Page last updated: 2024-12-06

remoxipride

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Description

Remoxipride is a dopamine D2 receptor antagonist with high affinity for D2 receptors, particularly in the mesolimbic pathway. It is studied for its potential therapeutic effects in treating conditions like schizophrenia, Tourette syndrome, and alcohol withdrawal syndrome. However, remoxipride has been associated with adverse effects such as extrapyramidal symptoms (EPS) and tardive dyskinesia. Research on remoxipride is limited and further studies are needed to evaluate its effectiveness and safety. It is currently not widely used in clinical practice.'

Remoxipride: An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID54477
CHEMBL ID22242
CHEBI ID92948
SCHEMBL ID121339
MeSH IDM0026320

Synonyms (86)

Synonym
(s)-remoxipride
AB00514647-06
BRD-K54094468-001-01-6
BRD-K54094468-003-03-8
a-33547
remoxipride (usan)
D02682
80125-14-0
remoxiprida [inn-spanish]
(-)-(s)-3-brom-n-((1-ethyl-2-pyrrolidinyl)methyl)-2,6-dimethoxybenzamid
(-)-(s)-3-bromo-n-((1-ethyl-2-pyrrolidinyl)methyl)-2,6-dimethoxybenzamide
benzamide, 3-bromo-n-((1-ethyl-2-pyrrolidinyl)methyl)-2,6-dimethoxy-, (s)-
remoxipride [usan:ban:inn]
brn 4323708
(s)-3-bromo-2,6-dimethoxy-n-((1-ethyl-2-pyrrolidinyl)methyl)benzamide
fla 731
a 33547
benzamide, 3-bromo-2,6-dimethoxy-n-((1-ethyl-2-pyrrolidinyl)methyl)-, (s)-
remoxipridum [inn-latin]
romoxipride
cas-73220-03-8
NCGC00024870-01
NCGC00016921-01
tocris-0916
BPBIO1_001171
PRESTWICK2_000971
BIOMOL-NT_000015
PRESTWICK3_000971
BSPBIO_001001
BPBIO1_001103
AB00514647
remoxipride
DB00409
NCGC00024870-02
PRESTWICK0_000971
PRESTWICK1_000971
SPBIO_002912
NCGC00024870-03
HMS2089L19
CHEMBL22242 ,
fla-731(-)
3-bromo-n-[[(2s)-1-ethylpyrrolidin-2-yl]methyl]-2,6-dimethoxybenzamide
(r,s)-3-bromo-n-(1-ethyl-pyrrolidin-2-ylmethyl)-2,6-dimethoxy-benzamide
bdbm50026045
3-bromo-n-((s)-1-ethyl-pyrrolidin-2-ylmethyl)-2,6-dimethoxy-benzamide
3-bromo-n-(1-ethyl-pyrrolidin-2-ylmethyl)-2,6-dimethoxy-benzamide
3-bromo-n-((r)-1-ethyl-pyrrolidin-2-ylmethyl)-2,6-dimethoxy-benzamide
3-bromo-n-(1-ethyl-pyrrolidin-2-ylmethyl)-2,6-dimethoxy-benzamide (remoxipride)
3-bromo-n-(1-ethyl-pyrrolidin-2-ylmethyl)-2,6-dimethoxy-benzamide(remoxipride)
(s)-3-bromo-n-(1-ethyl-pyrrolidin-2-ylmethyl)-2,6-dimethoxy-benzamide
NCGC00024870-04
remoxiprida
remoxipride [usan:inn:ban]
remoxipridum
unii-0223rd59pe
0223rd59pe ,
cas-80125-14-0
dtxcid4025668
dtxsid6045668 ,
tox21_110934
AKOS016014111
fla-731 free base
fla 731 free base
remoxipride [usan]
a-33547.hcl.h20
remoxipride [mi]
remoxipride [mart.]
remoxipride [who-dd]
remoxipride [inn]
SCHEMBL121339
NCGC00024870-06
tox21_110934_1
(-)-(s)-3-bromo-n-(( 1-ethyl-2-pyrrolidinyl)-methyl)-2,6-dimethoxybenzamide
GUJRSXAPGDDABA-NSHDSACASA-N
(s)-(-)-3-bromo-n-[(1-ethyl-2-pyrrolidinyl)methyl]-2,6-dimethoxybenzamide
(s)-3-bromo-n-((1-ethylpyrrolidin-2-yl)methyl)-2,6-dimethoxybenzamide
3-bromo-n-{[(2s)-1-ethylpyrrolidin-2-yl]methyl}-2,6-dimethoxybenzamide
3-bromo-n-[[(2s)-1-ethyl-2-pyrrolidinyl]methyl]-2,6-dimethoxybenzamide
CHEBI:92948
80125-14-0 (free base)
Q1169059
(-)-remoxipride
BRD-K54094468-003-05-3
EN300-18568278
CS-0021136
HY-101313

