Page last updated: 2024-11-04

u 78517f

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

Description

U 78517F: iron-catalyzed lipid peroxidation inhibitor; structure given in first source; RN given is for diHCl [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID107656
CHEMBL ID1203324
SCHEMBL ID3092488
MeSH IDM0182195

Synonyms (23)

Synonym
CHEMBL1203324
EU-0101225
2-methyl aminochroman
2h-1-benzopyran-6-ol, 2-((4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl)methyl)-3,4-dihydro-2,5,7,8-tetramethyl-, dihydrochloride
NCGC00094467-01
u 78517f
u78517f
u-83836 dihydrochloride
133681-84-2
U 6007
(-)-2-([4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl)methyl]-3,4-dihydro-2,5,7,8-tetramethyl-2h-1-benzopyran-6-ol dihydrochloride
2-((4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl)methyl)-3,4-dihydro-2,5,7,8-tetramethyl-2h-1-benzopyran-6-ol, dihydrochloride
CCG-207914
SCHEMBL3092488
AKOS025394342
J-004750
sr-01000076188
SR-01000076188-1
2-({4-[2,6-di(pyrrolidin-1-yl)pyrimidin-4-yl]piperazin-1-yl}methyl)-2,5,7,8-tetramethyl-3,4-dihydro-2h-1-benzopyran-6-ol--hydrogen chloride (1/2)
DTXSID40928239
2-[[4-(2,6-dipyrrolidin-1-ylpyrimidin-4-yl)piperazin-1-yl]methyl]-2,5,7,8-tetramethyl-3,4-dihydrochromen-6-ol;dihydrochloride
(-)2-((4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl)methyl)-3,4-dihydro-2,5,7,8-tetramethyl-2h-1-benzopyran-6-ol dihydrochloride
2h-1-benzopyran-6-ol, 2-[[4-(2,6-di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl]methyl]-3,4-dihydro-2,5,7,8-tetramethyl-, hydrochloride (1:2), (2r)-

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The compound U-83836E was unable to modify any toxic effects induced by DXR."( Cardiotoxicity of doxorubicin: effects of 21-aminosteroids.
Berrino, L; Falcone, G; Filippelli, A; Filippelli, W; Mastronardi, P; Mazzarella, B; Rossi, F; Tufano, R, 1998
)
0.3
" Results from this study, which is the first to explore the toxic effects of AT on renal tubular cells, demonstrate that toxic action of AT on kidney cells is partly through an ROS-mediated mechanism."( Role of oxidant stress and antioxidant protection in acephate-induced renal tubular cytotoxicity.
Kanji, VK; Poovala, VS; Salahudeen, AK; Tachikawa, H, 1998
)
0.3
" These data suggest that NAC and U-83836E mitigate the toxic effects of methanol on the antioxidant system of the rat brain."( N-acetylcysteine or trolox derivative mitigate the toxic effects of methanol on the antioxidant system of rat brain.
Farbiszewski, R; Skrzydlewska, E; Witek, A, 2000
)
0.31

Dosage Studied

ExcerptRelevanceReference
" In a separate series of experiments with the same focal ischemia model, identical dosing with U78517F enhanced the postischemic recovery of cortical extracellular calcium without any effect on ischemic or postischemic cortical blood flow."( Nonsteroidal lazaroid U78517F in models of focal and global ischemia.
Braughler, JM; Hall, ED; Jacobsen, EJ; Linseman, KL; Pazara, KE, 1990
)
0.28
" Based upon this preservation of a major Ca(2+) homeostatic mechanism, we have now performed dose-response and therapeutic window analyses of the ability of U-83836E to reduce post-traumatic calpain-mediated cytoskeletal (α-spectrin) proteolysis in ipsilateral cortical homogenates at its 24 h post-TBI peak."( Pharmacological inhibition of lipid peroxidation attenuates calpain-mediated cytoskeletal degradation after traumatic brain injury.
Carrico, KM; Hall, ED; Mustafa, AG; Wang, JA, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (16)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency14.12540.004023.8416100.0000AID485290
Chain A, Ferritin light chainEquus caballus (horse)Potency44.66845.623417.292931.6228AID2323
Chain A, CruzipainTrypanosoma cruziPotency39.81070.002014.677939.8107AID1476
endonuclease IVEscherichia coliPotency50.11870.707912.432431.6228AID1708
Microtubule-associated protein tauHomo sapiens (human)Potency11.22020.180013.557439.8107AID1460
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency35.48130.28189.721235.4813AID2326
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency31.62280.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency3.16230.540617.639296.1227AID2364; AID2528
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency30.131323.934123.934123.9341AID1967
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency7.07950.01789.637444.6684AID588834
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency17.78280.010323.856763.0957AID2662
gemininHomo sapiens (human)Potency11.41160.004611.374133.4983AID463097; AID504364
M-phase phosphoprotein 8Homo sapiens (human)Potency11.22020.177824.735279.4328AID488949
transient receptor potential cation channel subfamily V member 1Homo sapiens (human)Potency11.22020.09120.09120.0912AID488979
lamin isoform A-delta10Homo sapiens (human)Potency17.48820.891312.067628.1838AID1459; AID1487
neuropeptide S receptor isoform AHomo sapiens (human)Potency25.11890.015812.3113615.5000AID1461
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID180509Tested in vitro for the inhibition of iron-dependent lipid peroxidation against rat brain homogenates, by malondialdehyde (MDA) formation assay1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
2-(Aminomethyl)chromans that inhibit iron-dependent lipid peroxidation and protect against central nervous system trauma and ischemia.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID139247Lowest effective dosage in Mouse Head Injury Assay.1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
2-(Aminomethyl)chromans that inhibit iron-dependent lipid peroxidation and protect against central nervous system trauma and ischemia.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID131976Tested in vivo for neuroprotectant activity against mouse head injury(MHI) model.1992Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23
2-(Aminomethyl)chromans that inhibit iron-dependent lipid peroxidation and protect against central nervous system trauma and ischemia.
AID524793Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (116)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's91 (78.45)18.2507
2000's20 (17.24)29.6817
2010's4 (3.45)24.3611
2020's1 (0.86)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 (%)
Trials0 (0.00%)5.53%
Reviews2 (1.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other118 (98.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]