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Aminorex
Aminorex, sold under the brand names Menocil and Apiquel among others, is a weight loss (anorectic) stimulant drug. It was withdrawn from the market after it was found to cause pulmonary hypertension (PPH). In the United States, aminorex is a Schedule I controlled substance. Aminorex, in the 2-amino-5-aryloxazoline group, was developed by McNeil Laboratories in 1962. It is closely related to 4-methylaminorex (4-MAR). Aminorex has been shown to have locomotor-stimulant effects, lying midway between dextroamphetamine and methamphetamine. Aminorex effects have been attributed to the release of catecholamines. It can be produced as a metabolite of the deworming medication levamisole, which is sometimes used as a cutting agent of illicitly produced cocaine. Pharmacology Pharmacodynamics Aminorex is a serotonin–norepinephrine–dopamine releasing agent (SNDRA). Its values for induction of monoamine release are 26.4nM for norepinephrine, 49.4nM for dopamine, and 193nM fo ...
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4-methylaminorex
4-Methylaminorex (4-MAR, 4-MAX) is a stimulant drug of the 2-amino-5-aryloxazoline group that was first synthesized in 1960 by McNeil Laboratories. It is also known by its street name "U4Euh" ("Euphoria"). It is banned in many countries as a stimulant. 4-Methylaminorex has effects comparable to methamphetamine but with a longer duration. Chemistry 4-Methylaminorex exists as four stereoisomers : (±)-''cis'' and (±)-''trans''. The (±)-''cis'' isomers are the form used recreationally. Synthesis The (±)-''cis'' isomers acemate (1:1-mixture) of the (4''R'',5''S'')-isomer and the enantiomeric (4''S'',5''R'')-isomergenerally synthesized from dl-phenylpropanolamine in one step by cyclization with cyanogen bromide (sometimes prepared ''in situ'' by reacting sodium cyanide with bromine). Alternate synthesis routes generally involve more steps, such as replacing cyanogen bromide with sodium or potassium cyanate to form an intermediate and then reacting it with concentrated hydroch ...
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List Of Aminorex Analogues
This is a list of aminorex analogues, also known as substituted 2-amino-5-aryloxazolines. Aminorex itself is a stimulant drug with a 5-phenyl-2-amino-oxazoline structure. It was developed in the 1960s as an anorectic, but withdrawn from sale after it was discovered that extended use produced pulmonary hypertension, often followed by heart failure, which resulted in a number of deaths. A designer drug analogue 4-methylaminorex appeared on the illicit market in the late 1980s but did not attract significant popularity due to its steep dose-response curve and tendency to produce seizures. Pemoline, the 4-keto derivative of aminorex, had been discovered several years earlier, and derivatives of this type appeared to be effective stimulants with comparatively low toxicity. Pemoline was sold for around 25 years as a therapy for ADHD and relief of fatigue, before being withdrawn from the market in 2005 because of rare but serious cases of liver failure. More recently in around 2014 another ...
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Levamisole
Levamisole, sold under the brand name Ergamisol among others, is a medication used to treat parasitic worm infections, specifically ascariasis and hookworm infections. It is taken by mouth. Side effects may include abdominal pain, vomiting, headache, and dizziness. Use is not recommended during breastfeeding or the third trimester of pregnancy. Serious side effects may include an increased risk of infection. It belongs to the anthelmintic class of medications. Levamisole was invented in 1966 in Belgium by Janssen Pharmaceuticals. It is on the WHO Model List of Essential Medicines, World Health Organization's List of Essential Medicines. Levamisole is also used as a dewormer for cattle. Medical uses Worms Levamisole was originally used as an anthelmintic to treat worm infestations in both humans and animals. Levamisole works as a nicotinic acetylcholine receptor agonist that causes continued stimulation of the parasitic worm muscles, leading to paralysis. Levamisole has gai ...
