Drug intelligence / Profile preview

cinazepam

Development stage
Unknown
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Cinazepam is an atypical benzodiazepine derivative and a prodrug for 3-hydroxyphenazepam. It is primarily used for its pronounced hypnotic (sleep-inducing), sedative, and anxiolytic effects with minimal myorelaxant side effects. Unlike many other benzodiazepines and nonbenzodiazepine hypnotics (such as diazepam or zopiclone), cinazepam does not disrupt sleep architecture; it increases the continuity of slow-wave sleep and REM sleep. This results in a sleep state closer to physiological norms and may make it advantageous in treating insomnia or other sleep disorders. Cinazepam acts as a partial agonist at the GABA-A receptor benzodiazepine binding site—modulating GABAergic neurotransmission but with lower affinity than typical hypnotic benzodiazepines. It is rapidly metabolized in vivo to its main active metabolite 3-hydroxyphenazepam[1][5][8].

Brand names
Levana
Other names
4-{[7-bromo-5-(2-chlorophenyl)-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]oxy}-4-oxobutanoic acidButanedioic acid mono(7-bromo-5-(2-chlorophenyl)-2,3-dihydro-2-oxo-1H-1,4-benzodiazepin-3-yl) ester
02

Targets

BZD site (GABA-A receptor benzodiazepine site)

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