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Azaperone
Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine. It is uncommonly used in humans as an antipsychotic drug. Azaperone acts primarily as a dopamine antagonist (pharmacology), antagonist but also has some histamine, antihistaminic and choline, anticholinergic properties as seen with similar drugs such as haloperidol. Azaperone may cause hypotension and while it has minimal effects on respiration in pigs, high doses in humans can cause respiratory depression. Veterinary use The most common use for azaperone is in relatively small doses as a "serenic" (to reduce aggression) in farmed pigs, either to stop them fighting or to encourage sows to accept piglets. Higher doses are used for anesthesia in combination with other drugs such as xylazine, tiletamine and zolazepam. Azaperone is also used in combination with strong narcotics such as etorphine or carfentanil ...
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Azaperone Synthesis
Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine. It is uncommonly used in humans as an antipsychotic drug. Azaperone acts primarily as a dopamine antagonist (pharmacology), antagonist but also has some histamine, antihistaminic and choline, anticholinergic properties as seen with similar drugs such as haloperidol. Azaperone may cause hypotension and while it has minimal effects on respiration in pigs, high doses in humans can cause respiratory depression. Veterinary use The most common use for azaperone is in relatively small doses as a "serenic" (to reduce aggression) in farmed pigs, either to stop them fighting or to encourage sows to accept piglets. Higher doses are used for anesthesia in combination with other drugs such as xylazine, tiletamine and zolazepam. Azaperone is also used in combination with strong narcotics such as etorphine or carfentanil ...
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Fluanisone
Fluanisone is a typical antipsychotic and sedative of the butyrophenone chemical class. It is used in the treatment of schizophrenia and mania. It is also a component (along with fentanyl) of the injectable veterinary formulation fentanyl/fluanisone (Hypnorm) where it is used for rodent analgesia during short surgical procedures. See also * Enciprazine * BMY-14802 * Azaperone Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine. It is uncommonly used in humans as an antipsychotic drug. Azaperone acts ... References Butyrophenone antipsychotics Fluoroarenes Phenol ethers Piperazines Phenylpiperazines Typical antipsychotics {{nervous-system-drug-stub ...
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Pyridinylpiperazine
1-(2-Pyridinyl)piperazine is a chemical compound and piperazine derivative. Some derivatives of this substance are known to act as potent and selective α2-adrenergic receptor antagonists, such as 1-(3-fluoro-2-pyridinyl)piperazine. A few pyridinylpiperazine derivatives are drugs, including: * ABT-724 AR234960* Azaperol 804-05-9* Azaperone — antipsychotic * Atevirdine — antiretroviral BRN 0563047 9215-20-2"''Stimulating dopaminerginic activity''": Journal Ref (Cmp XVIII): * CP-226,269 * Delavirdine — antiretroviral * Mirtazapine — antidepressant MLS1547 15698-36-3Revenast 5673-87-6UMB38ref> XH-148 See also * Diphenylmethylpiperazine * Benzylpiperazine * Phenylpiperazine 1-Phenylpiperazine is a simple chemical compound featuring a phenyl group bound to a piperazine ring. The suffix ‘-piprazole’ is sometimes used in the names of drugs to indicate they belong to this class. List phenylpiperazine derivativesAlpe ... * Pyrimidinylpiperazine References P ...
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BMY-14802
BMY-14802, also known as BMS-181100, is a drug with antipsychotic effects which acts as both a sigma receptor antagonist and a 5-HT1A receptor agonist. It also has affinity for the 5-HT2 and D4 receptors. The drug reached phase III clinical trials for the treatment of psychosis but was never marketed. See also * Enciprazine * Ensaculin * Mafoprazine * Azaperone * Fluanisone Fluanisone is a typical antipsychotic and sedative of the butyrophenone chemical class. It is used in the treatment of schizophrenia and mania. It is also a component (along with fentanyl) of the injectable veterinary formulation fentanyl/flu ... References Abandoned drugs Secondary alcohols Organofluorides Piperazines Aminopyrimidines Serotonin receptor antagonists Serotonin receptor agonists Sigma antagonists {{nervous-system-drug-stub ...
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Enciprazine
Enciprazine (INN, BAN; enciprazine hydrochloride (USAN); developmental code names WY-48624, D-3112), is an anxiolytic and antipsychotic of the phenylpiperazine class which was never marketed. It shows high affinity for the α1-adrenergic receptor and 5-HT1A receptor, among other sites. The drug was initially anticipated to produce ''ortho''-methoxyphenylpiperazine (oMeOPP), a serotonin receptor agonist with high affinity for the 5-HT1A receptor, as a significant active metabolite, but subsequent research found this not to be the case. See also * Acaprazine * Batoprazine * Eltoprazine * Enpiprazole * Fluprazine * Lidanserin * Ensaculin * Mafoprazine * BMY-14802 * Azaperone * Fluanisone Fluanisone is a typical antipsychotic and sedative of the butyrophenone chemical class. It is used in the treatment of schizophrenia and mania. It is also a component (along with fentanyl) of the injectable veterinary formulation fentanyl/fluani ... References External links Enciprazine ...
