Details
Stereochemistry | RACEMIC |
Molecular Formula | C18H14ClFN2O3 |
Molecular Weight | 360.767 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCOC(=O)C1N=C(C2=CC=CC=C2F)C3=C(NC1=O)C=CC(Cl)=C3
InChI
InChIKey=CUCHJCMWNFEYOM-UHFFFAOYSA-N
InChI=1S/C18H14ClFN2O3/c1-2-25-18(24)16-17(23)21-14-8-7-10(19)9-12(14)15(22-16)11-5-3-4-6-13(11)20/h3-9,16H,2H2,1H3,(H,21,23)
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/6142848Curator's Comment: description was created based on several sources, including
http://meds.famguerra.com/?pagina=36557.htm
https://www.ncbi.nlm.nih.gov/pubmed/2861304
https://www.ncbi.nlm.nih.gov/pubmed/2866771
Sources: https://www.ncbi.nlm.nih.gov/pubmed/6142848
Curator's Comment: description was created based on several sources, including
http://meds.famguerra.com/?pagina=36557.htm
https://www.ncbi.nlm.nih.gov/pubmed/2861304
https://www.ncbi.nlm.nih.gov/pubmed/2866771
Ethyl loflazepate (Lof) has been used widely as a sedative and anxiolytic agent for nearly 20 years. Ethyl loflazepate was designed to be a prodrug for descarboxyloflazepate, its active metabolite. It is the active metabolite which is responsible for most of the pharmacological effects rather than ethyl loflazepate. The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-ydroxydescarbethoxyloflazepate which are the benzodiazepine receptor agonists. Ethyl loflazeplate is commercialized in Mexico, under the trade name Victan. It is officially approved for the following conditions Anxiety: Post-trauma anxiety; Anxiety associated with severe neuropathic pain; Generalized anxiety disorder (GAD); Panic attack; Delirium tremens. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Accumulation of the active metabolites of ethyl loflazepate are not affected by those with renal failure or impairment. The symptoms of an overdose of ethyl loflazepate include sleepiness, agitation and ataxia. Hypotonia may also occur in severe cases. These symptoms occur much more frequently and severely in children. High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2111392 Sources: http://www.ncbi.nlm.nih.gov/pubmed/15902983 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
Specific and sensitive analysis of nefopam and its main metabolite desmethyl-nefopam in human plasma by liquid chromatography-ion trap tandem mass spectrometry. | 2006 Nov 16 |
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Impaired prefrontal hemodynamic maturation in autism and unaffected siblings. | 2009 Sep 3 |
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Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method. | 2010 Dec |
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Pregnancy in woman with spinal cord stimulator for complex regional pain syndrome: a case report and review of the literature. | 2010 Dec |
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Effects of etizolam and ethyl loflazepate on the P300 event-related potential in healthy subjects. | 2010 Nov 3 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2904268
½ to 1½ tablet at day (1 ime or several tomes at day).
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/2861304
CM6912 (ethyl loflazepate ) inhibited the specific binding of 3H-diazepam by 25%, 75% and 90% at concentrations of 0.01 microM, 0.1 microM and 1 microM, respectively to the synaptosomal membrane fraction of rat cerebrum.
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C1012
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WHO-VATC |
QN05BA18
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DEA NO. |
2758
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WHO-ATC |
N05BA18
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C029617
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1092
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m5146
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3299
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C65566
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DTXSID60865475
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24524
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SUB07290MIG
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ETHYL LOFLAZEPATE
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VJB5FW9W9J
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4837
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100000090254
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249-489-4
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DB01545
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29177-84-2
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CHEMBL1213460
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ACTIVE MOIETY
METABOLITE ACTIVE (PARENT)