Page last updated: 2024-12-05

oxidopamine

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Description

Oxidopamine: A neurotransmitter analogue that depletes noradrenergic stores in nerve endings and induces a reduction of dopamine levels in the brain. Its mechanism of action is related to the production of cytolytic free-radicals. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

oxidopamine : A benzenetriol that is phenethylamine in which the hydrogens at positions 2, 4, and 5 on the phenyl ring are replaced by hydroxy groups. It occurs naturally in human urine, but is also produced as a metabolite of the drug DOPA (used for the treatment of Parkinson's disease). [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]

Cross-References

ID SourceID
PubMed CID4624
CHEMBL ID337702
CHEBI ID78741
SCHEMBL ID37507
MeSH IDM0025343

Synonyms (63)

Synonym
MLS002207128 ,
smr001306725
unii-8hw4ybz748
oxidopaminum
8hw4ybz748 ,
4-13-00-02916 (beilstein handbook reference)
oxidopamina
KBIO1_000362
DIVK1C_000362
NCI60_001890
SPECTRUM_000309
IDI1_000362
hydroxydopamine
oxidopaminum [inn-latin]
oxidopamina [inn-spanish]
einecs 214-842-3
6-hd
ccris 4342
6-hydroxydopamine
2,4,5-trihydroxyphenethylamine
brn 2211011
6-ohda
oxidopamine [usan:inn]
1,2,4-benzenetriol, 5-(2-aminoethyl)-
5-(2-aminoethyl)-1,2,4-benzenetriol
BSPBIO_003486
oxidopamine (usan/inn)
1199-18-4
D05294
5-(2-aminoethyl)benzene-1,2,4-triol
oxidopamine
KBIOSS_000789
KBIO2_005925
KBIOGR_000904
KBIO3_002706
KBIO2_003357
KBIO2_000789
SPECTRUM3_001753
SPECTRUM4_000462
NINDS_000362
SPBIO_001175
SPECTRUM2_001018
NCGC00167769-02
NCGC00167769-01
CHEMBL337702 ,
chebi:78741 ,
KUC106765N
ksc-11-228-9
AKOS006230272
oxidopamine [inn]
oxidopamine [usan]
SCHEMBL37507
topamine
cid_176170
bdbm81264
5-(2-aminoethyl)benzene-1,2,4-triol;hydrobromide
5-(2-azanylethyl)benzene-1,2,4-triol;hydrobromide
AB00053512_09
DTXSID0036768
6-hydroxy-dopamine
SBI-0051469.P003
6-hydroxy dopamine hydrobromide
Q780181

