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didesethylflurazepam

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

Description

didesethylflurazepam: major metbolite of flurazepam; RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

didesethylflurazepam : A primary amino compound resulting from the dealkylation of both ethyl groups of the anti-insomnia drug flurazepam. It is the major metabolite of flurazepam. [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 CID28647
CHEMBL ID1201372
CHEBI ID143439
SCHEMBL ID8124276
MeSH IDM0103826

Synonyms (25)

Synonym
didesethyl flurazepam
didesethylflurazepam
n,n-bisdesethylflurazepam
2h-1,4-benzodiazepin-2-one, 1-(2-aminoethyl)-7-chloro-5-(o-fluorophenyl)-1,3-dihydro-
ro 7-1986
brn 0706279
dideethylflurazepam
1-(2-aminoethyl)-7-chloro-5-(2-fluorophenyl)-1,3-dihydro-2h-1,4-benzodiazepin-2-one
2h-1,4-benzodiazepin-2-one, 1,3-dihydro-1-(2-aminoethyl)-7-chloro-5-(2-fluorophenyl)-
1-(2-aminoethyl)-7-chloro-5-(2-fluorophenyl)-3h-1,4-benzodiazepin-2-one
CHEBI:143439
17617-59-3
CHEMBL1201372
buj3jod7xf ,
unii-buj3jod7xf
21808-55-9
SCHEMBL8124276
MVAUDJDXZPBWOW-UHFFFAOYSA-N
2h-1,4-benzodiazepin-2-one, 1-(2-aminoethyl)-7-chloro-5-(2-fluorophenyl)-1,3-dihydro-
DTXSID80170093
7-chloro-1-(2-aminoethyl)-5-(2-fluorophenyl)-1,3-dihydro-2h-1,4-benzodiazepin-2-one
FT-0716640
Q6951355
YNL ,
(5m)-1-(2-aminoethyl)-7-chloro-5-(2-fluorophenyl)-1,3-dihydro-2h-1,4-benzodiazepin-2-one

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" This metabolite appeared in serum rapidly (within 2 h), reached a peak between 2 and 12 h and declined slowly, with an elimination half-life of about 90 h on average."( Pharmacokinetics of flutoprazepam, a novel benzodiazepine drug, in normal subjects.
Barzaghi, N; Leone, L; Monteleone, M; Perucca, E; Tomasini, G,
)
0.13

Bioavailability

ExcerptReferenceRelevance
" Temazepam has a relatively slow rate of absorption and an intermediate half-life in the range of 10 to 20 hours."( Pharmacokinetic properties of benzodiazepine hypnotics.
Abernethy, DR; Divoll, M; Greenblatt, DJ; Harmatz, JS; Shader, RI, 1983
)
0.27

Dosage Studied

ExcerptRelevanceReference
"" Midazolam caused a shift to the left of the GABA log dose-response curve."( Modulation of GABA-gated chloride ion flux in rat brain by acute and chronic benzodiazepine administration.
Chiu, TH; Rosenberg, HC; Yu, O, 1988
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
GABAA receptor agonistA GABA receptor agonist specific for GABAA receptors, ligand-gated ion channels (also known as ionotropic receptors).
anticonvulsantA drug used to prevent seizures or reduce their severity.
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.
sedativeA central nervous system depressant used to induce drowsiness or sleep or to reduce psychological excitement or anxiety.
drug metabolitenull
[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 (4)

ClassDescription
1,4-benzodiazepinone
monofluorobenzenesAny member of the class of fluorobenzenes containing a mono- or poly-substituted benzene ring carrying a single fluorine substitutent.
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
primary amino compoundA compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
[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]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID384955Intrinsic aqueous solubility at pH 10 by shake-flask method2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Molecular characteristics for solid-state limited solubility.
AID384956Dissociation constant, pKa of the compound2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Molecular characteristics for solid-state limited solubility.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19909 (50.00)18.7374
1990's3 (16.67)18.2507
2000's5 (27.78)29.6817
2010's1 (5.56)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (14.29%)5.53%
Reviews0 (0.00%)6.00%
Case Studies3 (14.29%)4.05%
Observational0 (0.00%)0.25%
Other15 (71.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]