Page last updated: 2024-12-05

methaqualone

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

Description

Methaqualone: A quinazoline derivative with hypnotic and sedative properties. It has been withdrawn from the market in many countries because of problems with abuse. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

methaqualone : A member of the class of quinazolines that is quinazolin-4-one substituted at positions 2 and 3 by methyl and o-tolyl groups respectively. A depressant that increases the activity of the GABA receptors in the brain and nervous system, it is used as a sedative and hypnotic medication. It became popular as a recreational drug and club drug in the late 1960s and 1970s. [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]

Cross-References

ID SourceID
PubMed CID6292
CHEMBL ID282052
CHEBI ID6821
SCHEMBL ID43892
MeSH IDM0013560

Synonyms (157)

Synonym
somnafac
methyl-o-tolylquinazolone
einecs 200-780-4
pro-dorm
brn 0211874
citexal
2-methyl-3-o-tolyl-4(3h)-chinazolinon [german]
dea no. 2565
metacualona [inn-spanish]
mequin
hsdb 3120
methachalonum
nsc 111388
metachalon [czech]
methaqualonum [inn-latin]
3,4-dihydro-2-methyl-4-oxo-3-o-tolylquinazoline
HMS2626L18
nsc-126877
nsc126877
nsc631628
nsc-631628
4(3h)-quinazolinone, 2-methyl-3-o--tolyl-
2-methyl-3-(o-tolyl)quinazolin-4-one
2-methyl-3-(2-methylphenyl)quinazolin-4(3h)-one
MLS000678342
smr000285241
cateudyl
fadormir
melsed
quaalude
methaqualoneinone
somberol
72-44-6
2-methyl-3-(2-methylphenyl)-4(3h)-quinazolinone
hyminal
cn 38703
aqual
2-methyl-3-(2-methylphenyl)-4-quinazolinone
sonal
nethaqualone
2-methyl-3-(o-tolyl)-3,4-dihydro-4-quinazolinone
nsc-111388
nobedorm
metakvalon
2-methyl-3-o-tolyl-4(3h)-chinazolinon
tr-495
sindesvel
2-methyl-3-tolyl-4-oxybensdiazine
methaqualone
dormigoa
dormutil
r-148
tr 495
sopor
hyptor base
nsc111388
tuazolone
tuazole
omnyl
maoa
mollinox
revonal
ortonal
2-methyl-3-o-tolyl-4(3h)-quinazolinone
ric 272
dorsedin
hyptor
melsomin
orthonal
wln: t66 bvn enj cr b1& d1
2-methyl-3-o-tolyl-4(3h)-chinazolone
4(3h)-quinazolinone, 2-methyl-3-(2-methylphenyl)-
methased
melsedin base
soverin
rorer 714
motolon
metolquizolone
dormogen
optinoxan
rorer 148
ci 705
ipnofil
2-methyl-3-(2-tolyl)quinazol-4-one
ci-705
qz 2
noctilene
somnomed
parminal
qz-2
torinal
metaqualon
holodorm
methaqualon
roulone
normi-nox
MTQ ,
rouqualone
2-methyl-3-o-tolyl-4-quinazolone
4(3h)-quinazolinone, 2-methyl-3-o-tolyl-
mozambin
dormigoa-schlafmittel
hypocol
C07560
DB04833
D00557
AKOS000509786
cn-38703
nsc-111388-
CHEMBL282052
chebi:6821 ,
NCGC00245236-01
NCGC00245236-02
2-methyl-3-(o-tolyl)-3h-quinazolin-4-one
methaqualonum
5-24-03-00132 (beilstein handbook reference)
unii-7zkh8mqw6t
metacualona
methaqualone [usan:usp:inn:ban]
metachalon
metaqualone
7zkh8mqw6t ,
tox21_112869
dtxsid7023279 ,
cas-72-44-6
dtxcid403279
tox21_112502
hypcol
tuazol
methaqualone [usan]
methaqualone [mart.]
methaqualone [ep impurity]
methaqualone [mi]
methaqualone [hsdb]
methaqualone [who-dd]
methaqualone [jan]
methaqualone [vandf]
methaqualone [inn]
STL386501
SCHEMBL43892
2-methyl-3-(o-tolyl)-quinazoline-4 (3h)-one
2-methyl-3-(o-tolyl)quinazolin-4(3h)-one
(2-methyl-3-(o-tolyl)-3,4-dihydro-4-(quinazolinone)
(.+/-.)-methaqualone
2-methyl-3-o-tolylquinazolin-4-one
J-511183
4(3h)-quinazolinone, 2-methyl-3-(2-methylphenyl)-, (-)-
methaqualone 1.0 mg/ml in methanol
methaqualone 0.1 mg/ml in methanol
mql
Q423912
reposil
ric-272
methaqualone (ep impurity)
methaqualone (mart.)
n05cm01
methaqualone, 1mg/ml in methanol

