Details
Stereochemistry | ACHIRAL |
Molecular Formula | C16H12ClFN2O |
Molecular Weight | 302.731 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C2=C(C=C(Cl)C=C2)C(=NCC1=O)C3=CC=CC=C3F
InChI
InChIKey=ROYOYTLGDLIGBX-UHFFFAOYSA-N
InChI=1S/C16H12ClFN2O/c1-20-14-7-6-10(17)8-12(14)16(19-9-15(20)21)11-4-2-3-5-13(11)18/h2-8H,9H2,1H3
DescriptionSources: https://www.drugbank.ca/drugs/DB01567Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/fludiazepam.html | https://www.ncbi.nlm.nih.gov/pubmed/8529781 | https://www.ncbi.nlm.nih.gov/pubmed/7895897 | https://www.ncbi.nlm.nih.gov/pubmed/7601294 | http://www.mims.com/india/drug/info/fludiazepam?mtype=generic
Sources: https://www.drugbank.ca/drugs/DB01567
Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/fludiazepam.html | https://www.ncbi.nlm.nih.gov/pubmed/8529781 | https://www.ncbi.nlm.nih.gov/pubmed/7895897 | https://www.ncbi.nlm.nih.gov/pubmed/7601294 | http://www.mims.com/india/drug/info/fludiazepam?mtype=generic
Fludiazepam is a potent benzodiazepine and 2ʹ-fluoro derivative of diazepam,[3] originally developed by Hoffman-La Roche in the 1960s. Fludiazepam is marketed in Japan and Taiwan under the brand name Erispan. Fludiazepam exerts its pharmacological properties via enhancement of GABAergic inhibition. Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than diazepam. Fludiazepam possesses anxiolytic, anticonvulsant, sedative, hypnotic and skeletal muscle relaxant properties.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2093872 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2857046 |
1.23 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Erispan Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Non-life-threatening leukopenia in a renal transplant recipient with acute overdose of mycophenolate mofetil. | 2008 Dec |
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Case report: Etizolam and its major metabolites in two unnatural death cases. | 2008 Nov 20 |
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Development and validation of an EI-GC-MS method for the determination of benzodiazepine drugs and their metabolites in blood: applications in clinical and forensic toxicology. | 2010 Aug 1 |
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Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method. | 2010 Dec |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7895897
Curator's Comment: http://www.mims.com/india/drug/info/fludiazepam?mtype=generic
PO 0.75 mg/day in 3 divided doses.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2857046
An aliquot (1 ml) of synaptosomal membrane suspension (1 mg protein) was added to the assay tubes containing FLUDIAZEPAM at varying concentrations (from 0.1 nM to 104 nM) and [3H]-diazepam (0.6 nM) in 2 ml of 50 mM Tris-HCl buffer (pH 7.4). The assay mixtures were incubated at 4 ° C for 15 min. The incubation was terminated by adding ice-cold 50 mM Tris-HCl buffer (5 ml) followed by rapid filtration through a Whatman GF/B filter. Each filter was immediately washed twice with ice-cold 50 mM Tris-HCl buffer (5 ml) The bound [3H]-diazepam retained on the filter was extracted with ACS II (Amersham)(10 ml) and counted. All incubations were done in triplicate. Nonspecific binding was determined in tubes containing diazepam at a final concentration of 103 nM.
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WHO-VATC |
QN05BA17
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WHO-ATC |
N05BA17
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DEA NO. |
2759
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NCI_THESAURUS |
C1012
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SUB07681MIG
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m5429
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7F64A2K16Z
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1190
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31618
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C006107
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FLUDIAZEPAM
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100000081236
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CHEMBL13291
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DTXSID00192277
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C65709
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3369
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4089
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DB01567
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3900-31-0
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ACTIVE MOIETY
METABOLITE ACTIVE (PARENT)