Page last updated: 2024-12-05

estazolam

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

Description

Estazolam: A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

estazolam : A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term management of insomnia. [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 CID3261
CHEMBL ID285674
CHEBI ID4858
SCHEMBL ID28766
MeSH IDM0007763

Synonyms (95)

Synonym
BIDD:GT0481
4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine, 8-chloro-6-phenyl-
u 33737
4h-(1,2,4)triazolo(4,3-a)(1,4)benzodiazepine, 8-chloro-6-phenyl-
8-chloro-6-phenyl-4h-s-triazolo(4,3-a)(1,4)benzodiazepine (iupac)
nsc 290818
estazolam [usan:inn:jan]
ccris 1955
prosom
8-chloro-6-phenyl-4h-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine
brn 1220868
4h-s-triazolo(4,3-a)(1,4)benzodiazepine, 8-chloro-6-phenyl-
nuctalon
8-chloro-6-phenyl-4h-(1,2,4)triazolo-(4,3-a)(1,4)benzodiazepine
abbott 47631
estazolamum [inn-latin]
8-chloro-6-phenyl-4h-s-triazolo(4,3-a)(1,4)benzodiazepine
einecs 249-982-4
esilgan
dea no. 2756
nsc-290818
4h-s-triazolo[4,4]benzodiazepine, 8-chloro-6-phenyl-
8-chloro-6-phenyl-4h-s-triazolo[4,4]benzodiazepine
wln: t b576 bn dnn hn ghj ir& lg
eurodin
d-40ta
julodin
4h-[1,4]triazolo[4,3-a][1,4]benzodiazepine, 8-chloro-6-phenyl-
nsc290818
d 40ta
8-chloro-6-phenyl-4h-[1,4]triazolo[4,3-a][1,4]benzodiazepine
C06981
29975-16-4
estazolam
DB01215
prosom (tn)
estazolam (jp17/usp/inn)
D00311
NCGC00168250-01
inchi=1/c16h11cln4/c17-12-6-7-14-13(8-12)16(11-4-2-1-3-5-11)18-9-15-20-19-10-21(14)15/h1-8,10h,9h2
cdchdcwjmgxxrh-uhfffaoysa-
abbott-47631
CHEMBL285674
estazolam civ
CHEBI:4858 ,
estazolamum
AKOS005064373
dtxsid5020572 ,
cas-29975-16-4
dtxcid50572
tox21_112609
A820132
8-chloro-6-phenyl-4h-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine
unii-36s3eqv54c
36s3eqv54c ,
nemurel
somnatrol
cannoc
MLS003899222
smr000238168
53180-72-6
AB07556
estazolam [who-dd]
8-chloro-6-phenyl-4h-s-triazolo[4,3-a][1,4]benzodiazepine
estazolam [usp monograph]
estazolam civ [usp-rs]
estazolam [usan]
estazolam [jan]
estazolam [mart.]
estazolam [iarc]
estazolam [inn]
estazolam [orange book]
estazolam [mi]
estazolam [vandf]
gtpl7550
SCHEMBL28766
8-chloro-6-phenyl-4h-s-triazolo-[4,3-a][1,4]benzodiazepine
8-chloro-6-phenyl-4h-s-triazolo [4,3-a][1,4] benzodiazepine
8-chloro-6-phenyl-4h-2,3,5,10b-tetraaza-benzo[e]azulene
Q-201071
8-chloro-6-phenyl-4h-(1,2,4)triazolo(4,3-a)(1,4)benzodiazepine
12-chloro-9-phenyl-2,4,5,8-tetraazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,8,11,13-hexaene
estazolam, united states pharmacopeia (usp) reference standard
estazolam 1.0 mg/ml in methanol
estazolam 0.1 mg/ml in methanol
Q3045264
BCP13317
12-chloro-9-phenyl-2,4,5,8-tetraazatricyclo[8.4.0.0?,?]tetradeca-1(14),3,5,8,10,12-hexaene
estazolam (usp monograph)
estazolam (iarc)
n05cd04
estazolam civ (usp-rs)
estazolam (mart.)
estazolamum (inn-latin)
estazolam, 1mg/ml in methanol

Research Excerpts

Overview

Estazolam (EZ) is a long-acting benzodiazepine (BZD) drug with high clinical consumption in China to treat anxiety, depression and other syndromes. Estazol am 2.0 mg is an effective hypnotic in patients with generalized anxiety disorder.

