Page last updated: 2024-11-05

fluanisone

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

Description

Fluanisone is a butyrophenone derivative with antipsychotic activity. It is a non-selective dopamine receptor antagonist with high affinity for D2 receptors. Fluanisone is used to treat schizophrenia and other psychotic disorders. It is also used to manage agitation and anxiety in patients with dementia. The synthesis of fluanisone involves a multi-step process starting from 4-fluoro-benzophenone. The compound exhibits a wide range of effects including antipsychotic, anxiolytic, and sedative effects. Fluanisone is studied due to its unique pharmacological profile and potential therapeutic applications in treating various neuropsychiatric disorders. It is also used as a research tool to investigate the role of dopamine in the brain.'

fluanisone: former provisional as haloanisone; structure; RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID15139
CHEMBL ID58792
CHEBI ID177744
SCHEMBL ID145054
MeSH IDM0046290

Synonyms (86)

Synonym
1-(4-luorophenyl)-4-[4-(2-methoxyphenyl)piperazin-1-yl]butan-1-one
CHEBI:177744
haloanison
fluanisone
1-butanone, 1-(4-fluorophenyl)-4-[4-(2-methoxyphenyl)-1-piperazinyl]-
nsc170977
2028 md
metorin
sedalande
4'-fluoro-4-[4-(o-methoxyphenyl)-1-piperazinyl]butyrophenone
4-[4-(o-methoxyphenyl)-1-piperazinyl]-p-fluorobutyrophenone
haloanisone
butyrophenone, 4'-fluoro-4-[4-(o-methoxyphenyl)-1-piperazinyl]-
r 2028
anti-pica
fluanison
1480-19-9
md 2028
wln: t6n dntj a3vr df& dr bo1
r 2167
nsc-170977
4'-fluoro-4-(4-(o-methoxyphenyl)-1-piperazinyl)butyrophenone
brn 0707524
1-butanone, 1-(4-fluorophenyl)-4-(4-(2-methoxyphenyl)-1-piperazinyl)-
fluanisona [inn-spanish]
fluanisone [inn:ban:dcf]
butyrophenone, 4'-fluoro-4-(4-(o-methoxyphenyl)-1-piperazinyl)-
fluanisonum [inn-latin]
4-(4-(o-methoxyphenyl)-1-piperazinyl)-p-fluorobutyrophenone
nsc 170977
einecs 216-038-8
D02621
fluanisone (inn)
OPREA1_227293
OPREA1_528183
smr000111851
MLS000107485
AKOS003669652
r-2028
CHEMBL58792 ,
md-2028
r-2167
1-(4-fluorophenyl)-4-[4-(2-methoxyphenyl)piperazin-1-yl]butan-1-one
L000740
FT-0668561
1-(4-fluoro-phenyl)-4-[4-(2-methoxy-phenyl)-piperazin-1-yl]-butan-1-one
bdbm50019959
1-(4-fluoro-phenyl)-4-[4-(2-methoxy-phenyl)-piperazin-1-yl]-butan-1-one(fluanisone)
A808723
NCGC00077304-02
1d0w98u1i4 ,
fluanisona
fluanisonum
unii-1d0w98u1i4
5-23-02-00213 (beilstein handbook reference)
tox21_110992
dtxcid2025711
cas-1480-19-9
dtxsid4045711 ,
NCGC00077304-01
HMS2231H24
4'-fluoro-4-)4-(o-methoxyphenyl)-1-piperazinyl)butyrophenone
fluanisone [who-dd]
fluanisone [mart.]
fluanisone [mi]
fluanisone [inn]
HMS3373P06
SCHEMBL145054
REGID_FOR_CID_15139
hypnorm (salt/mix)
1-(4-fluorophenyl)-4-[4-(2-methoxyphenyl)-1-piperazinyl]-1-butanone #
solusediv (salt/mix)
p-fluoro-.gamma.-[4-(o-methoxyphenyl)-1-piperazinyl]butyrophenone
sedavic (salt/mix)
IRYFCWPNDIUQOW-UHFFFAOYSA-N
4'-fluoro-4-[4(o-methoxyphenyl)-1-piperazinyl]buterophenone
SR-01000215056-1
sr-01000215056
Q5462605
DB13665
1-(4-fluorophenyl)-4-(4-(2-methoxyphenyl)piperazin-1-yl)butan-1-one
2028 md; nsc 170977; r 2028
BCP12114
SY267068
mfcd00366636
1-butanone,1-(4-fluorophenyl)-4-[4-(2-methoxyphenyl)-1-piperazinyl]-

