Page last updated: 2024-12-04

brotizolam

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

Description

brotizolam: structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2451
CHEMBL ID32479
CHEBI ID31308
SCHEMBL ID44067
MeSH IDM0075325

Synonyms (61)

Synonym
brotizolam
6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine, 2-bromo-4-(2-chlorophenyl)-9-methyl-
ladormin
lendormine
we-941
lendormin
indormyl
lendorm
2-bromo-4-(2-chlorophenyl)-9-methyl-6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
57801-81-7
D01744
brotizolam (jp17/usan/inn)
lendormin (tn)
brotizolamum [inn-latin]
c15h10brcln4s
8-bromo-6-(o-chlorophenyl)-1-methyl-4h-s-triazolo(3,4c)thieno(2,3e)-1,4-diazepine
we 941
einecs 260-964-5
2-bromo-4-(o-chlorophenyl)-9-methyl-6h-thieno(3,2-f)-s-triazolo(4,3-a)(1,4)diazepine
brn 0839277
2-bromo-4-(2-chlorophenyl)-9-methyl-6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepine
6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepine, 2-bromo-4-(2-chlorophenyl)-9-methyl-
sintonal
we-941-bs
CHEMBL32479 ,
nimbisan
mederantil
L000775
2-bromo-4-(2-chloro-phenyl)-9-methyl-6h-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulene
bdbm50011875
NCGC00183872-01
dtxcid902692
tox21_113601
dtxsid0022692 ,
cas-57801-81-7
AKOS016014338
brotizolamum
5xzm1r3dkf ,
brotizolam [usan:inn:ban:jan]
unii-5xzm1r3dkf
2-bromo-4-(o-chlorophenyl)-9-methyl-6h-thieno[3,2-f]-s-triazolo[4,3-a][1,4]diazepine
brotizolam [mart.]
8-bromo-6-(o-chlorophenyl)-1-methyl-4h-s-triazolo(3,4-c)thieno(2,3-e)-1,4-diazepine
brotizolam [inn]
brotizolam [jan]
brotizolam [usan]
brotizolam [ep monograph]
2-bromo-4-(2-chlorophenyl)-9-methyl-6h-thieno(3,2-f)-s-triazolo(4,3-a)(1,4)diazepine
brotizolam [who-dd]
brotizolam [mi]
SCHEMBL44067
2-bromo-4-(o-chlorophenyl)-9-methyl-6h-thieno[3,2-f]-s-triazolo[4,3-a]-[1,4]diazepine
we 941-bs
DB09017
CHEBI:31308
brotizolam 1.0 mg/ml in methanol
brotizolam; 2-bromo-4-(2-chlorophenyl)-9-methyl-6h-thieno-[3,2-f][1,2,4]-triazolo[4,3-a][1,4]diazepine
brotizolam 0.1 mg/ml in methanol
Q850074
4-n-pentylphenyl-4-trans-n-propylcyclohexylcarboxylate
4-bromo-7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaene

Research Excerpts

Overview

Brotizolam is a short-acting hypnotic in the benzodiazepine family. It is a rapidly absorbed hypnotic drug with a short elimination half-life. Fatal poisonings by an overdose are rare.

ExcerptReferenceRelevance
"Brotizolam is a short-acting hypnotic in the benzodiazepine family, and fatal poisonings by an overdose of brotizolam are rare. "( Deaths Associated With Brotizolam Poisoning From a Single Drug Overdose: Four Reported Cases.
Fukunaga, T; Hikiji, W; Kikuchi, Y; Saito, K; Sakai, K; Takada, A, 2018
)
2.23
"Brotizolam is a short-acting hypnotic."( Brotizolam: studies of effects on sleep and on performance in young adulthood and in middle age.
Nicholson, AN, 1983
)
2.43
"Thus brotizolam is a rapidly absorbed hypnotic drug with a short elimination half-life."( Pilot pharmacokinetic study of brotizolam, a thienodiazepine hypnotic, using electron-capture gas-liquid chromatography.
Greenblatt, DJ; Locniskar, A; Shader, RI, 1983
)
1.01
"4 Brotizolam is a short-acting hypnotic."( Studies on sleep and performance with a triazolo-1, 4-thienodiazepine (brotizolam).
Nicholson, AN; Pascoe, PA; Stone, BM, 1980
)
1.05
"Brotizolam is a new thienotriazolodiazepine derivative with a pharmacological profile similar to that of benzodiazepines. "( Brotizolam. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy as an hypnotic.
Clissold, SP; Langley, MS, 1988
)
3.16

Effects

Brotizolam has a pharmacologic spectrum of action similar to clinically useful benzodiazepines, while the closely related derivatives WE 973 and WE 1008 appear to lack hypnotic action. It has an elimination half-life of about 5 hours.

