Page last updated: 2024-12-04

hydroxyindoleacetic acid

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

Description

(5-hydroxyindol-3-yl)acetic acid : A member of the class of indole-3-acetic acids that is indole-3-acetic acid substituted by a hydroxy group at C-5. [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 CID1826
CHEMBL ID395915
CHEBI ID27823
SCHEMBL ID138121
MeSH IDM0010766

Synonyms (115)

Synonym
5-hiaa
5-hydroxyheteroauxin
1h-indole-3-acetic acid, 5-hydroxy-
5-hydroxy-1h-indole-3-acetic acid
5-hydroxyindoleacetic acid
5-hydroxyindol-3-ylacetic acid
5-oxyindoleacetic acid
54-16-0
5-hydroxyindolylacetic acid
indoleacetic acid, 5-hydroxy-
nsc90432
indole-3-acetic acid, 5-hydroxy-
nsc-90432
CBMICRO_013565
5-hydroxy-indole-3-acetic acid
BB 0260171
NCIOPEN2_001406
nsc 90432
ccris 4423
brn 0168797
5-hydroxy-iaa
einecs 200-195-4
hydroxyindoleacetic acid
EU-0100636
5-hydroxyindole-3-acetic acid, >=98% (hplc), crystalline
5-hydroxy-3-indoleacetic acid
5-hydroxyindole-3-acetic acid
NCGC00015522-01
lopac-h-8876
1321-73-9
C05635
5-hydroxyindoleacetate
smr000326665
MLS000859593
LOPAC0_000636
OPREA1_139007
NCGC00094003-02
5-hydroxyindolacetic acid
NCGC00094003-01
5-hydroxyindole acetic acid
H-6200
STK501256
(5-hydroxy-1h-indol-3-yl)acetic acid
NCGC00015522-02
indole-3-acetic acid, 5-hydroxy-, 1h-
H 8876
74C13742-18FA-4D80-8B54-1B85D9463949
NCGC00015522-04
(5-hydroxyindol-3-yl)acetic acid
CHEBI:27823 ,
CHEMBL395915 ,
HID ,
1h-indoleacetic acid, hydroxy-
BMSE000364
AKOS003382389
H0355
2-(5-hydroxy-1h-indol-3-yl)acetic acid
HMS3261P14
BBL012272
2-(5-hydroxyindol-3-yl)acetic acid
HMS2230M10
NCGC00015522-03
FT-0679205
unii-yhc763jy1p
yhc763jy1p ,
5-22-05-00203 (beilstein handbook reference)
LP00636
HMS3372G16
FT-0620472
CCG-221940
SCHEMBL138121
tox21_500636
NCGC00261321-01
5-hydroxyindol-3-acetic acid
5-hydroxy-indol-3-yl-acetic acid
5-hydroxyl indole-3-acetic acid
(5-hydroxy-1h-indol-3-yl)-acetic acid
56209-31-5
(5-hydroxy-1h-indol-3-yl)acetic acid #
FD13061
mfcd00005639
5-hydroxyindole-3-acetic-2,2-d2 acid
CS-W008253
5-hydroxyindolylaceticacid
5-ho-iaa
J-006135
sr-01000075583
SR-01000075583-1
5hiaa
5-hydroxy-indole-3-acetate
5-hydroxy-3-indolylacetate
5-hydroxyindole-3-acetate
5-hydroxy-1h-indole-3-acetate
5-hydroxyindol-3-ylacetate
5-oxyindoleacetate
hydroxyindoleacetate
HY-W008253
SY012014
5-hydroxy-indole acetate
DTXSID50861582
5-hydroxyindolessigsa currencyure
DS-15683
5-hydroxyindolyacetic acid,(s)
Q238532
5-hydroxyindole-3acetic acid
SDCCGSBI-0013441.P003
NCGC00015522-08
(1-amino-1-methylpropyl)phosphonicacidhydrate
bdbm50458878
(5-hydroxy-1h-indol-3-yl)aceticacid
1h-indole-3-aceticacid,5-hydroxy-
2-(5-hydroxy-1h-indol-3-yl)acetic acid;5-hiaa
PD015273
gtpl11900
EN300-7407243

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"The biochemical mechanisms of the renal toxicity of 5-hydroxy-L-tryptophan to rats were studied using Wistar and Sprague Dawley rats, which had different LD50 values."( Biochemical studies on the mechanism of difference in the renal toxicity of 5-hydroxy-L-tryptophan between Sprague Dawley and Wistar rats.
Hirai, M; Nakajima, T, 1979
)
0.26
" Subsequently, we identified serotonin (5HT), a major platelet product, as having toxic effects on neurons."( Further studies on platelet-mediated neurotoxicity.
Grunfeld, S; Joseph, R; Tsering, C; Welch, KM, 1992
)
0.28
"Regulation of neurotoxicants is generally based on setting allowable doses (exposures) by dividing a no observed adverse effect level (NOAEL) by uncertainty factors that hopefully account for interspecies and intraspecies differences for extrapolations of experimental results obtained in animals to humans."( Risk assessment for neurotoxic effects.
Gaylor, DW; Slikker, W, 1990
)
0.28
"Dexfenfluramine, a drug prescribed for appetite suppression, was evaluated in non-human primates for its potential to produce toxic effects on brain serotonin (5-HT) neurons."( Dexfenfluramine neurotoxicity in brains of non-human primates.
Katz, JL; Martello, AL; Martello, MB; Molliver, ME; Ricaurte, GA; Wilson, MA, 1991
)
0.28
" The results support the hypothesis of a positive correlation between the CSF HVA and the hypokinetic-rigid side effect and a negative correlation between the pretherapeutic dopamine turnover and the risk of neuroleptic Parkinsonism."( Hypokinetic-rigid extrapyramidal side effects of neuroleptics: the relationship of the silent period in EMG and HVA and 5-HIAA in CSF.
Baslo, A; Eroğlu, L; Hizal, A; Yazici, J; Yazici, O, 1986
)
0.27
" The 2,2 and 3,3-dimethyl analogs of 1-methyl-4-phenyl-2,3-dihydropyridinium cation which also cannot be oxidized to pyridinium species, reduced striatal dopamine, suggesting that these compounds are toxic in their own right."( On the mechanisms underlying 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine neurotoxicity: the effect of perinigral infusion of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, its metabolite and their analogs in the rat.
Arora, PK; Blue, P; Harik, SI; Iacofano, LA; Sayre, LM; Schmidley, JW, 1987
)
0.27
" The neurochemical and histological effects of PCA are very similar to those produced by a large dose of methylamphetamine (MA) in that both drugs are toxic to serotonergic nerve terminals and neuronal perikarya in the somatosensory cortex."( Endogenously produced 5,6-dihydroxytryptamine may mediate the neurotoxic effects of para-chloroamphetamine.
Axt, KJ; Commins, DL; Seiden, LS; Vosmer, G, 1987
)
0.27
" Reserpine did not alter survival time after NMTB or ANTU and did not shift the 14-day LD50 of NMTB."( The involvement of serotonin in the pneumotoxicity induced by N-methylthiobenzamide.
Feny, FJ; Gibbs, LS; Traiger, GJ, 1988
)
0.27
"Orchiectomy is considered a safe and simple procedure, free from serious side effects, in the treatment of prostatic carcinoma."( Flushing. Long-term side effect of orchiectomy in treatment of prostatic carcinoma.
Charig, CR; Rundle, JS, 1989
)
0.28
" However, a comparison of the relative toxic effects of MDMA and MBDB indicates that MBDB may be slightly less neurotoxic."( Neurotoxic effects of the alpha-ethyl homologue of MDMA following subacute administration.
Johnson, MP; Nichols, DE, 1989
)
0.28
" Taken together, these findings indicate that concern over possible dexfenfluramine neurotoxicity in humans is warranted, and that physicians and patients alike need to be aware of dexfenfluramine's toxic potential toward brain serotonin neurons."( Dexfenfluramine and serotonin neurotoxicity: further preclinical evidence that clinical caution is indicated.
Fischer, C; Hatzidimitriou, G; Katz, J; McCann, U; Ricaurte, G; Ridenour, A; Yuan, J, 1994
)
0.29
" None of the protective drugs inhibited the initial 5-HT loss following MDMA, rendering unlikely any proposal that they are protective because they inhibit 5-HT release and the subsequent formation ofa toxic indole derivative."( A study of the mechanism of MDMA ('ecstasy')-induced neurotoxicity of 5-HT neurones using chlormethiazole, dizocilpine and other protective compounds.
Colado, MI; Green, AR, 1994
)
0.29
" The third step is to define an adverse level for a response so that the probability (risk) of exceeding that level can be estimated as a function of dose."( Modeling for risk assessment of neurotoxic effects.
Gaylor, DW; Slikker, W, 1994
)
0.29
" Together with the results of the N(G)-monomethyl-L-arginine and N(G)-nitro-L-arginine experiments, the data suggest that NO plays little or no role in the toxic mechanism of action of METH or MDMA."( Nitric oxide and the neurotoxic effects of methamphetamine and 3,4-methylenedioxymethamphetamine.
Finnegan, KT; Taraska, T, 1997
)
0.3
" The toxic dose of MA markedly increased extracellular DA, and decreased DOPAC and 5-HIAA in both ST and NA."( [Experimental study of methamphetamine psychosis--role of glutamate and nitric oxide in methamphetamine-induced dopaminergic and serotonergic neurotoxicity in the rat brain].
Abekawa, T, 1997
)
0.3
" It is thus suggested that otherwise generally safe central nervous system 5-HT-active drugs may represent a potential hazard in patients with liver failure with or without PSE."( Effect of citalopram on brain serotonin release in experimental hepatic encephalopathy: implications for thymoleptic drug safety in liver insufficiency.
Apelqvist, G; Bengtsson, F; Bergqvist, PB; Hjorth, S; Wikell, C, 1997
)
0.3
" PHEN also significantly enhanced FEN's long-term toxic effects on 5-HT axons."( Neurotoxic effects of +/-fenfluramine and phenteramine, alone and in combination, on monoamine neurons in the mouse brain.
McCann, UD; Ricaurte, GA; Yuan, J, 1998
)
0.3
" These results extend our recent findings of additive toxic effects when METH is combined with MDMA."( MDMA ('Ecstasy') and methamphetamine combined: order of administration influences hyperthermic and long-term adverse effects in female rats.
Clemens, KJ; Cornish, JL; Hunt, GE; Li, KM; McGregor, IS, 2005
)
0.33
"3,4-Methylenedioxymethamphetamine (MDMA)'s O-demethylenated metabolite, 3,4-dihydroxymethamphetamine (HHMA), has been hypothesized to serve as a precursor for the formation of toxic catechol-thioether metabolites (e."( Inhibition of 3,4-methylenedioxymethamphetamine metabolism leads to marked decrease in 3,4-dihydroxymethamphetamine formation but no change in serotonin neurotoxicity: implications for mechanisms of neurotoxicity.
Maldonado Adrian, C; McCann, UD; Mueller, M; Ricaurte, GA; Yuan, J, 2011
)
0.37
" The primary safety and efficacy endpoints were incidence of treatment-emergent adverse events (TEAEs) and percent change from baseline in 24-h u5-HIAA at week 12."( Telotristat ethyl in carcinoid syndrome: safety and efficacy in the TELECAST phase 3 trial.
Anthony, LB; Benavent, M; Fleming, D; Fleming, R; Garcia-Carbonero, R; Gross, DJ; Hörsch, D; Jiang, W; Kassler-Taub, K; Kulke, MH; Kunz, PL; Lapuerta, P; Pavel, M; Perros, P; Srirajaskanthan, R; Warner, RRP; Wason, S; Weickert, MO, 2018
)
0.48