Research Excerpts

Overview

Remoxipride is an atypical antipsychotic displaying selective binding to the dopamine D2 receptor. It displaced [3H]spiperone (IC50 = 1570 nM) and did not inhibit striatal DA-sensitive adenylate cyclase in vitro. Remoxiprise is a novel substituted benzamide that more effectively blocks mesolimbic than striatal D2 dopamine receptors.

ExcerptReferenceRelevance
"Remoxipride is a selective dopamine D(2) receptor antagonist, and useful as a model compound in mechanism-based pharmacological investigations. "( Online solid phase extraction with liquid chromatography-tandem mass spectrometry to analyze remoxipride in small plasma-, brain homogenate-, and brain microdialysate samples.
Danhof, M; de Lange, EC; de Ridder, S; Niederländer, HA; Stevens, J; van den Berg, DJ; van der Graaf, PH, 2010
)
2.02
"Remoxipride is an atypical antipsychotic displaying selective binding to the dopamine D2 receptor. "( Characterization of glutathione conjugates of the remoxipride hydroquinone metabolite NCQ-344 formed in vitro and detection following oxidation by human neutrophils.
Erve, JC; Klasson-Wehler, E; Svensson, MA; von Euler-Chelpin, H, 2004
)
2.02
"Remoxipride was shown to be a selective dopamine D2 receptor antagonist since it displaced [3H]spiperone (IC50 = 1570 nM) but not [3H]flupentixol (IC50 greater than 100 000 nM) in rat striatum, and did not inhibit striatal DA-sensitive adenylate cyclase in vitro (IC50 greater than 100 000 nM)."( Remoxipride, a new potential antipsychotic compound with selective antidopaminergic actions in the rat brain.
Angeby, K; Florvall, L; Hall, H; Köhler, C; Lindbom, LO; Magnusson, O; Ogren, SO, 1984
)
2.43
"Remoxipride is a selective dopamine D2 antagonist with virtually no activity on other transmitter receptors. "( Overcoming the neuroleptic-induced deficit syndrome: clinical observations with remoxipride.
Lewander, T, 1994
)
1.96
"Remoxipride is a novel substituted benzamide that more effectively blocks mesolimbic than striatal D2 dopamine receptors. "( Remoxipride in Parkinson's disease: differential response in patients with dyskinesias fluctuations versus psychosis.
Duff, J; Lang, AE; Sandor, P, 1995
)
3.18
"Remoxipride is a dopamine (DA) D2 antagonist that produces fewer of the side effects normally associated with chronic DA antagonist administration. "( Effects of the atypical antipsychotic remoxipride on alcohol self-administration.
Denning, CE; Files, FJ; Samson, HH, 1998
)
2.01
"Remoxipride is a substituted benzamide that acts as a weak but very selective antagonist of dopamine D2 receptors. "( Pharmacology of the atypical antipsychotic remoxipride, a dopamine D2 receptor antagonist.
Nadal, R, 2001
)
2.02
"Thus remoxipride is a low clearance drug, with a systemic plasma clearance of about 120 ml/min, and without any first-pass metabolism."( Clinical pharmacokinetics of remoxipride.
Jostell, KG; Movin, G; von Bahr, C; Widman, M; Yisak, WA, 1990
)
1.03
"Remoxipride is a new antipsychotic drug that binds selectively to the D2-dopamine receptor subtype as demonstrated in animal studies in vitro and in vivo. "( Distribution of remoxipride to the human brain and central D2-dopamine receptor binding examined in vivo by PET.
Farde, L; von Bahr, C, 1990
)
2.07
"Remoxipride is a substituted benzamide of the same class as sulpiride, and has a pharmacodynamic profile consistent with central antidopaminergic activity. "( Remoxipride. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in schizophrenia.
Heel, RC; Wadworth, AN, 1990
)
3.16
"Remoxipride is a recently developed neuroleptic drug of the benzamide type."( Fatal intoxication by Remoxipride.
Lukkari, I; Penttilä, A; Segerberg-Konttinen, M; Vuori, E, 1989
)
1.31
"Remoxipride is a novel substituted benzamide derivative with specific dopamine-(D2)-receptor blocking properties and selective action on brain mesolimbic functions. "( An open study of remoxipride, a benzamide derivative, in schizophrenia.
Besev, G; Lindström, L; Stening, G; Widerlöv, E, 1985
)
2.05

Effects

Remoxipride has an advantage over haloperidol in respect to extrapyramidal side effects. It has a plasma half-life of 4-7 h and is eliminated by hepatic metabolism and renal excretion.