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Accordingly, we tested the ability of both fetal neural (striatum) and fetal non-neural (liver) tissue implants to protect the rat striatum against the toxic effects of a subsequent intrastriatal injection of 6-OHDA."( Sham transplantation protects against 6-hydroxydopamine-induced dopaminergic toxicity in rats: behavioral and morphological evidence.
Cadet, JL; Dollison, A; Fahn, S; Gash, DM; Jackson-Lewis, V; Kostic, V; Levivier, M; Przedborski, S, 1991
)
0.28
" One hundred to 300 microM was toxic for all cell types, and concentrations above 300 microM resulted in fixation."( Toxicity of 6-hydroxydopamine and dopamine for dopaminergic neurons in culture.
Hefti, F; Michel, PP, 1990
)
0.28
" Both substances were found to be more toxic against neuroblastoma cells than against hematopoietic stem cells."( Cytotoxic effects of 6-hydroxydopamine, merocyanine-540 and related compounds on human neuroblastoma and hematopoietic stem cells.
Bruchelt, G; Esterbauer, H; Grygar, G; Niethammer, D; Treuner, J, 1989
)
0.28
" When used adjunctively with oxygen radical generating chemotherapeutic agents in mice, however, WR2721 produces synergistic toxicity rather than attenuation of the toxic effects of such agents."( Mechanisms of synergistic toxicity of the radioprotective agent, WR2721, and 6-hydroxydopamine.
Schor, NF, 1988
)
0.27
"Determination of LD50 values showed 3 human neuroblastoma cell lines to be 2-8-fold more sensitive to 6-hydroxydopamine (6-OHDA) than a mouse sarcoma cell line."( Ascorbic acid enhances the cytotoxic effect of 6-hydroxydopamine for human neuroblastoma cell lines.
Perez-Polo, JR; Reynolds, CP, 1981
)
0.26
" These findings revealed that 6-OHDA is not equally toxic to all midbrain dopaminergic neurons in neonates and that the lateromedial vulnerability pattern shows similarities to those reported in Parkinson's disease."( Lateromedial gradient of the susceptibility of midbrain dopaminergic neurons to neonatal 6-hydroxydopamine toxicity.
Ibata, Y; Okamura, H; Yokoyama, C, 1995
)
0.29
" These data show that 6-OHDA is not equally toxic to all brain DA neurons in neonates, and that all hypothalamic DA neuronal groups resist the toxicity of 6-OHDA, despite their anatomical and functional differences."( Resistance of hypothalamic dopaminergic neurons to neonatal 6-hydroxydopamine toxicity.
Ibata, Y; Okamura, H; Yokoyama, C, 1993
)
0.29
"Altered glial function in the substantia nigra in Parkinson's disease may lead to the release of toxic substances that cause dopaminergic cell death or increase neuronal vulnerability to neurotoxins."( Altered glial function causes neuronal death and increases neuronal susceptibility to 1-methyl-4-phenylpyridinium- and 6-hydroxydopamine-induced toxicity in astrocytic/ventral mesencephalic co-cultures.
Jenner, P; McNaught, KS, 1999
)
0.3
" In this study, we show that the anti-oxidants catalase, glutathione and N-acetyl-cysteine are able to reverse the toxic effects of 6-OHDA."( Extracellular toxicity of 6-hydroxydopamine on PC12 cells.
Benabid, AL; Blum, D; Nissou, MF; Torch, S; Verna, JM, 2000
)
0.31
" Since both H(2)O(2) and 6-OHDA may injure cells via free radical and reactive oxygen species, the neuroprotection seen here may operate via a reversal of such a toxic mechanism."( Vitamin D(3) attenuates 6-hydroxydopamine-induced neurotoxicity in rats.
Borlongan, CV; Chen, HH; Cherng, TL; Hoffer, BJ; Wang, JY; Wang, Y; Wu, JN, 2001
)
0.31
" The safer and effective administration of lower doses of CsA combined with enhanced BBB permeability using Cereport, offers a novel way of producing protective effects in the CNS without the toxic liabilities of high-dose CsA."( Bradykinin receptor agonist facilitates low-dose cyclosporine-A protection against 6-hydroxydopamine neurotoxicity.
Bartus, RT; Borlongan, CV; Emerich, DF; Hoffer, BJ, 2002
)
0.31
" To verify this hypothesis, we investigated the influence of hypothermia on the toxic activity of both neurotoxins."( Apparent opposite effects of tetrabenazine and reserpine on the toxic effects of 1-methyl-4-phenylpyridinium or 6-hydroxydopamine on nigro-striatal dopaminergic neurons.
Cleren, C; Costentin, J; Naudin, B, 2003
)
0.32
" TEMPOL/PNA is also less toxic than TEMPOL in mice, allowing administration of higher doses of antioxidant."( Prevention of catecholaminergic oxidative toxicity by 4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl and its recycling complex with polynitroxylated albumin, TEMPOL/PNA.
Hsia, CJ; Kagan, VE; Ma, L; Nylander, KD; Schor, NF; Tyurin, VA; Weinberg, A; Yan, C, 2004
)
0.32
" Our data indicate that DJ-1 protects dopaminergic neurons from oxidative stress through up-regulation of glutathione synthesis and from the toxic consequences of mutant humanalpha-synuclein through increased expression of heat shock protein 70."( DJ-1 up-regulates glutathione synthesis during oxidative stress and inhibits A53T alpha-synuclein toxicity.
Freed, CR; Zhou, W, 2005
)
0.33
" Parkin is thought to be critical for protecting dopaminergic neurons from toxic insults by targeting misfolded or oxidatively damaged proteins for proteasomal degradation."( Parkin-deficient mice are not more sensitive to 6-hydroxydopamine or methamphetamine neurotoxicity.
Curtis, WR; Palmiter, RD; Perez, FA, 2005
)
0.33
" Mutant (A30P and A53T) alpha-synuclein isoforms cause increased vulnerability of cells towards various toxic insults and enhance dopamine transporter (DAT)-mediated toxicity of the selective dopaminergic neurotoxin and mitochondrial complex I inhibitor MPP(+) in vitro."( Dopamine transporter-mediated cytotoxicity of 6-hydroxydopamine in vitro depends on expression of mutant alpha-synucleins related to Parkinson's disease.
Lehmensiek, V; Lenk, T; Liebau, S; Schwarz, J; Storch, A; Tan, EM; Zettlmeisl, H, 2006
)
0.33
" However, angiotensin increased the toxic effect of 6-hydroxydopamine."( Angiotensin type-1-receptor antagonists reduce 6-hydroxydopamine toxicity for dopaminergic neurons.
Labandeira-Garcia, JL; Lopez-Real, A; Muñoz, A; Rey, P; Sanchez-Iglesias, S; Soto-Otero, R, 2007
)
0.34
" PGE(2), 16-phenyl tetranor PGE(2) (a stable synthetic analogue), and 17-phenyl trinor PGE(2) (an EP1 receptor-selective agonist) were significantly toxic to dopaminergic cells at nanomolar concentrations; EP2- and EP3-selective agonists were not."( PGE(2) receptor EP1 renders dopaminergic neurons selectively vulnerable to low-level oxidative stress and direct PGE(2) neurotoxicity.
Carrasco, E; Casper, D; Werner, P, 2007
)
0.34
" We detected a time-dependent action of quercetin and distinguished an early protective effect from a late toxic one."( Time-dependent protective and harmful effects of quercetin on 6-OHDA-induced toxicity in neuronal SH-SY5Y cells.
Kääräinen, TM; Männistö, PT; Ossola, B; Raasmaja, A, 2008
)
0.35
" The overexpression of GDNF, regardless of the promoter employed, had no obvious adverse effects on astroglia and the engineered cells stably produced and secreted GDNF for extended periods of time (> or =3 weeks)."( Astrocyte-secreted GDNF and glutathione antioxidant system protect neurons against 6OHDA cytotoxicity.
Gangaraju, S; Gardaneh, M; Iwasiow, R; Kiuchi, K; Lanthier, P; Ribecco-Lutkiewicz, M; Sandhu, JK; Sikorska, M; Tremblay, R, 2009
)
0.35
" They also suffer a range of toxic insults, being a chief target of prooxidants such as 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), 1-methyl-4-phenylpyridinium (MPP(+)), 6-hydroxydopamine (6-OHDA), 4-hydroxy-2-nonenal (HNE), and acrolein."( Cruciferous nutraceutical 3H-1,2-dithiole-3-thione protects human primary astrocytes against neurocytotoxicity elicited by MPTP, MPP(+), 6-OHDA, HNE and acrolein.
Jia, Z; Li, Y; Misra, HP; Zhu, H, 2009
)
0.35
" It is, therefore, suggested that the use of long-term l-DOPA therapy with isoquinoline derivatives including berberine may need to be examined for the presence of adverse symptoms."( Effects of berberine on 6-hydroxydopamine-induced neurotoxicity in PC12 cells and a rat model of Parkinson's disease.
Choi, HS; Hwang, BY; Kwon, IH; Lee, BK; Lee, CK; Lee, MK; Lim, SC; Shin, KS, 2010
)
0.36
" In this work we investigated the effect that a systemic administration of L-KYN+PROB exerted on the toxic model induced by 6-OHDA in rats."( Protective effect of L-kynurenine and probenecid on 6-hydroxydopamine-induced striatal toxicity in rats: implications of modulating kynurenate as a protective strategy.
Carrillo-Mora, P; Colín-Barenque, L; García, E; González-Herrera, IG; Pedraza-Chaverrí, J; Pérez-De La Cruz, V; Santamaría, A; Silva-Adaya, D; Villeda-Hernández, J,
)
0.13
" In the rat striatum, the SAC-induced activation of Nrf2 is likely to contribute to inhibit the toxic effects of 6-OHDA evidenced by phase 2 antioxidant enzymes up-regulation, glutathione recovery, and attenuation of reactive oxygen species (ROS), nitric oxide (NO), and lipid peroxides formation."( RETRACTED: S-allyl cysteine protects against 6-hydroxydopamine-induced neurotoxicity in the rat striatum: involvement of Nrf2 transcription factor activation and modulation of signaling kinase cascades.
Ali, SF; Cuadrado, A; Cuevas, E; González-Trujano, ME; Macías-Silva, M; Maldonado, PD; Pedraza-Chaverrí, J; Santamaría, A; Tobón-Velasco, JC; Vázquez-Victorio, G, 2012
)
0.38
" Both SOD and CAT have been shown to protect against the toxic effects caused by 6-OHDA on mitochondrial respiration."( Differential toxicity of 6-hydroxydopamine in SH-SY5Y human neuroblastoma cells and rat brain mitochondria: protective role of catalase and superoxide dismutase.
Hikima, A; Iglesias-González, J; Jenner, P; Méndez-Álvarez, E; Rose, S; Sánchez-Iglesias, S; Soto-Otero, R, 2012
)
0.38
" Furthermore, MDMA and MDMA-analogs have shown to have induced several adverse effects."( Elucidating the neurotoxic effects of MDMA and its analogs.
Ahuja, M; Bhattacharya, D; Clark, R; Deruiter, J; Dhanasekaran, M; Karuppagounder, SS; Suppiramaniam, V, 2014
)
0.4
" In both rodents and nonhuman primates, we observed successful engraftment and higher dopamine levels in hpNSC-transplanted animals compared to vehicle control animals, without any adverse events."( Proof of concept studies exploring the safety and functional activity of human parthenogenetic-derived neural stem cells for the treatment of Parkinson's disease.
Abramihina, T; Crain, A; Elsworth, JD; Garitaonandia, I; Gonzalez, R; Jiang, C; Laurent, LC; Morey, R; Noskov, A; Poustovoitov, M; Redmond, DE; Semechkin, R; Snyder, EY, 2015
)
0.42
" One of the hallmarks of the disease is the toxic accumulation of proteins within susceptible neurons due to major impairment in the degradation/clearance protein systems."( Loss of NEDD4 contributes to RTP801 elevation and neuron toxicity: implications for Parkinson's disease.
Alberch, J; Altas, B; Canal, M; Kawabe, H; Malagelada, C; Man, HY; Martín-Flores, N; Pérez-Sisqués, L; Romaní-Aumedes, J, 2016
)
0.43
" Importantly, CVL-751 efficacy is observed with less of the concomitant dyskinesia side effect associated with L-DOPA treatment."( D1 Agonist Improved Movement of Parkinsonian Nonhuman Primates with Limited Dyskinesia Side Effects.
Brevard, J; Fonseca, KR; Gray, DL; Kozak, R; Popiolek, M; Trapa, P; Young, D, 2020
)
0.56
" Oxidative stress is regarded as an important starting factor for neuronal cell loss and necrosis, is one of the causes of Parkinson's disease (PD), and is considered to be the cause of adverse reactions caused by the current PD commonly used treatment drug levodopa (l-DA)."( Fucoxanthin Prevents Long-Term Administration l-DOPA-Induced Neurotoxicity through the ERK/JNK-c-Jun System in 6-OHDA-Lesioned Mice and PC12 Cells.
Chen, H; Chen, J; Chen, S; Li, Q; Liu, J; Lu, Y; Shao, F; Tang, M; Wu, W; Xu, Z; Yang, D; Zhai, L, 2022
)
0.72
"Extracellular vesicles (EVs) play a crucial role in intercellular communication, participating in the paracrine trophic support or in the propagation of toxic molecules, including proteins."( RTP801 mediates transneuronal toxicity in culture via extracellular vesicles.
Alberch, J; Campoy-Campos, G; Chicote-González, A; Fernández-Irigoyen, J; Garcia-Segura, P; Malagelada, C; Martín-Flores, N; Pérez-Navarro, E; Pérez-Sisqués, L; Santamaría, E; Solana-Balaguer, J, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" In this study, we performed pharmacokinetic and pharmacodynamic (PK/PD) analyses of the antiparkinsonian effect of bromocriptine and evaluated drug-induced contralateral rotations in rats in which unilateral striatal lesions had been generated by microinjection of 6-hydroxydopamine (6-OHDA) into the medial forebrain bundle."( Pharmacokinetic and pharmacodynamic analyses, based on dopamine D2-receptor occupancy of bromocriptine, of bromocriptine-induced contralateral rotations in unilaterally 6-OHDA-lesioned rats.
Atsumi, M; Iga, T; Kawakami, J; Kotaki, H; Sato, H; Sawada, Y; Sugiyama, E; Yamada, Y, 2003
)
0.32
" Moreover, in this case a classical pharmacokinetic-pharmacodynamic relationship based on free brain concentrations seems to be less appropriate than target engagement pharmacodynamic readouts."( Effects of sarizotan in animal models of ADHD: challenging pharmacokinetic-pharmacodynamic relationships.
Bizot, JC; Brown, RW; Danysz, W; Dimpfel, W; Flik, G; Greco, S; Jatzke, CC; Jenssen, AK; Kostrzewa, R; McCreary, A; Parsons, CG; Tober, C, 2015
)
0.42

Compound-Compound Interactions

ExcerptReferenceRelevance
"Adrenal demedullation combined with chemical sympathectomy with 6-hydroxydopamine (ACS) lowered plasma glucagon and insulin levels in rats."( Effects of adrenal demedullation combined with chemical sympathectomy on cold-induced responses of endocrine pancreas in rats.
Habara, Y; Kuroshima, A; Ohno, T; Yahata, T, 1983
)
0.27
" The nicotinic agonists were given acutely and repeatedly either alone or in combination with a dopamine uptake inhibitor, nomifensine."( Comparison of the effects of nicotine and epibatidine given in combination with nomifensine on rotational behaviour in rats.
Ahtee, L; Janhunen, S; Tuominen, RK, 2005
)
0.33
" VU0364770 showed efficacy alone or when administered in combination with L-DOPA or an adenosine 2A (A2A) receptor antagonist currently in clinical development (preladenant)."( The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with L-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's disease.
Amalric, M; Blobaum, AL; Bode, J; Bridges, TM; Bubser, M; Conn, PJ; Daniels, JS; Dickerson, JW; Engers, DW; Hopkins, CR; Italiano, K; Jadhav, S; Jones, CK; Lindsley, CW; Morrison, RD; Niswender, CM; Thompson, AD; Turle-Lorenzo, N, 2012
)
0.38
" In a marmoset model of Parkinson's disease, which was generated by unilateral injections of 6-hydroxydopamine (6-OHDA) into the nigro-striatal projection pathway, complete loss of striatal DAT binding in combination with behavioral deficits was observed."( Visualizing dopamine transporter integrity with iodine-123-FP-CIT SPECT in combination with high resolution MRI in the brain of the common marmoset monkey.
Czéh, B; Fuchs, E; Garea-Rodríguez, E; Heckmann, C; Helms, G; König, J; Meller, B; Meller, J; Schlumbohm, C, 2012
)
0.38
" Curcumin (CMN) in combination with bioenhancer piperine (PP) in 6-hydroxydopamine-induced Parkinsonian rats was used to investigate the antioxidant, neuromodulatory and neuroprotective mechanisms."( Neuroprotective potential of curcumin in combination with piperine against 6-hydroxy dopamine induced motor deficit and neurochemical alterations in rats.
Kumar, P; Singh, S, 2017
)
0.46
" Summarizing, our findings substantiate that antagonization of the Nogo-receptor 1 promotes dopaminergic neurons but does not further increase the yield of dopaminergic neurons and their morphological complexity when combined with neurotrophin-4/5 hinting to the idea that these treatments might exert their effects by activating common downstream pathways."( Nogo-receptor 1 antagonization in combination with neurotrophin-4/5 is not superior to single factor treatment in promoting survival and morphological complexity of cultured dopaminergic neurons.
Andereggen, L; Di Santo, S; Sahli, S; Seiler, S; Widmer, HR, 2017
)
0.46
" Quercetin (QC) in combination with piperine (bioenhancer) acts as potential antioxidant, anti-inflammatory and neuroprotective against 6-OHDA rat model of PD."( Piperine in combination with quercetin halt 6-OHDA induced neurodegeneration in experimental rats: Biochemical and neurochemical evidences.
Kumar, P; Singh, S, 2018
)
0.48
" Therefore, we evaluated the effect of mangiferin alone and in combination with nNOS inhibitor 7-nitro-indazole (7-NI) in 6-OHDA lesioned rats."( Effects of mangiferin and its combination with nNOS inhibitor 7-nitro-indazole (7-NI) in 6-hydroxydopamine (6-OHDA) lesioned Parkinson's disease rats.
Chaudhary, MJ; Nath, R; Pal, R; Tiwari, PC, 2022
)
0.72
"NSCs transplantation combined with ethyl stearate ameliorated the behavioral deficits of PD rats."( Neural stem cells transplantation combined with ethyl stearate improve PD rats motor behavior by promoting NSCs migration and differentiation.
Chen, D; Huang, J; Li, C; Li, H; Li, X; Yang, X; Ye, S; Yi, L; Zheng, Q; Zhong, J, 2023
)
0.91
"These findings suggest that NSCs transplantation combined with ethyl stearate can improve the motor behavioral performance of PD rats by promoting NSCs migration from the striatum to the substantia nigra via CCL5/CCR5 and promoting the differentiation of NSCs into dopaminergic neurons."( Neural stem cells transplantation combined with ethyl stearate improve PD rats motor behavior by promoting NSCs migration and differentiation.
Chen, D; Huang, J; Li, C; Li, H; Li, X; Yang, X; Ye, S; Yi, L; Zheng, Q; Zhong, J, 2023
)
0.91

