Diclazepam

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Structural formula
Structural formula of diclazepam
General
Non-proprietary name Diclazepam
other names
  • Chlordiazepam
  • 2'-chlordiazepam
  • 7-chloro-5- (2-chlorophenyl) -1,3-dihydro-1-methyl-2 H -1,4-benzodiazepin-2-one
Molecular formula C 16 H 12 Cl 2 N 2 O
External identifiers / databases
CAS number 2894-68-0
PubChem 76168
Wikidata Q15408412
Drug information
Drug class
properties
Molar mass 318.03 g · mol -1
Physical state

firmly

safety instructions
GHS hazard labeling
no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Diclazepam (2'-Chlordiazepam) is a chemical compound from the group of benzodiazepines and works in a similar way to diazepam .

discovery

Diclazepam was first synthesized in 1960 by a collective led by Leo Sternbach at Hoffmann-La Roche . The effect is similar to that of other benzodiazepines: it has an anti-anxiety, anticonvulsant, hypnotic , calming, muscle-relaxing and amnesic effect .

It is estimated that the effect of 1 mg diclazepam is roughly equivalent to that of 5–10 mg diazepam.

Legal position

In Germany, diclazepam was made subject to the BtMG in Annex II as a marketable but not a prescription substance with the 30th ordinance amending the narcotics regulations of November 11, 2015 .

See also

literature

  • Bjoern Moosmann, Philippe Bisel, Volker Auwärter: Characterization of the designer benzodiazepine diclazepam and preliminary data on its metabolism and pharmacokinetics. In: Drug Testing and Analysis . 2014, doi : 10.1002 / dta.1628
  • Lauren C. O'Connor, Hazel J. Torrance, Denise A. McKeown: ELISA Detection of Phenazepam, Etizolam, Pyrazolam, Flubromazepam, Diclazepam and Delorazepam in Blood Using Immunalysis® Benzodiazepine Kit. In: Journal of Analytical Toxicology. , S. bkv122, doi : 10.1093 / jat / bkv122 .

Individual evidence

  1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
  2. ↑ US Patent 3136815 - Amino substituted benzophenone oximes and derivatives thereof.
  3. ↑ Yakubovs'ka et al .: Dopovidi Akademii Nauk Ukrains'koi. RSR, Seriya B: Geologichni, Khimichni ta Biologichni Nauki , 1977, p. 819.
  4. ↑ M. Babbini, M. Gaiardi, M. Bartoletti: anxiolytic versus sedative properties in the benzodiazepines series: differencies in structure - activity relationships. In: Life Sciences. 25, 1979, p. 15, doi : 10.1016 / 0024-3205 (79) 90484-3 .
  5. ↑ " Regarding the potency of this new drug, only limited data can be found in the literature. One study conducted by Babbini et al. showed that diclazepam is approximately 4–8 times more potent than diazepam in terms of reducing motor activity and conflict behavior in rats and studies carried out by Sternbach et al. found diclazepam to be approximately equally potent as diazepam with regard to muscle relaxant and sedative effects in mice and twice as potent than diazepam investigating the same effects in cats. The Ki value at recombinant wild-type α1β2γ2 γ-aminobutyric acid (GABAA) receptors demonstrated a 30 times higher binding affinity for diclazepam than for diazepam. However, Bradley et al. found that diclazepam given in the same doses as diazepam showed no differences in effects on the behavioral activity of monkeys. "
    • Bjoern Moosmann, Philippe Bisel, Volker Auwärter: Characterization of the designer benzodiazepine diclazepam and preliminary data on its metabolism and pharmacokinetics. In: Drug Testing and Analysis. 6, 2014, p. 757, doi : 10.1002 / dta.1628 .
  6. ↑ Thirtieth ordinance amending the provisions of the law on narcotics, printed matter 399/15 (PDF file)