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| Chemical and physical data | |
| Formula | C21H24N4O4 |
| Molar mass | 396.447 g·mol−1 |
| 3D model (JSmol) | |
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Methylenedioxynitazene (3',4'-Methylenedioxynitazene) is a benzimidazole derivative which has been sold as a designer drug over the internet and presumably has opioid effects. It is an analogue of etonitazene where the benzyl ring is substituted with a 3,4-methylenedioxy ring system rather than an ethoxy group. It was first reported in the UK in early 2024. [1]
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.
Triclabendazole, sold under the brand name Egaten among others, is a medication used to treat fascioliasis and paragonimiasis. It is very effective for both conditions. Treatment in hospital may be required. It is taken by mouth with typically one or two doses being required.
Etonitazene, also known as EA-4941 or CS-4640, is a benzimidazole opioid, first reported in 1957, that has been shown to have approximately 1,000 to 1,500 times the potency of morphine in animals.
Benzylmorphine (Peronine) is a semi-synthetic opioid narcotic introduced to the international market in 1896 and that of the United States very shortly thereafter. It is much like codeine, containing a benzyl group attached to the morphine molecule just as the methyl group creates codeine and the ethyl group creates ethylmorphine or dionine. It is about 90% as strong as codeine by weight.
DPI-221 is an opioid drug that is used in scientific research. It is a highly selective agonist for the δ-opioid receptor, which produces fewer convulsions than most drugs from this family.
These drugs are known in the UK as controlled drug, because this is the term by which the act itself refers to them. In more general terms, however, many of these drugs are also controlled by the Medicines Act 1968, there are many other drugs which are controlled by the Medicines Act but not by the Misuse of Drugs Act, and some other drugs are controlled by other laws.
MCOPPB is a drug which acts as a potent and selective agonist for the nociceptin receptor, with a pKi of 10.07 and much weaker activity at other opioid receptors. It has only moderate affinity for the mu opioid receptor, weak affinity for the kappa opioid receptor and negligible binding at the delta opioid receptor. In animal studies, MCOPPB produces potent anxiolytic effects, with no inhibition of memory or motor function, and only slight sedative side effects which do not appear until much higher doses than the effective anxiolytic dose range.
Metonitazene is an analgesic compound related to etonitazene, which was first reported in 1957, and has been shown to have approximately 1000 times the potency of morphine by central routes of administration, but if used orally it has been shown to have approximately 10 times the potency of morphine.
Isotonitazene is a benzimidazole-derived opioid analgesic drug related to etonitazene, which has been sold as a designer drug. It has only around half the potency of etonitazene in animal studies, but it is likely even less potent in humans as was seen with etonitazene. Isotonitazene was fully characterized in November 2019 in a paper where the authors performed a full analytical structure elucidation in addition to determination of the potency at the μ-opioid receptor using a biological functional assay in vitro. While isotonitazene was not compared directly to morphine in this assay, it was found to be around 2.5 times more potent than hydromorphone and slightly more potent than fentanyl.
Etodesnitazene 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 many times less potent than etonitazene itself, but still 70x more potent than morphine in animal studies. Corresponding analogues where the N,N-diethyl group is replaced by piperidine or pyrrolidine rings also retain significant activity. Etodesnitazene has been sold as a designer drug, first being identified in both Poland and Finland in March 2020.
Etonitazepyne is a benzimidazole derivative with potent opioid effects which has been sold over the internet as a designer drug and linked to numerous cases of overdose.
Etonitazepipne is a benzimidazole derivative with opioid effects around 100 times more potent than morphine, which has been sold over the internet as a designer drug.
Metodesnitazene is a benzimidazole derivative with opioid effects, though unlike related compounds such as metonitazene and etodesnitazene which are many times more potent, metodesnitazene is only around the same potency as morphine in animal studies. It was proposed by the DEA to be placed under legal control in the US in December 2021.
N-Desethylisotonitazene (norisotonitazene) is a benzimidazole opioid with potent analgesic effects which has been sold as a designer drug. It was first identified in 2023 as an active metabolite of the closely related compound isotonitazene, and was found to have similar potency. It is one of the strongest benzimidazole opioids discovered, with an analgesic strength 20 times stronger than fentanyl.
Protonitazepyne is a benzimidazole derivative with opioid effects, which has been sold as a designer drug over the internet, first being mentioned in mid 2022 and definitively identified in drug seizures in Canada in early 2023. It is an analogue of etonitazene where the ethoxy group has been extended to propoxy, and the N,N-diethyl substitution has been cyclised into a pyrrolidine ring. While formal studies into its pharmacology have yet to be carried out, it is believed to be slightly less potent than the ethoxy analogue etonitazepyne but still a potent opioid.
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. 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 agonists, and was found to be active though with fairly low potency of 960 nM at CB2, and negligible activity at CB1.
Etonitazene 5-cyano analogue (Etocyanazene, 5-cyanodesnitroetonitazene) 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 a nitrile (C≡N) group. It is described as having "reduced but still significant" potency compared to etonitazene itself. It was made illegal in Germany in July 2021.
Etoetonitazene 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 ethoxy sidechain has been extended to ethoxyethoxy. It is less potent than other benzimidazole class opioids, but is still a potent mu opioid receptor agonist with around 50x the potency of morphine, and has been sold as a designer drug since around 2022.
Flunitazene (Fluonitazene) 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 one of the least potent derivatives from this class to have appeared as a designer drug, with only around the same potency as morphine, but nevertheless has been sold since around 2020, and has been linked to numerous drug overdose cases.
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