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Bucinnazine
Bucinnazine (AP-237, 1-butyryl-4-cinnamylpiperazine) is an opioid analgesic drug that was widely used in China to treat pain in cancer patients as of 1986. It is one of the most potent compounds among a series of piperazine-amides first synthesized and reported in Japan in the 1970s. Bucinnazine has analgesic potency comparable to that of morphine, but with a relatively higher therapeutic index. The drug was initially claimed to be a non-narcotic analgesic. However, subsequent studies have shown bucinnazine and similar acyl piperazines to be potent and selective agonists of μ-opioid receptor (MOR) with relatively low affinity for the δ-opioid receptor and the κ-opioid receptor. In accordance with these studies, results from the Intravenous therapy, intravenous self-administration experiments in rats showed that bucinnazine has a marked reinforcing effect with Drug tolerance, tolerance and Substance dependence, dependence quickly developing. In addition, the opioid receptor ant ...
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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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Sunifiram
Sunifiram (developmental code name DM-235) is an experimental drug which has antiamnesic effects in animal studies and with significantly higher potency than piracetam. Sunifiram is a molecular simplification of unifiram (DM-232). Another analogue is sapunifiram (MN-19). As of 2016, sunifiram had not been subjected to toxicology testing, nor to any human clinical trials, and is not approved for use anywhere in the world. Pharmacology The mechanism of action of sunifiram is unknown. Sunifiram, as well as unifiram, were assayed at a wide panel of sites, including the most important receptors, ion channels, and transporters, but showed no affinity for any of the sites. They specifically did not bind to the glutamate, GABA, serotonin, dopamine, adrenergic, histamine, acetylcholine, or opioid receptors at concentrations of up to 1 μM. In addition, the drugs were tested on recombinant AMPA receptors and showed no potentiation of the receptors, indicating that they do not act a ...
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Diphenpipenol
Diphenpipenol 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 related to compounds such as MT-45 and AD-1211, but diphenpipenol is the most potent compound in the series, with the more active ''(S)'' enantiomer being around 105 times the potency of morphine in animal studies. This makes it a similar strength to fentanyl and its analogues, and consequently diphenpipenol can be expected to pose a significant risk of producing life-threatening respiratory depression, as well as other typical opioid side effects such as sedation, itching, nausea and vomiting. Diphenpipenol has been offered for sale online as a designer drug, though analysis of a sample of supposed diphenpipenol found it to instead contain a structural isomer with much weaker opioid activity, and it is unclear if genuine diphenpipenol has actually been sold. See also * 3C-PEP * Azaprocin * Bucinnazine * D ...
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Substance Dependence
Substance dependence, also known as drug dependence, is a biopsychological situation whereby an individual's functionality is dependent on the necessitated re-consumption of a psychoactive substance because of an adaptive state that has developed within the individual from psychoactive substance consumption that results in the experience of withdrawal and that necessitates the re-consumption of the drug. A ''drug addiction'', a distinct concept from substance dependence, is defined as compulsive, out-of-control drug use, despite negative consequences. An ''addictive drug'' is a drug which is both rewarding and reinforcing. ΔFosB, a gene transcription factor, is now known to be a critical component and common factor in the development of virtually all forms of behavioral and drug addictions, but not dependence. The International Classification of Diseases classifies substance dependence as a mental and behavioural disorder. In the ''Diagnostic and Statistical Manual of ...
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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 ...
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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 ...
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Azaprocin
Azaprocin is a drug which is an opioid analgesic with approximately ten times the potency of morphine Morphine, formerly also called morphia, is an opiate that is found naturally in opium, a dark brown resin produced by drying the latex of opium poppies (''Papaver somniferum''). It is mainly used as an analgesic (pain medication). There are ..., and a fast onset and short duration of action. It was discovered in 1963, but has never been marketed. The derivative substituted on the phenyl ring with a p-nitro group is more potent than the parent compound, around 25× the potency of morphine. The ring-opened 2,6-dimethylpiperazine analogues are also active, and a large family of opioid analgesic compounds derived from this parent structure have been developed over the last 40 years. One analogue, AP-237, has been used in China to treat the pain caused by cancer. References {{Opioidergics Synthetic opioids Propionamides Alkene derivatives Piperazines Mu-opioid rece ...
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AP-238
AP-238 is an opioid designer drug related to drugs such as azaprocin and bucinnazine, with around the same potency as morphine. It was first discovered in Italy in the 1960s but was never marketed, subsequently appearing on the illicit market around 2020 and being detected in both Slovenia and the USA. See also * 2F-Viminol * Diphenpipenol * Dipyanone * Etodesnitazene * MT-45 * Nortilidine * O-AMKD * O-DSMT * Piperidylthiambutene * SHR9352 SHR9352 is a drug which acts as a potent and selective biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment. It was structurally derived from oliceridine by replaci ... References Synthetic opioids Piperazines Mu-opioid receptor agonists {{analgesic-stub ...
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List Of United States Federal Prisons
The Federal Bureau of Prisons classifies prisons into seven categories: * United States penitentiaries * Federal correctional institutions * Private correctional institutions * Federal prison camps * Administrative facilities * Federal correctional complexes *Former Federal facilities This list does not include List of U.S. military prisons, military prisons, halfway houses, or prisons, jails, and other facilities operated by state or local governments that contract with the Federal Bureau of Prisons. It also does not include facilities operated by Immigration and Customs Enforcement (ICE). United States penitentiaries Most United States penitentiaries (USPs) are high-security facilities, which have highly secured perimeters with walls or reinforced fences, multiple and single-occupant cell housing, the highest staff-to-inmate ratio, and close control of inmate movement. The most restrictive facility in the federal prison system is USP Florence ADMAX, the federal supermax pri ...
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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, 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 ...
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