Chemistry:Cinazepam
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| Formula | C19H14BrClN2O5 |
| Molar mass | 465.68 g·mol−1 |
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Cinazepam (BD-798, sold under brand name Levana) is an atypical benzodiazepine derivative.[1] It produces pronounced hypnotic, sedative, and anxiolytic effects with minimal myorelaxant side effects.[2][3][4] 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.[2][3][4] 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.[2]
Cinazepam has an order of magnitude lower affinity for the benzodiazepine receptor of the GABAA complex relative to other well-known hypnotic benzodiazepines such as nitrazepam and phenazepam.[2] Moreover, in mice, it is rapidly metabolized, with only 5% of the base compound remaining within 30 minutes of administration.[2] As such, cinazepam is considered to be a benzodiazepine prodrug; specifically, to 3-hydroxyphenazepam, as the main active metabolite.[2]
See also
References
- ↑ Sleep Research. 26. Brain Information Service/Brain Research Institute, University of California.. 1997. p. 115. https://books.google.com/books?id=DWBQAAAAYAAJ.
- ↑ 2.0 2.1 2.2 2.3 2.4 2.5 "Elimination kinetics of the novel prodrug cinazepam possessing psychotropic activity in mice". Pharmacological Reports 63 (5): 1093–1100. 2011. doi:10.1016/s1734-1140(11)70628-4. PMID 22180351.
- ↑ 3.0 3.1 "Effect of cinazepam administration on the ligand affinity of neuromediator system receptors in rat brain". Pharmaceutical Chemistry Journal 41 (5): 249–252. 2007. doi:10.1007/s11094-007-0055-9. ISSN 0091-150X.
- ↑ 4.0 4.1 "Bioaccessibility of cinazepam introduced as inclusion complex with β-cyclodextrin". Pharmaceutical Chemistry Journal 32 (10): 513–515. 1998. doi:10.1007/BF02465736. ISSN 0091-150X.
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