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Monoamine Releasing Agent
A monoamine releasing agent (MRA), or simply monoamine releaser, is a drug that induces the release of one or more monoamine neurotransmitters from the presynaptic neuron into the synapse, leading to an increase in the extracellular concentrations of the neurotransmitters and hence enhanced signaling by those neurotransmitters. The monoamine neurotransmitters include serotonin, norepinephrine, and dopamine; MRAs can induce the release of one or more of these neurotransmitters. MRAs work by reversing the direction of the monoamine transporters (MATs), including the serotonin transporter (SERT), norepinephrine transporter (NET), and/or dopamine transporter (DAT), causing them to promote efflux of non-vesicular cytoplasmic monoamine neurotransmitter rather than reuptake of synaptic monoamine neurotransmitter. Many, but not all MRAs, also reverse the direction of the vesicular monoamine transporter 2 (VMAT2), thereby additionally resulting in efflux of vesicular monoamine neuro ...
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Cocaine
Cocaine is a tropane alkaloid and central nervous system stimulant, derived primarily from the leaves of two South American coca plants, ''Erythroxylum coca'' and ''Erythroxylum novogranatense, E. novogranatense'', which are cultivated almost exclusively in the Andes. Indigenous peoples of South America, Indigenous South Americans have traditionally used coca leaves for over a thousand years. Notably, there is no evidence that habitual coca leaf use causes addiction or withdrawal, unlike cocaine. Medically, cocaine is rarely employed, mainly as a topical medication under controlled settings, due to its high abuse potential, adverse effects, and expensive cost. Despite this, recreational drug use, recreational use is widespread, driven by its euphoric and aphrodisiac properties. Levamisole induced necrosis syndrome (LINES)-a complication of the common cocaine Lacing (drugs), cutting agent levamisole-and prenatal cocaine exposure is particularly harmful. Street cocaine is ...
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Serotonin–norepinephrine–dopamine Releasing Agent
A serotonin–norepinephrine–dopamine releasing agent (SNDRA), also known as a triple releasing agent (TRA), is a type of drug which induces the release of serotonin, norepinephrine/epinephrine, and dopamine in the brain and body. SNDRAs produce euphoriant, entactogen, and psychostimulant effects, and are almost exclusively encountered as recreational drugs. A closely related type of drug is a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI). Examples of SNDRAs Examples of SNDRAs include specific amphetamines such as MDMA, MDA, 4-methylamphetamine, methamphetamine (in high doses), certain substituted benzofurans such as 5-APB and 6-APB, naphthylisopropylamine; cathinones such as mephedrone and methylone; tryptamines such as αMT and αET; along with agents of other chemical classes such as 4,4'-DMAR, and 5-IAI.Bruce E. Blough, Richard Rothman, Antonio Landavazo, Kevin M. Page, Ann Marie Decker. Phenylmorpholines and analogues thereof. US Patent 2013/0 ...
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Anorectic
An anorectic is a drug that reduces appetite, resulting in lower food consumption, leading to weight loss. These substances work by affecting the central nervous system or certain neurotransmitters to create a feeling of fullness or reduce the desire to eat. The understanding of anorexiant effects is crucial in the development of interventions for weight management, eating disorders, and related health concerns. The anorexiant effect can be induced through diverse mechanisms, ranging from hormonal regulation to neural signaling. Ghrelin, leptin, and peptide YY are among the hormones involved in appetite control. Additionally, neurotransmitters such as serotonin and dopamine in the central nervous system contribute significantly to the regulation of food intake. By contrast, an appetite stimulant is referred to as orexigenic. The term is (from the Greek and ), and such drugs are also known as anorexigenic, anorexiant, or appetite suppressant. History Used on a short-term ...