Bioavailability

ExcerptReferenceRelevance
" Since this occurred following direct administration of l-DOPA into the striatum, the decrease could not be accounted for by peripheral pharmacodynamics or bioavailability of l-DOPA in the striatum."( Effects of repeated administration of l-DOPA and apomorphine on circling behavior and striatal dopamine formation.
Brannan, T; Prikhojan, A; Yahr, MD, 1998
)
0.3
" These results are consistent with previous work highlighting the importance of aberrant amine production in neurological disease and demonstrate that treatments that reduce endogenous melatonin bioavailability can ameliorate experimental PD."( A therapeutic role for melatonin antagonism in experimental models of Parkinson's disease.
Armstrong, SM; Willis, GL, 1999
)
0.3
"Neuroprotective effects of a natural antioxidant tangeretin, a citrus flavonoid, were elucidated in the 6-hydroxydopamine (6-OHDA) lesion rat model of Parkinson's disease (PD), after bioavailability studies."( Tissue distribution and neuroprotective effects of citrus flavonoid tangeretin in a rat model of Parkinson's disease.
Christidou, M; Datla, KP; Dexter, DT; Rooprai, HK; Widmer, WW, 2001
)
0.31
" Catechol-O-methyltransferase (COMT) inhibitors increase the half-life and bioavailability of levodopa, providing more continuous dopamine receptor stimulation."( Early administration of entacapone prevents levodopa-induced motor fluctuations in hemiparkinsonian rats.
Aguilar, E; Bonastre, M; Marin, C; Obeso, JA; Tolosa, E, 2005
)
0.33
" Individual differences in the central bioavailability of L-DOPA may provide a clue to the varying susceptibility to dyskinesia in Parkinson's disease."( Role of striatal L-DOPA in the production of dyskinesia in 6-hydroxydopamine lesioned rats.
Carta, M; Cenci, MA; Fadda, F; Lindgren, HS; Lundblad, M; Stancampiano, R, 2006
)
0.33
" Enhanced bioavailability may thus be a major factor contributing to the neuroprotective activity of pinostilbene."( Protective effects of pinostilbene, a resveratrol methylated derivative, against 6-hydroxydopamine-induced neurotoxicity in SH-SY5Y cells.
Chang, RC; Chao, J; Cheng, KW; Li, H; Wang, M; Yu, MS, 2010
)
0.36
" However, the stability and bioavailability of EGCG are restricted."( A pro-drug of the green tea polyphenol (-)-epigallocatechin-3-gallate (EGCG) prevents differentiated SH-SY5Y cells from toxicity induced by 6-hydroxydopamine.
Chan, TH; Chang, RC; Chao, J; Ho, YS; Huie, MJ; Lai, CS; Lam, WH; Lau, WK; Wang, M; Yu, MS; Yuen, WH, 2010
)
0.36
" Small molecules with neurotrophic actions that are easy to synthesize and modify to improve bioavailability are needed."( Dopamine neuron stimulating actions of a GDNF propeptide.
Ai, Y; Bradley, LH; Fuqua, J; Gash, DM; Gerhardt, GA; Glass, JD; Grondin, R; He, X; Huettl, P; Kelps, KA; Littrell, OM; Pomerleau, F; Richardson, A; Turchan-Cholewo, J; Zhang, Z, 2010
)
0.36
" MRZ-8676 (6,6-dimethyl-2-phenylethynyl-7,8-dihydro-6H-quinolin-5-one) is a novel proprietary, selective, orally bioavailable mGluR5 NAM."( Pharmacological characterization of MRZ-8676, a novel negative allosteric modulator of subtype 5 metabotropic glutamate receptors (mGluR5): focus on L: -DOPA-induced dyskinesia.
Danysz, W; Dekundy, A; Gravius, A; Hechenberger, M; Mela, F; Nagel, J; Parsons, CG; Pietraszek, M; Tober, C; van der Elst, M, 2011
)
0.37
" The enhanced stability and bioavailability of PEGylated rhFGF-2 make this molecule a great therapeutic candidate for neurodegenerative diseases such as PD and mood disorders."( PEGylated rhFGF-2 conveys long-term neuroprotection and improves neuronal function in a rat model of Parkinson's disease.
Chen, G; Feng, J; Feng, W; Huang, Z; Niu, J; Shi, L; Wang, Y; Ye, C; Zhu, G, 2015
)
0.42
" The water solubility and improved bioavailability may help reduce medication frequency associated with l-DOPA treatment of PD."( DopAmide: Novel, Water-Soluble, Slow-Release l-dihydroxyphenylalanine (l-DOPA) Precursor Moderates l-DOPA Conversion to Dopamine and Generates a Sustained Level of Dopamine at Dopaminergic Neurons.
Atlas, D, 2016
)
0.43
" Bioavailability studies also suggest the contribution of SFN metabolites, including erucin (ERN), to the neuroprotective effects of SFN."( Comparison of Adaptive Neuroprotective Mechanisms of Sulforaphane and its Interconversion Product Erucin in in Vitro and in Vivo Models of Parkinson's Disease.
Cantelli-Forti, G; D'Amico, M; Djemil, A; Hrelia, P; Morroni, F; Pruccoli, L; Sita, G; Tarozzi, A, 2018
)
0.48
" We also examined the bioavailability and behavioral improvement in a 6-hydroxydopamine-lesioned rat model of PD following 2 weeks' FUS-liposomal combinatorial treatment."( Efficient treatment of Parkinson's disease using ultrasonography-guided rhFGF20 proteoliposomes.
Guo, K; Huang, Z; Li, X; Niu, J; Song, L; Xia, F; Xie, J; Zhang, X; Zhao, X; Zhao, Y; Zhuge, D, 2018
)
0.48
"Methylphenidate (MPD) is a psychostimulant used for the treatment of ADHD and works by increasing the bioavailability of dopamine (DA) in the brain."( Acute and chronic methylphenidate administration in intact and VTA-specific and nonspecific lesioned rats.
Dafny, N; Ihezie, SA; Thomas, MM, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" A cicletanine concentration, which is attained by the dosage given to patients, is sufficient to produce these effects."( Potassium channel activation in vascular smooth muscle.
Emden, J; Mironneau, J; Siegel, G; Stock, G; Wenzel, K, 1992
)
0.28
" There was no change in dopamine-sensitive adenylate cyclase activity in the striata of supersensitive IC-lesioned rats, but there was a shift to the left in the dose-response curve in striata from rats bilaterally-lesioned in the substantia nigra, similar to what occurs in UNI lesioned rats."( Dopamine receptor 'supersensitivity' occurring without receptor up-regulation.
Lewis, MH; Mailman, RB; Mileson, BE, 1991
)
0.28
" Pretreatment with 6-OH-dopamine resulted in a shift of the dose-response curve for apomorphine to the left, suggesting supersensitivity of D2 receptors."( Cooperation between D1- and D2-dopamine receptors in the nucleus accumbens.
Szmigielski, A; Zalewska-Kaszubska, J, 1991
)
0.28
" For rats that sustained a 70% depletion of dopamine in the medial prefrontal cortex, the dose-response curve was an inverse function across the entire dose range tested."( Supersensitivity to the reinforcing effects of cocaine following 6-hydroxydopamine lesions to the medial prefrontal cortex in rats.
Horger, BA; Peltier, R; Schenk, S; Shelton, K, 1991
)
0.28
" It is suggested that continuous application of a high dosage of ascorbic acid might be a useful approach in neuroblastoma therapy."( Ascorbic acid enhances the effects of 6-hydroxydopamine and H2O2 on iron-dependent DNA strand breaks and related processes in the neuroblastoma cell line SK-N-SH.
Bruchelt, G; Cochrane, CG; Niethammer, D; Schraufstätter, IU, 1991
)
0.28
" The dose-response curve for amphetamine was shifted downward and to the right by reserpine but was flattened by AMPT."( Depletion of catecholamines in the brain of rats differentially affects stimulation of locomotor activity by caffeine, D-amphetamine, and methylphenidate.
Finn, IB; Holtzman, SG; Iuvone, PM, 1990
)
0.28
" Intraspinal 6-hydroxydopamine (6-OHDA) injections given 1 mo earlier did not alter dose-response curves in baroreceptor-intact rabbits."( Spinal noradrenergic pathways and pressor responses to central angiotensin II.
Elghozi, JL; Head, GA, 1990
)
0.28
" From dose-response curves, near-maximal intracisternal (i."( Differential blood pressure responses to intracisternal clonidine, alpha-methyldopa, and 6-hydroxydopamine in conscious normotensive and spontaneously hypertensive rats.
de Jong, W; Head, GA,
)
0.13
" An investigation of reserpine's effects on core temperature revealed that mice dosed with a combination of reserpine + NMTB presented with core temperatures lower than mice treated with either compound alone."( Effect of reserpine on N-methylthiobenzamide-induced pulmonary edema: role of lung norepinephrine and hypothermia.
Gibbs, LS; Traiger, GJ, 1989
)
0.28
" As in experiment 1, CCK produced "biphasic" dose-response effects with strong attenuation that persisted throughout the entire 60-min test at both high (1 microgram) and low (1 ng) doses."( CCK-8 injected into the nucleus accumbens attenuates the supersensitive locomotor response to apomorphine in 6-OHDA and chronic-neuroleptic treated rats.
Ettenberg, A; Koob, GF; Weiss, F, 1989
)
0.28
" Three weeks of pretreatment with 6-OHDA resulted in leftwards shifts of the dose-response curves for the positive chronotropic and inotropic responses of right and left atria to isoprenaline."( Cardiac postjunctional supersensitivity to beta-agonists after chronic chemical sympathectomy with 6-hydroxydopamine.
Broadley, KJ; Chess-Williams, RG; Culling, W; Grassby, PF; Penny, W; Sheridan, DJ, 1985
)
0.27
"This study was undertaken to investigate the dose-response relationship between the biological effect and noise exposure, and to consider the mechanism of the appearance of noise effects."( Study on the mechanism of the appearance of noise effects.
Ariizumi, M; Okada, A; Okamoto, G, 1985
)
0.27
" 6-hydroxydopamine (2 X 250 micrograms) there was a small increase in alpha 1-adrenoceptor binding sites but a parallel shift to the left in the noradrenaline [3H]inositol phosphate accumulation dose-response curve."( Alpha 1-adrenoceptor-mediated inositol phospholipid hydrolysis in rat cerebral cortex: relationship between receptor occupancy and response and effects of denervation.
Brown, E; Kendall, DA; Nahorski, SR, 1985
)
0.27
" After determination of these dose-response relationships, the rats were divided into two groups."( Effects of central dopamine depletion on the d-amphetamine discriminative stimulus in rats.
Cervo, L; Woolverton, WL, 1986
)
0.27
