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. Brain Information Service/Brain Research Institute, University of California. 1997.
- 1 2 3 4 5 6 Schukin SI, Zinkovsky VG, Zhuk OV (2011). "Elimination kinetics of the novel prodrug cinazepam possessing psychotropic activity in mice" (PDF). Pharmacol Rep. 63 (5): 1093–100. doi:10.1016/s1734-1140(11)70628-4. PMID 22180351.
- 1 2 Makan, S. Yu.; Boiko, I. A.; Smul’skii, S. P.; Andronati, S. A. (2007). "Effect of cinazepam administration on the ligand affinity of neuromediator system receptors in rat brain". Pharmaceutical Chemistry Journal. 41 (5): 249–252. doi:10.1007/s11094-007-0055-9. ISSN 0091-150X. S2CID 24532012.
- 1 2 Andronati, S. A.; Makan, S. Yu.; Neshchadin, D. P.; Yakubovskaya, L. N.; Sava, V. M.; Andronati, K. S. (1998). "Bioaccessibility of cinazepam introduced as inclusion complex with β-cyclodextrin". Pharmaceutical Chemistry Journal. 32 (10): 513–515. doi:10.1007/BF02465736. ISSN 0091-150X. S2CID 26513288.