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Serotonin
Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, memory, and physiological processes such as vomiting and vasoconstriction. In the CNS, serotonin regulates mood, appetite, and sleep. Most of the body's serotonin—about 90%—is synthesized in the gastrointestinal tract by enterochromaffin cells, where it regulates intestinal movements. It is also produced in smaller amounts in the brainstem's raphe nuclei, the skin's Merkel cells, pulmonary neuroendocrine cells, and taste receptor cells of the tongue. Once secreted, serotonin is taken up by platelets in the blood, which release it during clotting to promote vasoconstriction and platelet aggregation. Around 8% of the body's serotonin is stored in platelets, and 1–2% is found in the CNS. Serotonin acts as both a vasoconstrictor and vas ...
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Racemic Mixture
In chemistry, a racemic mixture or racemate () is a mixture that has equal amounts (50:50) of left- and right-handed enantiomers of a chiral molecule or salt. Racemic mixtures are rare in nature, but many compounds are produced industrially as racemates. History The first known racemic mixture was racemic acid, which Louis Pasteur found to be a mixture of the two enantiomeric isomers of tartaric acid. He manually separated the crystals of a mixture, starting from an aqueous solution of the sodium ammonium salt of racemate tartaric acid. Pasteur benefited from the fact that ammonium tartrate salt gives enantiomeric crystals with distinct crystal forms (at 77 °F). Reasoning from the macroscopic scale down to the molecular, he reckoned that the molecules had to have non-superimposable mirror images. A sample with only a single enantiomer is an ''enantiomerically pure'' or ''enantiopure'' compound. Etymology The word ''racemic'' derives from Latin , meaning pertaining to a ...
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Cutting Agent
Cutting is the separation or opening of a physical object, into two or more portions, through the application of an acutely directed force. Implements commonly used for cutting are the knife and saw, or in medicine and science the scalpel and microtome. However, any sufficiently sharp object is capable of cutting if it has a hardness sufficiently larger than the object being cut, and if it is applied with sufficient force. Even liquids can be used to cut things when applied with sufficient force (see water jet cutter). Cutting is a compressive and shearing phenomenon, and occurs only when the total stress generated by the cutting implement exceeds the ultimate strength of the material of the object being cut. The simplest applicable equation is: :\text = or \tau=\frac The stress generated by a cutting implement is directly proportional to the force with which it is applied, and inversely proportional to the area of contact. Hence, the smaller the area (i.e., the sharper ...
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Norepinephrine
Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic compound, organic chemical in the catecholamine family that functions in the brain and human body, body as a hormone, neurotransmitter and neuromodulator. The name "noradrenaline" (from Latin '':wikt:ad-, ad'', "near", and '':wikt:ren, ren'', "kidney") is more commonly used in the United Kingdom and the rest of the world, whereas "norepinephrine" (from Ancient Greek :wikt:ἐπί, ἐπῐ́ (''epí''), "upon", and :wikt:νεφρός, νεφρός (''nephrós''), "kidney") is usually preferred in the United States. "Norepinephrine" is also the international nonproprietary name given to norepinephrine (drug), the drug. Regardless of which name is used for the substance itself, parts of the body that produce or are affected by it are referred to as noradrenergic. The general function of norepinephrine is to mobilize the brain and body for action. Norepinephrine release is lowest during sleep, rise ...
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Metabolite
In biochemistry, a metabolite is an intermediate or end product of metabolism. The term is usually used for small molecules. Metabolites have various functions, including fuel, structure, signaling, stimulatory and inhibitory effects on enzymes, catalytic activity of their own (usually as a cofactor to an enzyme), defense, and interactions with other organisms (e.g. pigments, odorants, and pheromones). A primary metabolite is directly involved in normal "growth", development, and reproduction. Ethylene exemplifies a primary metabolite produced large-scale by industrial microbiology. A secondary metabolite is not directly involved in those processes, but usually has an important ecological function. Examples include antibiotics and pigments such as resins and terpenes etc. Some antibiotics use primary metabolites as precursors, such as actinomycin, which is created from the primary metabolite tryptophan. Some sugars are metabolites, such as fructose or glucose, which ar ...
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