Brotizolam has anxiolytic, anticonvulsant and muscle relaxant properties. Has an elimination half-life of about 5 hours. Has pharmacologic spectrum of action similar to clinically useful benzodiazepines.

ExcerptReferenceRelevance
"Brotizolam has a pharmacologic spectrum of action similar to clinically useful benzodiazepines, while the closely related derivatives WE 973 and WE 1008 appear to lack hypnotic action."( Pharmacological and neurochemical properties of 1,4-diazepines with two annelated heterocycles ('hetrazepines').
Böke-Kuhn, K; Danneberg, PB; Hommer, D; Kuhn, FJ; Lehr, E; Paul, SM; Skolnick, P; Weber, KH, 1985
)
0.99
"Brotizolam has an elimination half-life of about 5 hours, which is 'intermediate' compared with the shorter-acting hypnotic, triazolam, and longer-acting benzodiazepines."( Brotizolam. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy as an hypnotic.
Clissold, SP; Langley, MS, 1988
)
2.44
"Brotizolam has anxiolytic, anticonvulsant and muscle relaxant properties."( Pharmacology and hypnogenic properties of brotizolam in animals.
Böke-Kuhn, K; Danneberg, P; Kuhn, FJ; Lehr, E; Stockhaus, K, 1983
)
1.25
"Brotizolam has a pharmacologic spectrum of action similar to clinically useful benzodiazepines, while the closely related derivatives WE 973 and WE 1008 appear to lack hypnotic action."( Pharmacological and neurochemical properties of 1,4-diazepines with two annelated heterocycles ('hetrazepines').
Böke-Kuhn, K; Danneberg, PB; Hommer, D; Kuhn, FJ; Lehr, E; Paul, SM; Skolnick, P; Weber, KH, 1985
)
0.99
"Brotizolam has an elimination half-life of about 5 hours, which is 'intermediate' compared with the shorter-acting hypnotic, triazolam, and longer-acting benzodiazepines."( Brotizolam. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy as an hypnotic.
Clissold, SP; Langley, MS, 1988
)
2.44

Treatment

Treatment with brotizolam during hospitalization in internal medicine wards is linked to a higher risk of respiratory deterioration, delirium, and falls. The patients were older with more comorbidities and psychotropic medications.

ExcerptReferenceRelevance
"The brotizolam-treated patients were older with more comorbidities and psychotropic medications."( Safety of brotizolam in hospitalized patients.
Bejel, S; Lavon, O, 2018
)
1.36
"Treatment with brotizolam during hospitalization in internal medicine wards is linked to a higher risk of respiratory deterioration, delirium, and falls. "( Safety of brotizolam in hospitalized patients.
Bejel, S; Lavon, O, 2018
)
1.24

Pharmacokinetics

The elimination half-life of brotizolam was twice that of triazolam with mean values of 5.9 and 9. The mean Elimination Half-life was about twice as long in the elderly as in the young subjects.

ExcerptReferenceRelevance
" The pharmacokinetic properties of these newer drugs can best be understood by their categorisation according to range of elimination half-life and pathway of metabolism (oxidation versus conjugation)."( Clinical pharmacokinetics of the newer benzodiazepines.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Ochs, HR; Shader, RI,
)
0.13
" Elimination half-life was longer in patients than in controls."( Pharmacokinetics of oral brotizolam in patients with liver cirrhosis.
Breimer, DD; Jochemsen, R; Joeres, RP; Richter, E; Wesselman, JG, 1983
)
0.57
"1 ng ml h(-1)), and prolonged the elimination half-life (4."( Effect of itraconazole on the pharmacokinetics and pharmacodynamics of a single oral dose of brotizolam.
Kaneko, S; Kondo, T; Ohkubo, T; Osanai, T; Yasui, N, 2004
)
0.54
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Bioavailability

Brotizolam was relatively slow in the elderly with a mean peak time of 1. Inter-individual variability in absorption rate (peak times) was larger for brotizolham.

