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Nitazene
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] |
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] |
Nitazenes
Nitazenes are a chemically defined class of substances derived from the parent compound nitazene. Nitazenes were developed in the second half of the 1950s by the Swiss Ciba AG as pain-relieving agents. They are important as centrally active, selective μ-opioid receptor agonists. The high potency of fentanyl (in humans) is matched by only a few nitazenes and surpassed by etonitazene and isotonitazene. Due to unacceptable side effects, nitazenes were never included in the pharmacopoeia of human or veterinary medicine. Since 2019, highly potent nitazenes have proliferated as ″new synthetic opioids″ in the North American and European narcotics markets and as such have become a formative component of the opioid epidemic in the United States. Overdoses of nitazene opioids have led to several hundred documented fatalities. History In the mid-1950s, the pharmaceutical research department of the Ciba AG discovered the (low) analgesic effect of 1-(''β''-diethylaminoethyl)-2-benzyl ... [...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] |
Protonitazene
Protonitazene is a benzimidazole derivative with potent opioid effects which has been sold over the internet as a designer drug since 2019, and has been identified in various European countries, as well as Canada, the US and Australia. It has been linked to numerous cases of drug overdose, and is a Schedule I drug in the US. It was developed by a Swiss pharmaceutical company in the 1950s as an alternative to morphine, but was never adopted due to severe side effects. See also * 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 ... * Isotonitazene * Metonitazene * Secbutonitazene References Analgesics Designer drugs Benzimidazole opioids Nitroarenes {{Analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Butonitazene
Butonitazene is a benzimidazole derivative with opioid effects, which has been sold over the internet as a designer drug. It has relatively low potency compared to many related compounds, and has generally been encountered as a component of mixtures with other substances rather than in its pure form. However, it is still several times the potency of morphine and has been implicated in several cases of drug overdose. Butonitazene is a Schedule I drug in the US, along with several related compounds. See also * Etonitazene * Isotonitazene * Metonitazene * Protonitazene Protonitazene is a benzimidazole derivative with potent opioid effects which has been sold over the internet as a designer drug since 2019, and has been identified in various European countries, as well as Canada, the US and Australia. It has bee ... * Secbutonitazene References Analgesics Designer drugs Benzimidazole opioids Nitroarenes Ethers Tertiary amines {{Analgesic-stub ... [...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] |
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] |
Metodesnitazene
Metodesnitazene (also known as Metazene) is a benzimidazole derivative with opioid effects, though unlike related compounds such as metonitazene and etodesnitazene which are quite potent, metodesnitazene is only around the same potency as morphine in animal studies. It is illegal in both the US and UK. See also * Etonitazepyne * 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 eve ... * List of benzimidazole opioids References Analgesics Designer drugs Benzimidazole opioids Aromatic ethers {{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] |
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] |
