Pyrazolam

Pyrazolam (SH-I-04)[1] is a benzodiazepine derivative originally developed by a team led by Leo Sternbach at Hoffman-La Roche in the 1970s,[2] and subsequently "rediscovered" and sold as a designer drug starting in 2012.[3][4][5][6][7]

Pyrazolam
Clinical data
Routes of
administration		Oral, Sublingual, rectal
Legal status
Legal status
Pharmacokinetic data
Elimination half-life17 hours
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC16H12BrN5
Molar mass354.211 g·mol−1
3D model (JSmol)

Pyrazolam has structural similarities to alprazolam[8] and bromazepam. Unlike other benzodiazepines, pyrazolam does not appear to undergo metabolism, instead being excreted unchanged in the urine.[3] It is most selective for the α2 and α3 subtypes of the GABAA receptor.[9]

United Kingdom

In the UK, pyrazolam has been classified as a Class C drug by section 5 of the May 2017 amendment to The Misuse of Drugs Act 1971 along with several other designer benzodiazepine drugs.[10]

See also
  • List of benzodiazepine designer drugs

References
  1. Clayton T, Poe MM, Rallapalli S, Biawat P, Savić MM, Rowlett JK, et al. (2015). "A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model". International Journal of Medicinal Chemistry. 2015: 430248. doi:10.1155/2015/430248. PMC 4657098. PMID 26682068.
  2. US 3954728, "Preparation of triazolo benzodiazepines and novel compounds"
  3. Moosmann B, Hutter M, Huppertz LM, Ferlaino S, Redlingshöfer L, Auwärter V (July 2013). "Characterization of the designer benzodiazepine pyrazolam and its detectability in human serum and urine". Forensic Toxicology. 31 (2): 263–271. doi:10.1007/s11419-013-0187-4.
  4. Moosmann B, King LA, Auwärter V (June 2015). "Designer benzodiazepines: A new challenge". World Psychiatry. 14 (2): 248. doi:10.1002/wps.20236. PMC 4471986. PMID 26043347.
  5. Pettersson Bergstrand M, Helander A, Hansson T, Beck O (April 2017). "Detectability of designer benzodiazepines in CEDIA, EMIT II Plus, HEIA, and KIMS II immunochemical screening assays". Drug Testing and Analysis. 9 (4): 640–645. doi:10.1002/dta.2003. PMID 27366870.
  6. Høiseth G, Tuv SS, Karinen R (November 2016). "Blood concentrations of new designer benzodiazepines in forensic cases". Forensic Science International. 268: 35–38. doi:10.1016/j.forsciint.2016.09.006. PMID 27685473.
  7. Manchester KR, Maskell PD, Waters L (March 2018). "a and plasma protein binding values for benzodiazepines appearing as new psychoactive substances" (PDF). Drug Testing and Analysis. 10 (8): 1258–1269. doi:10.1002/dta.2387. PMID 29582576.
  8. Hester JB, Rudzik AD, Kamdar BV (November 1971). "6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines which have central nervous system depressant activity". Journal of Medicinal Chemistry. 14 (11): 1078–81. doi:10.1021/jm00293a015. PMID 5165540.
  9. Hester JB, Von Voigtlander P (November 1979). "6-Aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines. Influence of 1-substitution on pharmacological activity". Journal of Medicinal Chemistry. 22 (11): 1390–8. doi:10.1021/jm00197a021. PMID 42799.
  10. "The Misuse of Drugs Act 1971 (Amendment) Order 2017".
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