Pharmacokinetics

ExcerptReferenceRelevance
"A series of studies on the pharmacokinetic and pharmacodynamic properties of some tricyclic antidepressants is reviewed."( Treatment of depression with tricyclic drugs--pharmacokinetic and pharmacodynamic aspects.
Asberg, M, 1976
)
0.26
" Such pharmacokinetic behavior appeared to be related to the contractive effect of morphine on the bile duct, and naloxone facilitated the excretion of morphine via this route."( Naloxone affects both pharmacokinetics and pharmacodynamics of morphine. Application of direct correlation analysis.
Ishikawa, K; Kogure, M; Kubo, T; Shibanoki, S, 1991
)
0.28
" The present studies show that pharmacokinetic variations of imipramine in the brain might correlate with the altered levels of 5-HIAA, NE and MHPG."( Correlative changes of serotonin and catecholamines with pharmacokinetic alterations of imipramine in rat brain.
Kobayashi, A; Nakazawa, K; Sugita, S; Suzuki, S; Yoshida, T, 1989
)
0.28
" The assessment of TCA actions that may be additive, synergistic, or antagonistic requires precise knowledge of pharmacodynamic potency and control of pharmacokinetic behavior."( Active metabolites of antidepressants: pharmacodynamics and relevant pharmacokinetics.
Lane, EA; Potter, WZ; Rudorfer, MV, 1984
)
0.27
"The objectives of this study were to assess potential pharmacokinetic and pharmacodynamic interactions between moclobemide and selegiline."( Pharmacokinetic-pharmacodynamic interactions between two selective monoamine oxidase inhibitors: moclobemide and selegiline.
Dingemanse, J; Kettler, R; Kneer, J; Korn, A; Koulu, M; Wallnöfer, A; Zürcher, G, 1996
)
0.29
"In order to investigate the pharmacokinetic properties of psilocybin (PY), the main psychoactive compound of Psilocybe mushrooms, high performance liquid chromatographic procedures with column-switching coupled with electrochemical detection (HPLC-ECD) for reliable quantitative determination of the PY metabolites psilocin (PI) and 4-hydroxyindole-3-acetic acid (4HIAA) in human plasma were established."( Determination of psilocin and 4-hydroxyindole-3-acetic acid in plasma by HPLC-ECD and pharmacokinetic profiles of oral and intravenous psilocybin in man.
Bär, T; Bourquin, D; Brenneisen, R; Hasler, F; Vollenweider, FX, 1997
)
0.3
" Adverse events and vital signs were recorded and pharmacokinetic parameters of fluoxetine and moclobemide were determined."( Pharmacokinetic and pharmacodynamic interactions between fluoxetine and moclobemide in the investigation of development of the "serotonin syndrome".
Amrein, R; Dingemanse, J; Gieschke, R; Guentert, T; Wallnöfer, A, 1998
)
0.3
" 3,4-Dihydroxyphenylglycol, 5-hydroxyindoleacetic acid, and 3,4-dihydroxyphenylacetic acid plasma levels and serotonin uptake did not reveal a pharmacodynamic interaction."( Pharmacokinetic and pharmacodynamic interactions between fluoxetine and moclobemide in the investigation of development of the "serotonin syndrome".
Amrein, R; Dingemanse, J; Gieschke, R; Guentert, T; Wallnöfer, A, 1998
)
0.59
" The present results suggest that brain microdialysis methods may be applicable to pharmacokinetic and pharmacodynamic studies of psychotrophic agents."( Pharmacokinetic and pharmacodynamic analyses of trazodone in rat striatum by in vivo microdialysis.
Chen, CF; Cheng, FC; Kuo, JS; Tsai, TH; Wu, YS, 1999
)
0.3
" Ketamine exerts differential pharmacodynamic effects on behavior in animals stratified according to a measure of central serotonergic turnover."( Ondansetron modulates pharmacodynamic effects of ketamine on electrocardiographic signals in rhesus monkeys.
Bennett, AJ; Dee Higley, J; DePetrillo, PB; Karimullah, K; Shoaf, SE; Speers, D; Suomi, SJ, 2000
)
0.31
" Using nonlinear modeling, standard pharmacokinetic parameters were derived."( Fluoxetine: juvenile pharmacokinetics in a nonhuman primate model.
Golub, MS; Hogrefe, CE, 2014
)
0.4