Remoxipride has a low extrapyramidal syndrome (EPS) profile, and it is generally well tolerated. It is shown to be as effective in the treatment of schizophrenic patients as haloperidol in both short and long term double-blind trials.

ExcerptReferenceRelevance
"Remoxipride has a low extrapyramidal syndrome (EPS) profile, and it is generally well tolerated."( Overcoming the neuroleptic-induced deficit syndrome: clinical observations with remoxipride.
Lewander, T, 1994
)
1.24
"Remoxipride has an advantage over haloperidol in respect to extrapyramidal side effects."( Remoxipride and haloperidol in the acute phase of schizophrenia: a double-blind comparison.
Chanas, A; Deo, R; Edwards, JG; Levine, S; Mitchell, M; Plant, I; Rastogi, SC; Soni, S, 1990
)
2.44
"Remoxipride has a plasma half-life in the range of 4-7 h and is eliminated by both hepatic metabolism and renal excretion."( Clinical pharmacokinetics of remoxipride.
Jostell, KG; Movin, G; von Bahr, C; Widman, M; Yisak, WA, 1990
)
1.29
"Remoxipride has a low extrapyramidal syndrome (EPS) profile, and it is generally well tolerated."( Overcoming the neuroleptic-induced deficit syndrome: clinical observations with remoxipride.
Lewander, T, 1994
)
1.24
"Remoxipride has been shown to be as effective in the treatment of schizophrenic patients as haloperidol in both short and long term double-blind trials."( [Remoxipride, a selective antagonist of dopamine D2 receptors, in the treatment of delusional psychoses].
Köhler, C; Lewander, T; Ogren, SO; Von Bahr, C; Westerberg, SE,
)
1.76
"Remoxipride has an advantage over haloperidol in respect to extrapyramidal side effects."( Remoxipride and haloperidol in the acute phase of schizophrenia: a double-blind comparison.
Chanas, A; Deo, R; Edwards, JG; Levine, S; Mitchell, M; Plant, I; Rastogi, SC; Soni, S, 1990
)
2.44
"Remoxipride has a plasma half-life in the range of 4-7 h and is eliminated by both hepatic metabolism and renal excretion."( Clinical pharmacokinetics of remoxipride.
Jostell, KG; Movin, G; von Bahr, C; Widman, M; Yisak, WA, 1990
)
1.29

Actions

ExcerptReferenceRelevance
"Remoxipride was found to cause less parkinsonism than the prior neuroleptic therapy and appeared to have little masking effect on tardive dyskinesia."( Remoxipride in schizophrenia: effects on plasma prolactin.
Chouinard, G; Kallai-Sanfacon, MA; Turnier, L, 1985
)
2.43

Treatment

Remoxipride treatment reduced psychotic symptoms in eight of nine subjects while having no appreciable effect on the parkinsonian status of seven of nine Subjects. Pre-treatment with remoxipide (1.0 mg/kg i.v.) significantly attenuated the effect of quinpirole (0.1 mg/ kg i.V.)

ExcerptReferenceRelevance
"Remoxipride treatment reduced psychotic symptoms in eight of nine subjects while having no appreciable effect on the parkinsonian status of seven of nine subjects."( Remoxipride in the treatment of levodopa-induced psychosis.
Angus, C; Lang, AE; Sandor, P; Singal, S, 1996
)
2.46
"Pre-treatment with remoxipride (1.0 mg/kg i.v.) significantly attenuated the effect of quinpirole (0.1 mg/kg i.v.)."( Role of dopamine D1 and D2 receptors in the micturition reflex in conscious rats.
Andersson, KE; Igawa, Y; Ishizuka, O; Kaidoh, K; Nishizawa, O; Seki, S, 2001
)
0.63

Toxicity

ExcerptReferenceRelevance
"Compared to traditional neuroleptics, most of the new antipsychotics are characterized by a low extrapyramidal side effect (EPS) liability and varying antipsychotic efficacy."( New antipsychotics: classification, efficacy, and adverse effects.
Gerlach, J, 1991
)
0.28
" The total incidence of serious adverse events in the short-term double-blind programme was approximately 2% for both remoxipride and haloperidol."( Safety evaluation in both short- and long-term treatment of schizophrenia with remoxipride.
Englund, A; Lawrie, V; Lewander, T; Morrison, D; Schlachet, A; Westerbergh, SE, 1990
)
0.72

Pharmacokinetics

Remoxipride has a plasma half-life in the range of 4-7 h and is eliminated by both hepatic metabolism and renal excretion. AUC, Cmax and Cmin of both total and unbound remoxipide increased with increasing age.