" Following depletion of brain DA, but not NE, animals exhibited a "supersensitive" increase in plasma ACTH values, which was evidenced by a sixfold left shift in the dose-response properties of PHY."( Supersensitive endocrine response to physostigmine in dopamine-depleted rats: a model of depression?
Britton, KT; Downs, NS; Gibbs, DM; Koob, GF; Swerdlow, NR, 1986
)
0.27
" The amphetamine dose-response curve for stereotypy was shifted to the right by glucose but retained the same slope as the control curve, suggesting that glucose competes for amphetamine or dopamine receptors that mediate this behavior."( Effect of glucose on amphetamine-induced motor behavior.
Blackburn, J; White, NM, 1986
)
0.27
" The development of supersensitivity, defined as the leftward parallel shift of the dose-response curves for clonidine administered intrathecally, corresponded to the time course of NE depletion following 6-OHDA treatment on the days tested."( Effect of spinal norepinephrine depletion on descending inhibition of the tail flick reflex from the locus coeruleus and lateral reticular nucleus in the rat.
Gebhart, GF; Janss, AJ; Jones, SL, 1987
)
0.27
" To test this hypothesis, we compared the dose-response relationships between T and luteinizing hormone (LH) and between T and follicle-stimulating hormone (FSH) in adult male rats chronically depleted of hypothalamic norepinephrine (NE) to the dose-response curves exhibited by control animals."( Role of the central ascending noradrenergic system in the regulation of luteinizing hormone responsiveness to testosterone negative feedback in the adult male rat.
Clifton, DK; MacCalla, DL; Matsumoto, AM; Steiner, RA, 1987
)
0.27
" Dose-response curves to apomorphine were determined before and 21 days after 6-hydroxydopamine lesion of the contralateral nigrostriatal pathway."( Quantification of lesion-induced dopaminergic supersensitivity using the rotational model in the mouse.
Mandel, RJ; Randall, PK, 1985
)
0.27
" However, large differences were found when comparing apomorphine and pergolide dose-response curves as well as the patterns of rotational behaviour the compounds elicited."( Evidence that apomorphine and pergolide induce rotation in rats by different actions on D1 and D2 receptor sites.
Herrera-Marschitz, M; Ungerstedt, U, 1984
)
0.27
" The counteracting effect of substance P disclosed a clear dose-response relationship and was most effective when injected on postnatal days one and two, while practically no effects were observed after injection on postnatal days three and four."( Substance P modifies the 6-hydroxydopamine induced alteration of postnatal development of central noradrenaline neurons.
Hallman, H; Jonsson, G, 1982
)
0.26
"7-fold) toward increased sensitivity in the dose-response curve for adenylate cyclase activation by isoproterenol."( Independent regulation of beta-adrenergic receptor and nucleotide binding proteins of adenylate cyclase. Developmental and denervation-dependent responses in rat parotid.
Ludford, JM; Talamo, BR, 1983
)
0.27
" In rat mesenteric artery, the pA2 value for yohimbine against clonidine was not statistically different from values obtained with the other agonists; however, in the presence of prazosin the dose-response curve to clonidine was biphasic, suggesting that the action of clonidine is mediated through two distinct sites to which prazosin has different affinities."( Pharmacological characterization of the postsynaptic alpha adrenoceptors in vascular smooth muscle from canine and rat mesenteric vascular beds.
Agrawal, DK; Daniel, EE; Triggle, CR, 1984
)
0.27
" Cumulative dose-response curves were constructed for the effect of immune IgG on nice oviductal tracts from proestrus, estrus, metestrus and diestrus, comparing them with those obtained with norepinephrine."( Beta-adrenergic inhibitory effect of alloimmune antibody on isolated oviductal tract of mice.
Borda, ES; Cremaschi, GA; Genaro, AM; Sales, ME; Sterin-Borda, L, 1984
)
0.27
" In the present study dose-response curves were obtained from dog anterior tibial artery rings at lengths equal to or longer than Lmax."( Length-dependent sensitivity at lengths greater than Lmax in vascular smooth muscle.
Davis, DL; Knauss, EB; Price, JM, 1983
)
0.27
" Increasing the test-dose of apomorphine led to a biphasic effect, the spontaneous climbing behavior being decreased at low dosage and, then, both the percentage of climbing animals and the duration of the behavior were progressively increased at higher dosages."( Rat climbing behavior elicited by stimulation of cerebral dopamine receptors.
Bonnet, JJ; Costentin, J; Protais, P; Schwartz, JC, 1984
)
0.27
" The mesenteric arteries from all three types of hypertensive rats showed an increased reactivity to noradrenaline as characterized by a steeper dose-response curve and elevated maximal vasoconstriction when compared with normotensive controls."( Vascular reactivity of rats after prevention of hypertension by central administration of 6-hydroxydopamine.
Haeusler, G, 1984
)
0.27
" 6-OH-DA in the dosage applied, induces during its time of action in NR a smaller, in SHR a larger decrease of blood pressure and, presumably induced by intense NA-depletion of the myocardium, myocardial alterations."( [Functional and structural behavior of the cardiovascular system of normotonic and spontaneously hypertensive rats following chemical sympathectomy and angiotensin administration].
Becker, CH; Engler, E; Matthias, D; Moritz, V; Schmidt, R; Will-Shahab, L, 1981
)
0.26
" The dose-response curve of inactivation of transport or of metabolic function varied with the ROS generator used and conformed to one of two patterns of toxicity: either threshold-dependent or single-hit inactivation."( Localization of damage induced by reactive oxygen species in cultured cells.
Buxser, SE; Decker, DE; Vroegop, SM, 1995
)
0.29
" The dose-response curves for the effects of aminophylline in the presence of Ni2+ on Td and dT/dt max during direct single-pulse stimulation were significantly shifted to the right."( Some new evidence on antifatigue action of aminophylline on the isolated hemidiaphragm of the rat.
Prostran, M; Todorović, Z; Varagić, VM, 1993
)
0.29
" Furthermore, bradykinin did not modify the dose-response curves for added norepinephrine."( Importance of sympathetic innervation in the positive inotropic effects of bradykinin and ramiprilat.
Djokovic, A; Erdös, EG; Miletich, DJ; Minshall, RD; Rabito, SF; Vogel, SM; Yelamanchi, VP, 1994
)
0.29
" SKF 38393 dose-response curves demonstrated enhanced oral activity responses in rats lesioned neonatally with 150 or 200 micrograms of 6-OHDA."( Dose-related effects of a neonatal 6-OHDA lesion on SKF 38393- and m-chlorophenylpiperazine-induced oral activity responses of rats.
Fuller, RW; Gong, L; Kostrzewa, RM; Perry, KW, 1993
)
0.29
" A dose-response curve for the rotational response arising from apomorphine stimulation of the normosensitive striatum was obtained in animals bearing unilateral lesions of striatal efferents (predominantly the striato-nigral pathway as previously described)."( A quantitative estimate of the role of striatal D-2 receptor proliferation in dopaminergic behavioral supersensitivity: the contribution of mesolimbic dopamine to the magnitude of 6-OHDA lesion-induced agonist sensitivity in the rat.
Hartgraves, SL; Mandel, RJ; Randall, PK; Severson, JA; Wilcox, RE; Woodward, JJ, 1993
)
0.29
" Some 3H-noradrenaline was taken up and released in 6-OHDA-treated tissues which is consistent with the existence of nerve varicosities resistant to the present dosing regime of 6-OHDA, an observation substantiated by electron microscopy studies showing inconsistent lesions of nerve terminals."( Effects of 6-hydroxydopamine on pre- and post-junctional 5-HT1-like receptor-mediated responses in dog saphenous vein.
Deighton, NM; Kaumann, AJ; Medhurst, AD; Novotny, GE; Parker, SG, 1993
)
0.29
" Animals that were lesioned and treated with haloperidol chronically had longer durations of catalepsy at the first two dose-response determinations."( Partial 6-hydroxydopamine-induced lesions and haloperidol-induced catalepsy.
Fisher, H; Johnson, SK; Wagner, GC, 1993
)
0.29
" Animals were dosed with PCP (15 mg/kg, ip) its congener (+) MK-801 (0."( Drug-induced circling preference in rats. Correlation with monoamine levels.
Ali, SF; Gough, B; Kordsmeier, KJ,
)
0.13
" Apomorphine at a low dosage (0."( Time course of striatal changes induced by 6-hydroxydopamine lesion of the nigrostriatal pathway, as studied by combined evaluation of rotational behaviour and striatal Fos expression.
Guerra, MJ; Labandeira-Garcia, JL; Liste, I; Lopez-Martin, E; Rozas, G, 1996
)
0.29
" However, the intracerebroventricular administration of 6-hydroxydopamine, in a dosage regimen that does not lesion catecholaminergic pathways but causes oxidative stress, enhanced dramatically the level of metallothionein I mRNA in some brain areas such as hippocampus, arcuate nucleus, choroid plexus, and granular layer of cerebellum, but not in the caudate putamen."( 6-Hydroxydopamine-mediated induction of rat brain metallothionein I mRNA.
Cerutis, DR; Ebadi, M; Hao, R; Happe, HK; Murrin, LC; Pfeiffer, RF; Rojas, P, 1996
)
0.29
" LDEE injections produced significant and rapid elevations of striatal levodopa, dopamine, and DOPAC, which were similar to those achieved after levodopa administration, with similar dose-response curves."( Effect of subcutaneous administration of levodopa ethyl ester, a soluble prodrug of levodopa, on dopamine metabolism in rodent striatum: implication for treatment of Parkinson's disease.
Atlas, D; Djaldetti, R; Melamed, E, 1996
)
0.29
"Rats with 6-OHDA lesions were repeatedly treated with apomorphine and dose-response relationships compared before and after treatment to better understand the pharmacological mechanisms which result in sensitization."( Changes in apomorphine pharmacodynamics following repeated treatment in 6-hydroxydopamine-lesioned rats.
