| Stereochemistry | ACHIRAL |
| Molecular Formula | C17H15BrN4O2 |
| Molecular Weight | 387.231 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
NNC(=O)CN1C2=C(C=C(Br)C=C2)C(=NCC1=O)C3=CC=CC=C3
InChI
InChIKey=XLGCMZLSEXRBSG-UHFFFAOYSA-N
InChI=1S/C17H15BrN4O2/c18-12-6-7-14-13(8-12)17(11-4-2-1-3-5-11)20-9-16(24)22(14)10-15(23)21-19/h1-8H,9-10,19H2,(H,21,23)
Gidazepam (also known as hydazepam or hidazepam) is an anxiolytic and atypical benzodiazepine derivative, developed in the Soviet Union and used to treat the nervous system diseases. Interacts with benzodiazepine receptors, increases the sensitivity of GABA receptors to the mediator, increases the inhibitory effect of GABA in the central nervous system. Reduces the excitability of the subcortical structures of the brain, inhibits polysynaptic spinal reflexes. Reduces emotional tension, fear, anxiety. It has an activating effect, vegetostabilizing properties, mildly relaxed and relaxing substance. Virtually does not affect the productive symptoms of psychotic genesis (acute delusional, hallucinatory, affective disorders), there is rarely a decrease in affective tension. There is evidence of a positive effect on the cardiovascular system of patients with a neurological condition and in healthy people in stressful situations.
CNS Activity
Approval Year
PubMed
Patents
Sample Use Guides
In the range from 50 to 200 mg a day provides to gidazepa therapeutic action. A course dose of 100 mg a day the most optimum. Use of higher daily doses (150-200 mg) is followed by the increased day drowsiness, feeling of muscular weakness.
Route of Administration:
Oral
Rat brain homogenate was used for activity evaluation. Binding of [3H]Ro5-4864 (3171 TBq/mol; produced in St. Petersburg, Russia) was carried out in a final incubation volume of 500 mL, containing 100 mkL of radioligand, 100 mkL of tested compound (Gidazepam), 100 mkL of tris-HCl (pH 7.4, 0C) and 200 mkL of membrane suspension. All assay tubes were incubated for 90 min at 4C. The incubation was stopped by dilution with 6mL of ice-cold tris-HCl (pH 7.4, 0C) and rapid filtration on a 12-position harvester using Whatman GF/B filters. The filters were washed with 6mL of the same buffer. The dried filters were placed into the scintillation vials. The vials were filled with 10mL of standard Optifase scintillator (LKB, Sweden), kept for one night at 20C and the radioactivity was then counted with a scintillation counter Rackbeta 1219 Spectral.
ACTIVE MOIETY
PRODRUG (METABOLITE ACTIVE)