Research Excerpts

Overview

Methaqualone is a sedative hypnotic that is often abused. It is a potent quinazoline, a class of sedative-hypnotics.

ExcerptReferenceRelevance
"Methaqualone is a potent quinazoline, a class of sedative-hypnotics, that has a high potential for abuse. "( Treatment for methaqualone dependence in adults.
McCarthy, G; Myers, B; Siegfried, N, 2005
)
2.13
"Methaqualone is a sedative hypnotic that is often abused. "( Methaqualone withdrawal syndrome with photoparoxysmal responses and high-amplitude visual evoked potentials.
Faught, E, 1986
)
3.16

Effects

ExcerptReferenceRelevance
"Methaqualone injected i.v. has been reported to be a safe short-acting anaesthetic agent and a muscle relaxant in man. "( Electroencephalographic studies with i.v. methaqualone in man.
Agarwal, TN; Bhargava, KP; Saxena, RC; Suri, ML; Thacore, VR, 1977
)
1.96

Treatment

Methaqualone pretreatment significantly (P less than 0.005) delayed the disappearance of ethanol in the blood and brain over a period of 50 and 200 min after a loading dose of 2.0 g/kg, i.p., of ethanol. The treatment did not affect warfarin-induced hypoprothrombinemia.

ExcerptReferenceRelevance
"Methaqualone pretreatment only increased hepatic aminopyrine demethylase activity and wet liver weights."( A comparison of the inductive effects of phenobarbital, methaqualone, and methyprylon on hepatic mixed function oxidase enzymes in the rat.
O'Connor, MF; Piepho, RW; Reinke, LA; Stohs, SJ, 1975
)
1.22
"Methaqualone treatment of pregnant rats in doses of 100-200 mg/kg day produces resorption and a series of anomalies whose incidence increases with the dose-level employed."( The effect of methaqualone on prenatal development in the rat.
Petit, TL; Sterling, JW, 1977
)
2.06
"3. Methaqualone pretreatment significantly (P less than 0.005) delayed the disappearance of ethanol in the blood and brain over a period of 50 and 200 min after a loading dose of 2.0 g/kg, i.p., of ethanol."( Interactions between methaqualone and ethanol in rats and mice during acute and chronic states.
Ho, AK; Ho, CC,
)
0.96
"Methaqualone pretreatment for 3 or 6 days caused an induction of hepatic enzymes in the young male rat as measured by a reduction in hexobarbital-hypnosis. "( Age differences affecting induction of hepatic drug metabolizing enzymes by methaqualone and phenobarbital in the rat.
Boren, JA; Mathur, PP; Reavey-Cantwell, NH; Smyth, RD, 1975
)
1.93
"Methaqualone pretreatment did not affect warfarin-induced hypoprothrombinemia, whereas phenobarbital-pretreated animals showed a 32 to 64% reduction in response to the anticoagulant."( Induction of hepatic enzymes by methaqualone and effect on warfarin-induced hypoprothrombinemia.
Herczeg, T; Mathur, PP; Reavey-Cantwell, NH; Smyth, RD, 1976
)
1.26

Toxicity

ExcerptReferenceRelevance
" Tests of the efficacy, toxicity, stability and long-term effect of KR-100 were conducted, and it was show that the insecticide possessed strong and long-lasting effect against mosquitoes, flies and cockroaches but was by no means toxic to human."( [Efficacy, toxicity and mechanism of insecticide KR-100: a preliminary study].
Cai, SW; Chai, KS; Chen, JB; Chen, XG; Lin, LF; Zheng, XL; Zhi, GZ, 2002
)
0.31
" Observed symptoms and signs such as central nervous system depression alternating with excitation, psychomotor agitation, muscle hyperactivity, and tachycardia were compatible with methaqualone-induced adverse effects."( Acute neurotoxicity associated with recreational use of methylmethaqualone confirmed by liquid chromatography tandem mass spectrometry.
Ceschi, A; Elavumkudy, S; Giardelli, G; Hofer, KE; Manini, AF; Müller, DM; Rauber-Lüthy, C, 2013
)
0.82