Gancher, S; Mayer, A; Youngman, S, 1996
)
0.29
" PLG and the two novel analogues showed a bell-shaped dose-response relationship, suggesting that analogue A, B and PLG all manifest their effect through a similar mechanism and exhibit a window of therapeutic efficacy."( Modulation of dopaminergic neurotransmission in the 6-hydroxydopamine lesioned rotational model by peptidomimetic analogues of L-prolyl-L-leucyl-glycinamide.
Johnson, RL; Mishra, RK; Ott, MC, 1996
)
0.29
" Prazosin (10(-8) M - 10(-5) M) displaced agonist dose-response curves to the right."( Characterization of alpha-adrenoceptor subtype(s) mediating vasoconstriction in the perfused rabbit ovarian vascular bed.
Oriowo, MA; Williams, KI; Yousif, M, 1996
)
0.29
" Studies were performed at 5-7 days post lesion (group 1 animals), at 21 days (group 2) when denervation supersensitivity was evident by contralateral turning to apomorphine and at the same time but following 7 days dosing with LDME plus benserazide (group 3)."( Effect of L-dopa alone and with benserazide on the spontaneous activity of striatal neurones in normal and 6-hydroxydopamine-lesioned rats.
Chang, WY; Webster, RA, 1997
)
0.3
" The dose-response curve obtained from the denervated striatum showed a shift to the right."( Loss of regulation by presynaptic dopamine D2 receptors of exogenous L-DOPA-derived dopamine release in the dopaminergic denervated striatum.
Kannari, K; Maeda, T; Matsunaga, M; Suda, T, 1999
)
0.3
" The maximal effect of the dose-response curve for Expar was prevented by the alpha1-adrenergic blocking agent prazosin at 10 nM and 30 nM concentration dependently."( Sympathomimetic effects of Parquetina nigrescens (Periplocaceae) extract in isolated portal vein smooth muscle.
Datté, JY; Tillement, JP; Ziegler, A, 1999
)
0.3
" They both potentiated the effects of L-DOPA in the 6-hydroxydopamine-lesioned rat, a model of Parkinson's disease, dosed at 10 mg/kg ip, but 48 was not active at 30 mg/kg po."( Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(arylalkynyl)-4-benzylpiperidines.
Bigge, CF; Boxer, PA; Cai, SX; Gregory, TF; Hawkinson, JE; Konkoy, CS; Meltzer, LT; Serpa, K; Whittemore, ER; Wise, LD; Woodward, RM; Wright, JL; Zhou, ZL, 1999
)
0.3
" Peptidomimetics 3-5 each affected rotational behavior in a bell-shaped dose-response relationship producing maximal increases of 44% (1 microgram/kg,ip), 56% (0."( Synthesis and dopamine receptor modulating activity of substituted bicyclic thiazolidine lactam peptidomimetics of L-prolyl-L-leucyl-glycinamide.
Gleason, WB; Johnson, RL; Khalil, EM; Mishra, RK; Ojala, WH; Pradhan, A, 1999
)
0.3
" When dosed orally, this compound potentiates the effects of L-DOPA in the 6-hydroxydopamine-lesioned rat, a model of Parkinson's disease."( Discovery of subtype-selective NMDA receptor ligands: 4-benzyl-1-piperidinylalkynylpyrroles, pyrazoles and imidazoles as NR1A/2B antagonists.
Boxer, PA; Gregory, TF; Meltzer, LT; Serpa, KA; Wise, LD; Wright, JL, 1999
)
0.3
" Compound 11a also potentiated the effects of L-DOPA in a rat model of Parkinson's disease (the 6-hydroxydopamine-lesioned rat), dosed at 30 mg/kg orally."( Subtype-selective N-methyl-D-aspartate receptor antagonists: benzimidazalone and hydantoin as phenol replacements.
Meltzer, LT; Schelkun, RM; Serpa, K; Whittemore, ER; Wise, LD; Woodward, RM; Yuen, PW, 2000
)
0.31
" Furthermore, the inhibitory effects on striatal nerve cell firing rate by the D1 receptor agonist SKF 81297 were not different in noninnervated or reinnervated areas of the striatum compared to the control side as seen from the dose-response curves."( Fetal ventral mesencephalic grafts functionally reduce the dopamine D2 receptor supersensitivity in partially dopamine reinnervated host striatum.
Andbjer, B; Fuxe, K; Kehr, J; Strömberg, I, 2000
)
0.31
" While the persistence and Mn dose-response relationship of these neurobehavioral effects were not evaluated here, these results nonetheless suggest that chronic Mn exposure may increase the risk of neurobehavioral impairment in subpopulations that are in a pre-parkinsonism state."( The neurobehavioral effects of subchronic manganese exposure in the presence and absence of pre-parkinsonism.
Gwiazda, RH; Smith, DR; Witholt, R,
)
0.13
", was ineffective, suggesting a bell-shaped dose-response relationship which has also been observed in other paradigms."( CGP 3466 protects dopaminergic neurons in lesion models of Parkinson's disease.
Hengerer, B; Spooren, WP; Waldmeier, PC, 2000
)
0.31
" However, it is also known to accumulate in various tissues up to several times higher after standard oral dosing and we now have evidence from both in vivo and in vitro experiments with spontaneously hypertensive rats (SHR) that millimolar levels stimulate release of norepinephrine (NE) from vascular sympathetic nerve endings (SNEs)."( A possible indirect sympathomimetic action of metformin in the arterial vessel wall of spontanously hypertensive rats.
Lee, JM; Peuler, JD, 2001
)
0.31
" There was no difference in the average percentages of PCP-appropriate responding between vehicle and 6-OHDA-treated rats in the dose-response tests."( Involvement of dopaminergic system in the nucleus accumbens in the discriminative stimulus effects of phencyclidine.
Furukawa, H; Mamiya, T; Mori, A; Nabeshima, T; Nagai, T; Noda, Y, 2002
)
0.31
" However, immunosuppressant side effects (including nephrotoxicity and hepatotoxicity) are associated with such CsA dosing regimens."( Bradykinin receptor agonist facilitates low-dose cyclosporine-A protection against 6-hydroxydopamine neurotoxicity.
Bartus, RT; Borlongan, CV; Emerich, DF; Hoffer, BJ, 2002
)
0.31
" 6-Hydroxydopamine (6-OHDA) treatment markedly reduced, in a dose-response fashion, chromaffin cell viability."( Chromaffin cell death induced by 6-hydroxydopamine is independent of mitochondrial swelling and caspase activation.
Ceña, V; Galindo, MF; González-García, C; Jordán, J, 2003
)
0.32
" IP injection of rats with VK-28 (1 and 5 mg/kg) daily for 10 and 7 days, respectively, demonstrated significant neuroprotection against ICV 6-OHDA at the higher dose, with 68% protection against loss of dopamine at 5mg/kg dosage of VK-28."( Neuroprotection by a novel brain permeable iron chelator, VK-28, against 6-hydroxydopamine lession in rats.
Kahana, N; Kampel, V; Shachar, DB; Warshawsky, A; Youdim, MB, 2004
)
0.32
" In a primary culture of E14 murine ventral mesencephalic neurons, earlier treatment with the higher dosage of GDNF suppressed 6-OHDA-induced loss of dopaminergic neurons better than later treatment."( Early transplantation of an encapsulated glial cell line-derived neurotrophic factor-producing cell demonstrating strong neuroprotective effects in a rat model of Parkinson disease.
Date, I; Kameda, M; Kobayashi, K; Matsui, T; Miyoshi, Y; Muraoka, K; Shingo, T; Takeuchi, A; Wenji, Y; Yano, A; Yasuhara, T, 2005
)
0.33
" Following recovery, the phencyclidine dose-response curve was repeated in the fixed-interval paradigm."( Effects of phencyclidine on schedule-controlled responding following neurotoxic lesions of the striatum.
Carlson, KM; Wagner, GC, 2005
)
0.33
"The therapeutic success of L-3,4-dihydroxyphenylalanine (L-DOPA) treatment in Parkinson's disease (PD) patients remains controversial as many patients become tolerant requiring higher dosage regimens."( l-DOPA administration enhances 6-hydroxydopamine generation.
Daya, S; Maharaj, H; Mokokong, R; Scheepers, M; Sukhdev Maharaj, D, 2005
)
0.33
" Dose-response studies with 6-hydroxydopamine revealed that the application of 200 microg per animal caused hypokinetic signs (decreased ambulatory activity, increased inactivity, and reduced motor coordination), which paralleled several signs of degeneration of nigrostriatal dopaminergic neurons (dopamine depletion in the caudate-putamen, and decreased mRNA levels for tyrosine hydroxylase and superoxide dismutase-1 and -2 in the substantia nigra)."( Effects of rimonabant, a selective cannabinoid CB1 receptor antagonist, in a rat model of Parkinson's disease.
de Miguel, R; Fernández-Ruiz, J; García-Arencibia, M; González, S; Ramos, JA; Scorticati, C, 2006
)
0.33
" Further microinjections of lower doses (5 and 10 nmol) revealed a dose-response effect."( Blockade of mGluR glutamate receptors in the subthalamic nucleus ameliorates motor asymmetry in an animal model of Parkinson's disease.
Ackerson, LC; Lam, HA; Maidment, NT; Phillips, JM, 2006
)
0.33
" Moreover, 18 at a dosage of 10 mg/kg was found to be significantly neuroprotective in a mouse peripheral sympathetic nerve injury model induced by 8 mg/kg 6-hydroxydopamine."( FK506-binding protein ligands: structure-based design, synthesis, and neurotrophic/neuroprotective properties of substituted 5,5-dimethyl-2-(4-thiazolidine)carboxylates.
Hu, Y; Huang, W; Li, S; Liu, H; Wang, L; Xiao, J; Zhao, L; Zhong, W, 2006
)
0.33
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
" While it has been suggested that the daily dose of l-DOPA can play a critical role, the mechanisms linking l-DOPA dosage to the occurrence of motor complications have not yet been explored."( l-DOPA dosage is critically involved in dyskinesia via loss of synaptic depotentiation.
Angela Cenci, M; Bagetta, V; Barone, I; Bernardi, G; Calabresi, P; Ghiglieri, V; Lindgren, HS; Paillé, V; Picconi, B, 2008
)
0.35
" Edaravone might be a hopeful therapeutic option for PD, although the high therapeutic dosage remains to be solved for the clinical application."( Neuroprotective effects of edaravone-administration on 6-OHDA-treated dopaminergic neurons.
Agari, T; Baba, T; Date, I; Jing, M; Kameda, M; Leung, H; Matsui, T; Miyoshi, Y; Morimoto, T; Muraoka, K; Shingo, T; Tajiri, N; Uozumi, T; Wang, F; Yasuhara, T; Yuan, WJ, 2008
)
0.35
" Compared to resveratrol, OXY exhibited a wider effective dosage range."( Dietary oxyresveratrol prevents parkinsonian mimetic 6-hydroxydopamine neurotoxicity.
