Homofentanyl
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Homofentanyl
Homofentanyl (N-Phenylpropylnorfentanyl, Fentanyl propyl analogue) is an opioid derivative which has been sold as a designer drug. It is a homologue of fentanyl, with similar analgesic and sedative effects but lower potency, around 14x stronger than pethidine. See also * Acetylfentanyl * Benzylfentanyl * Butyrylfentanyl * Isofentanyl * Secofentanyl Secofentanyl is an opioid derivative which is an analogue of fentanyl where the piperidine ring has been cleaved to form an open-chain structure. It is around 40x less potent than fentanyl itself but still 5-6x the potency of morphine in animal t ... * OPPPP References Analgesics Designer drugs Opioids {{analgesic-stub ...
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Benzylfentanyl
Benzylfentanyl (R-4129) is a fentanyl analog. It was temporarily placed in the US Schedule I by emergency scheduling in 1985 due to concerns about its potential for abuse as a designer drug, but this placement was allowed to expire and benzylfentanyl was formally removed from controlled substance listing in 2010, after the DEA's testing determined it to be "essentially inactive" as an opioid. Benzylfentanyl has a Ki of 213 nM at the mu opioid receptor, binding around 1/200 as strong as fentanyl itself, though it is still slightly more potent than codeine. 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. Legal status In the United Stat ...
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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 fifteen 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 as a designer drug. 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 heroin or other opioids. Common 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 f ...
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Butyrylfentanyl
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. butyrylfentanyl > benzylfentanyl. The studies in inhibition studies on binding affinity achieved the same order of analogues. It means that butyrfentantyl is a less potent opioid-agonist than fentanyl. On the other side, during in vitro studies of cross-reactivity with the fentanyl antibody between fentanyl and the fentanyl analogs examined, revealed order: fentanyl = butyrylfentanyl > (±)-''cis''- 3-methylfentanyl > benzylfentanyl > alpha-methylfentanyl. High cross-reactivity may be the effect of the shape of the molecule - the shape of butyrfentanyl is closest to the original fentanyl molecule, which makes it easy to bind by fentanyl antibodies. ...
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Isofentanyl
Isofentanyl (3-methyl-benzylfentanyl) is an opioid analgesic that is an analog (and structural isomer) of fentanyl first invented in 1973, and which has been sold as a designer drug. 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 As a structural isomer of fentanyl itself, isofentanyl is banned under drug analogue laws in many jurisdictions around the world. In the United State ...
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Secofentanyl
Secofentanyl is an opioid derivative which is an analogue of fentanyl where the piperidine ring has been cleaved to form an open-chain structure. It is around 40x less potent than fentanyl itself but still 5-6x the potency of morphine in animal tests. See also * Benzylfentanyl * Homofentanyl * Diampromide * Isofentanyl * Phenampromide Phenampromide is an opioid analgesic from the ampromide family of drugs, related to other drugs such as propiram and diampromide. It was invented in the 1960s by American Cyanamid Co. Although never given a general release, it was trialled and ... References Analgesics Designer drugs Opioids {{analgesic-stub ...
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OPPPP
OPPPP (1-(3-Oxo-3-phenylpropyl)-4-phenyl-4-piperidinyl propionate) is an opioid drug related to medicines such as prodine. It is one of several compounds derived from MPPP, the reverse ester of pethidine, which were sold as designer drugs in the 1980s, but have been rarely encountered by law enforcement since the passage of the Federal Analogue Act in 1986. In animal studies it was found to be around 1000x the potency of pethidine, making it several times the potency of fentanyl and with similar hazards of respiratory depression and overdose. It is closely related to numerous compounds made by Janssen et al. for which the structure-activity relationship is well established. See also * Homofentanyl * PEPAP * LY-88329 LY-88329 is an opioid receptor ligand related to medicines such as pethidine. It has high affinity to the μ-opioid receptor, but unlike structurally related drugs such as 3-methylfentanyl and OPPPP, LY-88329 is a potent opioid antagonist. In ani ... References ...
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Opioid
Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid use disorder, reversing opioid overdose, and suppressing cough. Extremely potent opioids such as carfentanil are approved only for veterinary use. Opioids are also frequently used non-medically for their euphoric effects or to prevent withdrawal. Opioids can cause death and have been used for executions in the United States. Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms. The euphoria attracts recreational use, and frequent, escalating recreational use of ...
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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. Designer drugs include psychoactive substances that have been designated by the European Union as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these 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 trials, the use of some of these drugs may result i ...
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Homology (chemistry)
In chemistry, homology is the appearance of homologues. A homologue (also spelled as homolog) is a compound belonging to a series of compounds differing from each other by a repeating unit, such as a methylene bridge −−, a peptide residue, etc. A homolog is a special case of an analog. Examples are alkanes and compounds with alkyl side chains of different length (the repeating unit being a methylene group -CH2-). Periodic table On the periodic table, homologous elements share many electrochemical properties and appear in the same group (column) of the table. For example, all noble gases are colorless, monatomic gases with very low reactivity. These similarities are due to similar structure in their outer shells of valence electrons. Mendeleev used the prefix eka- for an unknown element below a known one in the same group. See also * Homologous series * Analog Analog or analogue may refer to: Computing and electronics * Analog signal, in which information is enco ...
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Fentanyl
Fentanyl, also spelled fentanil, is a very potent synthetic opioid used as a pain medication. Together with other drugs, fentanyl is used for anesthesia. It is also used illicitly as a recreational drug, sometimes mixed with heroin, cocaine, benzodiazepines or methamphetamine, among others. Its potentially deadly overdose effects can be neutralized by naloxone. Fentanyl is commonly used to create counterfeit pills disguised as OxyContin, Xanax, Adderall, among others. It has a rapid onset and its effects generally last under two hours. Medically, it is used by injection, nasal spray, or skin patch, or absorbed through the cheek as a lozenge or tablet. Common adverse effects of fentanyl include nausea, vomiting, constipation, itching, sedation, confusion, and injuries related to poor coordination. Serious adverse effects may include respiratory depression, hallucinations, serotonin syndrome, low blood pressure, or development of an opioid use disorder. Fentanyl works b ...
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Analgesic
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. 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, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing ...
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Sedative
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are CNS depressants and interact with brain activity causing its deceleration. Various kinds of sedatives can be distinguished, but the majority of them affect the neurotransmitter gamma-aminobutyric acid (GABA). In spite of the fact that each sedative acts in its own way, most produce relaxing effects by increasing GABA activity. This group is related to hypnotics. The term ''sedative'' describes drugs that serve to calm or relieve anxiety, whereas the term ''hypnotic'' describes drugs whose main purpose is to initiate, sustain, or lengthen sleep. Because these two functions frequently overlap, and because drugs in this class generally produce dose-dependent effects (ranging from anxiolysis to loss of consciousness) they are often referred to collectively as ''sedative-hypnotic'' drugs. Sedatives can be used to produce an overly-calming effect ( alcohol being the m ...
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