ExcerptReferenceRelevance
"Estazolam (EZ) is a long-acting benzodiazepine (BZD) drug with high clinical consumption in China to treat anxiety, depression and other syndromes. "( Formation and occurrence of disinfection byproducts of benzodiazepine drug estazolam in drinking water of Beijing.
Huang, X; Shao, B; Shi, J; Zhang, X, 2022
)
2.39
"Estazolam appeared to be a stable benzodiazepine during the six-month study, and ketazolam proved to be the most unstable benzodiazepine."( Benzodiazepine stability in postmortem samples stored at different temperatures.
Bastos, ML; Melo, P; Teixeira, HM,
)
0.85
"Estazolam is a new benzodiazepine hypnotic agent with an intermediate half-life of 12 to 15 hours. "( Hypnotic efficacy of estazolam compared with flurazepam in outpatients with insomnia.
Bremner, J; Cohn, JB; Ettinger, M; Wilcox, CS, 1991
)
2.04
"Estazolam 2.0 mg is an effective hypnotic in patients with generalized anxiety disorder and appears to have a favorable anxiolytic action."( Estazolam treatment of insomnia in generalized anxiety disorder: a placebo-controlled study.
Bailey, L; Bielski, RJ; Crowder, JE; Ferguson, JM; Houston, J; Patrick, RO; Pearlman, HG; Pierce, MW; Post, GL; Shu, VS, 1991
)
2.45
"Estazolam is an effective treatment for situational insomnia and significantly improves sleep in patients with insomnia associated with moderately severe anxiety or depression."( Efficacy of estazolam. The United States clinical experience.
Pierce, MW; Shu, VS, 1990
)
1.38

Effects

ExcerptReferenceRelevance
"Estazolam has been shown to produce anxiolytic-, hypnotic-, amnestic-, and sedative-like effects."( The anxiolytic-like effects of estazolam on a PTSD animal model.
Chen, J; Chen, LF; Gao, ZW; Lin, QF; Liu, ZL; Mao, WD; Shen, D; Su, J; Xu, JN, 2018
)
1.49

Toxicity

ExcerptReferenceRelevance
" Drug-specific adverse effects such as somnolence, dizziness, hypokinesia, and abnormal coordination occurred, but these are expected extensions of benzodiazepine pharmacologic activity."( Safety of estazolam. The United States clinical experience.
Groves, LJ; Pierce, MW; Shu, VS, 1990
)
0.68
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32

Pharmacokinetics

ExcerptReferenceRelevance
" No statistically significant differences were detected among the mean time of maximal plasma concentration (Tmax), maximal plasma concentration (Cmax), area under the plasma concentration-time curve from zero to 72 hours (AUC), or half-life values for the 2-mg doses."( The clinical pharmacokinetics of single doses of estazolam.
Carrigan, PJ; Gustavson, LE, 1990
)
0.53
"03 ml/min/kg), and elimination half-life (24."( Effects of the CYP2C19 genotype and cigarette smoking on the single oral dose pharmacokinetics and pharmacodynamics of estazolam.
Aoshima, T; Fukasawa, T; Gerstenberg, G; Miura, M; Ohkubo, T; Okuyama, N; Otani, K; Otsuji, Y; Sugawara, K, 2003
)
0.53

Compound-Compound Interactions

ExcerptReferenceRelevance
"This study aimed to evaluate the efficacy of medication in combination with a therapeutic approach drawn from TCM, Low Resistance Thought Induction Sleep-regulating Technique (TIP3-2), for acute treatment of insomnia."( Low Resistance Thought Induction Sleep-regulating Technique (TIP3-2) combined with medication for primary insomnia: a randomized controlled trial.
Hong, L; Huang, YY; Li, GX; Li, T; Lin, YN; Liu, YJ; Wang, F; Wang, WD; Yan, X; Zhao, Y, 2014
)
0.4
" Ninety primary insomnia patients were randomly assigned to receive TIP3-2 combined with medication (n = 45) or medication only (n = 45) for 4 weeks."( Low Resistance Thought Induction Sleep-regulating Technique (TIP3-2) combined with medication for primary insomnia: a randomized controlled trial.
Hong, L; Huang, YY; Li, GX; Li, T; Lin, YN; Liu, YJ; Wang, F; Wang, WD; Yan, X; Zhao, Y, 2014
)
0.4

Bioavailability

ExcerptReferenceRelevance
"To compare the bioavailability of two estazolam (CAS 29975-16-4) tablet formulations (Estalin 2 mg tablets as test formulation and 2 mg tablets of the originator product as reference formulation)."( Comparative bioavailability of two estazolam tablet formulations in Indonesian healthy volunteers.
Harahap, Y; Indriati, E; Lusthom, W; Prasaja, B; Sasongko, L, 2008
)
0.89
"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 purpose of this study was to determine the effect of oral estazolam at two and three times the usually recommended dosage (2 mg) on ventilation and respiratory drive during wakefulness. The neurobehavioral ability and balance function declined 1 h later after dosing estazlam.

