|
Etomethazene
Etomethazene (5-methyldesnitroetonitazene, 5-methyl etodesnitazene, Eto) is a benzimidazole derivative with opioid effects which has been sold as a designer drug over the internet since 2022, first being definitively identified in Sweden in January 2023. It is an analogue of etonitazene where the nitro (NO2) group has been replaced by a methyl (CH3) group. While formal studies into its pharmacology have yet to be carried out, it showed far less potency than etonitazene itself. Etomethazene has an analgesic potency around 20 times that of morphine with a relatively short duration of about 120 min. See also * Etoacetazene * Etocyanazene * Etodesnitazene * Etonitazepyne * Isotonitazene * Metonitazene * List of benzimidazole opioids Benzimidazole opioids are a class of synthetic opioids that contain a benzimidazole core structure. The pain-relieving properties of these substances were discovered in the mid-1950s by the Swiss company Ciba AG. The most important subgroup are ... ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Benzimidazole Opioids
Benzimidazole opioids are a class of synthetic opioids that contain a benzimidazole core structure. The pain-relieving properties of these substances were discovered in the mid-1950s by the Swiss company Ciba AG. The most important subgroup are the nitazene opioids, which since 2019 have become increasingly widespread as narcotics in North America and Europe. Due to unacceptable side effects like respiratory depression, there is no medical use for benzimidazole opioids. History In 1957, the pharmaceutical research department of Ciba AG published the discovery of the (low) analgesic effect of 1-(''β''-diethylaminoethyl)-2-benzylbenzimidazole (desnitazene). Shortly afterwards, the nitazenes were discovered in structure-activity relationship studies. Structure-activity relationship The class of substances is defined chemically by the presence of the benzimidazole core structure and pharmacologically by opioid activity. The compounds are derived from the historical prototype ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzimidazole Opioids
Benzimidazole opioids are a class of synthetic opioids that contain a benzimidazole core structure. The analgesic, pain-relieving properties of these substances were discovered in the mid-1950s by the Swiss company Ciba Specialty Chemicals, Ciba AG. The most important subgroup are the nitazenes, nitazene opioids, which since 2019 have become increasingly widespread as narcotics in North America and Europe. Due to unacceptable side effects like respiratory depression, there is no medical use for benzimidazole opioids. History In 1957, the pharmaceutical research department of Ciba AG published the discovery of the (low) analgesic effect of 1-(''β''-diethylaminoethyl)-2-benzylbenzimidazole (desnitazene). Shortly afterwards, the nitazenes were discovered in structure-activity relationship studies. Structure-activity relationship The class of substances is defined chemically by the presence of the benzimidazole core structure and pharmacologically by opioid activity. The compound ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Etoacetazene
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. See also * Etocyanazene * Etodesnitazene * Etomethazene * 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 ... * List of benzimidazole opioids Re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Etocyanazene
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. See also * Etoacetazene * Etodesnitazene * Etomethazene * MCHB-1 * List of benzimidazole opioids Benzimidazole opioids are a class of synthetic opioids that contain a benzimidazole core structure. The pain-relieving properties of these substances were discovered in the mid-1950s by the Swiss company Ciba AG. The most important subgroup are ... References Analgesics Designer drugs Benzimidazole opioids Aromatic ethers Diethylamino compounds Ethoxy compounds {{Analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 many times less potent than etonitazene itself, but still 70 times 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 (10 times and 20 times morphine, respectively). Etodesnitazene has been sold as a designer drug, first being identified in both Poland and Finland in March 2020. See also * Brorphine * Etonitazepyne * Etoacetazene * Etocyanazene * Etomethazene * Isotonitazene Isotonitazene is a synthetic opioid analgesic drug from the nitazene class and structural homolog of etonitazene, which has been sold as a designer drug. It has only around half the potency of etonitazene in animal studies, but ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 Benzimidazole was discovered during research on vitamin B12. The benzimidazole nucleus was found to be a stable platform on which drugs could be developed. Benzimidazole is produced by Condensation reaction, condensation of o-phenylenediamine with formic acid, or the equivalent trimethyl orthoformate: :C6H4(NH2)2 + HC(OCH3)3 → C6H4N(NH)CH + 3 CH3OH 2-Substituted derivatives are obtained when the condensation is conducted with aldehydes in place of formic acid, followed by oxidation. Reactions Benzimidazole is a Base (chemistry), base: :C6H4N(NH)CH + H+ → [C6H4(NH)2CH]+ It can also be deprotonated with stronger bases: :C6H4N(NH)CH + LiH → Li [C6H4N2CH] + H2 The imine can be alkylated and also serves as a ligand in coordinati ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aromatic Ethers
