Page last updated: 2024-11-07

gidazepam

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

Description

gidazepam: prodrug for 7-bromo-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepine-2-one [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID121919
CHEMBL ID1565882
SCHEMBL ID1004530
MeSH IDM0206968

Synonyms (35)

Synonym
(1-hydrazinocarbonyl)-7-bromo-5-phenyl-1,2-dihydro-3h-1,4-benzodiazepine-2-one
gidazepam
CHEMDIV1_027291
(7-bromo-2-oxo-5-phenyl-2,3-dihydro-benzo[e][1,4]diazepin-1-yl)-acetic acid hydrazide
MLS001012266 ,
smr000425069
OPREA1_121006
STK387500
2-(7-bromo-2-oxo-5-phenyl-2,3-dihydro-1h-1,4-benzodiazepin-1-yl)acetohydrazide
HMS664I11
2-(7-bromo-2-oxo-5-phenyl-3h-1,4-benzodiazepin-1-yl)acetohydrazide
AKOS001022554
NCGC00246439-01
unii-xmj87i93y9
xmj87i93y9 ,
129186-29-4
gidazepam [who-dd]
2-(9-bromo- 3-oxo- 6-phenyl- 2,5-diazabicyclo(5.4.0) undeca-5,8,10,12-tetraen- 2-yl) acetohydrazide
SCHEMBL1004530
CHEMBL1565882
2-(7-bromo-2-keto-5-phenyl-3h-1,4-benzodiazepin-1-yl)acetohydrazide
2-(7-bromanyl-2-oxidanylidene-5-phenyl-3h-1,4-benzodiazepin-1-yl)ethanehydrazide
bdbm45688
cid_121919
DTXSID00156091
1h-1,4-benzodiazepine-1-aceticacid,7-bromo-2,3-dihydro-2-oxo-5-phenyl-,hydrazide
SR-01000079103-1
sr-01000079103
Z56817662
HY-U00315
CS-7316
Q4138012
gidasepam;hidazepam; hydazepam
1h-1,4-benzodiazepine-1-acetic acid, 7-bromo-2,3-dihydro-2-oxo-5-phenyl-, hydrazide
EN300-1700024

Research Excerpts

Actions

ExcerptReferenceRelevance
"Gidazepam was shown to suppress the provocative arrhythmogenic effect of the stress test."( [Comparative anti-arrhythmia effectiveness of activators of body stress-limiting systems in patients with arrhythmia].
Meerson, FZ; Skibitskiĭ, VV, 1992
)
1

Pharmacokinetics

The basis for the development of tolerance to the myorelaxant effect of gidazepam given long to rats is biotransformational changes followed by varying pharmacokinetic parameters. decreases in the AUC and its desalkyl metabolite in plasma. redistribution of these substances between the plasma and brain of tolerant rats.

ExcerptReferenceRelevance
"It has been shown that the basis for the development of tolerance to the myorelaxant effect of gidazepam given long to rats is biotransformational changes followed by varying pharmacokinetic parameters: decreases in the AUC of gidazepam and its desalkyl metabolite in plasma, in brain in particular, redistribution of these substances between the plasma and brain of tolerant rats."( [An experimental study of the pharmacokinetic mechanisms for the development of gidazepam tolerance].
Garibova, TL; Kolyvanov, GB; Otabekova, SG; Voronina, TA; Zherdev, VP,
)
0.58
" Some pharmacokinetic parameters of gidazepam and its major metabolite desalkylgidazepam were determined."( [Gidazepam biotransformation and pharmacokinetics in different species of animals and man].
Chirkov, AM; Kolyvanov, GB; Litvin, AA; Otabekova, SG; Zherdev, VP,
)
1.32

Bioavailability

ExcerptReferenceRelevance
"When gidazepam was administered to rats in combination with 4% solutions of Tween 80 or polyvinylpyrrolidone, its bioavailability was higher than its combination with 4% polyethylene glycol 400 solution, as shown by high performance liquid chromatography."( [The effect of pharmaceutic aids on gidazepam biotransformation and bioavailability].
Kolyvanov, GB; Litvin, AA; Otabekova, SG; Vyrovshchikova, SM; Zherdev, VP,
)
0.92
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
serine-protein kinase ATM isoform aHomo sapiens (human)Potency39.81070.707925.111941.2351AID485349
ras-related protein Rab-9AHomo sapiens (human)Potency1.00000.00022.621531.4954AID485297
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
[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)
Coagulation factor XIIHomo sapiens (human)IC50 (µMol)50.00000.01043.889010.9666AID852
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (13)

Processvia Protein(s)Taxonomy
plasma kallikrein-kinin cascadeCoagulation factor XIIHomo sapiens (human)
Factor XII activationCoagulation factor XIIHomo sapiens (human)
blood coagulation, intrinsic pathwayCoagulation factor XIIHomo sapiens (human)
positive regulation of plasminogen activationCoagulation factor XIIHomo sapiens (human)
protein processingCoagulation factor XIIHomo sapiens (human)
protein autoprocessingCoagulation factor XIIHomo sapiens (human)
positive regulation of blood coagulationCoagulation factor XIIHomo sapiens (human)
zymogen activationCoagulation factor XIIHomo sapiens (human)
fibrinolysisCoagulation factor XIIHomo sapiens (human)
innate immune responseCoagulation factor XIIHomo sapiens (human)
response to misfolded proteinCoagulation factor XIIHomo sapiens (human)
positive regulation of fibrinolysisCoagulation factor XIIHomo sapiens (human)
blood coagulationCoagulation factor XIIHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
serine-type endopeptidase activityCoagulation factor XIIHomo sapiens (human)
calcium ion bindingCoagulation factor XIIHomo sapiens (human)
protein bindingCoagulation factor XIIHomo sapiens (human)
misfolded protein bindingCoagulation factor XIIHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
extracellular regionCoagulation factor XIIHomo sapiens (human)
extracellular spaceCoagulation factor XIIHomo sapiens (human)
plasma membraneCoagulation factor XIIHomo sapiens (human)
collagen-containing extracellular matrixCoagulation factor XIIHomo sapiens (human)
extracellular exosomeCoagulation factor XIIHomo sapiens (human)
extracellular spaceCoagulation factor XIIHomo sapiens (human)
rough endoplasmic reticulumCoagulation factor XIIHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay IDTitleYearJournalArticle
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.
AID651635Viability Counterscreen for Primary 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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's8 (66.67)18.2507
2000's1 (8.33)29.6817
2010's1 (8.33)24.3611
2020's2 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.75

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 Index53.75 (24.57)
Research Supply Index3.69 (2.92)
Research Growth Index4.20 (4.65)
Search Engine Demand Index83.57 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (53.75)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (14.71%)5.53%
Reviews1 (2.94%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other28 (82.35%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]