Pharmacokinetics

ExcerptReferenceRelevance
"0 ml min-1 on day 15), serum half-life shorter (mean t1/2 beta 16."( The influence of the menstrual cycle on the metabolism and clearance of methaqualone.
Burnett, D; Horth, CE; Oram, M; Wilson, K, 1982
)
0.5

Bioavailability

ExcerptReferenceRelevance
" The results indicate that there is no correlation between in vivo bioavailability and the modified NF in vitro dissolution test used."( Comparison of in vitro dissolution and in vivo bioavailability of methaqualone tablets in humans.
Chao, GC; Hoyt, HJ; Stoll, RG; Yacobi, A, 1978
)
0.5
"0 phosphate buffer, measured by the resin flask method, was shown to correlate with bioavailability in humans."( Correlation between dissolution characteristics and absorption of methaqualone from solid dosage forms.
Buehler, JD; Chemburkar, PB; Joslin, RS; Polk, A; Reavey-Cantwell, NH; Shah, PB; Smyth, RD, 1976
)
0.49
"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

Dosage Studied

The urinary excretion of five C-monohydroxy metabolites and the N-oxide metabolite of methaqualone has been measured in ninteen healthy adults. Diphenhydramine administered at the dosage level used in therapeutic combination products did not alter the blood levels of met Haqualone or its metabolite.

ExcerptRelevanceReference
" The urinary excretion of five C-monohydroxy metabolites and the N-oxide was studies in the 24 h period immediately after oral dosing with 250 mg methaqualone (Melsed)."( The metabolism of methaqualone in patients with biliary cirrhosis or secondary carcinoma of the liver.
Burnett, D; Reynolds, CN; Wilson, K, 1979
)
0.79
"The presence and mechanism of synergism of action between ethanol and amylobarbitone, phenobarbitone or methaqualone was determined by application of simple pharmacokinetic models to log dose-response curves and plasma concentration-time curves for the hypnotics alone or when ethanol was given concurrently."( Interaction of ethanol with amylobarbitone, phenobarbitone and methaqualone.
Reavey, PC; Tilstone, WJ, 1978
)
0.71
"The urinary excretion of five C-monohydroxy metabolites and the N-oxide metabolite of methaqualone in the 24 h period immediately after oral dosing with 250 mg methaqualone (Melsed) has been measured in ninteen healthy adults (13 male, 6 female) to assess interindividual variations and in five adults (3 male, 2 female) on five separate occasions to assess intraindividual variation."( Inter- and intra-individual variation in the metabolism of methaqualone in man after a single oral dose.
Burnett, D; Reynolds, CN; Wilson, K, 1978
)
0.72
" This has been applied to the analysis of some of these drugs in plasma taken from patients after therapeutic dosage and over-dosage."( A rapid micro-method for the screening and measurement of barbiturates and related compounds in plasma by gas-liquid chromatography.
Flanagan, RJ; Withers, G, 1972
)
0.25
"Gas chromatographic methods for the analysis of drug dosage forms consist of a simple extraction, dilution with an internal standard solution, and injection, or, even simpler, dilution with the internal standard solution and injection."( Performance characteristics of methods of analysis used for regulatory purposes. I. Drug dosage forms. B. Gas chromatographic methods.
Albert, R; Horwitz, W,
)
0.13
" Diphenhydramine administered at the dosage level used in therapeutic combination products did not alter the blood levels of methaqualone or its metabolite."( Methaqualone-diphenhydramine interaction study in humans.
Hindmarsh, KW; Korchinski, ED; Schneider, CB; Wallace, SM, 1983
)
1.92
" Based on the time of 50% recovery (RR performance recovering to 90 seconds or more), both chronic treatments resulted in a significant shift of the dose-response curves for PB, MQ and DZ to the right."( Tolerance and cross-tolerance to central nervous system depressants after chronic pentobarbital or chronic methaqualone administration.
Commissaris, RL; Rech, RH, 1983
)
0.48
" Urine was collected over a 72 h period from six healthy adults (4 male, 2 female) after oral dosing with 200 mg methaqualone (MTQ)."( Comparison of methaqualone excretion patterns using Abuscreen ONLINE and EMIT II immunoassays and GC/MS.
Bracher, K; Brenneisen, R; Brenner, C; ElSohly, MA; Ghodoussi, VD; Hui, R; Passarelli, J; Salamone, SJ; Wu, R, 1996
)
0.87
" MP was dosed orally at 10, 30 and 100mg/kg/day to 6-week-old male Crl:CD (SD) rats daily for 14 days."( The 14-day repeated dose liver micronucleus test with methapyrilene hydrochloride using young adult rats.
Doi, T; Inoue, K; Kawasako, K; Koda, A; Ochi, A; Wako, Y, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
GABA agonistA drug that binds to and activates gamma-aminobutyric acid receptors.
sedativeA central nervous system depressant used to induce drowsiness or sleep or to reduce psychological excitement or anxiety.
[role 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]

