Page last updated: 2024-11-12

lassbio-579

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Description

LASSBio-579: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11624518
CHEMBL ID597601
SCHEMBL ID6014220
MeSH IDM0508093

Synonyms (10)

Synonym
L022513
lassbio-579
CHEMBL597601 ,
bdbm50308002
1-[(1-(4-chlorophenyl)-1h-pyrazol-4-yl)methyl]-4-phenylpiperazine
591774-47-9
SCHEMBL6014220
1-[[1-(4-chlorophenyl)pyrazol-4-yl]methyl]-4-phenylpiperazine
DTXSID10469649
PD089339
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki4.57000.00010.601710.0000AID457689; AID734513
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki2.60000.00010.949010.0000AID763652
D(4) dopamine receptorHomo sapiens (human)Ki0.17500.00000.436210.0000AID734514; AID763658
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki2.49000.00000.937510.0000AID734510
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki8.53500.00010.954910.0000AID734511; AID763655
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki2.49000.00000.437510.0000AID734510
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (43)

Processvia Protein(s)Taxonomy
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral fear responseD(4) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(4) dopamine receptorHomo sapiens (human)
response to amphetamineD(4) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
adult locomotory behaviorD(4) dopamine receptorHomo sapiens (human)
positive regulation of sodium:proton antiporter activityD(4) dopamine receptorHomo sapiens (human)
positive regulation of kinase activityD(4) dopamine receptorHomo sapiens (human)
response to histamineD(4) dopamine receptorHomo sapiens (human)
social behaviorD(4) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(4) dopamine receptorHomo sapiens (human)
fear responseD(4) dopamine receptorHomo sapiens (human)
regulation of circadian rhythmD(4) dopamine receptorHomo sapiens (human)
positive regulation of MAP kinase activityD(4) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(4) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(4) dopamine receptorHomo sapiens (human)
rhythmic processD(4) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(4) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(4) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
inhibitory postsynaptic potentialD(4) dopamine receptorHomo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationD(4) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(4) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathwayD(4) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(4) dopamine receptorHomo sapiens (human)
chemical synaptic transmissionD(4) dopamine receptorHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(4) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
protein bindingD(4) dopamine receptorHomo sapiens (human)
potassium channel regulator activityD(4) dopamine receptorHomo sapiens (human)
SH3 domain bindingD(4) dopamine receptorHomo sapiens (human)
dopamine bindingD(4) dopamine receptorHomo sapiens (human)
identical protein bindingD(4) dopamine receptorHomo sapiens (human)
metal ion bindingD(4) dopamine receptorHomo sapiens (human)
epinephrine bindingD(4) dopamine receptorHomo sapiens (human)
norepinephrine bindingD(4) dopamine receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityD(4) dopamine receptorHomo sapiens (human)
neurotransmitter receptor activityD(4) dopamine receptorHomo sapiens (human)
serotonin bindingD(4) dopamine receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
centrosomeD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
membraneD(4) dopamine receptorHomo sapiens (human)
postsynapseD(4) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(4) dopamine receptorHomo sapiens (human)
plasma membraneD(4) dopamine receptorHomo sapiens (human)
dendriteD(4) dopamine receptorHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (37)

