Page last updated: 2024-11-06

setoperone

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

Setoperone is a dopamine antagonist and 5-HT2A receptor antagonist with antipsychotic properties. It was initially developed in the 1970s but never gained widespread clinical use. Setoperone is of interest in research because of its unique pharmacological profile, which may offer potential advantages over existing antipsychotic medications, such as a lower risk of extrapyramidal side effects. Setoperone's effects are characterized by its ability to block dopamine receptors, which are involved in the regulation of movement, motivation, and reward. Its antagonism of the 5-HT2A receptor suggests potential benefits in treating cognitive and negative symptoms of schizophrenia. Setoperone's synthesis involves a multi-step process that starts with the reaction of 1-methylpiperazine with a substituted benzophenone derivative. Research on setoperone aims to investigate its therapeutic potential for treating schizophrenia and other mental health conditions, as well as to understand its mechanism of action and its safety profile.'

Cross-References

ID SourceID
PubMed CID68604
CHEMBL ID2105437
SCHEMBL ID122185
MeSH IDM0131936

Synonyms (47)

Synonym
r-52245
setoperone
86487-64-1
setoperone (usan/inn)
D02686
PDSP1_001662
PDSP1_001224
PDSP2_001208
PDSP2_001646
setoperona [spanish]
6-(2-(4-(p-fluorobenzoyl)piperidino)ethyl)-2,3-dihydro-7-methyl-5h-thiazolo(3,2-alpha)pyrimidin-5-one
setoperone [usan:inn]
r 52,245
5h-thiazolo(3,2-a)pyrimidin-5-one, 6-(2-(4-(4-fluorobenzoyl)-1-piperidinyl)ethyl)-2,3-dihydro-7-methyl-
setoperonum [latin]
6-(2-(4-(p-fluorobenzoyl)piperidino)ethyl)-2,3-dihydro-7-methyl-5h-thiazolo(3,2-a)pyrimidin-5-one
L000809
6-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-7-methyl-2,3-dihydro-[1,3]thiazolo[3,2-a]pyrimidin-5-one
5h-thiazolo[3,2a]pyrimidin-5-one, 6-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2,3-dihydro-7-methyl-
cas_86487-64-1
septoperone
bdbm81814
setoperona
unii-bq67cs3q3e
setoperonum
bq67cs3q3e ,
CHEMBL2105437
6-(2-(4-(p-fluorobenzoyl)piperidino)ethyl)-2,3-dihydro-7-methyl-5h-thiazolo(3,2-.alpha.)pyrimidin-5-one
setoperone [inn]
setoperone [who-dd]
setoperone [usan]
SCHEMBL122185
dtxcid0031637
NCGC00262950-01
cas-86487-64-1
tox21_113942
dtxsid9057848 ,
6-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2,3-dihydro-7-methyl-5h-thiazolo[3,2-a]pyrimidin-5-one
RBGAHDDQSRBDOG-UHFFFAOYSA-N
setoperone > 95 %
AKOS030530828
6-(2-(4-(4-fluorobenzoyl)piperidin-1-yl)ethyl)-7-methyl-2h-thiazolo[3,2-a]pyrimidin-5(3h)-one
6-(2-(4-(4-fluorobenzoyl)piperidin-1-yl)ethyl)-7-methyl-2,3-dihydro-5h-thiazolo[3,2-a]pyrimidin-5-one
FT-0738877
Q7456821
5h-thiazolo[3,2a]pyrimidin-5-one,6-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2,3-dihydro-7-methyl-
6-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2,3-dihydro-7-methyl-5h-thiazolo[3,2a]pyrimidin-5-one

Research Excerpts

Overview

18F-setoperone is a well-validated and widely used PET radioligand for the study of neocortical 5HT2AR.

ExcerptReferenceRelevance
"18F-setoperone is a well-validated and widely used PET radioligand for the study of neocortical 5HT2AR."( Parametric PET imaging of 5HT2A receptor distribution with 18F-setoperone in the normal human neocortex.
Baron, JC; Barré, L; Landeau, B; Noël, MH; Onfroy, MC; Petit-Taboué, MC, 1999
)
1.02

Dosage Studied

ExcerptRelevanceReference
" RO was nearly complete at 4 hr after dosing (98%) and remained elevated at 18 hr (46%)."( Positron emission tomographic analysis of central 5-hydroxytryptamine2 receptor occupancy in healthy volunteers treated with the novel antipsychotic agent, ziprasidone.
Alpert, NM; Babich, JW; Bonab, AA; Elmaleh, DR; Fischman, AJ; Rauch, SL; Rubin, RH; Shoup, TM; Williams, SA, 1996
)
0.29
" The data suggest that daily dosing of > or =3 mg EMD 281014 should be sufficient to provide sustained high levels of 5HT2-receptor occupancy in future clinical trials."( EMD 281014, a specific and potent 5HT2 antagonist in humans: a dose-finding PET study.
Kapur, S; Mamo, D; Romach, MK; Sedman, E; Sellers, EM; Tillner, J, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency18.15850.002541.796015,848.9004AID1347395; AID1347397; AID1347398
GLI family zinc finger 3Homo sapiens (human)Potency8.04980.000714.592883.7951AID1259369; AID1259392
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency38.90180.01237.983543.2770AID1645841
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency11.42590.001530.607315,848.9004AID1224841; AID1224848; AID1224849; AID1259401; AID1259403
estrogen nuclear receptor alphaHomo sapiens (human)Potency19.93180.000229.305416,493.5996AID1259244; AID1259248
cytochrome P450 2D6Homo sapiens (human)Potency0.27540.00108.379861.1304AID1645840
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency14.18440.000627.21521,122.0200AID743202; AID743219
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency23.71010.001557.789015,848.9004AID1259244
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency23.71010.001551.739315,848.9004AID1259244
[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 2ARattus norvegicus (Norway rat)Ki0.00230.00010.601710.0000AID1855085
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.01200.00000.965010.0000AID1855087
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.02400.00000.437510.0000AID1855086
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (37)

Assay IDTitleYearJournalArticle
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1508628Confirmatory 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.
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.
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.
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.
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.
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.
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.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1855086Displacement of [3H]-haloperidol from rat striatal homogenate D2 receptor2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1855085Displacement of [3H]-spiperone from rat frontal cortex homogenate 5-HT2A receptor2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
AID1855087Displacement of [3H]-WB4101 from rat forebrain homogenate alpha 1 adrenergic receptor2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (65)

TimeframeStudies, This Drug (%)All Drugs %
pre-199012 (18.46)18.7374
1990's23 (35.38)18.2507
2000's15 (23.08)29.6817
2010's8 (12.31)24.3611
2020's7 (10.77)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.29

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index10.29 (24.57)
Research Supply Index4.33 (2.92)
Research Growth Index4.62 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.29)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (13.64%)5.53%
Reviews1 (1.52%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other56 (84.85%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]