Etonitazene 5-acetyl analogue explained
Etonitazene 5-acetyl analogue (Etoacetazene, 5-acetyldesnitroetonitazene) is a benzimidazole derivative with opioid effects, first developed in the 1950s as part of the research that led to better-known compounds such as etonitazene. It is an analogue of etonitazene where the 5-nitro (NO2) group has been replaced by an acetyl (COCH3) group.[1] [2] It is described as having "reduced but still significant" potency compared to etonitazene itself.[3] This compound was also tested as part of a series of cannabinoid receptor 2 agonists, and was found to be active though with fairly low potency of 960 nM at CB2, and negligible activity at CB1.[4]
See also
Notes and References
- Lecolier S, Trouiller G . Nouveaux benzimidazoles doués d'activité morphinique. . New benzimidazoles with opioid activity. . French . Chim. Ther. . 1967 . 2 . 16–24 .
- Sparatore F, Boido V, Fanelli F . Dialchilamminoalchilbenzimidazoli d'interesse farmacologico [Dialkylaminoalkylbenzimidazoles of pharmacological interest | trans-title = Dialkylaminoalkylbenzimidazoles of pharmacological interest | language = Italian | journal = Il Farmaco; Edizione Scientifica | volume = 23 | issue = 4 | pages = 344–59 | date = April 1968 | pmid = 5680377 | doi = | url = ].
- Web site: A review of the evidence on the use and harms of 2-benzyl benzimidazole ('nitazene') and piperidine benzimidazolone ('brorphine-like') opioids. . Advisory Council on the Misuse of Drugs . UK . July 2022 .
- Tonelli M, Cichero E, Mahmoud AM, Rabbito A, Tasso B, Fossa P, Ligresti A . Exploring the effectiveness of novel benzimidazoles as CB2 ligands: synthesis, biological evaluation, molecular docking studies and ADMET prediction . MedChemComm . 9 . 12 . 2045–2054 . December 2018 . 30647880 . 6301267 . 10.1039/c8md00461g .