ExcerptRelevanceReference
"The purpose of this study was to determine the effect of oral estazolam at two and three times the usually recommended dosage (2 mg) on ventilation and respiratory drive during wakefulness."( Ventilatory response to single, high dose estazolam in healthy humans.
Badr, S; Begle, RL; Juan, D; Skatrud, JB, 1990
)
0.78
" The dosage of 2 mg estazolam had no significant effect on stage REM, but delta-sleep decreased."( [Alterations of sleep stage patterns in humans and carry-over effects under estazolam / 1st comm.: effects of estazolam on sleep disturbed by jet fly-over noise (author's transl)].
Ehrenstein, W; Müller-Limmroth, W; Opfermann, M; Weber, F, 1982
)
0.82
" During the last 4 nights they were medicated in a double-blind cross-over test design with the benzodiazepine 8-chloro-6-phenyl-4H-s-triazolo (4,3-a)-(1,4)benzodiazepine (estazolam, BAY k 4200) at a dosage of 2 mg and placebo."( [Alterations of sleep stage pattern in human beings and hang-over effects under the influence of estazolam/2nd Comm.: Studies on the hang-over effect in psycho-physiological performance (author's transl)].
Müller, KW; Müller-Limmroth, W; Strasser, H, 1982
)
0.68
"6% and reflected a maximum-tolerated dosage (females)."( Carcinogenic evaluation of estazolam via diet in CD strain Sprague-Dawley rats and B6C3F1 mice for 2 years.
Buratto, B; Cusick, PK; Fort, FL; Heyman, IA; Kesterson, JW; Kimura, ET; Tekeli, S, 1984
)
0.56
"The neurobehavioral ability and balance function declined 1 h later after dosing estazolam."( [The influence of estazolam on human neurobehavioral function].
Bu, J; Zhuo, XY, 2010
)
0.92
" The dosage and usage of western medication were same as those in the western medication group; and acupoints in acupuncture treatment were same as those in the acupuncture group."( [Senile insomnia treated with integrated acupuncture and medication therapy: a randomized controlled trial].
Wang, J; Wang, L; Zhang, Y, 2015
)
0.42
" The increase in pH value led to a decrease in the reaction rate, while a higher dosage of chlorine resulted in a faster kinetic rate."( Formation and occurrence of disinfection byproducts of benzodiazepine drug estazolam in drinking water of Beijing.
Huang, X; Shao, B; Shi, J; Zhang, X, 2022
)
0.95
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
anxiolytic drugAnxiolytic drugs are agents that alleviate anxiety, tension, and anxiety disorders, promote sedation, and have a calming effect without affecting clarity of consciousness or neurologic conditions.
anticonvulsantA drug used to prevent seizures or reduce their severity.
GABA modulatorA substance that does not act as agonist or antagonist but does affect the gamma-aminobutyric acid receptor-ionophore complex. GABA-A receptors appear to have at least three allosteric sites at which modulators act: a site at which benzodiazepines act by increasing the opening frequency of gamma-aminobutyric acid-activated chloride channels; a site at which barbiturates act to prolong the duration of channel opening; and a site at which some steroids may act.
[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 (2)

ClassDescription
triazolesAn azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.
triazolobenzodiazepineAny organic heterotricyclic compound that is any benzodiazepine which is ortho-fused with a triazole.
[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 (1)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency2.68320.000214.376460.0339AID720691
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (56)