Chang, RC; Chao, J; Ho, YS; Wang, M; Yu, MS, 2008
)
0.35
" Although not present in neonate-lesioned rats treated with saline, these morphological changes persisted at least 21 days after repeated dosing with SKF-38393, and were not accompanied by markers of neurodegenerative change."( Changes in apical dendritic structure correlate with sustained ERK1/2 phosphorylation in medial prefrontal cortex of a rat model of dopamine D1 receptor agonist sensitization.
Blake, BL; Breese, GR; Halloran, C; McCown, TJ; Papadeas, ST, 2008
)
0.35
" The in vitro study showed that 1 microM OEA exerted a significantly neuroprotective effect on cultured nigral dopamine neurons, effects following U-shaped dose-response curves."( Oleoylethanolamide exerts partial and dose-dependent neuroprotection of substantia nigra dopamine neurons.
Bermudez-Silva, FJ; Fernandez-Espejo, E; Galan-Rodriguez, B; Gonzalez-Aparicio, R; Maldonado, R; Robledo, P; Rodriguez de Fonseca, F; Suarez, J, 2009
)
0.35
" This may allow for cell composition analysis and dosing to optimize the benefit to an individual patient."( Future of cell and gene therapies for Parkinson's disease.
Isacson, O; Kordower, JH, 2008
)
0.35
" Neuroprotective effects of Lf-modified NPs were examined in the 6-OHDA-lesioned PD model via a regimen of multiple dosing intravenous administrations."( Neuroprotection in a 6-hydroxydopamine-lesioned Parkinson model using lactoferrin-modified nanoparticles.
Han, L; Huang, R; Jiang, C; Ke, W; Li, J; Pei, Y; Ren, F, 2009
)
0.35
" Five injections of Lf-modified NPs loading hGDNF exhibited much more powerful neuroprotection than a single injection, indicating the effectiveness and feasibility of multiple dosing administrations."( Neuroprotection in a 6-hydroxydopamine-lesioned Parkinson model using lactoferrin-modified nanoparticles.
Han, L; Huang, R; Jiang, C; Ke, W; Li, J; Pei, Y; Ren, F, 2009
)
0.35
" Animals were tested once a week until each P(4) dosage was received; animals then had bilateral 6-hydroxydopamine (6-OHDA) or sham lesions to the VTA, NAc, or CN and were re-tested at each P(4) dosage on subsequent weeks."( 6-hydroxydopamine lesions enhance progesterone-facilitated lordosis of rats and hamsters, independent of effects on motor behavior.
DeBold, JF; Frye, CA; Petralia, SM; Rhodes, ME, 2010
)
0.36
" However, the dose-response relationship between NE and erythropoiesis remains unclear."( Dose-response relationship between norepinephrine and erythropoiesis: evidence for a critical threshold.
Kaiser, VL; Livingston, DH; Mohr, AM; Penn, A; Rameshwar, P; Shah, SG; Sifri, ZC, 2010
)
0.36
" SHAM rats with continuous infusion of exogenous NE show a clear dose-response inhibition of both BFU-E and CFU-E colony growth."( Dose-response relationship between norepinephrine and erythropoiesis: evidence for a critical threshold.
Kaiser, VL; Livingston, DH; Mohr, AM; Penn, A; Rameshwar, P; Shah, SG; Sifri, ZC, 2010
)
0.36
"In order to assess whether caffeine and theophylline have the same potency and efficacy to reverse the impairment of motor function caused by acute or chronic interruption of striatal dopamine transmission, a comparison of their dose-response relationship was made in the acute model of haloperidol-induced catalepsy, and the chronic model of unilateral lesion of the dopamine nigrostriatal pathway with 6-hydroxydopamine."( Caffeine has greater potency and efficacy than theophylline to reverse the motor impairment caused by chronic but not acute interruption of striatal dopaminergic transmission in rats.
Acuña-Lizama, MM; Alvarez-Cervera, FJ; Bata-García, JL; Góngora-Alfaro, JL, 2013
)
0.39
" To test this hypothesis in a rodent model, the A2A receptor antagonists SCH 412348 (3 mg/kg), vipadenant (10 mg/kg), caffeine (30 mg/kg), or istradefylline (3 mg/kg) were chronically (19-22 days) administered to Sprague Dawley rats, and dyskinetic behaviors were scored across this chronic dosing paradigm."( A2A receptor antagonists do not induce dyskinesias in drug-naive or L-dopa sensitized rats.
Bleickardt, C; Hodgson, R; Jones, N; Mullins, D; Parker, E, 2013
)
0.39
" Mitochondrial dysfunction, motor behavior asymmetry, and dopaminergic neuronal cell loss correlated with dosage (1."( 6-Hydroxydopamine impairs mitochondrial function in the rat model of Parkinson's disease: respirometric, histological, and behavioral analyses.
Debska-Vielhaber, G; Gellerich, FN; Gizatullina, Z; Heinze, HJ; Kupsch, A; Panther, P; Schmidt, W; Schwegler, H; Striggow, F; Vielhaber, S; Voges, J, 2014
)
0.4
" It is established that the antidyskinetic effect of the injectable dosage form of a new antiparkinsonian drug hemantane (5 mg/kg) after a single intravenous administration is weaker than that of the most effective in clinical practice antidyskinetic drug amantadine (20 mg/kg)."( [Influence of hemantane in injectable dosage form on levodopa-induced dyskinesia in rats with model parkinsonian syndrome].
Ivanova, EA; Kapitsa, IG; Kokshenev, II; Nepoklonov, AV; Val'dman, EA; Voronina, TA, 2014
)
0.4
" Three or 14 days after lesion, rats were dosed with XPro®1595 (10 mg/kg in saline, subcutaneous) every third day for 35 days."( Peripheral administration of the selective inhibitor of soluble tumor necrosis factor (TNF) XPro®1595 attenuates nigral cell loss and glial activation in 6-OHDA hemiparkinsonian rats.
Barnum, CJ; Chang, J; Chen, X; Chung, J; Grigoryan, N; Tansey, MG; Tesi, RJ; Williams, M, 2014
)
0.4
"Peripheral subcutaneous dosing of XPro®1595 achieved plasma levels of 1-8 microgram/mL and CSF levels of 1-6 ng/mL depending on the time the rats were killed after final XPro®1595 injection."( Peripheral administration of the selective inhibitor of soluble tumor necrosis factor (TNF) XPro®1595 attenuates nigral cell loss and glial activation in 6-OHDA hemiparkinsonian rats.
Barnum, CJ; Chang, J; Chen, X; Chung, J; Grigoryan, N; Tansey, MG; Tesi, RJ; Williams, M, 2014
)
0.4
" Our results confirm that systemic 6-OHDA dosing to nonhuman primates induces cardiac sympathetic neurodegeneration and loss of catecholaminergic enzymes in the adrenal medulla, and suggests that this model can be used as a platform to evaluate disease-modifying strategies aiming to induce peripheral neuroprotection."( Cardiac sympathetic denervation in 6-OHDA-treated nonhuman primates.
Dilley, K; Emborg, ME; Joers, V; Jones, C; Rahman, S; Shultz, J; Simmons, H, 2014
)
0.4
"05mg/kg) and high (1mg/kg) dosage and monitored their conditioned place preference Saline was administered on alternating days."( Place conditioning to apomorphine in rat models of Parkinson's disease: differences by dose and side-effect expression.
Campbell, JC; Chen, N; De La Cruz, P; Jeyamohan, SB; Pilitsis, JG; Shin, D, 2014
)
0.4
" Rats were dosed orally with Tozadenant, a selective A2A receptor antagonist, and three different doses of Radiprodil, an NR2B-selective NMDA receptor antagonist."( Behavioural Assessment of the A2a/NR2B Combination in the Unilateral 6-OHDA-Lesioned Rat Model: A New Method to Examine the Therapeutic Potential of Non-Dopaminergic Drugs.
De Wolf, C; Downey, P; Michel, A; Scheller, D; Schwarting, R; Van Damme, X, 2015
)
0.42
" In the full lesion model, vehicle dosing or liraglutide treatment was applied for a total of six weeks starting three weeks pre-lesion, or administered for three weeks starting on the lesion day."( Characterization of liraglutide, a glucagon-like peptide-1 (GLP-1) receptor agonist, in rat partial and full nigral 6-hydroxydopamine lesion models of Parkinson's disease.
Barkholt, P; Fabricius, K; Hansen, HH; Jelsing, J; Knudsen, LB; Mikkelsen, JD; Pyke, C; Vrang, N, 2016
)
0.43
" Following oral dosing in rats for 7 days, salbutamol and triflusal, but not dimethadione or trazodone, significantly elevated FGF20 levels in the nigrostriatal tract."( Targeted repositioning identifies drugs that increase fibroblast growth factor 20 production and protect against 6-hydroxydopamine-induced nigral cell loss in rats.
Doherty, P; Duty, S; Fletcher, EJR; Jamieson, AD; Williams, G, 2019
)
0.51
" The population-based human study analyzed the data from the Taiwan Longitudinal Health Insurance Database 2005 between January 2005 and December 2013 and then used the DXM dose-response curve to investigate the trend of its protective effect against PD."( The effect of dextromethorphan use in Parkinson's disease: A 6-hydroxydopamine rat model and population-based study.
Cheng, CY; Chien, WC; Chiu, CH; Huang, YS; Kao, LT; Li, IH; Liu, CT; Ma, KH; Shih, JH; Shiue, CY, 2019
)
0.51
"We found that the 10 mg/kg l-dopa dosing regimen induced LID in all animals (n = 5) and induced significant angiogenesis in the striatum and substantia nigra."( The Vasomotor Response to Dopamine Is Altered in the Rat Model of l-dopa-Induced Dyskinesia.
Anderson, C; Booth, S; Jackson, MF; Kirouac, G; Ko, JH; Lu, L; Ramadan, A; Zhang, D, 2021
)
0.62
" However, a U-shaped dose-response curve obtained with certain parameters may limit the therapeutic potential of this strategy and require further investigation."( Granisetron, a selective 5-HT3 antagonist, reduces L-3,4-dihydroxyphenylalanine-induced abnormal involuntary movements in the 6-hydroxydopamine-lesioned rat.
Bédard, D; Frouni, I; Hamadjida, A; Huot, P; Kwan, C, 2021
)
0.62
" Involuntary movements were assessed by two blinded raters prior and every 30 min after drug dosing using the Clinical Dyskinesia Rating Scale (CDRS)."( Comparison of dyskinesia profiles after L-DOPA dose challenges with or without dopamine agonist coadministration.
Cenci, MA; Espa, E; Grigoriou, S; Jakobsson, A; Odin, P; Timpka, J; von Grothusen, G, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
neurotoxinA poison that interferes with the functions of the nervous system.
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
drug metabolitenull
[role 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]