Compound-Compound Interactions

ExcerptReferenceRelevance
" In view of the observations made it is doubtful whether the therapeutic effect of 5-HTP combined with a peripheral decarboxylase inhibitor in depressions and myoclonus can in fact be atributed to activation of central serotonergic systems."( An unexpected effect of L-5 hydroxytryptophan-ethyl-ester combined with a peripheral decarboxylase inhibitor on human serum prolactin.
Korf, J; Lequin, RM; van Praag, HM, 1976
)
0.26
"5 g of levodopa daily for up to six months and in 30 patients receiving levodopa (800-1,000 mg) combined with a dopa decarboxylase inhibitor, benserazide (200-250 mg)."( Urinary excretion of monoamines and their metabolites in patients with Parkinson's disease. Response to long-term treatment with levodopa alone or in combination with a dopa decarboxylase inhibitor and clinical correlations.
Rinne, UK; Siirtola, T; Sonninen, V, 1975
)
0.25
"Thirty-one patients with malignant carcinoid tumors were treated with streptozocin--alone (n = 7) or in combination with FU (n = 24)."( Cytotoxic treatment in patients with malignant carcinoid tumors. Response to streptozocin--alone or in combination with 5-FU.
Lundqvist, G; Norheim, I; Oberg, K; Wide, L, 1987
)
0.27
"The time course of the effects of ethanol alone and in combination with the selective alpha 2-adrenoceptor agonist dexmedetomidine and the alpha-adrenoceptor antagonist atipamezole was studied in NIH-Swiss mice."( The effects of ethanol in combination with the alpha 2-adrenoceptor agonist dexmedetomidine and the alpha 2-adrenoceptor antagonist atipamezole on brain monoamine metabolites and motor performance of mice.
Björn, M; Idänpään-Heikkilä, JJ; Seppälä, T, 1995
)
0.29
" This study was conducted to evaluate parameters of serotonin metabolism following platinum-based chemotherapy given in combination with the serotonin type-3 antagonist tropisetron as an antiemetic agent."( Serotonin metabolism following platinum-based chemotherapy combined with the serotonin type-3 antagonist tropisetron.
de Vries, EG; Groenewegen, A; Kema, IP; Schröder, CP; Sleijfer, DT; van der Graaf, WT, 1995
)
0.29
" Of the 19 patients given alpha-interferon in combination with octreotide, 72% showed significant reduction in urinary 5-HIAA for a median of 10 months."( Long-term management of the carcinoid syndrome. Treatment with octreotide alone and in combination with alpha-interferon.
Janson, ET; Oberg, K, 1993
)
0.29
" Granisetron and its combination with dexamethasone for the treatment of delayed emesis following cisplatin (CDDP) administration were investigated using ferrets."( Effects of granisetron and its combination with dexamethasone on cisplatin-induced delayed emesis in the ferret.
Endo, T; Fukunaka, N; Hirafuji, M; Kudo, R; Minami, M; Sagae, S, 1998
)
0.3
"Direct-matrix derivatization in combination with LC-MS/MS is a powerful tool for the simultaneous quantification of all tryptophan-related indoles in platelet-rich plasma."( Quantitative Profiling of Platelet-Rich Plasma Indole Markers by Direct-Matrix Derivatization Combined with LC-MS/MS in Patients with Neuroendocrine Tumors.
Bouma, G; de Hosson, LD; de Vries, EGE; Kats-Ugurlu, G; Kema, IP; Peters, MAM; van Faassen, M; Walenkamp, AME, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
" The ratio of 5-HTP to carbidopa influenced the systemic bioavailability of single dose administered 5-HTP indicating dose dependent absorption kinetics."( Plasma accumulation of metabolism of orally administered single dose L-5-hydroxytryptophan in man.
Jensen, TS; Magnussen, I; Rand, JH; Van Woert, MH, 1981
)
0.26
" The bioavailability of 5-HTP after oral administration in combination with carbidopa was calculated as 48% +/- 15 (mean +/- SD)."( Kinetics of l-5-hydroxytryptophan in healthy subjects.
Gerritsen, TW; Meijer, BA; van Praag, HM; Westenberg, HG, 1982
)
0.26
" alpha MD ethyl ester administration resulted in higher alpha MD levels in CSF as compared with alpha MD administration, suggesting a higher bioavailability of the ethyl ester vs the free acid."( Determination of alphamethyldopa, dihydroxyphenylacetic acid and 5-hydroxyindolacetic acid in the cerebrospinal fluid of the rat: kinetic study.
Elghozi, JL; Laude, D; Meyer, P; Mignot, E, 1983
)
0.27
" Pharmacokinetic investigations showed that the oral bioavailability of tacrine was low and greatly varying between subjects."( Clinical experiences and biochemical findings with tacrine (THA).
Ahlin, A; Hassan, M; Junthé, T; Nybäck, H, 1993
)
0.29
" Estimates for the absolute bioavailability of PI after oral administration of PY were 52."( Determination of psilocin and 4-hydroxyindole-3-acetic acid in plasma by HPLC-ECD and pharmacokinetic profiles of oral and intravenous psilocybin in man.
Bär, T; Bourquin, D; Brenneisen, R; Hasler, F; Vollenweider, FX, 1997
)
0.3
" The pharmacokinetics of DMXAA in plasma, liver and tumour tissue indicated a bioavailability of 73%."( Oral activity and pharmacokinetics of 5,6-dimethylxanthenone-4-acetic acid (DMXAA) in mice.
Baguley, BC; Ching, LM; Kestell, P; Zhao, L, 2002
)
0.31
" Significant involution of thymus and spleen confirmed the bioavailability of the corticosterone at both dosages."( Chronic treatment with supraphysiological levels of corticosterone enhances D-MDMA-induced dopaminergic neurotoxicity in the C57BL/6J female mouse.
Johnson, EA; Miller, DB; O'Callaghan, JP, 2002
)
0.31
" Bioavailability was determined using AUC and peak plasma concentrations (C(max))."( A new formulation of selegiline: improved bioavailability and selectivity for MAO-B inhibition.
Brewer, F; Clarke, A; Corn, TH; Hartig, F; Johnson, ES; Mallard, N; Taylor, S, 2003
)
0.32
" We re-evaluated autoinhibition in single-unit recordings from deeply seated 5-hydroxytryptamine neurons in slices in which endogenous 5-hydroxytryptamine bioavailability was restored by supplementing its precursor L-tryptophan."( Differential autoinhibition of 5-hydroxytryptamine neurons by 5-hydroxytryptamine in the dorsal raphe nucleus.
Ballini, C; Corradetti, R; Della Corte, L; Mlinar, B; Nencioni, S; Tatini, F, 2005
)
0.33
" Our aim was to determine how this inflammatory lesion influenced 5-HT bioavailability and how changes in 5-HT related to the symptoms of nausea, vomiting, and diarrhea seen in untreated celiac patients."( Abnormalities of serotonin metabolism and their relation to symptoms in untreated celiac disease.
Blackshaw, E; Coleman, NS; Dunlop, SP; Foley, S; Holmes, GK; Marsden, CA; Perkins, AC; Singh, G; Spiller, RC; Wheatcroft, J, 2006
)
0.33
" Bioavailability of oral tramadol was reduced by rifampicin from 66 to 49 % (P = 0."( Rifampicin markedly decreases the exposure to oral and intravenous tramadol.
Hagelberg, NM; Laine, K; Neuvonen, M; Neuvonen, PJ; Olkkola, KT; Saari, TI; Saarikoski, T; Scheinin, M, 2013
)
0.39

Dosage Studied

Microdialysis technique was used to detect the extracellular levels of serotonin (5-HT) and its metabolite 5-hydroxyindoleacetic acid. The in vivo effects of dosing with duloxetine 60 mg once daily for 11 days in healthy subjects were assessed in 2 studies. However, the dose-response relationship between blood pressure changes and increases in brain serotonin was not related.