ExcerptReferenceRelevance
" The mean elimination half-life of total remoxipride was slightly longer on day 15 than day 1 (7."( Pharmacokinetics and effects on prolactin of remoxipride in patients with tardive dyskinesia.
Andersson, U; Nilsson, MI; von Bahr, C; Widerlöv, E, 1991
)
0.81
"Twenty-four stable, chronic schizophrenic inpatients were entered in a double-blind crossover study designed to compare single dose and steady state pharmacokinetic profiles of an immediate release formulation (IR) 200 mg BID and a controlled release formulation (CR) of remoxipride 400 mg once daily."( Steady-state pharmacokinetics of controlled release and immediate release formulations of remoxipride in patients with chronic schizophrenia.
Ashwood, T; Movin, G; Soni, SD; Tench, D, 1990
)
0.68
" AUC, Cmax and Cmin of both total and unbound remoxipride increased with increasing age."( Pharmacokinetics of remoxipride in elderly psychotic patients.
Franzén, G; Gustafson, L; Movin, G; Nilsson, L; Soni, SD; Tench, D; Widerlöv, E; Yisak, W, 1990
)
0.86
" Remoxipride has a plasma half-life in the range of 4-7 h and is eliminated by both hepatic metabolism and renal excretion."( Clinical pharmacokinetics of remoxipride.
Jostell, KG; Movin, G; von Bahr, C; Widman, M; Yisak, WA, 1990
)
1.48
" The other pharmacokinetic variables studied showed no difference."( Pharmacokinetics of an oral controlled release formulation of remoxipride: a double-blind, crossover comparison with conventional formulation in chronic schizophrenics.
Ashwood, TJ; Movin, G; Soni, SD; Tench, D, 1990
)
0.52
" Comparisons of AUC, t1/2 and tmax using the Wilcoxon's signed rank test showed no significant difference between single dose and steady state indicating that the pharmacokinetics of intramuscular remoxipride were linear."( Tolerability and pharmacokinetics of remoxipride after intramuscular administration.
Albaret, C; Kahn, JP; Laxenaire, M; Nilsson, L; Yisak, W; Zaar-Hedin, A, 1990
)
0.74
"Remoxipride is a substituted benzamide of the same class as sulpiride, and has a pharmacodynamic profile consistent with central antidopaminergic activity."( Remoxipride. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in schizophrenia.
Heel, RC; Wadworth, AN, 1990
)
3.16
" It consists of three parts: 1) the pharmacokinetics of remoxipride; 2) a physiological substance model for PRL, incorporating the synthesis of PRL and its release into and elimination from plasma; and 3) a pharmacodynamic model describing the influence of remoxipride on the PRL release from the pool."( Prolactin release after remoxipride by an integrated pharmacokinetic-pharmacodynamic model with intra- and interindividual aspects.
Hammarlund-Udenaes, M; Movin-Osswald, G, 1995
)
0.84
" In patients with severely decreased renal function, the AUC and Cmax of remoxipride were increased significantly, and t1/2 was prolonged, as compared with the control patients."( The pharmacokinetics of remoxipride and metabolites in patients with various degrees of renal function.
Boelaert, J; Hammarlund-Udenaes, M; Movin-Osswald, G; Nilsson, LB, 1993
)
0.82
" No significant differences in dose-corrected pharmacokinetic variables were found between the two groups."( Single dose pharmacodynamics of thioridazine and remoxipride in healthy younger and older volunteers.
Jackson, SH; Lee, DR; Maskrey, VL; Swift, CG; Tiplady, B; Yisak, W, 1999
)
0.56
" A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals."( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004
)
0.32
" Recent studies with a 103-compound dataset suggested that scaling from monkey pharmacokinetic data tended to be the most accurate method for predicting human clearance."( Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
Evans, CA; Jolivette, LJ; Nagilla, R; Ward, KW, 2006
)
0.33
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" Pharmacokinetic modeling is proposed to identify the existence of direct nose-to-brain transport in a quantitative manner."( Systemic and direct nose-to-brain transport pharmacokinetic model for remoxipride after intravenous and intranasal administration.
Danhof, M; de Lange, EC; Ploeger, BA; Stevens, J; van der Graaf, PH, 2011
)
0.6

