Page last updated: 2024-12-08

bifeprunox

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

Description

bifeprunox: an antipsychotic agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID208951
CHEMBL ID218166
CHEBI ID177517
SCHEMBL ID114371
MeSH IDM0497678

Synonyms (36)

Synonym
7-[4-[(3-phenylphenyl)methyl]piperazin-1-yl]-3h-1,3-benzoxazol-2-one
bifeprunox
CHEBI:177517
D06566
bifeprunox (usan/inn)
350992-10-8
bifeprunox [inn]
bdbm50241119
7-(4-biphenyl-3-ylmethyl-piperazin-1-yl)-3h-benzooxazol-2-one
CHEMBL218166 ,
L001659
2(3h)-benzoxazolone, 7-(4-((1,1'-biphenyl)-3-ylmethyl)-1-piperazinyl)-
ap69e83z79 ,
du 127090
7-(4-(biphenyl-3-ylmethyl)piperazin-1-yl)benzoxazol-2(3h)-one
bifeprunoxum
bifeprunox [usan:inn]
bifeprunoxum [inn-latin]
unii-ap69e83z79
7-[4-[(3-phenylphenyl)methyl]-1-piperazinyl]-3h-1,3-benzoxazol-2-one
A822533
AKOS015904572
7-[4-[(3-phenylphenyl)methyl]piperazin-1-yl]-3h-benzo[d]oxazol-2-one
bifeprunox [mi]
7-[4-(biphenyl-3-ylmethyl)piperazin-1-yl]benzoxazol-2(3h)-one
bifeprunox [who-dd]
bifeprunox [usan]
DB04888
SCHEMBL114371
CYGODHVAJQTCBG-UHFFFAOYSA-N
7-[4-[(3-phenylphenyl)methyl]piperazin-1-yl]-3h-benzooxazol-2-one
DTXSID80188592
7-[4-([1,1'-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3h)-benzoxazolone
Q4904729
HY-14547
CS-0003435

Research Excerpts

Overview

Bifeprunox is a novel antipsychotic drug designed to treat schizophrenia. It is a partial dopamine agonist with a unique receptor-binding profile.

ExcerptReferenceRelevance
"Bifeprunox is a novel antipsychotic drug designed to treat schizophrenia. "( Bifeprunox versus placebo for schizophrenia.
Chattopadhyay, A; Frey, S; Green, G, 2016
)
3.32
"Bifeprunox is a partial dopamine agonist with a unique receptor-binding profile and potential antipsychotic properties."( Efficacy and safety of bifeprunox in patients with an acute exacerbation of schizophrenia: results from a randomized, double-blind, placebo-controlled, multicenter, dose-finding study.
Casey, DE; Heisterberg, J; Sands, EE; Yang, HM, 2008
)
2.1

Treatment

ExcerptReferenceRelevance
"Treatment with Bifeprunox was found to significantly reduce all of the measured parameters except white fat mass compared to the control group."( Different effects of bifeprunox, aripiprazole, and haloperidol on body weight gain, food and water intake, and locomotor activity in rats.
De Santis, M; Deng, C; Huang, XF; Lian, J; Pan, B, 2014
)
1.06

Toxicity

The most common treatment-emergent adverse events (TEAEs) noted with bifeprunox were gastrointestinal. No clear dose-related trend in the incidence of any TEAE was observed.

ExcerptReferenceRelevance
" Safety and tolerability were assessed by monitoring adverse events, extrapyramidal symptoms (EPS), laboratory values, electrocardiograms, prolactin levels, and weight."( Efficacy and safety of bifeprunox in patients with an acute exacerbation of schizophrenia: results from a randomized, double-blind, placebo-controlled, multicenter, dose-finding study.
Casey, DE; Heisterberg, J; Sands, EE; Yang, HM, 2008
)
0.66
" The most common treatment-emergent adverse events (TEAEs) noted with bifeprunox were gastrointestinal; no clear dose-related trend in the incidence of any TEAE was observed in the bifeprunox groups."( Efficacy and safety of bifeprunox in patients with an acute exacerbation of schizophrenia: results from a randomized, double-blind, placebo-controlled, multicenter, dose-finding study.
Casey, DE; Heisterberg, J; Sands, EE; Yang, HM, 2008
)
0.89
" Bifeprunox appeared to be safe and well tolerated by patients in this 6-week study."( Efficacy and safety of bifeprunox in patients with an acute exacerbation of schizophrenia: results from a randomized, double-blind, placebo-controlled, multicenter, dose-finding study.
Casey, DE; Heisterberg, J; Sands, EE; Yang, HM, 2008
)
1.57
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
biphenylsBenzenoid aromatic compounds containing two phenyl or substituted-phenyl groups which are joined together by a single bond.
[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 (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.00860.00010.532610.0000AID1803435; AID4442; AID457695
D(2) dopamine receptorHomo sapiens (human)IC50 (µMol)0.00290.00000.74728.0000AID727074
D(2) dopamine receptorHomo sapiens (human)Ki0.00230.00000.651810.0000AID1154611; AID1803434; AID457694; AID458632; AID458633; AID63971; AID727075
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki3.31130.00010.601710.0000AID277974
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.06460.00010.739610.0000AID277973
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.00150.00000.437510.0000AID277975
TransporterRattus norvegicus (Norway rat)Ki0.00930.00010.76295.5000AID457695
[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)EC50 (µMol)0.32360.00010.25718.0000AID277976
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (112)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (33)