ExcerptRelevanceReference
" Urinary MHPG dosage seems to be one of the most interesting in this field."( [Respective position of antidepressants in therapeutics (author's transl)].
Moussaoui, D, 1979
)
0.26
" DbcAMP (in each dosage administered) decreased, NA content of cortex and of pons with medulla oblongata."( Influence of dibutyryl cyclic AMP on the level of catecholamines and 5-hydroxytryptamine in discrete areas of rat brain.
Drybański, A; Herman, ZS; Kmieciak-Kolada, K, 1977
)
0.26
" In the present trial, the 779704 combination was maintained without any alterations in dosage for six months, and the therapeutic effect persisted unchanged."( Potentiation by metyrosine of thioridazine effects in chronic schizophrenics. A long-term trial using double-blind crossover technique.
Carlsson, A; Roos, BE; Skott, A; Wålinder, J, 1976
)
0.26
" GABA both in DA- and in NA-predominated brain regions, the dose-response relations being complex."( The effect of intraperitoneally administered GABA on brain monoamine metabolism.
Biswas, B; Carlsson, A, 1977
)
0.26
" However, whereas this dosage regimen revealed a profound behavioral sensitization in response to challenge with amphetamine (2."( In vivo microdialysis reveals a diminished amphetamine-induced DA response corresponding to behavioral sensitization produced by repeated amphetamine pretreatment.
Kuczenski, R; Segal, DS, 1992
)
0.28
"The present research examined morphine dose-response effects on both the formalin test and on CNS monoamine (MA) levels and the metabolites dihydroxyphenylacetic acid (DOPAC) and 5-hydroxyindoleacetic acid (5-HIAA) in hypoalgesic (76) and hyperalgesic (SN) strains of domestic fowl."( Central monoaminergic changes induced by morphine in hypoalgesic and hyperalgesic strains of domestic fowl.
Hoganson, DA; Hughes, RA; Sufka, KJ, 1992
)
0.48
" Dose-response curves for DA and 5-HT release indicated no marked difference in the sensitivity to ethanol between the lines."( Ethanol enhances the release of dopamine and serotonin in the nucleus accumbens of HAD and LAD lines of rats.
Li, TK; Lumeng, L; McBride, WJ; Yoshimoto, K, 1992
)
0.28
" The shapes of the dose-response functions differed considerably between the drugs."( In vivo characterization of locally applied dopamine uptake inhibitors by striatal microdialysis.
Damsma, G; Fibiger, HC; Nomikos, GG; Wenkstern, D, 1990
)
0.28
" The concentration of dopamine in the arcuate nucleus-median eminence (ARC-ME) in pubertal rats significantly decreased after a lower dosage of progesterone was administered, but no change was found in the preoptic area concentration."( Effects of progesterone on concentrations of monoamines in hypothalamic areas and plasma prolactin levels in rats.
Mizoguchi, K; Tomogane, H; Yokoyama, A, 1990
)
0.28
" These results suggest that, at comparable dosage levels relative to their ED50s, fluoxetine and D-fenfluramine cause comparable reversible effects on brain serotonin release."( Effects of fluoxetine or D-fenfluramine on serotonin release from, and levels in, rat frontal cortex.
Gleason, R; Morse, AN; Sarkissian, CF; Wurtman, RJ, 1990
)
0.28
" Acute tetrahydroaminoacridine (THA) dosing caused lower brain (68%) and higher plasma (90%) ChE inhibition than the other drugs studied and increased levels of brain dihydroxyphenylacetic acid (DOPAC) (236%), homovanillic acid (HVA) (197%) and 5-hydroxyindoleacetic acid (5-HIAA) (130%)."( Effect of acute and chronic cholinesterase inhibition on biogenic amines in rat brain.
Shillcutt, S; Soininen, H; Unni, L, 1990
)
0.46
" In most animals, sexual behavior, both receptivity and proceptivity, was reduced within 60 min following the higher dosage of chlordecone."( Chlordecone (Kepone) on the night of proestrus inhibits female sexual behavior in CDF-344 rats.
Brown, HE; Salamanca, S; Stewart, G; Uphouse, L, 1991
)
0.28
"Enalapril (Renitec, Merck-Sharp-Dohne, Rahway, USA) administered alone (Group I), or in combination (Group II) in a dosage normalizing blood pressure (BP) was investigated for its ability to inhibit adrenergic and serotonergic systems in a one-year study."( Modulation of serotonergic and adrenergic systems by long-term antihypertensive treatment with enalapril.
Balazovjech, I; Dzúrik, R; Jurecková, K; Raucinová, M; Sebeková, K, 1991
)
0.28
" With the multiple dosing regimen utilized neither drug alone resulted in any changes in serotonergic parameters, including 5-HT, 5-HIAA and the number of 5-HT uptake sites."( Combined administration of a non-neurotoxic 3,4-methylenedioxymethamphetamine analogue with amphetamine produces serotonin neurotoxicity in rats.
Johnson, MP; Nichols, DE, 1991
)
0.28
"The administration to rats of tryptophan (CAS 73-22-3) in high dosage causes a significant increase in pain threshold values."( Potentiation of the analgesic effects of tryptophan by allopurinol in rats.
Malvezzi, L; Pinelli, A; Trivulzio, S; Zecca, L, 1991
)
0.28
" More importantly, if a subacute dosing regimen (every 12 hours for 4 days) was utilized, the combination of S-amphetamine with MDAI resulted in a marked long-term decrease in the levels of cortical, hippocampal and striatal 5-HT, 5-HIAA and the number of 5-HT uptake sites."( Serotonin neurotoxicity in rats after combined treatment with a dopaminergic agent followed by a nonneurotoxic 3,4-methylenedioxymethamphetamine (MDMA) analogue.
Huang, XM; Johnson, MP; Nichols, DE, 1991
)
0.28
" In 46 children from this sample it was dosed plasmatic cortisol and the urinary excretion of catecholamine, VMA, HVA and 5-HIAA."( Biochemical correlate of depression in children.
Basques, JC; Fabre, ZL; Fernandes, ML; Furtado, CR; Lippi, JR; Lombardi, AB; Peixoto, CC; Queiroz, EA; Soares, TA, 1991
)
0.28
"Amiflamine, a drug reported to be a reversible inhibitor of monoamine oxidase type A (MAO-A) selective for serotonergic neurons in rodents, was administered to rhesus monkeys over a 12-fold dosage range (0."( The effects of amiflamine on cerebrospinal fluid amine metabolites in the rhesus monkey.
Garrick, NA; Linnoila, M; Murphy, DL; Seppala, T, 1985
)
0.27
" injection of the drug at a dosage rate of 20 micrograms/kg."( Neurochemical changes in the brain and spinal cord of sheep: a basis for the immobilizing action of etorphine.
Kania, BF, 1985
)
0.27
" Dose-response relationships, examination of brain regions distant from the two injection sites and the temporal sequence of the changes described here suggest a close association between QUIN-induced neuronal degeneration and alterations in the serotonergic system."( Effects of intracerebral injections of quinolinic acid on serotonergic neurons in the rat brain.
Aldinio, C; Köhler, C; Mazzari, S; Schwarcz, R; Toffano, G, 1985
)
0.27
" Unfasted male CD-1 mice were dosed orally with 13, 130, or 650 mg/kg ASM in corn oil, while control animals received corn oil alone."( Neurobiochemical alterations induced by the artificial sweetener aspartame (NutraSweet).
Coulombe, RA; Sharma, RP, 1986
)
0.27
"Seven patients with progressive ileal or caecal carcinoid tumors and liver metastases were treated with human recombinant alpha-interferon (IFN alfa-2b) at a dosage of 2-4 x 10(6) U daily or every other day subcutaneously."( [Treatment of metastasized carcinoid tumor of the ileum and cecum with recombinant alpha-2b interferon].
Doberauer, C; Kloke, O; Kurschel, E; Niederle, N; Schmidt, CG, 1987
)
0.27
" In order to determine if MDMA produces lasting neurochemical alterations after oral administration, groups of six rats (adult male Sprague-Dawley) were dosed by gavage with either 40 or 80 mg/kg of MDMA or saline vehicle once every 12 hr for 4 days."( Neurochemical and neurohistological alterations in the rat and monkey produced by orally administered methylenedioxymethamphetamine (MDMA).
Ali, SF; Bailey, JR; Frith, CH; Newport, GD; Scallet, AC; Slikker, W, 1988
)
0.27
" The mixtures produced a dose-response decrease of free (by 34% after the lower dose and by 58% after the higher dose of the mixture) and total (by 10 and 31%) plasma tryptophan and of brain tryptophan (by 38 and 65%), serotonin (by 17 and 41%) and 5-hydroxyindole acetic acid (by 21 and 49%)."( Dose-response decrease in plasma tryptophan and in brain tryptophan and serotonin after tryptophan-free amino acid mixtures in rats.
Castoldi, D; Cipolla, P; Moja, EA; Tofanetti, O, 1989
)
0.28
" Decreases in 5-HIAA persisted throughout the chronic dosing regimen (36 days), while dopamine metabolites returned to control levels within 8 days."( Neurochemical changes in pigeon cerebrospinal fluid during chronic administration of buspirone or 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT).
Barrett, JE; Nader, MA, 1989
)
0.28
" Serum prolactin concentration increased in all subjects after L5HTP/C in comparison to placebo, mean (SD) prolactin (ng/ml) at 8 h after dosing was 19."( Effect of repeated doses of L-5-hydroxytryptophan and carbidopa on prolactin and aldosterone secretion in man.
Clementi, RA; Ferguson, RK; Rotmensch, HH; Swanson, BN; Vlasses, PH, 1989
)
0.28
"Urinary excretion of monoamine metabolites (noradrenaline-NA, adrenaline-A, 3-methoxy-4-hydroxyphenyl glycol-MHPG, homovanillic acid-HVA, 5-hydroxyindole acetic acid-5 HIAA) was studied in four groups of children as follows: Group I consisting of obese children subjected to caloric restriction and to a short term course of thyroid extract in "low" dosage (1-2 mg/kg bwt), Group II consisting of obese children subjected to diet alone, Group III consisting of children myxedema and subjected to a short term course of thyroid extract given in the "high" dosage (3-5 mg/kg bwt) and Group IV consisting of GH deficient short children having (many of them) thyrotropin deficiency and subjected to a short term course of thyroid extract in "very high" dosage (5-10 mg/bwt)."( Thyroid hormone-induced reduction of urinary 5-hydroxyindole acetic acid (5 HIAA) in obese children. Comparison with hypothyroid patients of similar age having either pituitary dwarfism or congenital myxedema.
Bartoc, R; Dimitriu, V; Dumitriu, L; Popa, M; Stefănescu, AM,
)
0.13
" Lumbar punctures were carried out prior to treatment and at the end of each dosage regimen and cerebrospinal fluid (CSF) evaluated for concentrations of free and total GABA, homocarnosine (GABA-histidine dipeptide), homovanillic acid (HVA), 5-hydroxyindole acetic acid (5-HIAA) and vigabatrin."( The effect of different vigabatrin treatment regimens on CSF biochemistry and seizure control in epileptic patients.
Ben-Menachem, E; Dahlgren, L; Haegele, KD; Hardenberg, J; Huebert, N; Mumford, JP; Persson, LI; Schechter, PJ, 1989
)
0.28
" L-DOPA administration, consisting of a daily dosage of 600 mg plus 150 mg aromatic L-amino acid decarboxylase inhibitor was continued in all cases for at least 3 months."( Unresponsiveness to L-DOPA in parkinsonian patients: a study of homovanillic acid concentration in the cerebrospinal fluid.
Araki, H; Kondo, T; Muramoto, S; Narabayashi, H; Nishi, K; Takubo, H, 1989
)
0.28
"The possible neurotoxic effects of the alpha-ethyl homologue of MDMA, N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (MBDB), were examined following a regimen of twice daily dosing for four days."( Neurotoxic effects of the alpha-ethyl homologue of MDMA following subacute administration.
Johnson, MP; Nichols, DE, 1989
)
0.28
" The results suggest, the BH4 in the dosage used, is not effective in the treatment of Parkinson's disease."( Tetrahydrobiopterin and Parkinson's disease.
