Difludiazepam

Difludiazepam
Difludiazepam structure.png
Identifiers
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC16H11ClF2N2O
Molar mass320.72 g·mol−1
3D model (JSmol)

Difludiazepam[1] (Ro07-4065) is a benzodiazepine derivative which is the 2',6'-difluoro derivative of fludiazepam. It was invented in the 1970s but was never marketed, and has been used as a research tool to help determine the shape and function of the GABAA receptors, at which it has an IC50 of 4.1nM.[2][3][4] Difludiazepam has subsequently been sold as a designer drug, and was first notified to the EMCDDA by Swedish authorities in 2017.[5]

See also[edit]


References[edit]

  1. ^ Maskell PD, Wilson NE. Designer Benzodiazepines: New Challenges and Treatment Options, in Corazza O, Roman-Urrestarazu. Handbook of Novel Psychoactive Substances: What Clinicians Should Know about NPS. Taylor & Francis, 2019. ISBN 978-1-138-06830-8
  2. ^ A. Winkler, David; R. Burden, Frank; Watkins, Andrew J. R. (January 1998). "Atomistic Topological Indices Applied to Benzodiazepines using Various Regression Methods". Quantitative Structure-Activity Relationships. 17 (1): 14–19. doi:10.1002/(SICI)1521-3838(199801)17:01<14::AID-QSAR14>3.0.CO;2-U.
  3. ^ So, SS; Karplus, M (1996). "Genetic neural networks for quantitative structure-activity relationships: improvements and application of benzodiazepine affinity for benzodiazepine/GABAA receptors". Journal of Medicinal Chemistry. 39 (26): 5246–5256. doi:10.1021/jm960536o. PMID 8978853.
  4. ^ Maddalena DJ, Johnston GA. Prediction of receptor properties and binding affinity of ligands to benzodiazepine/GABAA receptors using artificial neural networks. Journal of Medicinal Chemistry. 1995 Feb;38(4):715-24. doi:10.1021/jm00004a017
  5. ^ Europol 2017 Annual Report on the implementation of Council Decision 2005/387/JHA. EMCDDA, 2018