Stereochemistry | ACHIRAL |
Molecular Formula | C14H10BrN3O |
Molecular Weight | 316.153 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
BrC1=CC=C2NC(=O)CN=C(C3=CC=CC=N3)C2=C1
InChI
InChIKey=VMIYHDSEFNYJSL-UHFFFAOYSA-N
InChI=1S/C14H10BrN3O/c15-9-4-5-11-10(7-9)14(17-8-13(19)18-11)12-3-1-2-6-16-12/h1-7H,8H2,(H,18,19)
Molecular Formula | C14H10BrN3O |
Molecular Weight | 316.153 |
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 |
Bromazepam (marketed under several brand names, including Lectopam, Lexotan, Lexilium, Lexaurin, Brazepam, Rekotnil, and Lexotanil)[1] is a benzodiazepine derivative drug, patented by Roche in 1963 and developed clinically in the 1970s. It is mainly an anti-anxiety agent with similar side effects to diazepam (Valium). In addition to being used to treat anxiety or panic states, bromazepam may be used as a premedicant prior to minor surgery. Bromazepam typically comes in doses of 3 mg and 6 mg tablets.[5] Bromazepam is contraindicated and should be used with caution in women who are pregnant, the elderly, patients with a history of alcohol or other substance abuse disorders and children. Prolonged use of bromazepam causes tolerance and may lead to both physical and psychological dependence on the drug, and as a result, it is a medication which is controlled by international law. Bromazepam binds to the GABA receptor GABAA, causing a conformational change and increasing the inhibitory effects of GABA. Bromazepam is a long-acting benzodiazepine and is lipophilic and metabolized hepatically via oxidative pathways.
CNS Activity
Originator
Approval Year
PubMed
Patents
Sample Use Guides
Adults: Depending upon severity of symptoms- 6 mg to 18 mg, in equally divided doses. Treatment may be initiated at a lower dose.
Elderly: Maximum of 3 mg in equally divided doses. Dose can be increased gradually as needed and tolerated.
Route of Administration:
Oral
500mkl of this P2-suspension (corresponding to 10mg original brain tissue) was preincubated for 5 min with Bromazepam. 25 mkl of 3H-diazepam working solution (to give a final concentration of 1.9 X 10^-9 M or approximately 14,000 cpm) was then added and the incubation continued for an additional 15 min at 37°C. The samples were then cooled in an ice bath for 30 min. IC50 values, i.e. values for 50% inhibition of specific 3H-diazepam binding, were assessed with at least 3 and up to 7 concentrations of the Bromazepam in duplicate or triplicate.