Drug Classes (1)

ClassDescription
quinazolinesAny organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.
[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 (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency23.12630.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency60.98170.000221.22318,912.5098AID743035
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
estrogen nuclear receptor alphaHomo sapiens (human)Potency41.20210.000229.305416,493.5996AID743075; AID743079
aryl hydrocarbon receptorHomo sapiens (human)Potency30.24620.000723.06741,258.9301AID743085
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency68.27310.000323.4451159.6830AID743065; AID743067
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency44.66840.075215.225339.8107AID485360
lamin isoform A-delta10Homo sapiens (human)Potency0.31620.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)10.00000.00011.617910.0000AID31458
Glutamate receptor 2Rattus norvegicus (Norway rat)IC50 (µMol)10.00000.00011.700010.0000AID31458
Glutamate receptor 3Rattus norvegicus (Norway rat)IC50 (µMol)10.00000.00011.700010.0000AID31458
Glutamate receptor 4Rattus norvegicus (Norway rat)IC50 (µMol)10.00000.00011.700010.0000AID31458
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGlutamate receptor 1Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (101)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1896601Toxicity in ip dosed mouse2022Bioorganic & medicinal chemistry letters, 12-01, Volume: 77Design, synthesis, molecular docking and pharmacological evaluation of novel triazine-based triazole derivatives as potential anticonvulsant agents.
AID650787Anticonvulsant activity in mouse assessed as protection against picrotoxin-induced seizure at 1.4 mmol/kg, ip administered 30 min prior to picrotoxin-challenge measured after 60 mins relative to control2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Design and synthesis of novel 7-aminoquinazoline derivatives: antitumor and anticonvulsant activities.
AID131566Righting reflex effect in mice was tested when the compound was administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
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.
AID176594Hypomotility effect in rats was tested when the compound was administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID121841Anticonvulsant activity expressed as toxic dose in rotarod test (0.5 hr) in mice;Activity determined at time of peak effect (0.5 hr) and value ranges from(47-65).1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Synthesis of 3,4-dihydro-4-oxoquinazoline derivatives as potential anticonvulsants.
AID119063Ability to reinduce anesthesia (70 mg/kg, iv) following recovery of loss of righting reflex obtained with hexobarbital.1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Sleep-inducing N-alkyl-5-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinones and N-alkyl-3-(trifluoromethyl)cinnamamides.
AID650785Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizure at 1.4 mmol/kg, ip administered 30 min prior to maximal electroshock-challenge measured after 60 mins relative to control2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Design and synthesis of novel 7-aminoquinazoline derivatives: antitumor and anticonvulsant activities.
AID1133857Acute toxicity in ip dosed CFLP mouse1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Synthesis and central nervous system activity of quinazolones related to 2-methyl-3-(o-tolyl)-4(3H)-quinazolone (methaqualone).
AID134385Acute toxicity in mice after 72 hours when administered intraperitoneally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID136091Compound was determined in rotarod test and expressed as TD501984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
AID1896600Anticonvulsant activity in ip dosed mouse model of seizure2022Bioorganic & medicinal chemistry letters, 12-01, Volume: 77Design, synthesis, molecular docking and pharmacological evaluation of novel triazine-based triazole derivatives as potential anticonvulsant agents.
AID131590Ability to reinduce anesthesia in mice as a measure of in vivo sedative-hypnotic activity1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID650784Anticonvulsant activity in ip dosed mouse assessed as protection against pentylenetetrazol-induced seizure administered 30 min prior to pentylenetetrazol-challenge measured after 60 mins2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Design and synthesis of novel 7-aminoquinazoline derivatives: antitumor and anticonvulsant activities.
AID117815Ability to produce neurological deficit in the rotarod test (10 mice were used per dose, ip)1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Sleep-inducing N-alkyl-5-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinones and N-alkyl-3-(trifluoromethyl)cinnamamides.
AID128204Compound was tested for mortality in mice when administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID1133853Hypnotic activity in ip dosed CFLP mouse after 30 mins by rotary drum test1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Synthesis and central nervous system activity of quinazolones related to 2-methyl-3-(o-tolyl)-4(3H)-quinazolone (methaqualone).