Dissing, IC; Gerdes, AM; Güttler, F; Lou, H; Lykkelund, C; Pakkenberg, H; Rasmussen, V, 1989
)
0.28
" There was no dose-response effect of sulpiride on serum levels of the monoamine metabolites or the amino acids."( Monoamine metabolites and amino acids in serum from schizophrenic patients before and during sulpiride treatment.
Alfredsson, G; Wiesel, FA, 1989
)
0.28
"The authors investigated the cerebral metabolism of tryptophan in patients suffering from malignant pain by means of CSF dosage of tryptophan (Trp), 5-hydroxytryptophan (5-HTP), serotonin (5-HT) and 5-hydroxyindoleacetic acid (5-HIAA)."( Cerebral tryptophan metabolism in humans in relation to malignant pain.
Allegri, G; Ceccherelli, F; Costa, C; Giron, G; Ischia, A; Ischia, S,
)
0.32
"50 pmol/ml) did not change after 1 wk of Li dosing (1."( Differences in lithium effects in depressed and healthy subjects.
Karoum, F; Linnoila, M; Potter, WZ; Ross, RJ; Rudorfer, MV, 1985
)
0.27
" Treatment of reserpinized rats with pargyline, a non-selective inhibitor of monoamine oxidase, in order to increase cerebral 5-HT levels, shifts the PCA dose-response curve for inducing the 5-HT behavioural syndrome to the left."( 5-Hydroxytryptamine release in vivo from a cytoplasmic pool: studies on the 5-HT behavioural syndrome in reserpinized rats.
Kuhn, DM; Wolf, WA; Youdim, MB, 1985
)
0.27
" The dosage of both zimeldine and alaproclate was 200 mg daily."( Alaproclate a novel antidepressant? A biochemical and clinical comparison with zimeldine.
Aberg-Wistedt, A; Alvariza, M; Bertilsson, L; Malmgren, R; Wachtmeister, H, 1985
)
0.27
" Neither homovanillic acid nor 5-hydroxyindoleacetic acid concentrations changed significantly when 15 mg folic acid was given in divided dosage for one, two, and four weeks."( Effect of folic acid by mouth on cerebrospinal fluid homovanillic acid and 5-hydroxyindoleacetic acid concentration.
Barnes, J; Curzon, G; Duncan, C; Hunter, R; Kantamaneni, BD, 1971
)
0.76
"Biogenic amines in pons and striatum have been dosed in twenty-four months old Wistar male rats."( [Biochemical changes in 24-month-old Wistar rats].
Della Zuana, O; Duhault, J; Lonchampt, M; Roman, F; Saint Romas, G, 1984
)
0.27
" The dosage of urinary MHPG seems to be a valuable index for the choice of the drug."( [Therapeutic implications of the biochemical features about depressive illness (author's transl)].
Lôo, H, 1981
)
0.26
" The treatment inhibited mitochondrial monoamine oxidase activity of all three brain regions studied, although a dose-response inhibitory effect was found only in the mesencephalon."( Brain monoamine oxidase activity after in vivo-chronic iprindole treatment.
Carranza, J; Castro-Osuna, G; Esparza-Avalos, NS; Guzmán-Amaya, P; Ortega-Corona, BG; Sosa, A, 1981
)
0.26
"In a single-blind study, 12 men (mean age 63 years) with senile dementia were given nafronyl in a dosage of 100 mg eight times daily for a week, followed by 100 mg four times daily for 12 weeks."( Effect of nafronyl on lactate and pyruvate in the cerebrospinal fluid of patients with senile dementia.
Berger, PA; Hollister, LE; Tinklenberg, JR; Yesavage, JA, 1982
)
0.26
" The controls were comprised of naive rats (G-VI) and naive rats dosed in the same manner as the dependent rats."( Participant of serotonin turnover rate in the brain on barbital withdrawal convulsion.
Hiramori, T; Nakao, K; Tagashira, E; Urano, T; Yanaura, S, 1982
)
0.26
" In polyphasic sleepers like cats, we did not observe tryptophan's hypnotic effect with any dosage used (10, 30 or 135 mg/kg)."( L-Tryptophan's effects on brain chemistry and sleep in cats and rats: a review.
Radulovacki, M, 1982
)
0.26
" (+)-TCP at high dosage (30 mg/kg) decreased brain levels of 5-HIAA, whereas (-)-TCP failed to affect 5-HIAA levels."( Stereoselective effect of tranylcypromine enantiomers on brain serotonin.
Petersen, HN; Smith, DF, 1982
)
0.26
" However, the dose-response relationship between blood pressure changes and increases in brain serotonin and 5-hydroxyindoleacetic acid content produced by L-tryptophan was not related."( Effects of L-tryptophan on blood pressure in normotensive and hypertensive rats.
Kuhn, DM; Wolf, WA, 1984
)
0.48
"To establish dose-response relationships for nicotine (acute and subacute administration), we measured hemodynamic parameters as well as circulating and tissue catecholamines in sympathetically innervated organs in rats."( Changes in peripheral and central catecholaminergic and serotoninergic neurons of rats after acute and subacute administration of nicotine.
Dominiak, P; Grobecker, H; Kees, F, 1984
)
0.27
" Pretreatment with 5,7-dihydroxytryptamine (5,7-DHT) suppressed the allylnitrile-induced head twitching, and decreased the contents of 5-HT and 5-HIAA in almost all areas of the brain throughout the observation period, as well as the ratio of 5-HIAA/5-HT in the medulla oblongata plus pons from 1 to 30 days after dosing with allylnitrile."( Involvement of noradrenergic and 5-hydroxytryptaminergic systems in allylnitrile-induced head twitching.
Hashimoto, K; Huang, J; Tanii, H, 1993
)
0.29
" Dose escalation was required in order to control carcinoid symptoms, and the final dosage was 5,950 micrograms/day."( Long-term survival in a patient with malignant carcinoid treated with high-dose octreotide.
Deguchi, H; Deguchi, K; Iwasaki, E; Kobayashi, T; Murashima, S; Shirakawa, S; Tsuda, M; Tsukada, T, 1994
)
0.29
" We hypothesized that selegiline, at a dosage of 60 mg/d, would be at least partially effective but that the higher doses would not maintain the monoamine oxidase B selectivity observed with the lower doses of selegiline."( High-dose selegiline in treatment-resistant older depressive patients.
Cohen, RM; Lawlor, BA; Mellow, AM; Molchan, S; Mueller, EA; Murphy, DL; Newhouse, PA; Sunderland, T; Tariot, PN, 1994
)
0.29
"3 years) entered a double-blind, randomized, crossover study of placebo vs 3 weeks of selegiline at a dosage of 60 mg/d."( High-dose selegiline in treatment-resistant older depressive patients.
Cohen, RM; Lawlor, BA; Mellow, AM; Molchan, S; Mueller, EA; Murphy, DL; Newhouse, PA; Sunderland, T; Tariot, PN, 1994
)
0.29
" Population values for the model parameters were obtained by a two-stage method allowing for repeated dosing per subject."( Monoamine oxidase-A: pharmacodynamics in humans of moclobemide, a reversible and selective inhibitor.
Banken, L; Dingemanse, J; Guentert, TW; Holford, NH, 1994
)
0.29
" To determine if anticonvulsant doses of loreclezole increase extracellular serotonin, we determined anticonvulsant dose-response relationships in genetically epilepsy-prone rats (GEPRs)."( The anticonvulsant effect of the broad spectrum anticonvulsant loreclezole may be mediated in part by serotonin in rats: a microdialysis study.
Dailey, JW; Jo, M; Jobe, PC; Ko, KH; Seo, DO; Yan, QS, 1994
)
0.29
" REM sleep was suppressed irrespective of the dosage given."( Depletion of brain serotonin by 5,7-DHT: effects on the 8-OH-DPAT-induced changes of sleep and waking in the rat.
Jantos, H; Monti, JM; Prunell, G; Reyes-Parada, M; Scorza, C; Silveira, R, 1994
)
0.29
" In the second phase of this study the same 12 PDD patients were treated with GAP at a daily dosage of 250 lipasemic-releasing units for a period of 1 month and it was found that all four biochemical parameters shifted towards normal values during therapy with the changes in CSF 5-hydroxy-indole acetic acid levels attaining statistical significance."( Glycosaminoglycan polysulfate in primary degenerative dementia. Pilot study of biologic and clinical effects.
Ban, TA; Parnetti, L; Senin, U, 1995
)
0.29
"The serotonin uptake inhibitor fluvoxamine was assessed in treatment of alcohol-induced Korsakoff's syndrome (KS) using fixed (4 weeks, 200 mg/day) or individualized (6 weeks, plasma concentration > or = 400 ng/ml) dosing in randomized placebo-controlled double-blind crossover studies."( Fluvoxamine treatment of alcoholic amnestic disorder.
Adinoff, B; Bone, GA; Eckardt, MJ; Lane, E; Linnoila, M; Martin, PR; Stapleton, JM; Weingartner, H, 1995
)
0.29
" The current study evaluated the dose-response relationships of MDMA (1."( Oral administration of 3,4-methylenedioxymethamphetamine (MDMA) produces selective serotonergic depletion in the nonhuman primate.
Ali, SF; Bailey, JR; Binienda, Z; Ferguson, SA; Newport, GD; Paule, MG; Scallet, AC; Slikker, W,
)
0.13
" Additional studies are also needed to determine whether such changes represent a threshold effect of the steroid or a dose-response function."( Effects of chronic corticosterone ingestion on spatial memory performance and hippocampal serotonergic function.
Luine, VN; McEwen, BS; Spencer, RL, 1993
)
0.29
" After an initial acute dose-response assessment, escalating doses of MDMA (0."( Behavioral and neurochemical effects of chronic methylenedioxymethamphetamine (MDMA) treatment in rhesus monkeys.
Ali, SF; Allen, RR; Frederick, DL; Gillam, MP; Paule, MG; Slikker, W,
)
0.13
" The patient was submitted also to the following examination: 1) urinary dosage of 5 HIAA; 2) urinary dosage of 5 OHT; 3) Computed tomography of the abdomen; 4) Heart echography; 5) Endoscopy of the colon; 6) Endoscopy of the bronchus."( [Gastric carcinoid. A clinical case and review of the literature].
Capece, G; Conte, S; Luongo, M, 1996
)
0.29
"Diagnosis is based on urinary dosage of 5-HIAA (n."( [Gastric carcinoid. A clinical case and review of the literature].
Capece, G; Conte, S; Luongo, M, 1996
)
0.29
" The pharmacokinetic parameters of moclobemide and its metabolites changed on multiple dosing but were not influenced to a relevant extent by concomitant administration of selegiline."( Pharmacokinetic-pharmacodynamic interactions between two selective monoamine oxidase inhibitors: moclobemide and selegiline.
Dingemanse, J; Kettler, R; Kneer, J; Korn, A; Koulu, M; Wallnöfer, A; Zürcher, G, 1996
)
0.29
" Generalized tonic-clonic seizures observed in EP mice were inhibited by valproate, administered 1 h prior to testing, in a dose-response fashion."( Effects of valproate on amino acid and monoamine concentrations in striatum of audiogenic seizure-prone Balb/c mice.
Alexiuk, NA; Vriend, JP, 1996
)
0.29
" However, multiple dosing of moclobemide did not lead the excessive accumulation."( Pharmacokinetic and pharmacodynamic interactions between fluoxetine and moclobemide in the investigation of development of the "serotonin syndrome".
Amrein, R; Dingemanse, J; Gieschke, R; Guentert, T; Wallnöfer, A, 1998
)
0.3
" The repeated FEN dosing regimen dramatically reduced (> 50%) postmortem 5-HT levels in the mediobasal hypothalamus, basolateral amygdala, and hippocampus, while the lateral hypothalamus was unaffected."( In vivo correlates of central serotonin function after high-dose fenfluramine administration.
Ayestas, MA; Baumann, MH; Rothman, RB, 1998
)
0.3
" A review of the patient's file revealed that during the 3 weeks prior to the MI, she had been treated inadvertently with a fivefold lower dosage of octreotide."( Coronary vasospasm associated with uncontrolled carcinoid tumour.
Ben-Yehuda, A; Lotan, C; Muszkat, M; Shalit, M, 2000
)
0.31
" Surprisingly, no significant changes in striatal 5-HT or its metabolite were observed following the same dosage and time course."( Pharmacokinetic and pharmacodynamic analyses of trazodone in rat striatum by in vivo microdialysis.
Chen, CF; Cheng, FC; Kuo, JS; Tsai, TH; Wu, YS, 1999
)
0.3
