Butylamphetamine
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Butylamphetamine
Butylamphetamine (code name PAL-90; also known as ''N''-butylamphetamine or NBA) is a psychostimulant of the substituted amphetamine family which was never marketed. It is the ''N''-butyl analogue of amphetamine and is approximately 6-fold less potent than amphetamine in rats. The drug has been found to be inactive as a dopamine reuptake inhibitor or releasing agent ( and > 10,000nM, respectively). With regard to structure–activity relationships, the potency of ''N''-substituted amphetamine derivatives decreases with increasing chain length in terms of both ''in vitro'' and ''in vivo'' activity. The pharmacokinetics of butylamphetamine have been studied in humans. It can be metabolized by CYP2D6 via ring hydroxylation similarly to amphetamine. In addition, butylamphetamine can be ''N''- dealkylated into amphetamine (6–9% excreted in urine after 24hours). See also * Methamphetamine * Ethylamphetamine * Propylamphetamine * Isopropylamphetamine Isopropylamphetamine is a ...
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Substituted Amphetamine
Substituted amphetamines, or simply amphetamines, are a chemical class, class of compounds based upon the amphetamine structure; it includes all derivative (chemistry), derivative compounds which are formed by replacing, or substitution reaction, substituting, one or more hydrogen atoms in the amphetamine core structure with substituents. The compounds in this class span a variety of pharmacological subclasses, including stimulants, Empathogen-entactogen, empathogens, and hallucinogens, among others. Examples of substituted amphetamines are amphetamine (itself), methamphetamine, ephedrine, cathinone, phentermine, mephentermine, tranylcypromine, bupropion, methoxyphenamine, selegiline, amfepramone, amfepramone (diethylpropion), pyrovalerone, MDMA (ecstasy), and 2,5-dimethoxy-4-methylamphetamine, DOM (STP). Some of amphetamine's substituted Derivative (chemistry), derivatives occur in nature, for example in the leaves of ''Ephedra (genus), Ephedra'' and khat plants. Amphetamine w ...
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Propylamphetamine
Propylamphetamine (code name PAL-424; also known as ''N''-propylamphetamine or NPA) is a psychostimulant of the amphetamine family which was never marketed. It was first developed in the 1970s, mainly for research into the metabolism of, and as a comparison tool to, other amphetamines. Propylamphetamine is inactive as a dopamine releasing agent ''in vitro'' and instead acts as a low-potency dopamine reuptake inhibitor with an of 1,013nM. The drug can be ''N''- dealkylated to form amphetamine (10–20% excreted in urine after 24hours). A study in rats found propylamphetamine to be approximately 4-fold less potent than amphetamine. See also * Methamphetamine * Ethylamphetamine * Isopropylamphetamine * Butylamphetamine * Phenylpropylaminopentane 1-Phenyl-2-propylaminopentane (PPAP), also known as α,''N''-dipropylphenethylamine (DPPEA) and by the developmental code name MK-306, is an experimental drug related to selegiline which acts as a catecholaminergic activity enhan ...
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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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Ethylamphetamine
Etilamfetamine, also known as ''N''-ethylamphetamine and formerly sold under the brand names Apetinil and Adiparthrol, is a stimulant drug of the substituted amphetamine, amphetamine family. It was invented in the early 20th century and was subsequently used as an anorectic or appetite suppressant in the 1950s, but was not as commonly used as other amphetamines such as amphetamine, methamphetamine, and benzphetamine, and was largely discontinued once newer drugs such as phenmetrazine were introduced. Pharmacology Pharmacodynamics Monoamine releasing agent Ethylamphetamine is a potency (pharmacology), potent dopamine releasing agent (DRA) ''in vitro'', with an of 88.5nM. This is about 10-fold lower than the of dextroamphetamine. The values of ethylamphetamine for induction of norepinephrine and serotonin release were not reported. However, the values of its dextrorotatory enantiomer dextroethylamphetamine have been reported and were 44.1nM, 28.8nM, and 333nM for norepinep ...
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Dextroethylamphetamine
Etilamfetamine, also known as ''N''-ethylamphetamine and formerly sold under the brand names Apetinil and Adiparthrol, is a stimulant drug of the amphetamine family. It was invented in the early 20th century and was subsequently used as an anorectic or appetite suppressant in the 1950s, but was not as commonly used as other amphetamines such as amphetamine, methamphetamine, and benzphetamine, and was largely discontinued once newer drugs such as phenmetrazine were introduced. Pharmacology Pharmacodynamics Monoamine releasing agent Ethylamphetamine is a potent dopamine releasing agent (DRA) ''in vitro'', with an of 88.5nM. This is about 10-fold lower than the of dextroamphetamine. The values of ethylamphetamine for induction of norepinephrine and serotonin release were not reported. However, the values of its dextrorotatory enantiomer dextroethylamphetamine have been reported and were 44.1nM, 28.8nM, and 333nM for norepinephrine, dopamine, and serotonin, respectively. H ...
