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
Molecular Formula | C16H12ClFN2O |
Molecular Weight | 302.731 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
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.
CNS Activity
Approval Year
PubMed
Patents
Sample Use Guides
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.