" Rats that did not become hyperthermic when dosed with 15 mg/kg AMPH in a cold environment (10 degrees C) exhibited some hyperactivity and stereotypic behavior, but not overt convulsive behavior."( Seizure activity and hyperthermia potentiate the increases in dopamine and serotonin extracellular levels in the amygdala during exposure to d-amphetamine.
Bowyer, JF; Tor-Agbidye, J; Yamamoto, B, 2001
)
0.31
"Establishing functional deficits as a result of neurotoxic dosing regimens of MDMA has been difficult."( Effects of fenfluramine, m-CPP and triazolam on repeated-acquisition in squirrel monkeys before and after neurotoxic MDMA administration.
Delatte, MS; McCann, UD; Moerschbaecher, JM; Ricaurte, GA; Stevenson, MW; Winsauer, PJ; Yuan, J, 2002
)
0.31
" This dosing regimen causes substantial striatal dopamine depletion in mice."( 2'-NH(2)-MPTP [1-methyl-4-(2'-aminophenyl)-1,2,3,6-tetrahydropyridine] depletes serotonin and norepinephrine in rats: a comparison with 2'-CH(3)-MPTP [1-methyl-4-(2'-methylphenyl)-1,2,3,6-tetrahydropyridine].
Andrews, AM; Mazzola-Pomietto, P; Murphy, DL; Unger, EL, 2002
)
0.31
" The remaining animals were dosed ip with 0 (corn oil vehicle; 2 ml/kg), 100, 200, or 400 mg/kg CS2."( Disassociation of carbon disulfide-induced depression of flash-evoked potential peak N166 amplitude and norepinephrine levels.
Graff, JE; Herr, DW, 2003
)
0.32
" In the present study, we determined the effect of high-dose D-FEN or PCA, administered according to a "neurotoxic" dosing regimen, on the density of SERT sites using ligand binding methods and on SERT protein levels using Western blots."( High-dose fenfluramine administration decreases serotonin transporter binding, but not serotonin transporter protein levels, in rat forebrain.
Baumann, MH; Cadet, JL; Dersch, CM; Jayanthi, S; Prisinzano, T; Rice, KC; Rothman, RB; Wang, X, 2003
)
0.32
" Similarly to what has been reported concerning nicotine, the dose-response curve of epibatidine to increase the dopamine output in the caudate-putamen was bell-shaped and clearly differed from that in the accumbens."( Comparison of the effects of nicotine and epibatidine on the striatal extracellular dopamine.
Ahtee, L; Janhunen, S, 2004
)
0.32
"The technique of 'binge' dosing (several doses in one session) by recreational users of 3,4-methylenedioxymethamphetamine (MDMA, ecstasy) requires evaluation in terms of its consequences on the acute hyperthermic response and long-term neurotoxicity."( Effect of repeated ('binge') dosing of MDMA to rats housed at normal and high temperature on neurotoxic damage to cerebral 5-HT and dopamine neurones.
Colado, MI; Elliott, JM; Green, AR; O'shea, E; Saadat, KS; Sanchez, V, 2004
)
0.32
" This dosing regimen also produces deficits in sequential learning as measured in the Cincinnati water maze (CWM)."( Metyrapone attenuates the sequential learning deficits but not monoamine depletions following d,l-fenfluramine administration to adult rats.
Blankenmeyer, TL; Brown-Strittholt, CA; Gudelsky, GA; Skelton, MR; Vorhees, CV; Williams, MT, 2004
)
0.32
" Dose-response curves created with 8-OH DPAT for the serotonin behavioral syndrome were similar in bile duct-resected and sham-operated rats."( Fatigue of cholestasis and the serotoninergic neurotransmitter system in the rat.
Bozdayi, AM; Bozkaya, H; Celik, T; Cinar, K; Gören, MZ; Gürdal, H; Onder, FO; Tan, A; Terzioğlu, B; Uzunalimoğlu, O; Yurdaydin, C, 2005
)
0.33
" In order to evaluate the anabolic or toxic effects of the dosing regimens used, selected peripheral effects were monitored as well."( The effect of sub-chronic nandrolone decanoate treatment on dopaminergic and serotonergic neuronal systems in the brains of rats.
Ellermaa, S; Kankaanpää, A; Karila, T; Kurling, S; Seppälä, T, 2005
)
0.33
" A combined therapy with the addition of interferon-a was initiated in pts in whom, despite the increase of drug dosage and the shortening of administration intervals, a complete clinical and biochemical response was no more achieved with Somatostatin analogues alone."( Current diagnosis and treatment of gastrointestinal carcinoids in a series of 101 patients: the significance of serum chromogranin-A, somatostatin receptor scintigraphy and somatostatin analogues.
Giannatou, E; Lygidakis, NJ; Mallas, E; Nikou, GC; Pavlatos, S; Safioleas, M; Toubanakis, C; Tseleni-Balafouta, S,
)
0.13
" For this purpose, neuronal activity was measured in rats with rivastigmine-induced elevated ACh levels after a 95% 5-HT depletion obtained by dosing p-chlorophenylalanine followed by D,L-fenfluramine."( Serotonin depletion results in a decrease of the neuronal activation caused by rivastigmine in the rat hippocampus.
Aznar, S; Knudsen, GM; Kornum, BR; Moller, A; Ronn, LC; Weikop, P, 2006
)
0.33
" A more intensive dosing regimen (10 or 20 mg/kg twice daily for 4 days) was used to examine PMA/MDMA effects on cortical 5-HT content."( Repeated administration of the substituted amphetamine p-methoxyamphetamine produces reductions in cortical 5-HT transporter binding but not 5-HT content, unlike 3,4-methylenedioxyamethamphetamine.
Callaghan, PD; Daws, LC; Farrand, K; Hughes, P; Irvine, RJ; Salem, A, 2006
)
0.33
" Finally, after determination of basal levels of 3,4-dihydroxyphenylacetic acid (DOPAC), homovanillic acid (HVA), and 5-hydroxyindole-3-acetic acid (5-HIAA) in the rats, the rats were dosed with benserazide followed by l-3,4-dihydroxyphenylalanine (l-DOPA)."( Evaluation of an osmotic pump for microdialysis sampling in an awake and untethered rat.
Cooper, JD; Davies, MI; Heppert, KE; Lunte, SM, 2007
)
0.34
" Time of diagnosis, dosage of BH4 and neurotransmitter precursors, folinic acid substitution, and levels of 5-hydroxyindoleacetic acid (5HIAA) and homovanillic acid (HVA) in cerebrospinal fluid (CSF) are essential parameters in the follow-up of patients."( Outcome and long-term follow-up of 36 patients with tetrahydrobiopterin deficiency.
Ballhausen, D; Baumgartner, MR; Blau, N; Fiori, L; Giovannini, M; Hoffmann, GF; Ibel, H; Jäggi, L; Ponzone, A; Porta, F; Santer, R; Schuler, A; Wendel, U; Zurflüh, MR, 2008
)
0.56
" BSA-guided dosing is important."( Population pharmacokinetic-pharmacodynamic model of the vascular-disrupting agent 5,6-dimethylxanthenone-4-acetic acid in cancer patients.
Baguley, BC; Baker, SD; Jameson, MB; Li, J; Pili, R, 2008
)
0.35
"The purpose of the current study was to extend previous results on the acute effects of MDMA on behavioral thermoregulation to a repeated dosing regime, simulating regular weekend use of ecstasy, on measures of thermoregulation and heart rate (HR)."( The effect of long-term repeated exposure to 3,4-methylenedioxymethamphetamine on cardiovascular and thermoregulatory changes.
Irvine, RJ; Jaehne, EJ; Salem, A, 2008
)
0.35
" HR responses to MDMA over 6 weeks at both TAs progressively decreased with repeated dosing (P<0."( The effect of long-term repeated exposure to 3,4-methylenedioxymethamphetamine on cardiovascular and thermoregulatory changes.
Irvine, RJ; Jaehne, EJ; Salem, A, 2008
)
0.35
" This study was undertaken to examine effects of a long-term dosing regimen with selective MAOIs on cocaine and food reward."( Chronic treatment with monoamine oxidase-B inhibitors decreases cocaine reward in mice.
Cherng, CG; Chiang, CY; Chuang, JY; Ho, MC; Kao, SF; Tsai, YP; Yu, L, 2009
)
0.35
" JCM-16021 treatment significantly reduced the 5-HT concentrations (from high, middle and low dosage groups: 60."( Analgesic effects of JCM-16021 on neonatal maternal separation-induced visceral pain in rats.
Bian, ZX; Han, QB; Sung, JJ; Xu, HX; Zhang, M, 2010
)
0.36
" Microdialysis technique was used to detect the extracellular levels of serotonin (5-HT) and its metabolite 5-hydroxyindoleacetic acid (5-HIAA) in rat brain following the acute administration of the extract dosed at 100mg/kg."( Influence of Griffonia simplicifolia on male sexual behavior in rats: behavioral and neurochemical study.
Benelli, A; Carnevale, G; Di Viesti, V; Zanoli, P; Zavatti, M, 2011
)
0.58
" THC unexpectedly produced a modest hyperthermic effect when administered alone, but in animals co-treated with both THC and MDMA, there was an attenuation of MDMA-induced hyperthermia on dosing days."( Chronic administration of THC prevents the behavioral effects of intermittent adolescent MDMA administration and attenuates MDMA-induced hyperthermia and neurotoxicity in rats.
Ali, SF; Meyer, JS; Shen, EY, 2011
)
0.37
"Twenty-one adult female cynomolgus monkeys were housed in small, stable social groups, trained to participate in oral dosing, and began a 5-week cumulative dose-response study."( Sertraline effects on cerebrospinal fluid monoamines and species-typical socioemotional behavior of female cynomolgus monkeys.
Higley, JD; Register, TC; Shively, CA; Willard, SL, 2014
)
0.4
" Here, the in vivo effects of dosing with duloxetine 60 mg once daily for 11 days in healthy subjects were assessed in 2 studies: (1) centrally (n = 11), by measuring concentrations of 5-hydroxyindoleacetic acid, 3,4-dihydroxyphenylglycol (DHPG), and NE in cerebrospinal fluid, and (2) versus escitalopram 20 mg/d (n = 32) in a 2-period crossover study by assessing the ΔDHPG/ΔNE ratio in plasma during orthostatic testing and by pharmacokinetic/pharmacodynamic modeling of reuptake inhibition using subjects' serum in cell lines expressing cloned human 5-HTT or NET."( Effects of duloxetine on norepinephrine and serotonin transporter activity in healthy subjects.
Chappell, JC; Dean, RA; Detke, MJ; Eisenhofer, G; Haber, H; Iyengar, S; Knadler, MP; Lachno, DR; Lobo, ED; Mitchell, MI; Nemeroff, CB; Owens, MJ; Pangallo, B, 2014
)
0.59
"5-year-old rhesus monkeys, n = 6) received single administration of doses of 1, 2, and 4 mg/kg day fluoxetine on a background of chronic dosing at an intermediate level to provide steady-state conditions to model therapeutic administration."( Fluoxetine: juvenile pharmacokinetics in a nonhuman primate model.
Golub, MS; Hogrefe, CE, 2014
)
0.4
" A dosage of 2 mg/kg day given over a 14-week period led to steady-state serum concentrations of active agent (fluoxetine + norfluoxetine) similar to those recorded from drug monitoring studies in children."( Fluoxetine: juvenile pharmacokinetics in a nonhuman primate model.
Golub, MS; Hogrefe, CE, 2014
)
0.4
" Behavioral deficits at the end of the 14-day dosing regime and on day 28 (i."( Noradrenergic and serotonergic neurochemistry arising from intranasal inoculation with α-synuclein aggregates which incite parkinsonian-like symptoms.
Davydova, TV; Fomina, VG; Gruden, MA; Kudrin, VS; Morozova-Roche, LA; Narkevich, VB; Sewell, RD; Wang, C, 2015
)
0.42
" depression), so these results should be complied in analgesic dosage adjustment."( Impairment in Pain Perception in Adult Rats Lesioned as Neonates with 5.7-Dihydroxytryptamine.
Lewkowicz, Ł; Malinowska-Borowska, J; Muchacki, R; Nowak, PG; Szkilnik, R; Żelazko, A,
)
0.13
" Here, we employ the same alcohol dosing regimen, where zebrafish eggs are immersed into 0% or 1% (vol/vol) alcohol for 2 h, but we perform the immersion at 5, 10, 16, 24, 36, or 48 hpf."( Developmental stage-dependent deficits induced by embryonic ethanol exposure in zebrafish: A neurochemical analysis.
Bailleul, C; Chatterjee, D; Facciol, A; Gerlai, R; Nguyen, S, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
drug metabolitenull
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
mouse metaboliteAny mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus).
[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 (1)

