Page last updated: 2024-12-04

afloqualone

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

Cross-References

ID SourceID
PubMed CID2040
CHEMBL ID2105918
CHEBI ID31177
SCHEMBL ID400184
MeSH IDM0104009

Synonyms (62)

Synonym
AC-1608
afloqualona [inn-spanish]
afloqualon
hq 495
afloqualonum [inn-latin]
afloqualone [inn:jan]
brn 0819769
4(3h)-quinazolinone, 6-amino-2-(fluoromethyl)-3-(2-methylphenyl)-
6-amino-2-(fluoromethyl)-3-o-tolyl-4(3h)-quinazolinone
c16h14fn3o
6-amino-2-(fluoromethyl)-3-o-tolyl-4(3h)-chinazolinon
6-amino-3,4-dihydro-2-fluoromethyl-3-(2-methylphenyl)-4-chinazolinon
AKOS015842375
arofuto
afloqualone
hq-495
6-amino-2-(fluoromethyl)-3-(2-methylphenyl)quinazolin-4(3h)-one
airomate (tn)
afloqualone (jp17/inn)
56287-74-2
D01638
FT-0653844
6-amino-2-(fluoromethyl)-3-(2-methylphenyl)quinazolin-4-one
6-azanyl-2-(fluoranylmethyl)-3-(2-methylphenyl)quinazolin-4-one
A830986
6-amino-2-(fluoromethyl)-3-(2-methylphenyl)-4-quinazolinone
tox21_112447
dtxsid5022562 ,
dtxcid802562
cas-56287-74-2
6-amino-2-(fluoromethyl)-3-(2-methylphenyl)-quinazolin-4-one
airomate
CHEMBL2105918
S3663
unii-co4u2c8orz
afloqualona
afloqualonum
co4u2c8orz ,
MLS006010086
smr004701231
afloqualone [mi]
afloqualone [inn]
afloqualone [who-dd]
afloqualone [jan]
afloqualone [mart.]
2-fluoromethyl-3-(o-tolyl)-6-amino-4(3h)-quinazolinone
VDOSWXIDETXFET-UHFFFAOYSA-N
CS-5009
SCHEMBL400184
HY-B1833
6-amino-2-(fluoromethyl)-3-(o-tolyl)quinazolin-4(3h)-one
6-amino-2-(fluoromethyl)-3-(2-methylphenyl)-4(3h)-quinazolinone
CHEBI:31177
6-amino-2-(fluoromethyl)-3-o-tolylquinazolin-4(3h)-one
Q4689289
mfcd00867693
AS-11726
BCP13264
HMS3885G19
CCG-267278
NCGC00167443-02
D95096

Research Excerpts

Overview

Aloqualone is an oral muscle relaxant. It evokes ultraviolet A (UVA)-induced photosensitivity dermatitis as a side effect.

ExcerptReferenceRelevance
"Afloqualone (AQ) is an oral muscle relaxant and evokes ultraviolet A (UVA)-induced photosensitivity dermatitis as a side effect. "( Afloqualone photosensitivity: immunogenicity of afloqualone-photomodified epidermal cells.
Ogai, M; Takigawa, M; Tokura, Y; Yagi, H, 1994
)
3.17

Bioavailability

ExcerptReferenceRelevance
" Similarly, clinical myotonolytic activity of eperisone would only be expected at high doses unless its functional bioavailability were to be much better in man than in either the mouse or rabbit."( Comparison of the myotonolytic activity of tizanidine, eperisone and afloqualone in mouse and rabbit.
Coward, DM; White, TG,
)
0.37
"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]

Drug Classes (1)

ClassDescription
organic molecular entityAny molecular entity that contains carbon.
[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 (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency26.60320.000221.22318,912.5098AID743040
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency7.07950.01237.983543.2770AID1346984
estrogen nuclear receptor alphaHomo sapiens (human)Potency23.49050.000229.305416,493.5996AID743075; AID743077; AID743079
aryl hydrocarbon receptorHomo sapiens (human)Potency29.01450.000723.06741,258.9301AID743085; AID743122
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency5.62340.009610.525035.4813AID1479145
[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 (8)

Assay IDTitleYearJournalArticle
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.
AID1137315Induction of CNS depressant activity in ip dosed ddk mouse assessed as protection against maximal electroshock-induced tonic hind limb extensor seizures administered 30 mins prior to electroshock challenge1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on biologically active halogenated compounds. 1. Synthesis and central nervous system depressant activity of 2-(fluoromethyl)-3-aryl-4(3H)-quinazolinone derivatives.
AID1137312Acute toxicity in ip dosed ddk mouse assessed as lethality after 72 hrs1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on biologically active halogenated compounds. 1. Synthesis and central nervous system depressant activity of 2-(fluoromethyl)-3-aryl-4(3H)-quinazolinone derivatives.
AID1137313Induction of CNS depressant activity in ip dosed ddk mouse assessed as loss of righting reflex activity over 20 secs1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on biologically active halogenated compounds. 1. Synthesis and central nervous system depressant activity of 2-(fluoromethyl)-3-aryl-4(3H)-quinazolinone derivatives.
AID1137314Induction of CNS depressant activity in ip dosed ddk mouse after 30 mins by rotating rod test1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on biologically active halogenated compounds. 1. Synthesis and central nervous system depressant activity of 2-(fluoromethyl)-3-aryl-4(3H)-quinazolinone derivatives.
AID1137316Induction of CNS depressant activity in ip dosed ddk mouse assessed as protection against pentylenetetrazole-induced tonic extensive convulsions administered 30 mins prior to pentylenetetrazole challenge1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
Studies on biologically active halogenated compounds. 1. Synthesis and central nervous system depressant activity of 2-(fluoromethyl)-3-aryl-4(3H)-quinazolinone derivatives.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (32)

TimeframeStudies, This Drug (%)All Drugs %
pre-199016 (50.00)18.7374
1990's7 (21.88)18.2507
2000's3 (9.38)29.6817
2010's5 (15.63)24.3611
2020's1 (3.13)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 37.28

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index37.28 (24.57)
Research Supply Index3.58 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index49.81 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (37.28)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (2.94%)5.53%
Reviews0 (0.00%)6.00%
Case Studies7 (20.59%)4.05%
Observational0 (0.00%)0.25%
Other26 (76.47%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]