BDBM50000766 CHEMBL12 DIAZEPAM US9271961, Diazepam
Ro5-4864 4 -chlorodiazepam 7-chloro-5-(4-chlorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one BDBM22040 4' Cl-diazepam CHEMBL286346 Ro 5-4864 7-chloro-5-(4-chlorophenyl)-1-methyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one Ro-4864 Ro-05-4864
- Wieland, HA; Lüddens, H Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. J Med Chem 37: 4576-80 (1995)
- Gunnersen, D; Kaufman, CM; Skolnick, P Pharmacological properties of recombinant "diazepam-insensitive" GABAA receptors. Neuropharmacology 35: 1307-14 (1996)
- Braestrup, C; Squires, RF Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H)diazepam binding. Proc Natl Acad Sci U S A 74: 3805-9 (1977)
- Yang, W; Drewe, JA; Lan, NC Cloning and characterization of the human GABAA receptor alpha 4 subunit: identification of a unique diazepam-insensitive binding site. Eur J Pharmacol 291: 319-25 (1995)
- ChEBML_178942 Anxiolytic activity by displacement of [3H]diazepam from GABA-A receptor in rat synaptosomal membranes
- ChEMBL_774144 Mechanism based inhibition of dog cytochrome P450 CYP2B11 measured by Diazepam N1-demethylation using liver microsomes
- ChEMBL_774145 Mechanism based inhibition of dog cytochrome P450 CYP2B11 measured by Diazepam N1-demethylation using recombinant enzyme
- Biological Assay Example 8 Using a procedure similar to that described in Biological Test Example 6, the inhibition of cytochrome P450 2C19-isoenzyme catalysed N-demethylation of [N-methyl-14C]-Diazepam by the test compound was assayed at 37° C. with human recombinant cytochrome P450 2C19.
- Biological Assay Example 8 Using a procedure similar to that described in Biological Test Example 6, the inhibition of cytochrome P450 2C19-isoenzyme catalysed N-demethylation of [N-methyl-14C]-Diazepam by the test compound was assayed at 37° C. with human recombinant cytochrome P450 2C19.
- Radioligand Binding Assay Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell memebranes, [3H]flumazenil at a concentration of 1 nM for α1, α2, α3 subunits and 0.5 nM for α5 subunits and the test compound in the range of 10-10−3x10−6 M. Nonspecific binding was defined by 10−5 M diazepam and typically represented less than 5% of the total binding. Assays were incubated to equilibrium for 1 hour at 4 C. and harvested onto GF/C uni-filters (Packard) by filtration using a Packard harvester and washing with ice-cold wash buffer (50 mM Tris; pH 7.5). After drying, filter-retained radioactivity was detected by liquid scintillation counting.
- Radioligand Binding Assay Radioligand binding assays were carried out in a volume of 200 mL (96-well plates) which contained 100 mL of cell membranes, [3H]flumazenil at a concentration of 1 nM for α1, α2, α3 subunits and 0.5 nM for α5 subunits and the test compound in the range of 10-10−3×10−6 M. Nonspecific binding was defined by 10−5 M diazepam and typically represented less than 5% of the total binding. Assays were incubated to equilibrium for 1 hour at 4° C. and harvested onto GF/C uni-filters (Packard) by filtration using a Packard harvester and washing with ice-cold wash buffer (50 mM Tris; pH 7.5). After drying, filter-retained radioactivity was detected by liquid scintillation counting.