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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 It is an analogue of etonitazene where the 5-nitro (NO2) group has been replaced by a nitrile (C≡N) group.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] |
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] |
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] |
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] |
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] |
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, including analgesic, pain relief. The terms "opioid" and "opiate" are sometimes used interchangeably, but the term "opioid" is used to designate all substances, both natural and synthetic, that bind to opioid receptors in the brain. Opiates are alkaloid compounds naturally found in the opium poppy plant ''Papaver somniferum''. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, and Cold medicine, suppressing cough. The opioid receptor antagonist naloxone is used to reverse opioid overdose. Extremely potent opioids such as carfentanil are approved only for Veterinary medicine, veterinary use. Opioids are also frequently use ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 animals. Because it is characterized by a strong drug dependence, dependency potential and a tendency to produce profound respiratory depression, it is not used in humans. It is, however, useful in animal models for addiction studies, particularly those requiring the animals to drink or ingest the agent, because it is not as bitter as opiate salts like morphine sulfate. Synthesis Etonitazene and related nitazenes, nitazene opioids were discovered in the late 1950s, by a team of Swiss researchers working at the pharmaceutical firm CIBA (now Novartis). One of the first compounds investigated by the Swiss team was 1-(β-diethylaminoethyl)-2-benzylbenzimidazole, which was found to possess 10% of the analgesic activity of morphine when tested in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nitrile
In organic chemistry, a nitrile is any organic compound that has a functional group. The name of the compound is composed of a base, which includes the carbon of the , suffixed with "nitrile", so for example is called " propionitrile" (or propanenitrile). The prefix '' cyano-'' is used interchangeably with the term ''nitrile'' in industrial literature. Nitriles are found in many useful compounds, including methyl cyanoacrylate, used in super glue, and nitrile rubber, a nitrile-containing polymer used in latex-free laboratory and medical gloves. Nitrile rubber is also widely used as automotive and other seals since it is resistant to fuels and oils. Organic compounds containing multiple nitrile groups are known as cyanocarbons. Inorganic compounds containing the group are not called nitriles, but cyanides instead. Though both nitriles and cyanides can be derived from cyanide salts, most nitriles are not nearly as toxic. Structure and basic properties The N−C−C geom ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 3.7nM at CB2). It has been sold online as a designer drug, first being identified in Germany in December 2013. See also * AZD1940 * AZ-11713908 * BIM-018 * Etazen 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 ... * Etoacetazene References Benzimidazoles Cannabinoids Designer drugs {{cannabinoid-stub ... [...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] |
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] |