AID1896598Anticonvulsant activity in MES induced mouse model of seizure assessed as protection against seizure at 1 mmol/Kg, ip relative to control2022Bioorganic & medicinal chemistry letters, 12-01, Volume: 77Design, synthesis, molecular docking and pharmacological evaluation of novel triazine-based triazole derivatives as potential anticonvulsant agents.
AID176302Ataxia effect in rats was tested when the compound was administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID131017Compound was tested for rotarod motor coordination in mice when administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID184601Acute toxicity in rats after 2 hours when administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID639224Anticonvulsant activity in Swiss albino mouse assessed as protection against PTZ-induced clonic seizure at 200 mg/kg, ip administered 30 mins before challenge2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Synthesis and anticonvulsant evaluation of some new 2,3,8-trisubstituted-4(3H)-quinazoline derivatives.
AID131211Docility effect in mice was tested when the compound was administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID1133856Anticonvulsant activity in po dosed CFLP mouse assessed as inhibition of benzoquinone-induced writhing1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Synthesis and central nervous system activity of quinazolones related to 2-methyl-3-(o-tolyl)-4(3H)-quinazolone (methaqualone).
AID114181Effective dose against loss of righting reflex in mice (10 mice per dose, ip)1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Sleep-inducing N-alkyl-5-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinones and N-alkyl-3-(trifluoromethyl)cinnamamides.
AID650780Protective index, ratio of TD50 for mouse to ED50 for pentylenetetrazol-induced seizure in mouse2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Design and synthesis of novel 7-aminoquinazoline derivatives: antitumor and anticonvulsant activities.
AID29305Median toxic dose was measured at time of peak neurologic deficit1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Synthesis and anticonvulsant activity of some new 2-substituted 3-aryl-4(3H)-quinazolinones.
AID650793Anticonvulsant activity in mouse assessed as protection against pentylenetetrazol-induced seizure at 1.4 mmol/kg, ip administered 30 min prior to pentylenetetrazol-challenge measured after 60 mins relative to control2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Design and synthesis of novel 7-aminoquinazoline derivatives: antitumor and anticonvulsant activities.
AID650782Therapeutic index, ratio of LD50 for mouse to ED50 for pentylenetetrazol-induced seizure in mouse2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Design and synthesis of novel 7-aminoquinazoline derivatives: antitumor and anticonvulsant activities.
AID650781Toxicity in ip dose mouse assessed as mortality2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Design and synthesis of novel 7-aminoquinazoline derivatives: antitumor and anticonvulsant activities.
AID131015Compound was tested for rotarod motor coordination in mice when administered intraperitoneally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID1133855Anticonvulsant activity in ip dosed CFLP mouse assessed as inhibition of pentylenetetrazole-induced seizure1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Synthesis and central nervous system activity of quinazolones related to 2-methyl-3-(o-tolyl)-4(3H)-quinazolone (methaqualone).
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID184647Lethal dose was obtained by 2-h post administration (ip), using four male Royal Hart Wistar rats1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Sleep-inducing N-alkyl-5-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinones and N-alkyl-3-(trifluoromethyl)cinnamamides.
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.
AID1915718Activation of GABA receptor (unknown origin)2021European journal of medicinal chemistry, Feb-05, Volume: 211Therapeutic progression of quinazolines as targeted chemotherapeutic agents.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID650783Neurotoxicity in ip dosed mouse assessed as impaired motor coordination administered 30 mins prior to test by chimney test2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Design and synthesis of novel 7-aminoquinazoline derivatives: antitumor and anticonvulsant activities.
AID131565Righting reflex effect in mice was tested when the compound was administered intraperitoneally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID176647Righting reflex effect in rats was tested when the compound was administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID639298Protective index, ratio of TD50 for neurotoxicity to ED50 for anticonvulsant activity in Swiss albino mouse2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Synthesis and anticonvulsant evaluation of some new 2,3,8-trisubstituted-4(3H)-quinazoline derivatives.