Compound-Compound Interactions

ExcerptReferenceRelevance
"The effects of remoxipride, alone and in combination with ethanol and diazepam, on sensory, cognitive, and neuromotor performance were studied in 12 healthy volunteers (7 men, 5 women)."( Effects of remoxipride on psychomotor performance, alone and in combination with ethanol and diazepam.
Mattila, ME; Mattila, MJ, 1990
)
1.02

Bioavailability

The mean relative bioavailability with regard to the amount of remoxipride absorbed after administration in CR form as compared with the IR form was 97%. The rate of absorption of remxipride CR was significantly lower than the IR formulation and tmax was prolonged.

ExcerptReferenceRelevance
" After oral administration the drug is rapidly and almost completely absorbed with a bioavailability above 90%."( Clinical pharmacokinetics of remoxipride.
Jostell, KG; Movin, G; von Bahr, C; Widman, M; Yisak, WA, 1990
)
0.57
" The mean relative bioavailability with regard to the amount of remoxipride absorbed after administration in CR form as compared with the IR form was 97%."( Pharmacokinetics of an oral controlled release formulation of remoxipride: a double-blind, crossover comparison with conventional formulation in chronic schizophrenics.
Ashwood, TJ; Movin, G; Soni, SD; Tench, D, 1990
)
0.76
" Due to the good absorption properties, it is reasonable to expect a low variation in the extent of bioavailability of remoxipride after administration in an extended-release, multiple-unit capsule formulation."( Plasma concentrations of remoxipride and the gastrointestinal transit of 111In-marked extended-release coated spheres.
Graffner, C; Nilsson, MI; Wagner, Z; Widerlöv, E, 1990
)
0.79
" The mean oral bioavailability was 96%."( Remoxipride--a new potential antipsychotic compound. Tolerability and pharmacokinetics after single oral and intravenous administration in healthy male volunteers.
Grind, M; Nilsson, L; Nilsson, MI; Oxenstierna, G; Sedvall, G; Wahlén, A, 1989
)
1.72
" The bioavailability of remoxipride was investigated in two studies in healthy volunteers after administration of a 100-mg dose in suspension."( In vivo validation of the release rate and palatability of remoxipride-modified release suspension.
Ekman, I; Graffner, C; Sinclair, W; Sjöqvist, R; Woods, JP, 1993
)
0.84
" However, the bioavailability was low in the rodents (< 10% in mice and hamsters and < 1% in rats) due to an extensive first-pass elimination in the hepato-portal system."( Disposition of remoxipride in different species. Species differences in metabolism.
Bryske, B; Lundström, J; Nilsson, LB; Widman, M, 1993
)
0.64
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
"Intranasal (IN) administration could be an attractive mode of delivery for drugs targeting the central nervous system, potentially providing a high bioavailability because of avoidance of a hepatic first-pass effect and rapid onset of action."( Systemic and direct nose-to-brain transport pharmacokinetic model for remoxipride after intravenous and intranasal administration.
Danhof, M; de Lange, EC; Ploeger, BA; Stevens, J; van der Graaf, PH, 2011
)
0.6
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Remoxipride had comparable therapeutic efficacy to that of haloperidol. The dose-response curve for antagonism of GBL-reversal was superimposable over that for antagonistic apomorphine-induced stereotypies.

