Cinazepam
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| Formula | C19H14BrClN2O5 |
| Molar mass | 465.68g·mol−1 |
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Cinazepam(BD-798,sold under brand nameLevana) is an atypicalbenzodiazepinederivative.[1]It produces pronouncedhypnotic,sedative,andanxiolyticeffects with minimalmyorelaxantside effects.[2][3][4]In addition, unlike many other benzodiazepine andnonbenzodiazepinehypnotics such asdiazepam,flunitrazepam,andzopiclone,cinazepam does not violatesleep architecture,and the continuity ofslow-wave sleepandREM sleepare 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 ofinsomniaand othersleep disorders.[2]
Cinazepam has an order of magnitude loweraffinityfor thebenzodiazepine receptorof theGABAAcomplexrelative to other well-known hypnotic benzodiazepines such asnitrazepamandphenazepam.[2]Moreover, in mice, it is rapidlymetabolized,with only 5% of the base compound remaining within 30 minutes of administration.[2]As such, cinazepam is considered to be a benzodiazepineprodrug;specifically, to3-hydroxyphenazepam,as the mainactive metabolite.[2]
See also
[edit]References
[edit]- ^Sleep Research.Vol. 26. Brain Information Service/Brain Research Institute, University of California. 1997. p. 115.
- ^abcdefSchukin SI, Zinkovsky VG, Zhuk OV (2011). "Elimination kinetics of the novel prodrug cinazepam possessing psychotropic activity in mice".Pharmacological Reports.63(5): 1093–1100.doi:10.1016/s1734-1140(11)70628-4.PMID22180351.S2CID4744087.
- ^abMakan SY, Boiko IA, Smul'skii SP, Andronati SA (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.ISSN0091-150X.S2CID24532012.
- ^abAndronati SA, Makan SY, Neshchadin DP, Yakubovskaya LN, Sava VM, Andronati KS (1998). "Bioaccessibility of cinazepam introduced as inclusion complex with β-cyclodextrin".Pharmaceutical Chemistry Journal.32(10): 513–515.doi:10.1007/BF02465736.ISSN0091-150X.S2CID26513288.
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