Page last updated: 2024-11-10

timiperone

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

Description

timiperone: structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3033151
CHEMBL ID2107117
CHEBI ID135631
SCHEMBL ID145839
SCHEMBL ID11797177
MeSH IDM0082150

Synonyms (47)

Synonym
dd-3480
tolopelon
timiperone
1-(4-fluorophenyl)-4-[4-(2-thioxo-2,3-dihydro-1h-benzimidazol-1-yl)piperidin-1-yl]butan-1-one
butyrophenone, 4'-fluoro-4-(4-(2-thioxobenzimidazol-1-yl)piperidino)-
timiperonum [inn-latin]
4-(4-(2,3-dihydro-2-thioxo-1h-benzimidazol-1-yl)-1-piperidinyl)-1-(4-fluorophenyl)-1-butanone
timiperone [inn:jan]
4-fluoro-4-(4-(2-thioxo-1-benzimidazolinyl)piperidino)butyrophenone
4'-fluoro-4-(4-(2-thioxo-1-benzimidazolinyl)piperidino)butyrophenone
1-(1-(3-(p-fluorobenzoyl)propyl)-4-piperidyl)-2-benzimidazolinethione
1-butanone, 4-(4-(2,3-dihydro-2-thioxo-1h-benzimidazol-1-yl)-1-piperidinyl)-1-(4-fluorophenyl)-
2-benzimidazolinethione, 1-(1-(3-(p-fluorobenzoyl)propyl)-4-piperidyl)-
timiperona [inn-spanish]
dd 3480
einecs 260-880-9
D02035
timiperone (jan)
tolopelon (tn)
57648-21-2
CHEBI:135631
1-(4-fluorophenyl)-4-[4-(2-sulfanylidene-3h-benzimidazol-1-yl)piperidin-1-yl]butan-1-one
NCGC00182555-01
cas-57648-21-2
dtxcid803673
dtxsid9023673 ,
tox21_113628
CHEMBL2107117
FT-0675238
timiperona
626dq7n19l ,
timiperonum
unii-626dq7n19l
timiperone [jan]
timiperone [mart.]
timiperone [inn]
timiperone [who-dd]
timiperone [mi]
SCHEMBL145839
1-[1-(3-(4-fluorobenzoyl)propyl)-4-piperidyl]-2-mercaptobenzimidazole
SCHEMBL11797177
1-butanone, 4-[4-(2,3-dihydro-2-thioxo-1h-benzimidazol-1-yl)-1-piperidinyl]-1-(4-fluorophenyl)-
AKOS025396887
Q7806745
NCGC00387301-01
timiperone-d4(major)(containd0)
?timiperone

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Timiperone treatment of mice increased both the porphyrin content of the Harderian gland and the serum prolactin levels."( Effect of hyperprolactinemia induced by neuroleptic agent, timiperone, on porphyrin content of mouse harderian gland.
Kajimura, T; Nomura, M; Satoh, H, 1997
)
1.26

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

Dosage Studied

Haloperidol and sulpiride were superior to propericiazine and timiperone because they displayed a wider dose range. Blood concentrations of 14C indicate that absorption of [14C]timiperone on repeated dosage may be similar to that after a single dose.

ExcerptRelevanceReference
" By comparing the dose-response curves of four drugs tested in the same fashion, haloperidol and sulpiride were superior to propericiazine and timiperone because they displayed a wider dose range for the maintenance treatment of remitted schizophrenic outpatients."( Prophylactic effects of neuroleptics in symptom-free schizophrenics: a comparative dose-response study of timiperone and sulpiride.
Koga, I; Nishikawa, T; Tanaka, M; Tsuda, A; Uchida, Y, 1989
)
0.69
" Blood concentrations of 14C indicate that absorption of [14C]timiperone on repeated dosage may be similar to that after a single dose."( Disposition of timiperone, 4'-fluoro-4-[4-(2-thioxo-1-benzimidazolinyl)piperidino]butyrophenone, a neuroleptic, in the rat on repeated oral dosage.
Sano, M; Sudo, K; Tachizawa, H, 1981
)
0.86
[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 (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency33.49830.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency26.83250.000221.22318,912.5098AID743035; AID743063
estrogen nuclear receptor alphaHomo sapiens (human)Potency23.81950.000229.305416,493.5996AID743069; AID743078; AID743079; AID743080; AID743091
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency26.83250.001019.414170.9645AID743094
aryl hydrocarbon receptorHomo sapiens (human)Potency11.55080.000723.06741,258.9301AID743085; AID743122
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency18.83360.001723.839378.1014AID743083
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency26.60320.000323.4451159.6830AID743065; AID743067
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency23.71010.011917.942071.5630AID651632
Ataxin-2Homo sapiens (human)Potency23.71010.011912.222168.7989AID651632
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (18)

Processvia Protein(s)Taxonomy
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (16)

Assay IDTitleYearJournalArticle
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.
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.
AID1146540Ratio of ED50 for po dosed albino Wistar rat assessed as induction of catalepsy to ED50 for apomorphine-induced stereotyped behavior in po dosed albino Wistar rat1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1146536Inhibition of methamphetamine-induced stereotyped behavior in po dosed albino Wistar rat administered 2 hrs before methamphetamine challenge measured up to 3 hrs1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1146538Toxicity in po dosed albino Wistar rat assessed as induction of catalepsy after 8 hrs1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1146541Acute toxicity in po dosed STD-ddY mouse assessed as mortality up to 7 days1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1146545Ratio of benperidol ED50 to compound ED50 for apomorphine-induced stereotyped behavior in po dosed albino Wistar rat1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1146539Ratio of ED50 for po dosed albino Wistar rat assessed as induction of catalepsy to ED50 for methamphetamine-induced stereotyped behavior in po dosed albino Wistar rat1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1146543Ratio of benperidol ED50 to compound ED50 for methamphetamine-induced stereotyped behavior in po dosed albino Wistar rat1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1146544Ratio of haloperidol ED50 to compound ED50 for apomorphine-induced stereotyped behavior in po dosed albino Wistar rat1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1146542Ratio of haloperidol ED50 to compound ED50 for methamphetamine-induced stereotyped behavior in po dosed albino Wistar rat1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1146535Neuroleptic activity in po dosed STD-ddY mouse assessed as inhibition of spontaneous motor activity by measuring number of revolution of cage for 5 mins1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1146537Inhibition of apomorphine-induced stereotyped behavior in po dosed albino Wistar rat administered 2 hrs before apomorphine challenge measured after 20 mins1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
AID1146534Neuroleptic activity in po dosed STD-ddY mouse assessed as protection against methamphetamine-induced toxicity administered 1 hr before methamphetamine challenge measured after 24 hrs1978Journal of medicinal chemistry, Nov, Volume: 21, Issue:11
Psychotropic agents. 3. 4-(4-Substituted piperidinyl)-1-(4-fluorophenyl)-1-butanones with potent neuroleptic activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (28)

TimeframeStudies, This Drug (%)All Drugs %
pre-199019 (67.86)18.7374
1990's4 (14.29)18.2507
2000's1 (3.57)29.6817
2010's2 (7.14)24.3611
2020's2 (7.14)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.83

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 Index18.83 (24.57)
Research Supply Index3.53 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.83)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (13.79%)5.53%
Reviews1 (3.45%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other24 (82.76%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]