|Systematic (IUPAC) name|
|Biological half-life||~42 hours|
|Molar mass||319.185 g/mol|
|(what is this?)|
Diclazepam (Ro5-3448), also known as chlorodiazepam and 2'-chloro-diazepam, is a benzodiazepine designer drug and functional analog of diazepam. It was first synthesized by Leo Sternbach and his team at Hoffman-La Roche in 1960. It is not currently approved for use as a medication, but rather sold as a designer drug. Efficacy and safety have not been tested in humans.
Metabolism of this compound has been assessed, revealing diclazepam has an approximate elimination half-life of 42 hours and undergoes N-demethylation to delorazepam, which can be detected in urine for 6 days following administration of the parent compound. Other metabolites detected were lorazepam and lormetazepam which were detectable in urine for 19 and 11 days, respectively, indicating hydroxylation by cytochrome P450 enzymes occurring concurrently with N-demethylation. The protein-binding of this compound has not been analysed but the figures for the metabolites are, delorazepam >90%, lorazepam 91.5% (parenterally) & 85% (orally) and delorazepam >90%.
- Delorazepam (Nordiclazepam)
- Ro5-4864 (4'-Chlorodiazepam)
- Moosmann B, Bisel P, Auwärter V (July–August 2014). "Characterization of the designer benzodiazepine diclazepam and preliminary data on its metabolism and pharmacokinetics". Drug Testing and Analysis 6 (7-8): 757–63. doi:10.1002/dta.1628. PMID 24604775.
- US 3136815, "Amino substituted benzophenone oximes and derivatives thereof"
- Madeleine Pettersson Bergstrand; Anders Helander; Therese Hansson; Olof Beck (2016). "Detectability of designer benzodiazepines in CEDIA, EMIT II Plus, HEIA, and KIMS II immunochemical screening assays". Drug Testing and Analysis. doi:10.1002/dta.2003. PMID 27366870.
- Bareggi SR, Truci G, Leva S, Zecca L, Pirola R, Smirne S (1988). "Pharmacokinetics and bioavailability of intravenous and oral chlordesmethyldiazepam in humans". European Journal of Clinical Pharmacology 34 (1): 109–112. doi:10.1007/bf01061430. PMID 2896126.