Page last updated: 2024-12-06

lenperone

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

Description

lenperone: antipsychotic of the butyrophenone class; like other major tranquilizers, it has some alpha-adrenergic blocking action & is antiemetic; minor descriptor (76-85); on-line & Index Medicus search BUTYROPHENONES (76-85); RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID32593
CHEMBL ID316004
SCHEMBL ID121686
MeSH IDM0262986

Synonyms (52)

Synonym
CHEMBL316004 ,
ahr-2277 [as hydrochloride]
24678-13-5
D02668
lenperone (usan)
lenperona [inn-spanish]
einecs 246-399-7
lenperona [spanish]
lenperone [usan:inn]
lenperonum [latin]
lenperone
1-butanone, 4-(4-(4-fluorobenzoyl)-1-piperidinyl)-1-(4-fluorophenyl)-
lenperonum [inn-latin]
brn 1554429
4'-fluoro-4-(4-(p-fluorobenzoyl)piperidino)butyrophenone
4-[4-(4-fluorobenzoyl)-1-piperidyl]-1-(4-fluorophenyl)butan-1-one
1-butanone, {4-[4-(4-fluorobenzoyl)-1-piperidinyl]-1-(4-fluorophenyl)-,} hydrochloride
4-(4-(4-fluorobenzoyl)-1-piperidinyl)-1-(4-fluorophenyl)-1-butanone
butyrophenone, 4'-fluoro-4-[4-(p-fluorobenzoyl)piperidino]-
lenperone hydrochloride (*hydrochloride*)
butyrophenone, {4'-fluoro-4-[4-(p-fluorobenzoyl)piperidino]-,} hydrochloride
1-butanone, 4-[4-(4-fluorobenzoyl)-1-piperidinyl]-1-(4-fluorophenyl)-
4-[4-(4-fluoro-benzoyl)-piperidin-1-yl]-1-(4-fluoro-phenyl)-butan-1-one
NCGC00160383-01
MLS001205808
smr000504164
4-[4-(4-fluorobenzoyl)piperidin-1-yl]-1-(4-fluorophenyl)butan-1-one
4-[4-(4-fluorobenzoyl)-1-piperidinyl]-1-(4-fluorophenyl)-1-butanone
bdbm50004320
HMS2834C09
cas-24678-13-5
dtxsid7046120 ,
dtxcid5026120
tox21_111775
5-21-08-00146 (beilstein handbook reference)
13p4gx22es ,
lenperonum
unii-13p4gx22es
lenperona
FT-0670760
lenperone [usan]
lenperone [who-dd]
ahr-2277 free base
lenperone [inn]
SCHEMBL121686
WCIBOXFOUGQLFC-UHFFFAOYSA-N
tox21 111775
1-(4-fluorophenyl)-4-{4-[(4-fluorophenyl)carbonyl]piperidin-1-yl}butan-1-one
Q6523202
4-(4-(4-fluorobenzoyl)piperidin-1-yl)-1-(4-fluorophenyl)butan-1-one
NCGC00160383-02
AKOS040747035

Research Excerpts

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]

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency1.41250.044717.8581100.0000AID485294
TDP1 proteinHomo sapiens (human)Potency19.93870.000811.382244.6684AID686978; AID686979
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.25890.01237.983543.2770AID1346984
pregnane X nuclear receptorHomo sapiens (human)Potency15.84890.005428.02631,258.9301AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency19.32800.000229.305416,493.5996AID743069; AID743075; AID743079
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency19.95260.354828.065989.1251AID504847
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency28.18383.548119.542744.6684AID743266
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency0.08910.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency32.55480.000323.4451159.6830AID743065; AID743067
gemininHomo sapiens (human)Potency20.59620.004611.374133.4983AID624296
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency31.62280.009610.525035.4813AID1479145
[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)Ki0.17460.00020.667710.0000AID4755; AID4766; AID5225; AID5295
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.00420.00010.601710.0000AID5225; AID5295
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.30500.00010.739610.0000AID4338
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.00420.00020.590910.0000AID5225; AID5295
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (43)

Assay IDTitleYearJournalArticle
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
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.
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.
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.
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.
AID4766Tested for binding affinity against 5-hydroxytryptamine 1C receptor from rat frontal cortical regions using [3H]mesulergine as radioligand1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist.
AID232692Selectivity ratio, Ki against 5-HT1C versus 5-HT21993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
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]
AID5225Binding affinity against 5-hydroxytryptamine 2 receptor in rat using [3H]ketanserin as radioligand1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' 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]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
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]
AID4338Tested for binding affinity against 5-hydroxytryptamine 1A receptor from rat frontal cortical regions using [3H]8-OH-DPAT as radioligand1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' 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
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID4755Binding affinity against 5-hydroxytryptamine 1C receptor in rat using [3H]mesulergine as radioligand1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
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]
AID232235Selectivity ratio for 5-HT1C compared to 5-HT2 receptors.1992Journal of medicinal chemistry, Dec-25, Volume: 35, Issue:26
Ketanserin analogues: structure-affinity relationships for 5-HT2 and 5-HT1C serotonin receptor binding.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID5295Tested for binding affinity against 5-hydroxytryptamine 2 receptor from rat frontal cortical regions using [3H]ketanserin as radioligand1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Antagonism of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane stimulus with a newly identified 5-HT2- versus 5-HT1C-selective antagonist.
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]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (29.41)18.7374
1990's4 (23.53)18.2507
2000's1 (5.88)29.6817
2010's5 (29.41)24.3611
2020's2 (11.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies1 (5.56%)4.05%
Observational0 (0.00%)0.25%
Other17 (94.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]