Assay IDTitleYearJournalArticle
AID763656Displacement of [3H]-ketanserin from 5HT2A receptor in rat brain cortical membranes after 15 mins by liquid scintillation counting2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
AID734514Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID734509Displacement of [3H]-prazosin from alpha1B adrenergic receptor in Wistar rat liver membrane after 45 mins by liquid scintillation counting2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID457691Selectivity index, ratio of Ki for Wistar rat striatum D2-like receptor to Ki for Wistar rat cortex 5HT2A 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.
AID763635Antipsychotic activity in CF1 mouse assessed as prevention of apomorphine-induced climbing behaviour at 0.1 to 10 mg/kg, ip administered 30 mins prior apomorphine challenge measured 5 to 30 mins post challenge2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
AID734512Displacement of [3H]-OH-8-DPAT from 5HT1A receptor in Wistar rat hippocampal membrane after 15 mins by liquid scintillation counting2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID763657Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in rat brain hippocampal membranes after 15 mins by liquid scintillation counting2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
AID734510Displacement of [3H]-RX821002 from alpha2A adrenergic receptor in Wistar rat cortical membrane after 45 mins by liquid scintillation counting2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID457697Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 15 mg/kg, po after 30 mins (Rvb = 1.8 +/- 1.1 sec)2010Bioorganic & 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.
AID734511Displacement of [3H]-mesulergine from human 5HT2C receptor after 60 mins by liquid scintillation counting2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID457689Displacement of [3H]ketanserin from 5HT2A receptor in Wistar rat cortex homogenate2010Bioorganic & 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.
AID457700Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 30 mg/kg, po after 30 mins (Rvb = 1.8 +/- 1.1 sec)2010Bioorganic & 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.
AID457687Displacement of [3H]nemonapride from D2-like receptor in Wistar rat striatum homogenate2010Bioorganic & 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.
AID457699Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 15 mg/kg, po after 90 mins (Rvb = 2.4 +/- 2.6 sec)2010Bioorganic & 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.
AID457692Selectivity index, ratio of Ki for Wistar rat hippocampus 5HT1A receptor to Ki for Wistar rat cortex 5HT2A 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.
AID734520Drug metabolism in Wistar rat assessed as CYP1A2-mediated p-hydroxylated metabolite formation at 50 mg/kg, ip after 48 hrs by HPLC analysis2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID457696Antipsychotic activity in CF1 mouse assessed as reduction in apomorphine-induced climbing at 15 mg/kg, po2010Bioorganic & 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.
AID457706Toxicity in CF1 mouse assessed as induction of motor impairment by measuring permanence time at 15 mg/kg, po by rotarod test (Rvb = 241.4 +/- 18.0 sec)2010Bioorganic & 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.
AID763654Displacement of [3H]-RX821002 from alpha2 adrenoreceptor in rat brain cortical membranes after 45 mins by liquid scintillation counting2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
AID734513Displacement of [3H]-ketanserin from 5HT2A receptor in Wistar rat cortical membrane after 15 mins by liquid scintillation counting2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID457688Displacement of [3H]-8-OH-DPAT from 5HT1A receptor in Wistar rat hippocampus homogenate2010Bioorganic & 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.
AID734517Drug metabolism in Wistar rat assessed as CYP1A2-mediated decrease in parent compound level at 50 mg/kg, ip after 30 mins by HPLC analysis2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID734515Displacement of [3H]-YM-09151-2 from D2 dopamine receptor in Wistar rat brain striatal membrane after 60 mins by liquid scintillation counting2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID734518Drug metabolism in Wistar rat assessed as CYP1A2-mediated p-hydroxylated metabolite formation at 50 mg/kg, ip after 30 mins by HPLC analysis2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID763652Displacement of [3H]-prozosin from alpha1B adrenoreceptor in rat liver membranes after 45 mins by liquid scintillation counting2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
AID763651Displacement of [3H]-QNB from muscarinic receptor in rat brain cortical membranes at 30 uM after 60 mins by liquid scintillation counting2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
AID763659Displacement of [3H]-YM-09151-2 from D2 receptor in rat brain striatal membranes after 60 mins by liquid scintillation counting2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
AID734516Drug metabolism in Wistar rat plasma assessed as p-hydroxylated metabolite level at 50 mg/kg, ip after 24 hrs2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID457698Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 15 mg/kg, po after 60 mins (Rvb = 2.7 +/- 2.9 sec)2010Bioorganic & 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.
AID763629Selectivity ratio of Ki for dopamine D2 receptor in rat brain striatal membranes to Ki for 5HT2A receptor in rat brain cortical membranes2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
AID457701Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 30 mg/kg, po after 60 mins (Rvb = 2.7 +/- 2.9 sec)2010Bioorganic & 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.
AID734519Drug metabolism in Wistar rat assessed as CYP1A2-mediated decrease in parent compound level at 50 mg/kg, ip after 48 hrs by HPLC analysis2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID763655Displacement of [3H]-mesulergine from human 5HT2C receptor after 60 mins by liquid scintillation counting2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
AID457690Selectivity index, ratio of Ki for Wistar rat striatum D2-like receptor to Ki for Wistar rat hippocampus 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.
AID734508Displacement of [3H]-QNB from muscarinic receptor in Wistar rat brain membrane after 60 mins by liquid scintillation counting2013European journal of medicinal chemistry, Apr, Volume: 62Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
AID763658Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579.
AID457702Toxicity in CF1 mouse assessed as induction of catalepsy by measuring time spent on elevated wood bar at 30 mg/kg, po after 90 mins (Rvb = 2.4 +/- 2.6 sec)2010Bioorganic & 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (30.00)29.6817
2010's7 (70.00)24.3611
2020's0 (0.00)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%
Reviews1 (10.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (90.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]