ExcerptRelevanceReference
" Both drugs were given in a dosage range of 50-200 mg/day."( Remoxipride versus thioridazine in elderly psychotic patients.
Link, C; Phanjoo, AL, 1990
)
1.72
" It was concluded that, from a pharmacokinetic point of view, the CR formulation of remoxipride was suitable for a once daily dosage schedule."( Pharmacokinetics of an oral controlled release formulation of remoxipride: a double-blind, crossover comparison with conventional formulation in chronic schizophrenics.
Ashwood, TJ; Movin, G; Soni, SD; Tench, D, 1990
)
0.74
" Remoxipride, at both dosage ranges used, thus had comparable therapeutic efficacy to that of haloperidol."( A double-blind multicentre comparison of remoxipride, at two dose levels, and haloperidol.
Agussol, P; Alby, JM; Brion, S; Burnat, G; Castelnau, D; Deluermoz, S; Dufour, H; Ferreri, M; Goudemand, M; Patris, M, 1990
)
1.46
" For remoxipride, the dose-response curve for antagonism of GBL-reversal was superimposable over that for antagonism of apomorphine-induced stereotypies, with an ED50 value about 12 times higher than that for antagonism of apomorphine-induced hyperactivity."( Comparison of the effects of haloperidol, remoxipride and raclopride on "pre"- and postsynaptic dopamine receptors in the rat brain.
Fowler, CJ; Magnusson, O; Mohringe, B; Ogren, SO; Wijkström, A, 1988
)
1.05
" Heterogenous binding sites were found since various types of compounds inhibited the binding of 3H-remoxipride with shallow dose-response curves."( Heterogenous binding of 3H-remoxipride to membranes of rat liver and brain.
Ross, SB, 1995
)
0.8
" The mean duration of illness before entering the study was 21 years and the pre-study neuroleptic dosage in chlorpromazine equivalents was 930 mg/day."( A long-term study of remoxipride in chronic schizophrenic patients.
Hagert, U; Lang, S; Leinonen, E; Putkonen, A; Tolvanen, U; Vartiainen, H, 1993
)
0.6
"0 mg/kg) produced a rightward shift in the (+)-7-OH-DPAT dose-response curve."( Antagonism of the discriminative stimulus effects of (+)-7-OH-DPAT by remoxipride but not PNU-99194A.
Baker, LE; Christian, AJ; Goodwin, AK, 2001
)
0.54
" D2 receptor blockade, a dose-response study was employed to determine whether low doses of these atypical antipsychotics would also upregulate hippocampal BDNF mRNA in the absence of significant D2 receptor blockade."( Differential regulation of hippocampal BDNF mRNA by typical and atypical antipsychotic administration.
Ashe, P; Chlan-Fourney, J; Juorio, AV; Li, XM; Nylen, K, 2002
)
0.31
" Although NCQ-344 has been detected in plasma of humans dosed with remoxipride, to date, no experimental evidence for the formation of the corresponding para-quinone has been obtained."( Characterization of glutathione conjugates of the remoxipride hydroquinone metabolite NCQ-344 formed in vitro and detection following oxidation by human neutrophils.
Erve, JC; Klasson-Wehler, E; Svensson, MA; von Euler-Chelpin, H, 2004
)
0.81
" Initially, dose-response experiments were performed with intrahippocampal perfusions of GBR-12909 and citalopram, respectively, selective dopamine and serotonin re-uptake blockers."( Anticonvulsant action of GBR-12909 and citalopram against acute experimentally induced limbic seizures.
Clinckers, R; Ebinger, G; Meurs, A; Michotte, Y; Smolders, I, 2004
)
0.32
" In this study we integrated pharmacometabolomics with pharmacokinetic/pharmacodynamic (PKPD) modeling to identify and quantify the multiple endogenous metabolite dose-response relations for the dopamine D2 antagonist remoxipride."( Multivariate pharmacokinetic/pharmacodynamic (PKPD) analysis with metabolomics shows multiple effects of remoxipride in rats.
de Lange, ECM; Elassaiss-Schaap, J; Gonzalez-Amoros, B; Hankemeier, T; Harms, AC; van den Brink, WJ; van der Graaf, PH, 2017
)
0.85
" The MTT test was conducted to identify oxidative and reductive enzymes and to specify appropriate dosage at four concentrations of dopamine and Cabergoline on MCF-7 and SKBR-3 cells."( The Expression of Dopamine Receptors Gene and their Potential Role in Targeting Breast Cancer Cells with Selective Agonist and Antagonist Drugs. Could it be the Novel Insight to Therapy?
Ahangari, G; Bakhtou, H; Deezagi, A; Olfatbakhsh, A, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