ExcerptReferenceRelevance
" Inter-individual variability in absorption rate (peak times) was larger for brotizolam."( Comparative pharmacokinetics of brotizolam and triazolam in healthy subjects.
Breimer, DD; Hermans, J; Jochemsen, R; van Boxtel, CJ; Wesselman, JG, 1983
)
0.78
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" The main reason for the difference appears to be due to differences in the rate of absorption of the main drug."( [Comparative study of drug efficacy and drug additives between generic drugs and original drugs].
Katoh, H; Ozawa, K; Yoshii, M, 2007
)
0.34
"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

Brotizolam levels measured several times during the study 10 h after dosing were between 1.5 and 2.0. There was evidence of impairment of performance in the reaction time test, the digit-symbol substitution test, and a tracking task.

ExcerptRelevanceReference
"Dissolution testing of solid oral dosage forms plays a very important part both in the development of new products and in quality control."( The automation of dissolution testing of solid oral dosage forms.
Lamparter, E; Lunkenheimer, CH,
)
0.13
" Used in the recommended dosage it may be particularly useful for patients in whom daytime impairment of performance is unacceptable."( Brotizolam. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy as an hypnotic.
Clissold, SP; Langley, MS, 1988
)
1.72
" There was evidence of impairment of performance, although not statistically significant, for the first 4-6 h after brotizolam dosage in the reaction time test, the digit-symbol substitution test, and a tracking task."( Kinetic and dynamic interaction of brotizolam and ethanol.
Greenblatt, DJ; Harmatz, JS; Scavone, JM; Shader, RI, 1986
)
0.76
" The dose-response curve of the maximum prolongation of the latencies was linear."( Effect of brotizolam on the averaged photopalpebral reflex in man.
Inanaga, K; Isozaki, H; Mizuki, Y; Tanaka, M, 1983
)
0.67
" Ten of the studies are dose-response evaluations."( Sleep spindles: pharmacological effects in humans.
Hirshkowitz, M; Karacan, I; Thornby, JI, 1982
)
0.26
[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 (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency33.49830.000811.382244.6684AID686978
AR proteinHomo sapiens (human)Potency8.22020.000221.22318,912.5098AID743035; AID743042; AID743054; AID743063
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency10.68220.000214.376460.0339AID720692
estrogen nuclear receptor alphaHomo sapiens (human)Potency8.56380.000229.305416,493.5996AID743069; AID743078; AID743079; AID743080; AID743091
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency10.59090.001723.839378.1014AID743083
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency24.71040.000323.4451159.6830AID743065; AID743067
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency24.65590.011917.942071.5630AID651632; AID720516
Ataxin-2Homo sapiens (human)Potency23.71010.011912.222168.7989AID651632
[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)
Platelet-activating factor receptorHomo sapiens (human)IC50 (µMol)0.30000.00030.63183.7000AID157741
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (47)

