Furanylfentanyl
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Furanylfentanyl
Furanylfentanyl (Fu-F) is an opioid analgesic that is an analog of fentanyl and has been sold as a designer drug. It has an ED50 value of 0.02 mg/kg in mice. Research done in the 1980's showed that in humans furanylfentanyl is 50-100 times more potent than morphine, making it roughly half as potent as fentanyl, toxicology reports seem to confirm this finding after furanylfentanyl began appearing on the illicit drug market in 2015. Side effects Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear. Life-threatening adverse reactions caused by furanylfentanyl use have been observed in Sweden and Canada. At least seven deaths in Cook C ...
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List Of Fentanyl Analogues
The following is a list of fentanyl Structural analog, analogues (sometimes referred to as fentalogs), and includes both compounds developed by pharmaceutical companies for legitimate medical use, and those which have been sold as designer drugs. The latter have been reported to national drug control agencies such as the Drug Enforcement Administration, DEA, and some to transnational agencies such as the EMCDDA and UNODC. This is not a comprehensive or exhaustive list of fentanyl analogues, as more than 1400 compounds from this family have been described in the scientific and patent literature. However, this list does include many notable compounds that have reached late-stage human clinical trials, and compounds which have been sold as designer drugs, as well as representative examples of significant structural variations reported in the scientific and patent literature. The structural variations among fentanyl analogues can impart profound pharmacological differences between each ...
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Acrylfentanyl
Acrylfentanyl (also known as acryloylfentanyl) is a highly potent opioid analgesic that is an analog of fentanyl and has been sold online as a designer drug. In animal studies the IC50 (the half maximal inhibitory concentration for acrylfentanyl to displace naloxone) is 1.4 nM, being slightly more potent than fentanyl itself (1.6 nM) as well as having a longer duration of action. Side effects Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear. As acrylamide derivatives are often used in drug discovery to make covalent inhibitors which will bind irreversibly to its target, acrylfentanyl is claimed to be naloxone resistant. H ...
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4-Fluorofentanyl
Parafluorofentanyl (4-fluorofentanyl, pFF) is an opioid analgesic analogue of fentanyl developed by Janssen Pharmaceuticals in the 1960s. 4-Fluorofentanyl was sold briefly on the US black market in the early 1980s, before the introduction of the Federal Analog Act which for the first time attempted to control entire families of drugs based on their structural similarity rather than scheduling each drug individually as they appeared. 4-Fluorofentanyl is made by the same synthetic route as fentanyl, but by substituting para-fluoroaniline for aniline in the synthesis. Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea, and potentially serious respiratory depression, which can be life-threatening. Fentanyl analogs have killed thousands of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear. In 2020, the Drug E ...
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Mirfentanil
Mirfentanil is a fentanyl derivative with strong selectivity for the μ opioid receptor. At lower doses, it antagonizes the analgesic effects of alfentanil and substitutes for naloxone in morphine-treated monkeys; however, it also reverses naloxone-precipitated withdrawal in pigeons trained to discriminate morphine from naloxone. At high doses, it exhibits analgesic activity which is not fully reversed by opioid antagonists, suggesting that the drug has both opioid and non-opioid mechanisms of action. Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear. Synthesis Mirfentanil was synthesized via acylation of the product of the reaction ...
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Butyrfentanyl
Butyrfentanyl or butyrylfentanyl is a potent short-acting synthetic opioid analgesic drug. It is an analog of fentanyl with around one quarter of its potency. One of the first mentions of this drug can be found in document written by The College on Problem of Drug Dependence, where it is mentioned as ''N''-butyramide fentanyl analog., Foreword to the Drug Evaluation Committee (DEC) Analgesic, Stimulant, and Depressant Drug Indices This document also states that the article describing its clinical effects (analgesic studies, μ-, δ-, κ-opioid receptor binding, and ''in vitro'' measures of drug efficacy, antinociceptive, and narcotic properties) was published in 1987. It is an agonist for the μ-opioid receptors. Butyrfentanyl has no current legitimate clinical applications; however, it is being sold as a designer drug. Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea, and potentially serious respiratory depression which c ...
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Benzoylfentanyl
Benzoylfentanyl, also known as phenylfentanyl, is an opioid analgesic that is an analog of fentanyl and has been sold as a designer drug. In the United States, benzoylfentanyl was first identified in Drug Enforcement Administration drug seizures in 2018. Side effects Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear. A new wave of fentanyl analogues and associated deaths began in around 2014 in the US, and have continued to grow in prevalence; especially since 2016 these drugs have been responsible for hundreds of overdose deaths every week. Legal status In the United States, fentanyl-related substances are Schedule I controlled s ...
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Acetylfentanyl
Acetylfentanyl (acetyl fentanyl) is an opioid analgesic drug that is an analog of fentanyl. Studies have estimated acetylfentanyl to be 15 times more potent than morphine, which would mean that despite being somewhat weaker than fentanyl, it is nevertheless still several times stronger than pure heroin. It has never been licensed for medical use and instead has only been sold on the illicit drug market. Acetylfentanyl was discovered at the same time as fentanyl itself and had only rarely been encountered on the illicit market in the late 1980s. However, in 2013, Canadian police seized 3 kilograms of acetylfentanyl. As a μ-opioid receptor agonist, acetylfentanyl may serve as a direct substitute for oxycodone, heroin or other opioids. Common side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea, and potentially fatal respiratory depression. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet rep ...
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3-Methylbutyrfentanyl
3-Methylbutyrfentanyl (3-MBF) is an opioid analgesic that is an analog of butyrfentanyl. Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear. See also * 3-Methylfentanyl * 4-Fluorobutyrfentanyl * 4-Fluorofentanyl * α-Methylfentanyl * Acetylfentanyl * Furanylfentanyl * List of fentanyl analogues The following is a list of fentanyl Structural analog, analogues (sometimes referred to as fentalogs), and includes both compounds developed by pharmaceutical companies for legitimate medical use, and those which have been sold as designer drugs. ... References Synthetic opioids Piperidines Propionamides Anilides Mu-opioid recep ...
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α-Methylfentanyl
α-Methylfentanyl (or ''alpha''-Methylfentanyl, α-MF) an opioid analgesic that is an analog of fentanyl. It is sometimes sold as "China White". History α-Methylfentanyl was discovered by a team at Janssen Pharmaceutica in the 1960s. In 1976, it began to appear mixed with heroin, as an additive, and the mixture was sometimes also called "China White". It was first identified in the bodies of two drug overdose victims in Orange County, California, in December 1979, who appeared to have died from opiate overdose but tested negative for any known drugs of this type. Over the next year, there were 13 more deaths, and eventually the responsible agent was identified as α-methylfentanyl. α-Methylfentanyl was placed on the U.S. Schedule I list in September 1981, only two years after its appearance on the street, but already other fentanyl analogs were being developed. Following the appearance of α-methylfentanyl on the market, dozens of new fentanyl analogs have been reported, ...
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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 ...
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Piperidines
Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic compound, heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). It is a colorless liquid with an odor described as objectionable, typical of amines. The name comes from the genus name ''Piper (genus), Piper'', which is the Latin word for Black pepper, pepper. Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids, such as natural-occurring Solenopsin, solenopsins. Production Piperidine was first reported in 1850 by the Scottish chemist Thomas Anderson (chemist), Thomas Anderson and again, independently, in 1852 by the French chemist Auguste André Thomas Cahours, Auguste Cahours, who named it. Both of them obtained piperidine by reacting piperine with nitric acid. Industrially, piperidine is produced by the hydrogenation of p ...
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