dimethoxybenzeneAny methoxybenzene that consists of a benzene skeleton substituted with two methoxy groups and its derivatives.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
USP1 protein, partialHomo sapiens (human)Potency63.09570.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency31.67680.000811.382244.6684AID686978; AID686979
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency1.99530.00137.762544.6684AID914; AID915
cytochrome P450 2D6Homo sapiens (human)Potency19.49710.00108.379861.1304AID1645840
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency0.19950.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency39.81070.00255.840031.6228AID899
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency15.84890.01789.637444.6684AID588834
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency0.14130.251215.843239.8107AID504327
[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)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)92.66670.11007.190310.0000AID1443980; AID1449628; AID1473738
D(2) dopamine receptorHomo sapiens (human)IC50 (µMol)0.44060.00000.74728.0000AID537694; AID62768
D(2) dopamine receptorHomo sapiens (human)Ki0.21700.00000.651810.0000AID65888
D(4) dopamine receptorHomo sapiens (human)IC50 (µMol)3.87200.00011.14239.3280AID65934
D(4) dopamine receptorHomo sapiens (human)Ki3.87200.00000.436210.0000AID63538
D(2) dopamine receptorChlorocebus aethiops (grivet)Ki0.87300.00480.27820.8730AID62007
D(3) dopamine receptorChlorocebus aethiops (grivet)Ki4.60300.00301.69074.6030AID64802
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)1.57000.00010.54948.4000AID64295; AID64609
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd3.98110.00010.95285.0119AID438555
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (166)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral fear responseD(4) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(4) dopamine receptorHomo sapiens (human)
response to amphetamineD(4) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
adult locomotory behaviorD(4) dopamine receptorHomo sapiens (human)
positive regulation of sodium:proton antiporter activityD(4) dopamine receptorHomo sapiens (human)
positive regulation of kinase activityD(4) dopamine receptorHomo sapiens (human)
response to histamineD(4) dopamine receptorHomo sapiens (human)
social behaviorD(4) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
fear responseD(4) dopamine receptorHomo sapiens (human)
regulation of circadian rhythmD(4) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(4) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(4) dopamine receptorHomo sapiens (human)
rhythmic processD(4) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(4) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(4) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
inhibitory postsynaptic potentialD(4) dopamine receptorHomo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationD(4) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(4) dopamine receptorHomo sapiens (human)
chemical synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (42)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
protein bindingD(4) dopamine receptorHomo sapiens (human)
potassium channel regulator activityD(4) dopamine receptorHomo sapiens (human)
SH3 domain bindingD(4) dopamine receptorHomo sapiens (human)
dopamine bindingD(4) dopamine receptorHomo sapiens (human)
identical protein bindingD(4) dopamine receptorHomo sapiens (human)
metal ion bindingD(4) dopamine receptorHomo sapiens (human)
epinephrine bindingD(4) dopamine receptorHomo sapiens (human)
norepinephrine bindingD(4) dopamine receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityD(4) dopamine receptorHomo sapiens (human)
neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
serotonin bindingD(4) dopamine receptorHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (39)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
centrosomeD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
membraneD(4) dopamine receptorHomo sapiens (human)
postsynapseD(4) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
dendriteD(4) dopamine receptorHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (133)