Assay IDTitleYearJournalArticle
AID1803435Binding Affinity Assay from Article 10.3109/14756366.2013.776556: \\Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.\\2014Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 29, Issue:2
Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.
AID1803434Binding Affinity Assay from Article 10.3109/14756366.2013.776556: \\Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.\\2014Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 29, Issue:2
Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.
AID1474758Agonist activity at D2 long receptor (unknown origin) expressed in Flp-In-CHO cells assessed as change in transduction coefficient by measuring induction of ERK1/2 phosphorylation after 5 mins by Alphascreen assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.
AID727075Displacement of [3H]raclopride from human D2 dopamine receptor expressed in CHO cell membranes2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Synthesis and SAR of aminothiazole fused benzazepines as selective dopamine D2 partial agonists.
AID457694Agonist activity at dopamine D2 receptor2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors.
AID458634Selectivity ratio of Ki for human dopamine D2 receptor at low affinity state to Ki for human dopamine D2 receptor at high affinity state2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID1474757Agonist activity at D2 long receptor (unknown origin) expressed in Flp-In-CHO cells co-expressing Rluc8-tagged Galphai1 assessed as change in transduction coefficient by measuring Galphai1 activation after 5 mins in presence of coelenterazine by BRET assa2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.
AID277975Displacement of [3H]YM-09151-2 from rat striatum D2 receptor2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID63971Binding affinity for dopamine receptor D2 determined using [3H]spiperone2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID177715In vivo suppression of the conditioned avoidance response (CAR) in rats after po administration of the compound2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID458635Activity at dopamine D2L receptor expressed in HEK293 cells coexpressing Galphaqi5 assessed as maximal efficacy relative to control2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID1154611Displacement of [3H]nemonapride from dopamine D2L receptor (unknown origin) expressed in African green monkey COS7 cells2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands.
AID458652Reduction in amphetamine-induced locomotor activity in Sprague-Dawley rat striatum at 7.68 umol/kg, sc relative to control2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID4442Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID458633Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID1474756Agonist activity at D2 long receptor (unknown origin) expressed in Flp-In-CHO cells co-expressing Rluc8-tagged GalphaoB assessed as change in transduction coefficient by measuring GalphaoB activation in presence of coelenterazine by BRET assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.
AID457695Agonist activity at 5HT1A receptor2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Searching for multi-target antipsychotics: Discovery of orally active heterocyclic N-phenylpiperazine ligands of D2-like and 5-HT1A receptors.
AID277973Displacement of [3H]OH-DPAT from rat cortex 5HT1A receptor2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID1474755Agonist activity at Rluc8-tagged D2 long receptor (unknown origin) expressed in Flp-In-CHO cells co-expressing YFP-tagged beta-arrestin2 assessed as change in transduction coefficient by measuring beta-arrestin2 recruitment measured after 5 mins by BRET a2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.
AID277976Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTP-gamma-S binding2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID277974Displacement of [3H]ketanserin from rat cortex 5HT2A receptor2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID1474754Displacement of [3H]spiperone from D2 long receptor (unknown origin) expressed in Flp-In-CHO cell membranes assessed as transduction coefficient by measuring dissociation half life after 5 mins by liquid scintillation counter method2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.
AID727076Intrinsic agonist activity at human D2 dopamine receptor expressed in CHO cell membrane using cellular CD spectroscopy by Cell-Key assay2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Synthesis and SAR of aminothiazole fused benzazepines as selective dopamine D2 partial agonists.
AID458632Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID130711In vivo inhibition of the apomorphine-induced climbing behavior in mice2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID458647Reduction in spontaneous locomotor activity in Sprague-Dawley rat striatum at 7.68 umol/kg, sc relative to control2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
AID1474759Agonist activity at D2 long receptor (unknown origin) expressed in Flp-In-CHO cells assessed as change in transduction coefficient by measuring inhibition of forskolin-induced cAMP production measured after 5 mins in presence of coelenterazine by BRET ass2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.
AID727074Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Synthesis and SAR of aminothiazole fused benzazepines as selective dopamine D2 partial agonists.
AID277977Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation of [35S]GTPgammaS binding relative to serotonin2007Journal of medicinal chemistry, Feb-22, Volume: 50, Issue:4
Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
AID179817Tested for occurrence of lower lip retraction in rat after po administration of the compound2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
AID1474767Agonist activity at D2 long receptor (unknown origin) expressed in Flp-In-CHO cells assessed as change in transduction coefficient by measuring cellular impedance measured immediately at 15 secs interval for 90 mins by xCELLigence assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective.
AID1154614Intrinsic activity at human dopamine D2L receptor expressed in Sf9 cell membrane by [35S]GTPgammaS binding assay2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands.
AID458630Reduction in 3,4-dihydroxyphenylacetic acid level in Sprague-Dawley rat striatum at 7.68 umol/kg, sc relative to saline treated control2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
Synthesis and evaluation of a set of 4-phenylpiperidines and 4-phenylpiperazines as D2 receptor ligands and the discovery of the dopaminergic stabilizer 4-[3-(methylsulfonyl)phenyl]-1-propylpiperidine (huntexil, pridopidine, ACR16).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (30)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's16 (53.33)29.6817
2010's14 (46.67)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.80

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 Index28.80 (24.57)
Research Supply Index3.47 (2.92)
Research Growth Index4.42 (4.65)
Search Engine Demand Index32.40 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.80)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (3.33%)5.53%
Reviews4 (13.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other25 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]