Compounds > lassbio-581
Page last updated: 2024-11-12

lassbio-581

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

Description

LASSBio-581: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10338184
CHEMBL ID609043
SCHEMBL ID6014209
MeSH IDM0472849

Synonyms (15)

Synonym
L022512
CHEMBL609043 ,
lassbio-581
1-[(1-(4-chlorophenyl)-1h-1,2,3-triazol-4-yl)methyl]-4-phenylpiperazine
1-((1-(4-chlorophenyl)-1h-1,2,3-triazol-4-yl)methyl)-4-phenylpiperazine
bdbm50308003
591774-48-0
SCHEMBL6014209
1-[[1-(4-chlorophenyl)triazol-4-yl]methyl]-4-phenylpiperazine
DTXSID20438381
AKOS033299537
1-{[1-(4-chlorophenyl)-1h-1,2,3-triazol-4-yl]methyl}-4-phenylpiperazine
EN300-22170015
PD089335
Z1376870650

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"2%), where the half-life was three times bigger than in the other tissues (1."( Pharmacokinetics and tissue distribution of a new heterocyclic N-phenylpiperazine derivative (LASSBio-581) in rats.
Barreiro, E; Costa, TD; Eifler-Lima, V; Fraga, CA; Menegatti, R; Neves, G; Rates, SM; Tasso, L, 2005)		0.55

Bioavailability

ExcerptReferenceRelevance
" The oral bioavailability ( approximately 25%) was approximately half of the intra-peritoneal one ( approximately 47%)."( Pharmacokinetics and tissue distribution of a new heterocyclic N-phenylpiperazine derivative (LASSBio-581) in rats.
Barreiro, E; Costa, TD; Eifler-Lima, V; Fraga, CA; Menegatti, R; Neves, G; Rates, SM; Tasso, L, 2005)		0.55
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki5.46050.00010.601710.0000AID457689; AID480674
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (9)

Assay IDTitleYearJournalArticle
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.
AID480674Displacement of [3H]ketanserin from 5HT2A receptor in rat cortex membrane2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Design of new dopamine D2 receptor ligands: biosynthesis and pharmacological evaluation of the hydroxylated metabolite of LASSBio-581.
AID480672Displacement of [3H]YM-9151-2 from D2 like receptor in rat striatal membrane2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Design of new dopamine D2 receptor ligands: biosynthesis and pharmacological evaluation of the hydroxylated metabolite of LASSBio-581.
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.
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.
AID480673Displacement of [3H]8-OH-DPAT from 5HT1A receptor in rat hippocampal membrane2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Design of new dopamine D2 receptor ligands: biosynthesis and pharmacological evaluation of the hydroxylated metabolite of LASSBio-581.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (66.67)29.6817
2010's2 (33.33)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%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
haloperidol
Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.		2.4520aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
phenylpiperazine
phenylpiperazine: RN given refers to parent cpd		2.4320
aripiprazole
Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.. aripiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders.		2.0510aromatic ether;
delta-lactam;
dichlorobenzene;
N-alkylpiperazine;
N-arylpiperazine;
quinolone		drug metabolite;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic agonist
bifeprunox
bifeprunox: an antipsychotic agent		2.0510biphenyls
lassbio-579
LASSBio-579: structure in first source		7.7430
clozapine
Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.		2.0510benzodiazepine;
N-arylpiperazine;
N-methylpiperazine;
organochlorine compound		adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
GABA antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
xenobiotic
ConditionIndicatedRelationship StrengthStudiesTrials
Dementia Praecox
[description not available]		02.0510
Schizophrenia
A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.		02.0510
Hypothermia, Accidental
[description not available]		02.0410
Hypothermia
Lower than normal body temperature, especially in warm-blooded animals.		07.0410