Bromazolam

From Wikipedia, the free encyclopedia
Jump to navigation Jump to search
Bromazolam
Bromazolam structure.png
Identifiers
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC17H13BrN4
Molar mass353.223 g·mol−1
3D model (JSmol)

Bromazolam (XLI-268) is a benzodiazepine derivative which was first synthesised in 1976, but was never marketed.[1] It has subsequently been sold as a designer drug, first being definitively identified by the EMCDDA in Sweden in 2016.[2] It is the bromo instead of chloro analogue of alprazolam, and has similar sedative and anxiolytic effects.[3][4] Bromazolam is a non subtype selective agonist at the benzodiazepine site of GABAA receptors, with a binding affinity of 2.81nM at the α1 subtype, 0.69nM at α2 and 0.62nM at α5.[5]


See also[edit]


References[edit]

  1. ^ Manchester KR, et al. The emergence of new psychoactive substance (NPS) benzodiazepines: A review. Drug Testing and Analysis 2017 May; 10(1):1-17. doi:10.1002/dta.2211
  2. ^ Europol 2016 Annual Report on the implementation of Council Decision 2005/387/JHA. EMCDDA, 2017
  3. ^ Waters L, Manchester KR, Maskell PD, Haegeman C, Haider S. The use of a quantitative structure-activity relationship (QSAR) model to predict GABA-A receptor binding of newly emerging benzodiazepines. Science and Justice. 2018 Jan 8. doi:10.1016/j.scijus.2017.12.004
  4. ^ Zawilska JB, Wojcieszak J. An expanding world of New Psychoactive Substances – Designer benzodiazepines. NeuroToxicology 2019 July; 73: 8-16. doi:10.1016/j.neuro.2019.02.015
  5. ^ Clayton T, et al. A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model. Int J Med Chem. 2015; 2015: 430248. doi:10.1155/2015/430248 PMID 26682068