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.
AID1708411Anti-insomnia activity pentobarbital-induced mouse model of insomnia assessed as time of sleep latency at 0.029 mg/kg, ig administered daily for 15 days followed by pentobarbital addition at 1 hr post last dose (Rvb = 8.1 +/- 6.06 min)2021European journal of medicinal chemistry, Feb-15, Volume: 212Large-scale isolation and antitumor mechanism evaluation of compounds from the traditional Chinese medicine Cordyceps Militaris.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID648848Binding affinity to CREBBP assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1148193CNS activity in po dosed mouse assessed as antifighting activity by foot shock test1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Quinazolines and 1,4-benzodiazepines. 81. s-Triazolo[4,3-a][1,4]benzodiazepines by oxidative cyclization of hydrazones.
AID648845Binding affinity to BRD4-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID131573Sedative activity was determined by measuring the loss of the righting reflux induced by thiopental sodium in mice1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID648844Binding affinity to BRD3-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID389440Displacement of [3H]flunitrazepam from GABAA benzodiazepine receptor in rat brain membrane2008Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21
Axial chirality and affinity at the GABA(A) receptor of pyrimido[1,2-a][1,4]benzodiazepines and related compounds.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID648858Binding affinity to BRD3-BD2 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID131571Sedative activity was determined by measuring the inhibition of spontaneous motor activity1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.
AID648846Binding affinity to BRDT-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID648850Binding affinity to PB1 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID131572Sedative activity was determined by measuring the loss of the righting reflux induced by chlorprothixene in mice1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.
AID1708407Anti-insomnia activity pentobarbital-induced mouse model of insomnia assessed as number of forelimb lifts at 0.029 mg/kg, ig administered daily for 15 days followed by pentobarbital addition at 1 hr post last dose (Rvb = 9.2 +/- 4.31 No_unit)2021European journal of medicinal chemistry, Feb-15, Volume: 212Large-scale isolation and antitumor mechanism evaluation of compounds from the traditional Chinese medicine Cordyceps Militaris.
AID1708419Anti-insomnia activity pentobarbital-induced mouse model of insomnia assessed as sleep rate at 0.029 mg/kg, ig administered daily for 15 days followed by pentobarbital addition at 1 hr post last dose relative to control2021European journal of medicinal chemistry, Feb-15, Volume: 212Large-scale isolation and antitumor mechanism evaluation of compounds from the traditional Chinese medicine Cordyceps Militaris.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1597743Half life in human at 1 to 2 mg2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Sleep modulating agents.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1148194CNS activity in po dosed mouse assessed as antagonism against pentylenetetrazole-induced response1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Quinazolines and 1,4-benzodiazepines. 81. s-Triazolo[4,3-a][1,4]benzodiazepines by oxidative cyclization of hydrazones.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID131236Muscle relaxation was determined by using rotatory drum (rotarod) in mice, activity is expressed as ED50 values1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.
AID648847Binding affinity to BAZ2B assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID129148Anticonvulsant activity was determined as the degree of protection against convulsions induced by pentylenetetrazole in mice1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.
AID648857Binding affinity to BRD2-BD2 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
AID648851Binding affinity to PCAF assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID648849Binding affinity to LOC93349 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID128826Antianxiety activity was determined by measuring the antagonism of foot shock induced fighting (taming) in mice1982Journal of medicinal chemistry, Dec, Volume: 25, Issue:12
Amino acid amide derivatives of 2-[3-(aminomethyl)-4H-1,2,4-triazol-4-yl]benzophenones, a novel class of annelated peptidoaminobenzophenones.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID648843Binding affinity to BRD2-BD1 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
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.
AID648859Binding affinity to BRD4-BD2 assessed as change in melting temperature at 10 uM by protein stability shift assay2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1148192CNS activity in po dosed mouse by inclined screen test1977Journal of medicinal chemistry, Dec, Volume: 20, Issue:12
Quinazolines and 1,4-benzodiazepines. 81. s-Triazolo[4,3-a][1,4]benzodiazepines by oxidative cyclization of hydrazones.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1708415Anti-insomnia activity pentobarbital-induced mouse model of insomnia assessed as time of sleep duration at 0.029 mg/kg, ig administered daily for 15 days followed by pentobarbital addition at 1 hr post last dose (Rvb = 17.1 +/- 5.15 min)2021European journal of medicinal chemistry, Feb-15, Volume: 212Large-scale isolation and antitumor mechanism evaluation of compounds from the traditional Chinese medicine Cordyceps Militaris.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (111)

TimeframeStudies, This Drug (%)All Drugs %
pre-199031 (27.93)18.7374
1990's22 (19.82)18.2507
2000's23 (20.72)29.6817
2010's24 (21.62)24.3611
2020's11 (9.91)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 76.72

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 Index76.72 (24.57)
Research Supply Index5.06 (2.92)
Research Growth Index4.58 (4.65)
Search Engine Demand Index133.90 (26.88)
Search Engine Supply Index2.01 (0.95)

This Compound (76.72)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials35 (28.69%)5.53%
Reviews6 (4.92%)6.00%
Case Studies8 (6.56%)4.05%
Observational0 (0.00%)0.25%
Other73 (59.84%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The First Affiliated Hospital of Guangzhou University of Chinese Medicine [NCT03997058]Phase 4120 participants (Anticipated)Interventional2019-03-01Active, not recruiting
A Randomized, Open-Label, Active-Controlled, Parallel-Group Study to Evaluate the Efficacy and Safety of Zolpidem Modified Release (MR) in Patients With Primary Insomnia [NCT00956319]Phase 442 participants (Actual)Interventional2009-05-31Completed
A Randomised, Double-blinded, Double-dummy, Multi-center, Paralleled Study to Investigate the Safety and Efficacy of Brotizolam (Lendormin) Compared With Estazolam in Insomnia Outpatients. [NCT00347295]Phase 3253 participants Interventional2006-06-30Completed
Clinical Normative Evaluation of Chronic Insomnia Treated by Traditional Chinese Medicine According to Yin Yang Theory and Its Correlation With Circadian Rhythm [NCT05452577]186 participants (Anticipated)Interventional2021-01-22Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]