Gidazepam

Gidazepam, also known as hydazepam or hidazepam,^[2] is a drug which is an atypical benzodiazepine derivative, developed in the Soviet Union.^[3][4] It is a selectively anxiolytic benzodiazepine.^[5] It also has therapeutic value in the management of certain cardiovascular disorders.^{[6][7][8][9][10]}

Gidazepam

Clinical data
Trade names	Gidazepam IC
Routes of administration	Oral
Legal status
Legal status	CA: Schedule IV US: Unscheduled (UA): Rx-Only [1]
Pharmacokinetic data
Metabolism	Hepatic
Elimination half-life	~87 hours
Excretion	Renal
Identifiers
IUPAC name 2-(9-Bromo-3-oxo-6-phenyl-2,5-diazabicyclo[5.4.0]undeca-5,8,10,12-tetraen-2-yl)acetohydrazide
CAS Number	129186-29-4
PubChem CID	121919
DrugBank	? N
ChemSpider	108764 Y
UNII	XMJ87I93Y9
CompTox Dashboard (EPA)	DTXSID00156091
Chemical and physical data
Formula	C17H15BrN4O2
Molar mass	387.237 g·mol−1
3D model (JSmol)	Interactive image
SMILES BrC1=CC2=C(C=C1)N(CC(NN)=O)C(CN=C2C3=CC=CC=C3)=O
InChI 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) Y Key:XLGCMZLSEXRBSG-UHFFFAOYSA-N Y
NY (what is this?)  (verify)

Pharmacology

Gidazepam and several of its analogs, in contrast to other benzodiazepines, are comparatively more selective agonists of TSPO (formerly the peripheral benzodiazepine receptor) than the benzodiazepine receptor.^[5]

Gidazepam acts as a prodrug to its active metabolite 7-bromo-2,3-dihydro-5-phenyl-1H-1,4-benzodiazepin-2-one (desalkylgidazepam or bromo-nordazepam).^[11][12] Its anxiolytic effects can take several hours to manifest presumably due to its slow metabolism (half-life 87 hours). The onset and intensity of anxiolytic effects correlate with blood levels of desalkylgidazepam.^[13]

Gidazepam active metabolite (desalkylgidazepam), responsible for its therapeutic effects

See also

• Phenazepam—another benzodiazepine widely used in Russia and other CIS countries
• Cinazepam
• Cloxazolam
• List of Russian drugs