmetric Diabetic Proximal Motor Neuropathy
[description not available]		07.29131
Diabetic Neuropathies
Peripheral, autonomic, and cranial nerve disorders that are associated with DIABETES MELLITUS. These conditions usually result from diabetic microvascular injury involving small blood vessels that supply nerves (VASA NERVORUM). Relatively common conditions which may be associated with diabetic neuropathy include third nerve palsy (see OCULOMOTOR NERVE DISEASES); MONONEUROPATHY; mononeuropathy multiplex; diabetic amyotrophy; a painful POLYNEUROPATHY; autonomic neuropathy; and thoracoabdominal neuropathy. (From Adams et al., Principles of Neurology, 6th ed, p1325)		07.29131
Diabetes Mellitus, Adult-Onset
[description not available]		03.8321
Condition, Preneoplastic
[description not available]		02.110
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		03.8321
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		02.7430
Precancerous Conditions
Pathological conditions that tend eventually to become malignant.		02.110
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.1110
Colorectal Cancer
[description not available]		02.1110
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		02.1110
Nerve Pain
[description not available]		02.9610
Neuralgia
Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.		02.9610
Injury, Ischemia-Reperfusion
[description not available]		02.7430
Reperfusion Injury
Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.		07.7430
Acute Kidney Failure
[description not available]		02.4720
Ischemia
A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION.		02.0510
Necrosis
The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.		02.0510
Acute Kidney Injury
Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.		07.4720
Diabetic Retinopathy
Disease of the RETINA as a complication of DIABETES MELLITUS. It is characterized by the progressive microvascular complications, such as ANEURYSM, interretinal EDEMA, and intraocular PATHOLOGIC NEOVASCULARIZATION.		04.3340
Angiogenesis, Pathologic
[description not available]		02.0610
Invasiveness, Neoplasm
[description not available]		02.0610
Experimental Hepatoma
[description not available]		02.0610
Autoimmune Disease
[description not available]		02.4720
Neuroretinitis
[description not available]		02.0610
Autoimmune Diseases
Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides.		02.4720
Retinitis
Inflammation of the RETINA. It is rarely limited to the retina, but is commonly associated with diseases of the choroid (CHORIORETINITIS) and of the OPTIC DISK (neuroretinitis).		02.0610
Uveitis
Inflammation of part or all of the uvea, the middle (vascular) tunic of the eye, and commonly involving the other tunics (sclera and cornea, and the retina). (Dorland, 27th ed)		02.4720
Hay Fever
[description not available]		02.4820
Rhinitis, Allergic, Seasonal
Allergic rhinitis that occurs at the same time every year. It is characterized by acute CONJUNCTIVITIS with lacrimation and ITCHING, and regarded as an allergic condition triggered by specific ALLERGENS.		02.4820
Inflammatory Response Syndrome, Systemic
[description not available]		02.0710
Systemic Inflammatory Response Syndrome
A systemic inflammatory response to a variety of clinical insults, characterized by two or more of the following conditions: (1) fever		07.0710
Diabetic Angiopathies
VASCULAR DISEASES that are associated with DIABETES MELLITUS.		02.9410
Central Retinal Edema, Cystoid
[description not available]		02.9410
Macular Edema
Fluid accumulation in the outer layer of the MACULA LUTEA that results from intraocular or systemic insults. It may develop in a diffuse pattern where the macula appears thickened or it may acquire the characteristic petaloid appearance referred to as cystoid macular edema. Although macular edema may be associated with various underlying conditions, it is most commonly seen following intraocular surgery, venous occlusive disease, DIABETIC RETINOPATHY, and posterior segment inflammatory disease. (From Survey of Ophthalmology 2004; 49(5) 470-90)		02.9410
Cerebral Infarction, Middle Cerebral Artery
[description not available]		02.0310
Acute Brain Injuries
[description not available]		02.0310
Cerebral Ischemia
[description not available]		02.0310
Brain Injuries
Acute and chronic (see also BRAIN INJURIES, CHRONIC) injuries to the brain, including the cerebral hemispheres, CEREBELLUM, and BRAIN STEM. Clinical manifestations depend on the nature of injury. Diffuse trauma to the brain is frequently associated with DIFFUSE AXONAL INJURY or COMA, POST-TRAUMATIC. Localized injuries may be associated with NEUROBEHAVIORAL MANIFESTATIONS; HEMIPARESIS, or other focal neurologic deficits.		02.0310
Brain Ischemia
Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.		02.0310
Infarction, Middle Cerebral Artery
NECROSIS occurring in the MIDDLE CEREBRAL ARTERY distribution system which brings blood to the entire lateral aspects of each CEREBRAL HEMISPHERE. Clinical signs include impaired cognition; APHASIA; AGRAPHIA; weak and numbness in the face and arms, contralaterally or bilaterally depending on the infarction.		02.0310
Prediabetes
[description not available]		02.0310
Prediabetic State
The time period before the development of symptomatic diabetes. For example, certain risk factors can be observed in subjects who subsequently develop INSULIN RESISTANCE as in type 2 diabetes (DIABETES MELLITUS, TYPE 2).		02.0310
Choked Disk
[description not available]		02.0310
Papilledema
Swelling of the OPTIC DISK, usually in association with increased intracranial pressure, characterized by hyperemia, blurring of the disk margins, microhemorrhages, blind spot enlargement, and engorgement of retinal veins. Chronic papilledema may cause OPTIC ATROPHY and visual loss. (Miller et al., Clinical Neuro-Ophthalmology, 4th ed, p175)		02.0310
Retinal Diseases
Diseases involving the RETINA.		02.0310
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.9140
Autoimmune Diabetes
[description not available]		03.3911
Hypesthesia
Absent or reduced sensitivity to cutaneous stimulation.		03.3911
Ache
[description not available]		03.3911
Dysesthesia
[description not available]		03.3911
Diabetes Mellitus, Type 1
A subtype of DIABETES MELLITUS that is characterized by INSULIN deficiency. It is manifested by the sudden onset of severe HYPERGLYCEMIA, rapid progression to DIABETIC KETOACIDOSIS, and DEATH unless treated with insulin. The disease may occur at any age, but is most common in childhood or adolescence.		03.3911
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		03.3911