Processvia Protein(s)Taxonomy
positive regulation of cellular extravasationPlatelet-activating factor receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIPlatelet-activating factor receptorHomo sapiens (human)
chemotaxisPlatelet-activating factor receptorHomo sapiens (human)
inflammatory responsePlatelet-activating factor receptorHomo sapiens (human)
immune responsePlatelet-activating factor receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
parturitionPlatelet-activating factor receptorHomo sapiens (human)
response to symbiotic bacteriumPlatelet-activating factor receptorHomo sapiens (human)
lipopolysaccharide-mediated signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of interleukin-6 productionPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of tumor necrosis factor productionPlatelet-activating factor receptorHomo sapiens (human)
inositol trisphosphate biosynthetic processPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of neutrophil degranulationPlatelet-activating factor receptorHomo sapiens (human)
transcytosisPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of translationPlatelet-activating factor receptorHomo sapiens (human)
negative regulation of blood pressurePlatelet-activating factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processPlatelet-activating factor receptorHomo sapiens (human)
cellular response to gravityPlatelet-activating factor receptorHomo sapiens (human)
cellular response to cAMPPlatelet-activating factor receptorHomo sapiens (human)
cellular response to fatty acidPlatelet-activating factor receptorHomo sapiens (human)
response to dexamethasonePlatelet-activating factor receptorHomo sapiens (human)
positive regulation of leukocyte tethering or rollingPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of transcytosisPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of maternal process involved in parturitionPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of gastro-intestinal system smooth muscle contractionPlatelet-activating factor receptorHomo sapiens (human)
cellular response to 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholinePlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
lipopolysaccharide bindingPlatelet-activating factor receptorHomo sapiens (human)
lipopolysaccharide immune receptor activityPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled receptor activityPlatelet-activating factor receptorHomo sapiens (human)
platelet activating factor receptor activityPlatelet-activating factor receptorHomo sapiens (human)
protein bindingPlatelet-activating factor receptorHomo sapiens (human)
phospholipid bindingPlatelet-activating factor receptorHomo sapiens (human)
mitogen-activated protein kinase bindingPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityPlatelet-activating factor receptorHomo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
plasma membranePlatelet-activating factor receptorHomo sapiens (human)
membranePlatelet-activating factor receptorHomo sapiens (human)
secretory granule membranePlatelet-activating factor receptorHomo sapiens (human)
tertiary granule membranePlatelet-activating factor receptorHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID76841In vivo inhibitory dose against PAF-induced bronchoconstriction in guinea pig upon intravenous administration after one-minute pre-treatment time.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2.
AID1692392Displacement of [3H]flunitrazepam from Benzodiazepine receptor in Sprague-Dawley rat cerebral cortex membrane measured after 30 mins by liquid scintillation spectrometry analysis2020European journal of medicinal chemistry, Aug-15, Volume: 200Design, synthesis and biological evaluation of 7-substituted 4-phenyl-6H-imidazo[1,5-a]thieno[3,2-f] [1,4]diazepines as safe anxiolytic agents.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID157741In vitro for platelet activating factor receptor antagonist activity in a binding assay using washed whole dog platelets.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2.
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.
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.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID78323In vivo inhibition against PAF-induced bronchoconstriction in guinea pig at 1 mg/kg dose upon peroral administration after one-minute pre-treatment time.1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2.
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.
AID29813Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (164)

TimeframeStudies, This Drug (%)All Drugs %
pre-199094 (57.32)18.7374
1990's20 (12.20)18.2507
2000's28 (17.07)29.6817
2010's16 (9.76)24.3611
2020's6 (3.66)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 60.88

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 Index60.88 (24.57)
Research Supply Index5.39 (2.92)
Research Growth Index4.34 (4.65)
Search Engine Demand Index102.31 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (60.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials50 (29.59%)5.53%
Reviews5 (2.96%)6.00%
Case Studies6 (3.55%)4.05%
Observational0 (0.00%)0.25%
Other108 (63.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (8)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Lendormin D® Tablet (Drug Use Result Survey) [NCT02224014]485 participants (Actual)Observational2005-06-30Completed
A Randomized, Single-dose, Two-way Cross-over Study to Assess the Bioequivalence of Lendormin Tablets 0.25 mg (Delpharm Reims) vs. Lendormin Tablets 0.25 mg (Synmosa Biopharma Co. Ltd.) Administered to Healthy Adult Volunteers [NCT01361022]Phase 124 participants (Actual)Interventional2011-08-31Completed
The Influence of Short Term Treatment With Benzodiazepine After Cardiac Surgery [NCT02776228]Phase 3200 participants (Anticipated)Interventional2016-12-31Not yet recruiting
Clinical Pharmacological Study on Absorption From Mucous Membrane of Oral Cavity of WE 941 OD Tablets [NCT02218671]Phase 110 participants Interventional2000-03-31Completed
The Bioequivalence Between WE 941 OD Tablets (0.25mg as the Basis) Taken Without Water and Brotizolam Conventional Tablets (Lendormin® Tablets, 0.25 mg as the Basis) Taken With Water, as a Single Administration in Healthy Adult Male Subjects (Open-labelle [NCT02218658]Phase 130 participants (Actual)Interventional2000-07-31Completed
The Bioequivalence Between WE 941 OD Tablets (0.25mg as the Basis) and Brotizolam Conventional Tablets (Lendormin® Tablets, 0.25 mg as the Basis), Both Taken With Water, as a Single Administration in Healthy Adult Male Subjects (Open-labelled, 2-way Cross [NCT02218645]Phase 130 participants (Actual)Interventional2000-08-31Completed
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
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
[information is prepared from clinicaltrials.gov, extracted Sep-2024]