U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

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
Structure of GIDAZEPAM

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)

HIDE SMILES / InChI

Molecular Formula C17H15BrN4O2
Molecular Weight 387.231
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: The description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/15188766 | https://www.ncbi.nlm.nih.gov/pubmed/12503630 |

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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
710.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Гидазепам

Approved Use

Unknown
Primary
Гидазепам

Approved Use

Unknown
Primary
Гидазепам

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
[Is it possible to predict individual stress resistance by evaluating low dose benzodiazepine effect in modeled emotional stress].
2001 Mar-Apr
[Chemiluminescent immunoenzyme method for determining gidazepam].
2001 Mar-Apr
[Effect of gidazepam on the motivational component of operator activity].
2001 May-Jun
Affinities of gidazepam and its analogs for mitochondrial benzodiazepine receptors.
2002 Feb-Nov
[Stress-induced alteration of the anticonflict effect of anxiolytics].
2002 Jul-Aug
[Experimental and clinical rationale for complex treatment of mental disorders in clean-up workers of the Chernobyl nuclear plant accident].
2002 Mar-Apr
[Pharmacological regulation of emotional stress reactions].
2003
[Pharmacokinetic evaluation of the tablet dosage forms of gidazepam prepared by various technologies].
2004 Mar-Apr
Patents

Patents

Sample Use Guides

In Vivo Use Guide
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.
Substance Class Chemical
Created
by admin
on Fri Dec 15 18:46:03 UTC 2023
Edited
by admin
on Fri Dec 15 18:46:03 UTC 2023
Record UNII
XMJ87I93Y9
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GIDAZEPAM
WHO-DD  
Common Name English
2-(9-BROMO- 3-OXO- 6-PHENYL- 2,5-DIAZABICYCLO(5.4.0) UNDECA-5,8,10,12-TETRAEN- 2-YL) ACETOHYDRAZIDE
Common Name English
Gidazepam [WHO-DD]
Common Name English
(1-HYDRAZINOCARBONYL)-7-BROMO-5-PHENYL-1,2-DIHYDRO-3H-1,4-BENZODIAZEPINE-2-ONE
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C1012
Created by admin on Fri Dec 15 18:46:03 UTC 2023 , Edited by admin on Fri Dec 15 18:46:03 UTC 2023
Code System Code Type Description
PUBCHEM
121919
Created by admin on Fri Dec 15 18:46:03 UTC 2023 , Edited by admin on Fri Dec 15 18:46:03 UTC 2023
PRIMARY
NCI_THESAURUS
C98136
Created by admin on Fri Dec 15 18:46:03 UTC 2023 , Edited by admin on Fri Dec 15 18:46:03 UTC 2023
PRIMARY
MESH
C077010
Created by admin on Fri Dec 15 18:46:03 UTC 2023 , Edited by admin on Fri Dec 15 18:46:03 UTC 2023
PRIMARY
SMS_ID
100000086901
Created by admin on Fri Dec 15 18:46:03 UTC 2023 , Edited by admin on Fri Dec 15 18:46:03 UTC 2023
PRIMARY
EPA CompTox
DTXSID00156091
Created by admin on Fri Dec 15 18:46:03 UTC 2023 , Edited by admin on Fri Dec 15 18:46:03 UTC 2023
PRIMARY
CAS
129186-29-4
Created by admin on Fri Dec 15 18:46:03 UTC 2023 , Edited by admin on Fri Dec 15 18:46:03 UTC 2023
PRIMARY
EVMPD
SUB22925
Created by admin on Fri Dec 15 18:46:03 UTC 2023 , Edited by admin on Fri Dec 15 18:46:03 UTC 2023
PRIMARY
WIKIPEDIA
GIDAZEPAM
Created by admin on Fri Dec 15 18:46:03 UTC 2023 , Edited by admin on Fri Dec 15 18:46:03 UTC 2023
PRIMARY
FDA UNII
XMJ87I93Y9
Created by admin on Fri Dec 15 18:46:03 UTC 2023 , Edited by admin on Fri Dec 15 18:46:03 UTC 2023
PRIMARY
Related Record Type Details
PRODRUG -> METABOLITE ACTIVE
Related Record Type Details
ACTIVE MOIETY