ClassDescription
indole-3-acetic acidsAn indol-3-yl carboxylic acid in which the carboxylic acid specified is acetic acid.
[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 (14)

PathwayProteinsCompounds
Neuronal System16650
Transmission across Chemical Synapses12250
Neurotransmitter clearance725
Clearance of seratonin313
Metabolism of serotonin211
Tryptophan Metabolism1855
Tryptophan degradation ( Tryptophan degradation )6454
Neurotransmitter clearance in synaptic cleft022
Melatonin metabolism and effects016
Biochemical pathways: part I0466
Amino acid metabolism094
Biosynthesis and regeneration of tetrahydrobiopterin and catabolism of phenylalanine1519
Neurotransmitter disorders819
Sudden infant death syndrome (SIDS) susceptibility pathways07

Protein Targets (29)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
endonuclease IVEscherichia coliPotency2.23870.707912.432431.6228AID1708
thioredoxin reductaseRattus norvegicus (Norway rat)Potency22.25290.100020.879379.4328AID488773; AID588453; AID588456
Fumarate hydrataseHomo sapiens (human)Potency17.78280.00308.794948.0869AID1347053
USP1 protein, partialHomo sapiens (human)Potency0.15850.031637.5844354.8130AID743255
NFKB1 protein, partialHomo sapiens (human)Potency5.62340.02827.055915.8489AID895; AID928
GLS proteinHomo sapiens (human)Potency1.58490.35487.935539.8107AID624146
Smad3Homo sapiens (human)Potency35.48130.00527.809829.0929AID588855
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency3.16230.001318.074339.8107AID926; AID938
hypothetical protein, conservedTrypanosoma bruceiPotency16.94410.223911.245135.4813AID624147
regulator of G-protein signaling 4Homo sapiens (human)Potency21.19230.531815.435837.6858AID504845
polyproteinZika virusPotency17.78280.00308.794948.0869AID1347053
alpha-galactosidaseHomo sapiens (human)Potency12.58934.466818.391635.4813AID2107
IDH1Homo sapiens (human)Potency18.35640.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency12.13960.035520.977089.1251AID504332
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency42.561523.934123.934123.9341AID1967
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.81070.00636.904339.8107AID883
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency22.38720.001815.663839.8107AID894
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency50.11870.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency29.93490.006026.168889.1251AID488953
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency11.22020.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency11.22020.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency11.22020.15855.287912.5893AID540303
gemininHomo sapiens (human)Potency18.57460.004611.374133.4983AID624296; AID624297
M-phase phosphoprotein 8Homo sapiens (human)Potency26.67950.177824.735279.4328AID488949
lamin isoform A-delta10Homo sapiens (human)Potency35.48130.891312.067628.1838AID1459
neuropeptide S receptor isoform AHomo sapiens (human)Potency3.16230.015812.3113615.5000AID1461
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.81070.00638.235039.8107AID883
[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)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (6)

