Page last updated: 2024-12-06

befuraline

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

Description

Befuraline is a synthetically produced compound that acts as a selective serotonin reuptake inhibitor (SSRI) and has demonstrated antidepressant activity in preclinical studies. It is structurally related to other SSRIs, such as fluoxetine (Prozac) and sertraline (Zoloft). Befuraline's synthesis typically involves multiple steps, starting with commercially available starting materials. It has shown promising results in animal models of depression, suggesting its potential as a novel antidepressant. However, it is currently not approved for clinical use. Research into befuraline is ongoing, focusing on its efficacy, safety, and potential therapeutic applications for depression and other related conditions. Due to its unique pharmacological properties, befuraline has generated interest in the field of drug discovery and development.'

befuraline: RN given refers to parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68664
CHEMBL ID1076256
SCHEMBL ID499156
MeSH IDM0065175

Synonyms (28)

Synonym
NCGC00160526-01
befuraline
1-benzofuran-2-yl-(4-benzylpiperazin-1-yl)methanone
CHEMBL1076256
dtxsid2046206 ,
dtxcid0026206
tox21_111873
cas-41717-30-0
AKOS015969748
unii-787aq35ghr
787aq35ghr ,
befuraline [inn]
41717-30-0
befuralina [inn-spanish]
befuralinum [inn-latin]
befuralinum
befuralina
1-(2-benzofuranylcarbonyl)-4-benzylpiperazine
n-benzo(b)furan-2-ylcarbonyl-n'-benzylpiperazine hydrochloride
MLS006011484
smr004703268
SCHEMBL499156
SRIJFPBZWUFLFD-UHFFFAOYSA-N
benzofuran-2-yl(4-benzylpiperazin-1-yl)methanone
Q4880386
FT-0720961
1-(1-benzofuran-2-carbonyl)-4-benzylpiperazine
EN300-6492975

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 (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency28.69540.007215.758889.3584AID624030
USP1 protein, partialHomo sapiens (human)Potency89.12510.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency30.05340.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency14.43930.000221.22318,912.5098AID743042; AID743054
estrogen nuclear receptor alphaHomo sapiens (human)Potency12.60820.000229.305416,493.5996AID743080; AID743091
aryl hydrocarbon receptorHomo sapiens (human)Potency23.71010.000723.06741,258.9301AID743085
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency6.68240.001723.839378.1014AID743083
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency22.38720.10009.191631.6228AID1346983
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency11.22020.00798.23321,122.0200AID2551
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency14.38180.005612.367736.1254AID624032
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (6)

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.
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.
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.
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.
AID464775Antagonist activity at PAR1 expressed in CHO cells assessed as inhibition of SFLLR-NH2-induced calcium release at 10 uM by FLIPR assay2010Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
Exploration of a new series of PAR1 antagonists.
AID468443Inhibition of human FAAH at 1 uM2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907 (58.33)18.7374
1990's0 (0.00)18.2507
2000's1 (8.33)29.6817
2010's3 (25.00)24.3611
2020's1 (8.33)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 (%)
Trials1 (7.69%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (92.31%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]