AID131029Compound was tested for tonic convulsions when administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID1896602Toxicity in ip dosed mouse assessed as lethal dose2022Bioorganic & medicinal chemistry letters, 12-01, Volume: 77Design, synthesis, molecular docking and pharmacological evaluation of novel triazine-based triazole derivatives as potential anticonvulsant agents.
AID131210Docility effect in mice was tested when the compound was administered ip1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID129454Ataxia effect in mice was tested when the compound was administered intraperitoneally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID639295Neurotoxicity in ip dosed Swiss albino mouse measured after 30 mins by chimney test2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Synthesis and anticonvulsant evaluation of some new 2,3,8-trisubstituted-4(3H)-quinazoline derivatives.
AID184602Acute toxicity in rats after 72 hours when administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID131421Prehensile effect in mice was tested when the compound was administered intraperitoneally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID1896603Therapeutic index, ratio of LD50 for toxicity in ip dosed mouse to ED50 for anticonvulsant activity in ip dosed mouse model of seizure2022Bioorganic & medicinal chemistry letters, 12-01, Volume: 77Design, synthesis, molecular docking and pharmacological evaluation of novel triazine-based triazole derivatives as potential anticonvulsant agents.
AID130052Evaluated for seizure threshold test at a dose 30 mg/kg &MMT is the maximal metrazole threshold to tonic flexion.1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
AID132439Hypomotility effect in mice was tested when the compound was administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID130193Evaluated for seizure threshold test at a dose 50 mg/kg &MST is the metrazole seizure threshold to persistent clonus1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
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.
AID639294Anticonvulsant activity in ip dosed Swiss albino mouse assessed as protection against PTZ-induced seizure compound administered 30 mins before challenge measured after 60 mins2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Synthesis and anticonvulsant evaluation of some new 2,3,8-trisubstituted-4(3H)-quinazoline 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.
AID639296Neurotoxicity in ip dosed Swiss albino mouse assessed as mortality2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Synthesis and anticonvulsant evaluation of some new 2,3,8-trisubstituted-4(3H)-quinazoline derivatives.
AID650790Anticonvulsant activity in mouse assessed as protection against strychnine-induced seizure at 1.4 mmol/kg, ip administered 30 min prior to strychnine-challenge measured after 60 mins relative to control2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Design and synthesis of novel 7-aminoquinazoline derivatives: antitumor and anticonvulsant activities.
AID130053Evaluated for seizure threshold test at a dose 30 mg/kg &MST is the metrazole seizure threshold to persistent clonus1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
AID114701Effective dose against Mice docility, ip administration1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Sleep-inducing N-alkyl-5-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinones and N-alkyl-3-(trifluoromethyl)cinnamamides.
AID131028Compound was tested for tonic convulsions when administered intraperitoneally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID31458Antagonist potency against functional AMPA receptor by kainate-induced Ca+2 in rat cerebellar granule neurons in primary culture2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Methaqualone derivatives are potent noncompetitive AMPA receptor antagonists.
AID1133852Hypnotic activity in ip dosed CFLP mouse assessed as loss of righting reflex1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Synthesis and central nervous system activity of quinazolones related to 2-methyl-3-(o-tolyl)-4(3H)-quinazolone (methaqualone).
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.
AID639225Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizure at 200 mg/kg, ip administered 30 mins before challenge2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Synthesis and anticonvulsant evaluation of some new 2,3,8-trisubstituted-4(3H)-quinazoline derivatives.
AID134381Acute toxicity in mice after 2 hours when administered intraperitoneally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID113445Anticonvulsant activity against N-sulfamoylhexahydrozepine (10 mice were used per dose, ip)1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Sleep-inducing N-alkyl-5-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinones and N-alkyl-3-(trifluoromethyl)cinnamamides.
AID131372Effective dose (ED50) was determined in sc Met (pentylenetetrazole) seizure threshold test1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