Processvia Protein(s)Taxonomy
negative regulation of inflammatory response to antigenic stimulusUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
oligodendrocyte differentiationUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
chemokine-mediated signaling pathwayUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
positive regulation of Rho protein signal transductionUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
chemokine receptor activityUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
receptor serine/threonine kinase bindingUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
G protein-coupled receptor activityUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
plasma membraneUracil nucleotide/cysteinyl leukotriene receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (89)

Assay IDTitleYearJournalArticle
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
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.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347347UWB1.289 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347361HEK293 12hr Apoptosis Induction qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347352COV-362 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347396qHTS for inhibitors of Wild type Zika virus screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347379qHTS for Inflammasome Signaling Inhibitors: IL-1-beta AlphaLISA screen against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347394Vero-766 cells viability qHTS against the NCATS CANVASS Library: Counterscreen for Zika virus inhibition assay2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347374qHTS for Hypoxia signaling pathway (HIF-1) antagonists against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347373qHTS for Constitutive Androstane Receptor (CAR) Agonist screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347351U-118MG Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347346HPAF-II Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347378qHTS for H2AX Agonists against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347400Viability qHTS for inhibitors of the SERCaMP assay screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347393qHTS for inhibitors of ER calcium dysfunction: SERCaMP assay screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347362Diaphorse counterscreen qHTS: Assay Interference Panel against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347402qHTS for inhibitors of Rabies Virus screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347370qHTS for ATAD5 Antagonist screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347350SW1088 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347363Firefly luciferase counterscreen qHTS: Assay Interference Panel against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347381Inflammasome Signaling qHTS Counterscreen: IL-1-beta AlphaLISA counterscreen against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347365SDT Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347353A2780 Cisplatin Sensitive Ovarian Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347357HEK293 18hr Apoptosis Induction qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347391qHTS for activators of Nrf2/ARE signaling pathway screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347359HEK293 24hr Apoptosis Induction qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347392qHTS for activators of dead-cell proteases activity screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347390Secretion counterscreen for inhibitors of the SERCaMP assay screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347366KB-3-1 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347349Panc-1005 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347389qHTS assay for small molecule disruptors of mitochondrial membrane potential screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347388qHTS for Activators of p53 Stress Response Pathway screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347380qHTS for Antimalaria activity screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347345OV-KATE Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347356HPAF-II 24hr Apoptosis Induction qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347387Cytotoxicity qHTS for assessment of Hepg2 cells membrane integrity screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347401Redox Reaction Profiling qHTS: Assay Interference Panel against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347364KB-8-5-11 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347371J3T Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID134737610-beta competent E. coli microbial cell viability qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347348OV-SAHO Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347358HPAF-II 12hr Apoptosis Induction qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347355HEK-293 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347367qHTS for ATAD5 Agonist screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347160Primary screen NINDS Rhodamine 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.
AID1347369MCF7 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347354UWB1.289-WTBRCA1 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347372qHTS for Constitutive Androstane Receptor (CAR) Antagonist screened against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347360HPAF-II 18hr Apoptosis Induction qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347375qHTS for Hypoxia signaling pathway (HIF-1) agonists against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347377DH5-alpha competent E. coli microbial cell viability qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1347368G06 Cancer Cell Toxicity qHTS against the NCATS CANVASS Library2018ACS central science, Dec-26, Volume: 4, Issue:12
Canvass: A Crowd-Sourced, Natural-Product Screening Library for Exploring Biological Space.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID681410TP_TRANSPORTER: inhibition of Indoxyl sulfate uptake (Indoxyl sulfate: 2 uM, 5-Hydroxyindole acetic acid: 1000 uM) in Xenopus laevis oocytes2002Journal of neurochemistry, Oct, Volume: 83, Issue:1
Role of blood-brain barrier organic anion transporter 3 (OAT3) in the efflux of indoxyl sulfate, a uremic toxin: its involvement in neurotransmitter metabolite clearance from the brain.
AID296505Octanol-water partition coefficient, log Kow of the compound2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Binding of ring-substituted indole-3-acetic acids to human serum albumin.
AID1385404Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization at >30 nM after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
AID1385398Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of MDL 29,951-induced calcium mobilization after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
AID296506Binding affinity to human serum albumin2007Bioorganic & medicinal chemistry, Jul-01, Volume: 15, Issue:13
Binding of ring-substituted indole-3-acetic acids to human serum albumin.
AID682179TP_TRANSPORTER: inhibition of benzylpenicillin uptake by 5-Hydroxyindole-3-acetic acid at a concentration of 1000uM in Oat3-expressing oocyte cells2004The Journal of pharmacology and experimental therapeutics, Jun, Volume: 309, Issue:3
Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1385400Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of calcium mobilization at >30 uM after 1 hr by Oregon Green BAPTA-1/AM dye-based fluorescence assay relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8,418)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904737 (56.27)18.7374
1990's1981 (23.53)18.2507
2000's1013 (12.03)29.6817
2010's555 (6.59)24.3611
2020's132 (1.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 66.99

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index66.99 (24.57)
Research Supply Index9.13 (2.92)
Research Growth Index4.23 (4.65)
Search Engine Demand Index122.06 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (66.99)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials322 (3.61%)5.53%
Reviews334 (3.75%)6.00%
Case Studies255 (2.86%)4.05%
Observational2 (0.02%)0.25%
Other7,998 (89.75%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]