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
"When establishing a rabbit model for cardiovascular research in our laboratory we have used midazolam in combination with fentanyl/fluanisone (MFF) and nitrous oxide as anaesthesia."( Midazolam in combination with fentanyl/fluanisone and nitrous oxide as anaesthesia in rabbits--cardiovascular parameters.
Fosse, RT; Hessevik, I; Hexeberg, E; Hexeberg, S, 1995
)
0.76

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
[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 (20)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency19.67070.000811.382244.6684AID686978; AID686979
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency6.30960.01237.983543.2770AID1346984
pregnane X nuclear receptorHomo sapiens (human)Potency7.94330.005428.02631,258.9301AID1346985
P53Homo sapiens (human)Potency35.48130.07319.685831.6228AID504706
aryl hydrocarbon receptorHomo sapiens (human)Potency13.06820.000723.06741,258.9301AID743085; AID743122
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency79.43283.548119.542744.6684AID743266
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency1.41250.01789.637444.6684AID588834
DNA polymerase betaHomo sapiens (human)Potency89.12510.022421.010289.1251AID485314
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency36.12540.005612.367736.1254AID624032
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency31.62280.316212.765731.6228AID881
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency31.62280.00638.235039.8107AID881
[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)
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.05200.00020.667710.0000AID5218; AID5294
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.05200.00010.601710.0000AID5218; AID5294
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.00090.00010.949010.0000AID35421; AID37170
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.00100.00010.739610.0000AID4425
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.00090.00000.575110.0000AID35421; AID37170
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.05200.00020.590910.0000AID5218; AID5294
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.00090.00000.965010.0000AID35421; AID37170
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.00270.00000.437510.0000AID63823; AID65108; AID65884
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (21)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (96)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID133847Anticonvulsant activity against electroshock-induced convulsions, after 5 hour of peroral administration in mouse at a dose of 40 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID133855Anticonvulsant activity against pentylenetetrazole-induced convulsions, after 1 hour of peroral administration in mouse at a dose of 40 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID135364Inhibitory activity against tremorine-induced tremors, after 1 hour of peroral administration in mouse at a dose of 60 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID139321Inhibitory activity against pentobarbital induced-sleeping after 5 hr of peroral administration in mouse; NT means not tested1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID23961logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID128987Anticonvulsant activity against tryptamine-induced convulsions, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID23968logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID128671Antagonism of apomorphine-induced climbing behavior in mice after peroral administration1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID131206Contractile activity in skeletal muscles, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID183181Antagonistic activity against apomorphine-induced stereotypy, after 5 hour of peroral administration in rats at a dose of 100 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID63305Inhibitory activity against apomorphine induced emesis, after 1 hr of peroral administration in dog; NT means not tested1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID23959logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID113114Antagonism of apomorphine-induced climbing in mice when administered intraperitoneally 60 min prior to apomorphine (1 mg/kg)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID131589Suppression of aggressive behavior, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177741Activity to evoke catalepsy, after 1 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID4029Binding affinity was evaluated by determining in vitro displacement of [3H]8-OH-DPAT from the central 5-hydroxytryptamine 1A receptor recognition site in rat frontal cortex homogenate.1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.
AID63328Antagonistic activity against apomorphine-induced emesis, after 5 hour of peroral administration in dogs1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID26296Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID5294Potency to displace [3H]- Spiperone from 5-hydroxytryptamine 2 receptor in rat striatum1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID134580Lethal dose in mice (LD50) following i.p. dosing1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177948Antagonistic activity against amphetamine-induced stereotypy, after 1 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID23970logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID197391Inhibitory activity against body weight gain after 5 hr of peroral administration in rat; NT means not tested1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID135368Inhibitory activity against tremorine-induced tremors, after 5 hour of peroral administration in mouse at a dose of 60 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID128819Antagonistic activity against amphetamine-induced hypermotility, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID37170Ability to inhibit [3H]WB-4101 binding to alpha-1 adrenergic receptor was determined in rat1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID65884Displacement of [3H]-Spiperone from Dopamine receptor D2 in rat striatum1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID5218Ability to inhibit [3H]spiperone binding to 5-hydroxytryptamine 2 receptor determined in rat1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID176808Suppression of conditioned avoidance behavior in rats when administered perorally 60 min before measurement1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID139322Inhibitory activity against tryptamine induced convulsions after 5 hr of peroral administration in mouse; NT means not tested1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID139319Inhibitory activity against apomorphine induced turning, after 5 hr of peroral administration in mouse; NT means not tested1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177952Antagonistic activity against apomorphine-induced stereotypy in rats, by administering perorally1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID130908Inhibition of spontaneous motor activity after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID133681Activity of inclined screen