AID1896604Protective index, ratio of TD50 for toxicity in ip dosed mouse to ED50 for anticonvulsant activity in ip dosed mouse model of seizure2022Bioorganic & medicinal chemistry letters, 12-01, Volume: 77Design, synthesis, molecular docking and pharmacological evaluation of novel triazine-based triazole derivatives as potential anticonvulsant agents.
AID132438Hypomotility effect in mice was tested when the compound was administered intraperitoneally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID1896599Anticonvulsant activity in PTZ induced mouse model of seizure assessed as protection against seizure at 1 mmol/Kg, ip relative to control2022Bioorganic & medicinal chemistry letters, 12-01, Volume: 77Design, synthesis, molecular docking and pharmacological evaluation of novel triazine-based triazole derivatives as potential anticonvulsant agents.
AID113787Anticonvulsant activity in mice using MES seizure test;Activity determined at time of peak effect (0.5 hr) and value ranges from (48-56).1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Synthesis of 3,4-dihydro-4-oxoquinazoline derivatives as potential anticonvulsants.
AID131422Prehensile effect in mice was tested when the compound was administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID131013Compound was tested for reinduction of anesthesia in mice when administered intraperitoneally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID126803Ratio of the oral dose of the test compound relative to that of methaqualone (15 mg/kg, po) to induce sleep in Cebus monkey1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Sleep-inducing N-alkyl-5-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinones and N-alkyl-3-(trifluoromethyl)cinnamamides.
AID114174Effective dose against Mice ataxia, ip administration1985Journal of medicinal chemistry, Jan, Volume: 28, Issue:1
Sleep-inducing N-alkyl-5-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinones and N-alkyl-3-(trifluoromethyl)cinnamamides.
AID134382Acute toxicity in mice after 2 hours when administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID134386Acute toxicity in mice after 72 hours when administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID130192Evaluated for seizure threshold test at a dose 50 mg/kg &MMT is the maximal metrazole threshold to tonic flexion.1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of previously inaccessible quinazolines and 1,4-benzodiazepines as potential anticonvulsants.
AID129455Ataxia effect in mice was tested when the compound was administered perorally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID639297Therapeutic index, ratio of LD50 for mortality to ED50 for anticonvulsant activity in Swiss albino mouse2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Synthesis and anticonvulsant evaluation of some new 2,3,8-trisubstituted-4(3H)-quinazoline derivatives.
AID128202Compound was tested for mortality in mice when administered intraperitoneally1981Journal of medicinal chemistry, May, Volume: 24, Issue:5
A potent, new, sedative--hypnotic agent: 5,7-dihydro-5,5,7,7-tetramethyl-3-(3-nitrophenyl)furo[3,4-e]-as-triazine 4-oxide.
AID113798Anticonvulsant activity in mice using sc Met seizure test;Activity determined at time of peak effect (0.5 hr) and value ranges from(28-40).1983Journal of medicinal chemistry, Oct, Volume: 26, Issue:10
Synthesis of 3,4-dihydro-4-oxoquinazoline derivatives as potential anticonvulsants.
AID1133854Anticonvulsant activity in ip dosed CFLP mouse assessed as inhibition of maximum electroshock-induced seizure1977Journal of medicinal chemistry, Mar, Volume: 20, Issue:3
Synthesis and central nervous system activity of quinazolones related to 2-methyl-3-(o-tolyl)-4(3H)-quinazolone (methaqualone).
AID131585Subcutaneous metrazole (scMet) test was conducted and median effective dose was determined at the time of peak anticonvulsant and sedative effect1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Synthesis and anticonvulsant activity of some new 2-substituted 3-aryl-4(3H)-quinazolinones.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (743)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990677 (91.12)18.7374
1990's22 (2.96)18.2507
2000's17 (2.29)29.6817
2010's16 (2.15)24.3611
2020's11 (1.48)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 67.77

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

MetricThis Compound (vs All)
Research Demand Index67.77 (24.57)
Research Supply Index6.78 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index120.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (67.77)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials74 (9.23%)5.53%
Reviews25 (3.12%)6.00%
Case Studies49 (6.11%)4.05%
Observational0 (0.00%)0.25%
Other654 (81.55%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Evaluation of the Overall Effectiveness Including Cardiovascular Effects of the Custom-made, Titratable Duoblock Flex SomnoDent® MAS in the Treatment of Obstructive Sleep Apnea [NCT02320877]100 participants (Actual)Interventional2014-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]