Assay IDTitleYearJournalArticle
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID185005Compound was tested in vio for concomitant ability to antagonize the locomotor activity of rat induced by Di-Pr-5,6-ADTN1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID169618Evaluated biochemically in reserpine-pretreated habituated rats for (100 umol/kg) subcuteneous dose in rat striatum (DOPAacc), Value expressed as counts/30 min1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID221061Inhibition of apomorphine-induced climbing behavior in mice, after intraperitoneal administration1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID26362Ionization constant (pKa)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID540223Volume of distribution at steady state in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID194724Evaluated biochemically in reserpine-pretreated habituated rats for (100 umol/kg) subcuteneous dose, Value expressed as locomotor activity (LMA)1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID537694Antagonist activity at dopamine D2 receptor2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
QSAR prediction of D2 receptor antagonistic activity of 6-methoxy benzamides.
AID177976Compound was evaluated in vivo its antagonist activity against apomorphine induced behavioral syndrome such as Stereotypy in rat after intraperitoneal administration; activity value ranges from 6.2-6.71985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.
AID540224Clearance in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID169627Evaluated for DOPAC level in nonpretreated habituated rats after subcuteneous dose of 100 micro mol/kg in rat striatum1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID540225Volume of distribution at steady state in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID184626Compound was tested for its acute toxicity in rat after ip administration1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
AID7783Unbound fraction (plasma)2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID62768Binding affinity to dopamine receptor D2 cloned from human, using [3H]- YM09151 as competitive ligand2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
AID185044Minimum effective dose that produced a significant effect relative to the amphetamine alone control using a Fisher's LSD post hoc test (P<0.05)2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID64802Displacement of [3H]-YM 09151 from african monkey Dopamine receptor D31995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID540222Clearance in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID62727Antidopamine activity in vitro by ability to displace [3H]spiperone from rat brain striatal preparations.1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID540226Clearance in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID63538Displacement of [3H]-YM 09151 from human Dopamine receptor D41995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID781328pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 20052014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID194722Evaluated biochemically in nonhabituated rats for (100 umol/kg) subcuteneous dose, Value expressed as locomotor activity (LMA)1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID225271Dose required to induce 50% maximum catalepsy in rat administered perorally1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
AID178320In vivo inhibition of apomorphine induced hyperactivity in rats.1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID221064Inhibition of apomorphine-induced hyperactivity behavior in mice, after peroral administration1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID540228Clearance in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID438555Binding affinity to 5HT1A receptor2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Physical binding pocket induction for affinity prediction.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID169620Evaluated for DOPA accumulation (DOPAacc) level in nonhabituated rats after subcuteneous dose (100 uM/kg) in rat striatum1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID65888Tested for affinity against cloned mammalian dopamine autoreceptor (DA) D2 receptors expressed in CHO-K1 cells using [3H]spiperone as radioligand1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID64609Tested in vitro for inhibition of [3H]spiperone binding to dopamine receptor D21993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Conformationally restricted analogues of remoxipride as potential antipsychotic agents.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID468443Inhibition of human FAAH at 1 uM2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID184872Minimum effective dose observed in rat catalepsy experiments2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
AID36713Binding affinity to alpha-1 adrenergic receptor from rat brain homogenate, using [3H]- prazosin as the competitive ligand2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
AID177791Compound was evaluated in vivo for antagonist activity against apomorphine induced behavioral syndrome such as Hyperactivity in rat after intraperitoneal administration; activity value ranges from 0.81-0.981985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.
AID176178Compound was tested in vivo for its ability to antagonize extrapolatory behavior impairment induced by DOPA in rats upon intraperitoneal administration1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents.
AID62007Displacement of [3H]-YM 09151 from african green monkey Dopamine receptor D21995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
1-Phenyl-3-(aminomethyl)pyrroles as potential antipsychotic agents. Synthesis and dopamine receptor binding.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID540229Volume of distribution at steady state in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID225447Inhibition of apomorphine-induced stereotypy in rat, after peroral administration1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID678721Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID8002Observed volume of distribution2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics.
AID540227Volume of distribution at steady state in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID178322In vivo inhibition of apomorphine induced stereotypy in rats.1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Potential neuroleptic agents. 4. Chemistry, behavioral pharmacology, and inhibition of [3H]spiperone binding of 3,5-disubstituted N-[(1-ethyl-2-pyrrolidinyl)methyl]-6-methoxysalicylamides.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID64295In vitro binding affinity at Dopamine receptor D2 in rat by displacing [3H]- spiperone from rat striatal membrane1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Potential neuroleptic agents. 3. Chemistry and antidopaminergic properties of substituted 6-methoxysalicylamides.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID65934Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
AID64772Tested in vitro for inhibition of [3H]-spiperone binding to dopamine receptor D2 at the dose of 10 e-5 M1993Journal of medicinal chemistry, Oct-29, Volume: 36, Issue:22
Conformationally restricted analogues of remoxipride as potential antipsychotic agents.
AID211852Acute toxicity on male outbred albino mice upon intraperitoneal administration1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID175345Compound was tested in vivo for its ability to displace DA receptor agonist (Di-Pr-5,6-ADTN) from rat striatal binding sites at 0.25 uM/Kg sc. dose1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Substituted (S)-phenylpiperidines and rigid congeners as preferential dopamine autoreceptor antagonists: synthesis and structure-activity relationships.
AID176339Compound was tested in vivo for its ability to induce catalepsy in rats upon intraperitoneal administration1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents.
AID113139Compound was tested in vivo for its ability to antagonize apomorphine-induced climbing response in mice upon intraperitoneal administration1998Journal of medicinal chemistry, Jan-29, Volume: 41, Issue:3
Design of N-acylprolyltyrosine "tripeptoid" analogues of neurotensin as potential atypical antipsychotic agents.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical 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.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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 (265)

TimeframeStudies, This Drug (%)All Drugs %
pre-199033 (12.45)18.7374
1990's168 (63.40)18.2507
2000's35 (13.21)29.6817
2010's23 (8.68)24.3611
2020's6 (2.26)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.73

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 Index28.73 (24.57)
Research Supply Index5.82 (2.92)
Research Growth Index4.89 (4.65)
Search Engine Demand Index39.34 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.73)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials65 (23.90%)5.53%
Reviews19 (6.99%)6.00%
Case Studies9 (3.31%)4.05%
Observational0 (0.00%)0.25%
Other179 (65.81%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]