Etonitazene_5-acetyl_analogue

Etonitazene 5-acetyl analogue

Etonitazene 5-acetyl analogue

Chemical compound

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 It is an analogue of etonitazene where the 5-nitro (NO2) group has been replaced by an acetyl (COCH3) group.[1][2] It is described as having "reduced but still significant" potency compared to etonitazene itself.[3] This compound was also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]

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See also

References

  1. [1]
    Lecolier S, Trouiller G (1967). "Nouveaux benzimidazoles doués d'activité morphinique" [New benzimidazoles with opioid activity.]. Chim. Ther. (in French). 2: 16–24.
  2. [2]
    Sparatore F, Boido V, Fanelli F (April 1968). "Dialchilamminoalchilbenzimidazoli d'interesse farmacologico [Dialkylaminoalkylbenzimidazoles of pharmacological interest" [Dialkylaminoalkylbenzimidazoles of pharmacological interest]. Il Farmaco; Edizione Scientifica (in Italian). 23 (4): 344–59. PMID 5680377.
  3. [3]
    "A review of the evidence on the use and harms of 2-benzyl benzimidazole ('nitazene') and piperidine benzimidazolone ('brorphine-like') opioids" (PDF). UK: Advisory Council on the Misuse of Drugs. July 2022.
  4. [4]
    Tonelli M, Cichero E, Mahmoud AM, Rabbito A, Tasso B, Fossa P, Ligresti A (December 2018). "Exploring the effectiveness of novel benzimidazoles as CB2 ligands: synthesis, biological evaluation, molecular docking studies and ADMET prediction". MedChemComm. 9 (12): 2045–2054. doi:10.1039/c8md00461g. PMC 6301267. PMID 30647880.



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