Cinazepam

The following article will address the topic of Cinazepam, which has currently generated great interest and debate. For a long time, Cinazepam has been the subject of study and analysis by experts in the area, and its impact has reached various spheres of society. On this occasion, we will seek to thoroughly analyze the most relevant aspects of Cinazepam, as well as address different perspectives that allow us to understand its importance and impact. Through a detailed and rigorous analysis, it is intended to offer a comprehensive view of Cinazepam, in order to provide the reader with a broad and complete understanding of this topic.

Cinazepam
Clinical data
ATC code
  • None
Identifiers
  • 4-{oxy}-4-oxobutanoic acid
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC19H14BrClN2O5
Molar mass465.68 g·mol−1
3D model (JSmol)
  • c1ccc(c(c1)C2=NC(C(=O)Nc3c2cc(cc3)Br)OC(=O)CCC(=O)O)Cl
  • InChI=1S/C19H14BrClN2O5/c20-10-5-6-14-12(9-10)17(11-3-1-2-4-13(11)21)23-19(18(27)22-14)28-16(26)8-7-15(24)25/h1-6,9,19H,7-8H2,(H,22,27)(H,24,25)
  • Key:NQTRBZXDWMDXAQ-UHFFFAOYSA-N

Cinazepam (BD-798, sold under brand name Levana) is an atypical benzodiazepine derivative. 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 GABAA 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.

See also

References

  1. ^ Sleep Research. Vol. 26. Brain Information Service/Brain Research Institute, University of California. 1997. p. 115.
  2. ^ a b c d e f Schukin 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. PMID 22180351. S2CID 4744087.
  3. ^ a b Makan 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. ISSN 0091-150X. S2CID 24532012.
  4. ^ a b Andronati 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. ISSN 0091-150X. S2CID 26513288.
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