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Piperazine
Piperazine () is an organic compound that consists of a six-membered ring containing two nitrogen atoms at opposite positions in the ring. Piperazine exists as small alkaline deliquescent crystals with a saline taste. The piperazines are a broad class of chemical compounds, many with important pharmacological properties, which contain a core piperazine functional group. Origin and naming Piperazines were originally named because of their chemical similarity with piperidine, part of the structure of piperine in the black pepper plant (''Piper nigrum''). The -az- infix added to "piperazine" refers to the extra nitrogen atom, compared to piperidine. It is important to note, however, that piperazines are ''not'' derived from plants in the '' Piper'' genus. Chemistry Piperazine is freely soluble in water and ethylene glycol, but insoluble in diethyl ether. It is a weak base with two pKb of 5.35 and 9.73 at 25 °C.; the pH of a 10% aqueous solution of piperazine is 10.8–11.8. Pi ...
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Maximum Residue Limit
The maximum residue limit (also maximum residue level, MRL), is the maximum amount of pesticide residue that is expected to remain on food products when a pesticide is used according to label directions, that will not be a concern to human health. Determination The MRL is usually determined by repeated (on the order of 10) field trials, where the crop has been treated according to good agricultural practice (GAP) and an appropriate pre harvest interval or withholding period has elapsed. For many pesticides this is set at the Limit of determination (LOD) – since only major pesticides have been evaluated and understanding of acceptable daily intake (ADI) is incomplete (i.e. producers or public bodies have not submitted MRL data – often because these were not required in the past). LOD can be considered a measure of presence/absence, but certain residues may not be quantifiable at very low levels. For this reason the limit of quantification (LOQ) is often used instead of the ...
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European Medicines Agency
The European Medicines Agency (EMA) is an agency of the European Union (EU) in charge of the evaluation and supervision of medicinal products. Prior to 2004, it was known as the European Agency for the Evaluation of Medicinal Products or European Medicines Evaluation Agency (EMEA).Set up by EC Regulation No. 2309/93 as the European Agency for the Evaluation of Medicinal Products, and renamed by EC Regulation No. 726/2004 to the European Medicines Agency, it had the acronym EMEA until December 2009. The European Medicines Agency does not call itself EMA either – it has no official acronym but may reconsider if EMA becomes commonly accepted (secommunication on new visual identity an). The EMA was set up in 1995, with funding from the European Union and the pharmaceutical industry, as well as indirect subsidy from member states, its stated intention to harmonise (but not replace) the work of existing national medicine regulatory bodies. The hope was that this plan would not onl ...
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Carfentanil
Carfentanil or carfentanyl, sold under the brand name Wildnil, is a very potent opioid analgesic which is used in veterinary medicine to anesthetize large animals such as elephants and rhinoceroses. It is typically administered in this context by tranquilizer dart. Carfentanil has also been used in humans for imaging of opioid receptors. It has additionally been used as a recreational drug, typically by injection, insufflation, or inhalation. Deaths have been reported in association with carfentanil. Effects and side effects of carfentanil in humans are similar to those of other opioids and include euphoria, relaxation, pain relief, pupil constriction, drowsiness, sedation, slowed heart rate, low blood pressure, lowered body temperature, loss of consciousness, and suppression of breathing. The effects of carfentanil, including overdose, can be reversed by the opioid antagonists naloxone and naltrexone, though higher or multiple doses than usual may be necessary compared ...
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Etorphine
Etorphine (M99) is a semi-synthetic opioid possessing an analgesic potency approximately 1,000–3,000 times that of morphine. It was first prepared in 1960 from oripavine, which does not generally occur in opium poppy extract but rather the related plants ''Papaver orientale'' and ''Papaver bracteatum''. It was later reproduced in 1963 by a research group at MacFarlan Smith in Gorgie, Edinburgh, led by Kenneth Bentley. It can also be produced from thebaine. Veterinary use Etorphine is available legally only for veterinary use and is strictly governed by law. It is often used to immobilize elephants and other large mammals. Diprenorphine (Revivon) is an opioid receptor antagonist that can be administered in proportion to the amount of etorphine used (1.3 times) to reverse its effects. Veterinary-strength etorphine is fatal to humans. For this reason the package as supplied to vets always includes the human antidote along with the etorphine. The human antidote is generally na ...
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Zolazepam
Zolazepam (Flupyrazapon) is a pyrazolodiazepinone derivative structurally related to the benzodiazepine drugs, which is used as an anaesthetic for a wide range of animals in veterinary medicine. Zolazepam is usually administered in combination with other drugs such as the NMDA antagonist tiletamine or the α2 adrenergic receptor agonist xylazine, depending on what purpose it is being used for. It is around four times the potency of diazepam (0.32 mg/kg versus 1.2 mg/kg in animal models) but it is both water-soluble and un-ionized at physiological pH meaning that its onset is very fast. Zolazepam was developed by Horace A. de Wald and Donald E. Butler for Parke-Davis and was the result of a very detailed analysis of the benzodiazepine structure ( filed in 1969). Zolazepam, in combination with tiletamine, has been used in the tranquilization of wild animals, such as gorillas and polar bears, and has been found to be superior to ketamine because of reduced side-effects. A ...
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