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Bioassay
A bioassay is an analytical method to determine the potency or effect of a substance by its effect on animal testing, living animals or plants (''in vivo''), or on living cells or tissues (''in vitro''). A bioassay can be either quantal or quantitative, direct or indirect. If the measured response is binary, the assay is mwod:quantal, quantal; if not, it is Quantitative research, quantitative. A bioassay may be used to detect biological hazards or to give an assessment of the quality of a mixture. A bioassay is often used to monitor water quality as well as wastewater discharges and its impact on the surroundings. It is also used to assess the environmental impact and safety of new technologies and facilities. Bioassays are essential in pharmaceutical, medical and agricultural sciences for development and launching of new drugs, vitamins, etc. Principle A bioassay is a biochemical test to estimate the potency of a sample compound. Usually this potency can only be measured rela ...
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Psychostimulant
Stimulants (also known as central nervous system stimulants, or psychostimulants, or colloquially as uppers) are a class of drugs that increase alertness. They are used for various purposes, such as enhancing attention, motivation, cognition, mood, and physical performance. Some stimulants occur naturally, while others are exclusively synthetic. Common stimulants include caffeine, nicotine, amphetamines, cocaine, methylphenidate, and modafinil. Stimulants may be subject to varying forms of regulation, or outright prohibition, depending on jurisdiction. Stimulants increase activity in the sympathetic nervous system, either directly or indirectly. Prototypical stimulants increase synaptic concentrations of excitatory neurotransmitters, particularly norepinephrine and dopamine (e.g., methylphenidate). Other stimulants work by binding to the receptors of excitatory neurotransmitters (e.g., nicotine) or by blocking the activity of endogenous agents that promote sleep (e.g., ca ...
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Dextromethamphetamine
Methamphetamine (contracted from ) is a potent central nervous system (CNS) stimulant that is mainly used as a recreational or performance-enhancing drug and less commonly as a second-line treatment for attention deficit hyperactivity disorder (ADHD). It has also been researched as a potential treatment for traumatic brain injury. Methamphetamine was discovered in 1893 and exists as two enantiomers: levo-methamphetamine and dextro-methamphetamine. ''Methamphetamine'' properly refers to a specific chemical substance, the racemic mixture, racemic free base, which is an equal mixture of levomethamphetamine and dextromethamphetamine in their pure amine forms, but the hydrochloride salt, commonly called crystal meth, is widely used. Methamphetamine is rarely prescribed over concerns involving its potential for recreational use as an aphrodisiac and euphoriant, among other concerns, as well as the availability of safer substitute good, substitute drugs with comparable treatment ...
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Pharmacokinetics
Pharmacokinetics (from Ancient Greek ''pharmakon'' "drug" and ''kinetikos'' "moving, putting in motion"; see chemical kinetics), sometimes abbreviated as PK, is a branch of pharmacology dedicated to describing how the body affects a specific substance after administration. The substances of interest include any chemical xenobiotic such as pharmaceutical drugs, pesticides, food additives, cosmetics, etc. It attempts to analyze chemical metabolism and to discover the fate of a chemical from the moment that it is administered up to the point at which it is completely eliminated from the body. Pharmacokinetics is based on mathematical modeling that places great emphasis on the relationship between drug plasma concentration and the time elapsed since the drug's administration. Pharmacokinetics is the study of how an organism affects the drug, whereas pharmacodynamics (PD) is the study of how the drug affects the organism. Both together influence dosing, benefit, and adverse effe ...
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Metabolism
Metabolism (, from ''metabolē'', "change") is the set of life-sustaining chemical reactions in organisms. The three main functions of metabolism are: the conversion of the energy in food to energy available to run cellular processes; the conversion of food to building blocks of proteins, lipids, nucleic acids, and some carbohydrates; and the elimination of metabolic wastes. These enzyme-catalyzed reactions allow organisms to grow and reproduce, maintain their Structures#Biological, structures, and respond to their environments. The word ''metabolism'' can also refer to the sum of all chemical reactions that occur in living organisms, including digestion and the transportation of substances into and between different cells, in which case the above described set of reactions within the cells is called intermediary (or intermediate) metabolism. Metabolic reactions may be categorized as ''catabolic''—the ''breaking down'' of compounds (for example, of glucose to pyruvate by c ...
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