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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] |
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] |
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] |
U-47700
U-47700, also known as U4, pink heroin, pinky, and pink, is an opioid analgesic drug developed by a team at Upjohn in the 1970s which has around 7.5 times the potency of morphine in animal models. U-47700 is a structural isomer of the earlier opioid AH-7921 and the result of a great deal of work elucidating the quantitative structure–activity relationship of the scaffold. Upjohn looked for the key moiety (chemistry), moieties which gave the greatest activity and posted over a dozen patents on related compounds, each optimizing one moiety until they discovered that U-47700 was the most active. U-47700 became the lead compound of selective kappa-opioid receptor ligands such as U-50488, U-51754 (containing a pyrrolidine rather than a dimethylamine substituent) and U-69,593, which share very similar structures. Although not used medically, the selective kappa ligands are used in research. Pharmacology U-47700 is an agonist of the μ-opioid receptor (Ki ) and possesses significant ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MT-45
MT-45 (IC-6) is an opioid analgesic drug invented in the 1970s by Dainippon Pharmaceutical Co. It is chemically a 1-substituted-4-(1,2-diphenylethyl) piperazine derivative, which is structurally unrelated to most other opioid drugs. Racemic MT-45 has around 80% the potency of morphine, with almost all opioid activity residing in the (S) enantiomer (the opposite stereochemistry from the related drug lefetamine). It has been used as a lead compound from which a large family of potent opioid drugs have been developed, including full agonists, partial agonists, and antagonists at the three main opioid receptor subtypes. Fluorinated derivatives of MT-45 such as 2F-MT-45 are significantly more potent as μ-opioid receptor agonists, and one of its main metabolites 1,2-diphenylethylpiperazine also blocks NMDA receptors. ] Side effects Recreational use of MT-45 has been associated with unconsciousness and overdose, as well as a range of unusual side effects not typically seen with other ... [...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] |
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] |
Abandoned Drugs
Abandon, abandoned, or abandonment may refer to: Common uses * Abandonment (emotional), a subjective emotional state in which people feel undesired, left behind, insecure, or discarded * Abandonment (legal), a legal term regarding property ** Child abandonment, the extralegal abandonment of children ** Lost, mislaid, and abandoned property, legal status of property after abandonment and rediscovery * Abandonment (mysticism) Art, entertainment, and media Film * ''Abandon'' (film), a 2002 film starring Katie Holmes * ''Abandoned'' (1949 film), starring Dennis O'Keefe * ''Abandoned'' (1955 film), the English language title of the Italian war film ''Gli Sbandati'' * ''Abandoned'' (2001 film), a Hungarian film * ''Abandoned'' (2010 film), starring Brittany Murphy * ''Abandoned'' (2015 film), a television movie about the shipwreck of the ''Rose-Noëlle'' in 1989 * ''Abandoned'' (2022 film), starring Emma Roberts * ''The Abandoned'' (1945 film), a 1945 Mexican film * ''The Aba ... [...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] |
Piperidylthiambutene
Piperidylthiambutene (Piperidinohton) is a synthetic opioid analgesic drug from the thiambutene family, which has around the same potency as morphine. Piperidylthiambutene is structurally distinct from fentanyl, its analogues, and other synthetic opioids previously reported. If sold or obtained for the purpose of human consumption it could be considered a controlled substance analogue in some countries such as the US, Australia and New Zealand. Piperidylthiambutene has been sold as a designer drug 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. ..., first appearing in late 2018. Synthesis The Grignard reaction between 3-Piperidinobutyric acid ethyl esterCID:10774378(1) and 2-Bromothiophene 003-09-4(2) gives 3. Dehydration in acid completes the synthesis. References Opioi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesic
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'' derive ... [...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] |
1971 Convention On Psychotropic Substances
The Convention on Psychotropic Substances of 1971 is a United Nations treaty designed to control psychoactive drugs such as amphetamine-type stimulants, barbiturates, benzodiazepines, and psychedelics signed in Vienna, Austria on 21 February 1971. The Single Convention on Narcotic Drugs of 1961 did not ban the many newly discovered psychotropics, since its scope was limited to drugs with Cannabis (drug), cannabis, coca and opium-like effects. During the 1960s, such recreational drug use, drugs became widely available, and government authorities opposed this for numerous reasons, arguing that along with negative health effects, drug use led to lowered moral standards. The Convention, which contains import and export restrictions and other rules aimed at limiting drug use to scientific and medical purposes, came into force on 16 August 1976. As of 2013, 183 member states of the United Nations, member states are Parties to the treaty. The treaty is not self-implementing; individu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