in mouse, after 5 hour of peroral administration in mouse at a dose of 60 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID178998Inhibitory activity against norepinephrine-induced lethality, after 5 hour of peroral administration in rat1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID130909Inhibition of spontaneous motor activity after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID178997Inhibitory activity against norepinephrine-induced lethality, after 1 hour of peroral administration in rat1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177724Induction of catalepsy in rats when administered intraperitoneally 4 hr prior to measurement to groups of nine animals1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID23973Partition coefficient (logD, measured by HPLC, log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID231638Binding affinity against the D2 dopamine receptor and ratio of IC50(+Na+) / IC50(-Na(+)) [from 2-4 experiments]1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID19647Partition coefficient (logP)1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.
AID177725Induction of catalepsy in rats when administered intraperitoneally 4 hr prior to measurement to groups of 9 animals. value is based on at least three dose levels(40% of animals showed catalepsy)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID226319Activity calculated as Na+ ratio [IC50 (+Na+) / IC50 (-Na+)]1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID130874Inhibition against apomorphine-induced climbing, after 5 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID131419Potentiation against pentobarbital-induced sleeping, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID131588Suppression of aggressive behavior, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID131204Contractile activity in skeletal muscles, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID128818Antagonistic activity against amphetamine-induced hypermotility, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID133845Anticonvulsant activity against electroshock-induced convulsions, after 1 hour of peroral administration in mouse at a dose of 40 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID176663Suppression of conditioned avoidance behavior in rats following p.o. administration.1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID63823pKi value against rat Dopamine receptor D2.1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.
AID176326Body weight gain, after 2 hour of period of conditioned feeding in rats,1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID135224Inhibitory activity against tremorine-induced salivation, after 5 hour of peroral administration in mouse at a dose of 60 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID128670Antagonism of apomorphine-induced climbing behavior in mice after ip administration1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID128815Antagonistic activity against amphetamine-induced Hypermobility in mouse by administering perorally1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID35421Potency to displace [3H]- WB-4101 from alpha-1 adrenergic receptor in rat striatum1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID177954Antagonistic activity against apomorphine-induced stereotypy, after 1 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID133859Anticonvulsant activity against pentylenetetrazole-induced convulsions, after 5 hour of peroral administration in mouse at a dose of 40 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID135222Inhibitory activity against tremorine-induced salivation, after 1 hour of peroral administration in mouse at a dose of 60 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177742Activity to evoke catalepsy, after 5 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID4425pKi value against rat 5-hydroxytryptamine 1A receptor.1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.
AID113115Antagonism of apomorphine-induced climbing in mice when administered perorally 60 min prior to apomorphine (1 mg/kg)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID176807Suppression of conditioned avoidance behavior in rats when administered intraperitoneally 60 min before measurement1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID130911Inhibition of spontaneous motor activity in mouse, by administering perorally1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID134519Effect on skeletal muscle tone, after 1 hour of peroral administration in mouse at a dose of 100 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177732Inhibition against conditioned avoidance response, after 5 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID130873Inhibition against apomorphine-induced climbing, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177949Antagonistic activity against amphetamine-induced stereotypy, after 5 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID23965logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID128162Activity of inclined screen in mouse, after 1 hour of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID176662Suppression of conditioned avoidance behavior in rats after ip administration1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
AID65108In vitro displacement of [3H]spiperone from Dopamine receptor D2 binding site in rat striatum.1997Journal of medicinal chemistry, Jan-31, Volume: 40, Issue:3
5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.
AID23971logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID64931Ability to inhibit the [3H]spiperone binding to striatum Dopamine receptor D2 was determined in rat1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
AID23963logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID177739Activity to evoke catalepsy in rats, by administering perorally1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID177731Inhibition against conditioned avoidance response, after 1 hour of peroral administration in rats1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID130877Inhibition against apomorphine-induced turning, after 1 hr of peroral administration in mouse1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
AID134522Effect on skeletal muscle tone, after 5 hour of peroral administration in mouse at a dose of 100 mg/kg1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
5-Piperazinylalkyl-2(3H)-oxazolones with neuroleptic activity.
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.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (55)

TimeframeStudies, This Drug (%)All Drugs %
pre-199025 (45.45)18.7374
1990's11 (20.00)18.2507
2000's7 (12.73)29.6817
2010's9 (16.36)24.3611
2020's3 (5.45)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.55

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 Index28.55 (24.57)
Research Supply Index4.16 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index36.71 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.55)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (5.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies1 (1.67%)4.05%
Observational0 (0.00%)0.25%
Other56 (93.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]