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Open Access Articles- Top Results for Cinazepam

Cinazepam

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Cinazepam
File:Cinazepam.svg
Systematic (IUPAC) name
4-{[7-Bromo-5-(2-chlorophenyl)-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]oxy}-4-oxobutanoic acid
Clinical data
Identifiers
172986-25-3
None
PubChem CID 629281
ChemSpider 546502
Chemical data
Formula C19H14BrClN2O5
465.682 g/mol

Cinazepam (BD-798) is an atypical benzodiazepine derivative which was never marketed.[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

  1. Sleep Research. Brain Information Service/Brain Research Institute, University of California. 1997. 
  2. 2.0 2.1 2.2 2.3 2.4 2.5 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. PMID 22180351. 
  3. 3.0 3.1 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. ISSN 0091-150X. doi:10.1007/s11094-007-0055-9. 
  4. 4.0 4.1 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. ISSN 0091-150X. doi:10.1007/BF02465736. 



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