Drug Classes (3)

ClassDescription
primary amino compoundA compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
benzenetriolA triol in which three hydroxy groups are substituted onto a benzene ring.
catecholamine4-(2-Aminoethyl)pyrocatechol [4-(2-aminoethyl)benzene-1,2-diol] and derivatives formed by substitution.
[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]

Pathways (1)

PathwayProteinsCompounds
5q35 copy number variation012

Protein Targets (19)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency9.71470.003245.467312,589.2998AID2517; AID2572; AID2573
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.31620.004023.8416100.0000AID485290
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency5.61010.140911.194039.8107AID2451
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency67.40220.125919.1169125.8920AID2549; AID2708
phosphopantetheinyl transferaseBacillus subtilisPotency6.30960.141337.9142100.0000AID1490
Bloom syndrome protein isoform 1Homo sapiens (human)Potency14.12540.540617.639296.1227AID2528
runt-related transcription factor 1 isoform AML1bHomo sapiens (human)Potency19.49980.02007.985839.8107AID504370; AID504374; AID504375
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency56.23410.354828.065989.1251AID504847
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency39.81070.010039.53711,122.0200AID1469
core-binding factor subunit beta isoform 2Homo sapiens (human)Potency19.49980.02007.985839.8107AID504370; AID504374; AID504375
DNA polymerase kappa isoform 1Homo sapiens (human)Potency1.50030.031622.3146100.0000AID588579
Glutamate receptor 1Rattus norvegicus (Norway rat)Potency0.56230.01418.602439.8107AID2572
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency0.56230.001551.739315,848.9004AID2572
Glutamate receptor 3Rattus norvegicus (Norway rat)Potency0.56230.01418.602439.8107AID2572
Glutamate receptor 4Rattus norvegicus (Norway rat)Potency0.56230.01418.602439.8107AID2572
[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)
Glyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)IC50 (µMol)8.00006.00007.33338.0000AID500286
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)Ki0.01200.00030.37088.1600AID65474
DNA repair protein RAD52 homologHomo sapiens (human)IC50 (µMol)0.77900.25502.63016.7000AID1639797
TransporterRattus norvegicus (Norway rat)Ki0.05100.00010.866710.0000AID145874
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (26)

Processvia Protein(s)Taxonomy
microtubule cytoskeleton organizationGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
positive regulation of cytokine productionGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
glucose metabolic processGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
glycolytic processGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
negative regulation of endopeptidase activityGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
regulation of macroautophagyGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
negative regulation of translationGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
killing of cells of another organismGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
positive regulation of type I interferon productionGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
peptidyl-cysteine S-trans-nitrosylationGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
protein stabilizationGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
defense response to fungusGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
neuron apoptotic processGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
killing by host of symbiont cellsGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptideGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
cellular response to type II interferonGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
DNA double-strand break processing involved in repair via single-strand annealingDNA repair protein RAD52 homologHomo sapiens (human)
cellular response to oxidative stressDNA repair protein RAD52 homologHomo sapiens (human)
regulation of nucleotide-excision repairDNA repair protein RAD52 homologHomo sapiens (human)
DNA recombinase assemblyDNA repair protein RAD52 homologHomo sapiens (human)
double-strand break repairDNA repair protein RAD52 homologHomo sapiens (human)
DNA recombinationDNA repair protein RAD52 homologHomo sapiens (human)
double-strand break repair via homologous recombinationDNA repair protein RAD52 homologHomo sapiens (human)
mitotic recombinationDNA repair protein RAD52 homologHomo sapiens (human)
double-strand break repair via single-strand annealingDNA repair protein RAD52 homologHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

Processvia Protein(s)Taxonomy
glyceraldehyde-3-phosphate dehydrogenase (NAD+) (phosphorylating) activityGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
protein bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
microtubule bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
aspartic-type endopeptidase inhibitor activityGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
peptidyl-cysteine S-nitrosylase activityGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
identical protein bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
NADP bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
NAD bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
disordered domain specific bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
DNA bindingDNA repair protein RAD52 homologHomo sapiens (human)
single-stranded DNA bindingDNA repair protein RAD52 homologHomo sapiens (human)
protein bindingDNA repair protein RAD52 homologHomo sapiens (human)
identical protein bindingDNA repair protein RAD52 homologHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
nucleusGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
cytoplasmGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
lipid dropletGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
cytosolGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
plasma membraneGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
microtubule cytoskeletonGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
membraneGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
nuclear membraneGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
vesicleGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
intracellular membrane-bounded organelleGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
perinuclear region of cytoplasmGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
extracellular exosomeGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
GAIT complexGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
ribonucleoprotein complexGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
cytosolGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
plasma membraneGlutamate receptor 1Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
nucleusDNA repair protein RAD52 homologHomo sapiens (human)
nucleoplasmDNA repair protein RAD52 homologHomo sapiens (human)
protein-containing complexDNA repair protein RAD52 homologHomo sapiens (human)
protein-DNA complexDNA repair protein RAD52 homologHomo sapiens (human)
nucleusDNA repair protein RAD52 homologHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (65)

