Cinazepam

Cinazepam (BD-798) is an atypical benzodiazepine derivative which was never marketed. It produces pronounced hypnotic, sedative, and anxiolytic effects with minimal myorelaxant side effects. In addition, unlike many other benzodiazepine and nonbenzodiazepine hypnotics such as diazepam, flunitrazepam, and zopiclone, cinazepam does not violate sleep architecture, and the continuity of slow-wave sleep and REM sleep are proportionally increased. As such, cinazepam produces a sleep state close to physiological, and for that reason, may be advantageous compared to other, related drugs in the treatment of insomnia and other sleep disorders.

Cinazepam has an order of magnitude lower affinity for the benzodiazepine receptor of the GABA_A complex relative to other well-known hypnotic benzodiazepines such as nitrazepam and phenazepam. Moreover, in mice, it is rapidly metabolized, with only 5% of the base compound remaining within 30 minutes of administration. As such, cinazepam is considered to be a benzodiazepine prodrug; specifically, to 3-hydroxyphenazepam, as the main active metabolite.