In organic chemistry, aromaticity is a chemical property describing the way in which a conjugated ring of unsaturated bonds, lone pairs, or empty orbitals exhibits a stabilization stronger than would be expected from conjugation alone. The earliest use of the term was in an article by August Wilhelm Hofmann in 1855. There is no general relationship between aromaticity as a chemical property and the olfactory properties of such compounds. Aromaticity can also be considered a manifestation of cyclic delocalization and of resonance. This is usually considered to be because electrons are free to cycle around circular arrangements of atoms that are alternately single- and double- bonded to one another. This commonly seen model of aromatic rings, namely the idea that benzene was formed from a six-membered carbon ring with alternating single and double bonds (cyclohexatriene), was developed by Kekulé (see History section below). Each bond may be seen as a hybrid of a single bond a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Designer Drugs
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Designer drugs include psychoactive substances that have been designated by the European Union, Australia, and New Zealand, as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these designer drugs were originally synthesized by academic or industrial researchers in an effort to discover more potent derivatives with fewer side effects and shorter duration (and possibly also because it is easier to apply for patents for new molecules) and were later co-opted for recreational use. Other designer drugs were prepared for the first time in clandestine laboratories. Because the efficacy and safety of these substances have not been thoroughly evaluated in animal and human tr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesics
An analgesic drug, also called simply an analgesic, antalgic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, recent research has suggested that classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants may be considered as an alternative. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing to the substantial risks and high chances of overdose, misuse, and addiction in the absence of medical supervision. Etymology The word ''analgesic'' derives ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Etonitazepyne
Etonitazepyne (''N''-pyrrolidino etonitazene) 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. See also * Etazene * Etonitazene * Etonitazepipne * Isotonitazene * Metonitazene Metonitazene is an analgesic compound related to etonitazene, which was first reported in 1957, and has been shown to have approximately 100 times the potency of morphine by central routes of administration, but if used orally it has been shown t ... * Protonitazepyne References Analgesics Designer drugs Benzimidazole opioids Nitroarenes 1-Pyrrolidinyl compounds {{Analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metonitazene
Metonitazene is an analgesic compound related to etonitazene, which was first reported in 1957, and has been shown to have approximately 100 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. Its effects are similar to other opioids such as fentanyl and heroin, including analgesia, euphoria, and sleepiness. Adverse effects include vomiting, and respiratory depression that can potentially be fatal. Because of high dependency potential and dangerous adverse effects it has never been introduced into pharmacotherapy. It is instead commonly used in the illicit manufacture of counterfeit oxycodone opioid pills. Legal status In the United States, metonitazene is a Schedule I controlled substance under the Controlled Substances Act. Metonitazene is not controlled under the 1971 Convention on Psychotropic Substances; however, in many countries possession or intent to sell for hum ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isotonitazene
Isotonitazene is a synthetic opioid analgesic drug from the nitazene class and structural homolog of 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 (1000 times as potent as morphine in animal models yet only 60 times as potent in humans). Isotonitazene (obtained from an online vendor) 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. Side effects Side effects of benzimidazole derived opioids are likely to be similar to those of fentanyl, which include itching, nause ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