Assay IDTitleYearJournalArticle
AID139810Long term depletion of Norepinephrine (NE) in Whole mouse Brain region of medulla-pons at a high dose (300 nmol) with respect to control value(100+/-9)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139820Long term depletion of Serotonin(5-HT) in Whole mouse Brain region of hypothalamus at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139660Long term depletion of Dopamine(DA) in Whole mouse Brain region of hypothalamus at a high dose (300 nmol) with respect to control value(100+/-14)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139807Long term depletion of Norepinephrine (NE) in Whole mouse Brain region of hippocampus at a high dose (300 nmol) with respect to control value(100+/-10)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139815Long term depletion of Serotonin(5-HT) in Whole mouse Brain at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139811Long term depletion of Norepinephrine (NE) in Whole mouse Brain region of striatum at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139822Long term depletion of Serotonin(5-HT) in Whole mouse Brain region of medulla-pons at a high dose (300 nmol) with respect to control value(100+/-6)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139668Long term depletion of Norepinephrine (NE) in Whole mouse Brain region of cerebellum at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139662Long term depletion of Dopamine(DA) in Whole mouse Brain region of medulla-pons at a high dose (300 nmol) with respect to control value(100+/-8)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139834Noradrenergic effect was determined by depletion effect of Dopamine(DA) in mouse brain regions expressed as d501995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID182682Ability to inhibit norepinephrine uptake in rat atria was determined at 97 umol/kg1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Synthesis and physicochemical and neurotoxicity studies of 1-(4-substituted-2,5-dihydroxyphenyl)-2-aminoethane analogues of 6-hydroxydopamine.
AID500287Induction of rabbit GAPDH tetramer segregation into monomers at 10 uM after 30 mins by SDS-PAGE2007Nature chemical biology, Jan, Volume: 3, Issue:1
Forward chemical genetic approach identifies new role for GAPDH in insulin signaling.
AID139805Long term depletion of Norepinephrine (NE) in Whole mouse Brain region of cortex at a high dose (300 nmol) with respect to control value(100+/-6)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID145874Evaluated for the Competitive inhibition of uptake of norepinephrine1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID182676Ability to inhibit norepinephrine uptake in rat atria was determined at 486 umol/kg1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Synthesis and physicochemical and neurotoxicity studies of 1-(4-substituted-2,5-dihydroxyphenyl)-2-aminoethane analogues of 6-hydroxydopamine.
AID139665Long term depletion of Dopamine(DA) in Whole mouse Brain, region of midbrain at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID540237Phospholipidosis-positive literature compound observed in rat
AID1807009Neurotoxicity in human SH-SY5Y cells assessed as reduction in cell viability at 100 uM measured after 48 hrs by MTT reduction assay (Rvb= 100 +/- 2.79%)2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery of New Potent Positive Allosteric Modulators of Dopamine D
AID139835Noradrenergic effect was determined by depletion effect of Nerepinephrine (NE) in mouse brain regions expressed as d501995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139663Long term depletion of Dopamine(DA) in Whole mouse Brain region of striatum at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139654Long term depletion of Dopamine(DA) in Whole mouse Brain at a low dose (60 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139653Long term depletion of Dopamine(DA) in Whole mouse Brain at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID175698Evaluated for the stimulation of synaptosomal release of norepinephrine (release constant)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139824Long term depletion of Serotonin(5-HT) in Whole mouse Brain region of thalamus at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139812Long term depletion of Norepinephrine (NE) in Whole mouse Brain region of thalamus at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID182678Ability to inhibit norepinephrine uptake in rat atria was determined at 49 uM/kg1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Synthesis and physicochemical and neurotoxicity studies of 1-(4-substituted-2,5-dihydroxyphenyl)-2-aminoethane analogues of 6-hydroxydopamine.
AID182683Ability to inhibit norepinephrine uptake in rat atria was determined at 122 umol/kg1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Synthesis and physicochemical and neurotoxicity studies of 1-(4-substituted-2,5-dihydroxyphenyl)-2-aminoethane analogues of 6-hydroxydopamine.
AID139664Long term depletion of Dopamine(DA) in Whole mouse Brain region of thalamus at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139825Long term depletion of Serotonin(5-HT) in Whole mouse Brain, region of midbrain at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID27360Compound was tested for neurotoxic property after intracranial administration in mice1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Oxidation of 5-hydroxytryptamine and 5,7-dihydroxytryptamine. A new oxidation pathway and formation of a novel neurotoxin.
AID139814Long term depletion of Norepinephrine (NE) in Whole mouse Brain, region of midbrain at a high dose (300 nmol) with respect to control value(100+/-8)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID65474Evaluated for the Competitive inhibition of uptake of dopamine transporter1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID139656Long term depletion of Dopamine(DA) in Whole mouse Brain region of cerebellum at a high dose (300 nmol) with respect to control value(100+/-9)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID311934Dissociation constant, pKa of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID139658Long term depletion of Dopamine(DA) in Whole mouse Brain region of hippocampus at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139838Noradrenergic effect was determined by depletion effect of Nerepinephrine (NE) in mouse brain regions expressed as log d501995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139839Noradrenergic effect was determined by depletion effect of Serotonin(5-HT) in mouse brain regions expressed as log d501995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139666Long term depletion of Norepinephrine (NE) in Whole mouse Brain at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139836Noradrenergic effect was determined by depletion effect of Serotonin(5-HT) in mouse brain regions expressed as d501995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID1131063Neurotoxicity in Sprague-Dawley rat heart atria assessed as inhibition of [3H]norepinephrine uptake at 10 mg/kg, iv after 24 hrs by scintillation counting analysis1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Synthesis, redox characteristics, and in vitro norepinephrine uptake inhibiting properties of 2-(2-mercapto-4,5-dihydroxyphenyl)ethylamine (6-mercaptodopamine).
AID139819Long term depletion of Serotonin(5-HT) in Whole mouse Brain region of hippocampus at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID1135266Inhibition of norepinephrine release in sc dosed mouse heart administered 60 mins before [3H]-norepinephrine challenge1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
N-(2,4,5-Trihydroxyphenehtyl)normetazocine, a potential irreversible inhibitor of the narcotic receptor.
AID1807013Cytotoxicity against human differentiated SH-SY5Y cells assessed as reduction in cell viability at 100 uM measured after 48 hrs by phase contrast microscopic analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery of New Potent Positive Allosteric Modulators of Dopamine D
AID139667Long term depletion of Norepinephrine (NE) in Whole mouse Brain at a low dose (60 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID500286Inhibition of GAPDH2007Nature chemical biology, Jan, Volume: 3, Issue:1
Forward chemical genetic approach identifies new role for GAPDH in insulin signaling.
AID139818Long term depletion of Serotonin(5-HT) in Whole mouse Brain region of cortex at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139808Long term depletion of Norepinephrine (NE) in Whole mouse Brain region of hypothalamus at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139817Long term depletion of Serotonin(5-HT) in Whole mouse Brain region of cerebellum at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID1131062Pressor activity in iv dosed normotensive Sprague-Dawley rat assessed as dose required for increasing systolic blood pressure to 30 mm Hg1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Synthesis, redox characteristics, and in vitro norepinephrine uptake inhibiting properties of 2-(2-mercapto-4,5-dihydroxyphenyl)ethylamine (6-mercaptodopamine).
AID500282Inhibition of GAPDH in mouse 3T3-L1 cells assessed as 2-NBD-glucose uptake after 15 mins2007Nature chemical biology, Jan, Volume: 3, Issue:1
Forward chemical genetic approach identifies new role for GAPDH in insulin signaling.
AID175697Evaluated for the stimulation of synaptosomal release of Dopamine (release constant)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID6410Antagonistic activity against serotonin 5-HT receptor obtained from rat stomach fundus preparation (resulted in discoloration in the oxygenated muscle bath to give varying results).1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Demethyl analogues of psychoactive methoxyphenalkylamines: synthesis and serotonin receptor affinities.
AID139826Ratio of IC50 value against Serotonin transporter to that of dopamine transporter1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID360418Cytotoxicity against rat PC12 cells after 24 hrs by MTT assay2007The Journal of biological chemistry, Feb-16, Volume: 282, Issue:7
Proteasome inhibition induces glutathione synthesis and protects cells from oxidative stress: relevance to Parkinson disease.
AID182671Ability to inhibit norepinephrine uptake in rat atria was determined at 24 uM/kg1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Synthesis and physicochemical and neurotoxicity studies of 1-(4-substituted-2,5-dihydroxyphenyl)-2-aminoethane analogues of 6-hydroxydopamine.
AID139837Noradrenergic effect was determined by depletion effect of Dopamine(DA) in mouse brain regions expressed as log d501995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID139657Long term depletion of Dopamine(DA) in Whole mouse Brain region of cortex at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID1807008Neurotoxicity in human SH-SY5Y cells assessed as reduction in cell viability at 200 uM measured after 48 hrs by MTT reduction assay (Rvb= 100 +/- 2.79%)2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery of New Potent Positive Allosteric Modulators of Dopamine D
AID182679Ability to inhibit norepinephrine uptake in rat atria was determined at 73 uM/kg1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Synthesis and physicochemical and neurotoxicity studies of 1-(4-substituted-2,5-dihydroxyphenyl)-2-aminoethane analogues of 6-hydroxydopamine.
AID182672Ability to inhibit norepinephrine uptake in rat atria was determined at 243 umol/kg1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Synthesis and physicochemical and neurotoxicity studies of 1-(4-substituted-2,5-dihydroxyphenyl)-2-aminoethane analogues of 6-hydroxydopamine.
AID139823Long term depletion of Serotonin(5-HT) in Whole mouse Brain region of striatum at a high dose (300 nmol)1995Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
In vivo and in vitro studies on the neurotoxic potential of 6-hydroxydopamine analogs.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8,348)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901740 (20.84)18.7374
1990's2044 (24.48)18.2507
2000's1958 (23.45)29.6817
2010's2036 (24.39)24.3611
2020's570 (6.83)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 26.58

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 Index26.58 (24.57)
Research Supply Index9.06 (2.92)
Research Growth Index4.61 (4.65)
Search Engine Demand Index42.09 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (26.58)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (0.07%)5.53%
Reviews210 (2.43%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8,414 (97.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]