Etonitazene 5-acetyl analogue (Etoacetazene, 5-acetyldesnitroetonitazene) is a
benzimidazole
Benzimidazole is a heterocyclic aromatic organic compound. This bicyclic compound may be viewed as fused rings of the aromatic compounds benzene and imidazole. It is a white solid that appears in form of tabular crystals.
Preparation
Benzimi ...
derivative with
opioid
Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ...
effects, first developed in the 1950s as part of the research that led to better-known compounds such as
etonitazene
Etonitazene, also known as EA-4941 or CS-4640, is a List of benzimidazole opioids, benzimidazole opioid, first reported in 1957, that has been shown to have approximately 1,000 to 1,500 times the potency (pharmacology), potency of morphine in anim ...
. It is an analogue of etonitazene where the 5-nitro (NO
2) group has been replaced by an acetyl (COCH
3) group.
It is described as having "reduced but still significant" potency compared to etonitazene itself.
This compound was also tested as part of a series of
cannabinoid receptor 2
The cannabinoid receptor 2 (CB2), is a G protein-coupled receptor from the cannabinoid receptor family that in humans is encoded by the ''CNR2'' gene. It is closely related to the cannabinoid receptor 1 (CB1), which is largely responsible for ...
agonists, and was found to be active though with fairly low potency of 960 nM at CB
2, and negligible activity at CB
1.
See also
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Etocyanazene
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Etodesnitazene
Etodesnitazene (also known as desnitroetonitazene, etazen, etazene, and etazone) is a benzimidazole-derived opioid analgesic drug, which was originally developed in the late 1950s alongside etonitazene and a range of related derivatives. It is m ...
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Etomethazene
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MCHB-1
MCHB-1 is a benzimidazole derived drug which was researched as an analgesic but never developed for medical use. It acts as a potent agonist of the CB2 receptor, with an EC50 of 0.52nM at CB2, and ~30x selectivity over CB1 (Ki of 110nM at CB1 vs ...
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List of benzimidazole opioids
References
Analgesics
Designer drugs
Benzimidazole opioids
Aromatic ethers
Diethylamino compounds
Ethoxy compounds
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