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Naphthylmorpholine
Naphthylmorpholine (code name PAL-678), also known as 2-(2′-naphthyl)morpholine, is a monoamine releasing agent of the arylmorpholine and naphthylethylamine families. It is the derivative of 2-phenylmorpholine with a 2-naphthalene ring instead of a phenyl ring. Naphthylmorpholine is a close analogue of naphthylmetrazine (PAL-704; a naphthalene analogue of phenmetrazine), but lacks naphthylmetrazine's methyl group at the 3 position of the morpholine ring. The drug is a potent monoamine releasing agent. Its values for induction of monoamine release have not been reported, but it released 92% of serotonin, 88% of norepinephrine, and 79% of dopamine at a concentration of 10,000nM in rat brain synaptosome A synaptosome is an isolated synaptic terminal from a neuron. Synaptosomes are obtained by mild homogenization of nervous tissue under isotonic conditions and subsequent fractionation using differential and density gradient centrifugation. Liquid ...s. Hence, it appears to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Substituted Naphthylethylamine
The substituted naphthylethylamines are a class of chemical compounds based on naphthalene. Many naphthylethylamines are naphthylaminopropanes (also known as naphthylisopropylamines) due to the presence of a methyl group at the alpha carbon of the alkyl chain. The naphthylethylamines are derivatives of the phenethylamines, while the naphthylaminopropanes are derivatives of the amphetamines. There are two types of naphthylethylamines based on positional isomerism: 1-naphthylethylamines and 2-naphthylethylamines. Examples of these include 1-naphthylaminopropane (1-NAP) and 2-naphthylaminopropane (2-NAP), respectively. List of substituted naphthylethylamines The substituted napthylethylamines include the following compounds: Additional naphthylethylamines include 4-NEMD, centanafadine (EB-1020), nafimidone, naphazoline, and xaliproden (SR-57746). Some synthetic cannabinoids such as THJ-018 and THJ-2201 are also naphthylethylamines. Related compounds Some related compounds t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Naphthylmetrazine
Naphthylmetrazine (code name PAL-704), also known as 3-methyl-2-(2′-naphthyl)morpholine, is a monoamine releasing agent (MRA) and monoamine reuptake inhibitor (MRI) of the phenylmorpholine and naphthylaminopropane families related to phenmetrazine. It is a analogue of phenmetrazine in which the phenyl ring has been replaced with a naphthalene ring. The drug acts as a hybrid norepinephrine–dopamine releasing agent (NDRA) and serotonin reuptake inhibitor (SRI). Its values for induction of monoamine release are 111nM for dopamine, 203nM for norepinephrine, and inactive for serotonin in rat brain synaptosomes, whereas its for serotonin reuptake inhibition is 105nM. Hence, it is about equipotent in inducing dopamine release and inhibiting serotonin reuptake and is about 2-fold more potent in these actions than in inducing norepinephrine release. In terms of chemical structure, naphthylmetrazine is to phenmetrazine as naphthylisopropylamine (PAL-287) is to amphetamine. Other ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dextroamphetamine
Dextroamphetamine (international nonproprietary name, INN: dexamfetamine) is a potent central nervous system (CNS) stimulant and enantiomer of amphetamine that is used in the treatment of attention deficit hyperactivity disorder (ADHD) and narcolepsy. It is also used illicitly to enhance Nootropic, cognitive and athletic Performance-enhancing substance, performance, and recreationally as an aphrodisiac and euphoriant. Dextroamphetamine is generally regarded as the prototype drug, prototypical stimulant. The amphetamine molecule exists as two enantiomers, levoamphetamine and dextroamphetamine. Dextroamphetamine is the Levorotation and dextrorotation, dextrorotatory, or 'right-handed', enantiomer and exhibits more pronounced effects on the central nervous system than levoamphetamine. Pharmaceutical dextroamphetamine sulfate is available as both a brand name and generic drug in a variety of dosage forms. Dextroamphetamine is sometimes prescribed as the inactive prodrug lisdexamfet ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenmetrazine
Phenmetrazine, sold under the brand name Preludin among others, is a stimulant drug first chemical synthesis, synthesized in 1952 and originally used as an appetite suppressant, but withdrawn drug, withdrawn from the market in the 1980s due to widespread drug misuse, misuse. It was initially replaced by its structural analog, analogue phendimetrazine (under the brand name Prelu-2) which functions as a prodrug to phenmetrazine, but now it is rarely prescribed, due to concerns of misuse and drug addiction, addiction. Chemically, phenmetrazine is a substituted amphetamine containing a morpholine ring (chemistry), ring or a substituted phenylmorpholine. Medical uses Phenmetrazine has been used as an appetite suppressant for purposes of weight loss. It was used therapeutically for this indication at a dosage of 25mg two or three times per day (or 50–75mg/day total) in adults. Phenmetrazine has been found to produce similar weight loss to dextroamphetamine in people with obesity. I ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ethylnaphthylaminopropane
Ethylnaphthylaminopropane (ENAP; developmental code name PAL-1045) is a monoamine releasing agent (MRA) of the amphetamine and naphthylaminopropane families that is related to naphthylaminopropane (NAP; PAL-287) and methamnetamine (MNAP; PAL-1046). It acts specifically as a serotonin–norepinephrine–dopamine releasing agent (SNDRA). However, ENAP is unusual in being a partial releaser of serotonin and dopamine and a full releaser of norepinephrine. The () values of ENAP in terms of monoamine release induction are 12nM (66%) for serotonin, 46nM (78%) for dopamine, and 137nM (94%) for norepinephrine in rat brain synaptosomes. In contrast to NAP and MNAP, which produce clearly dose-dependent increases in locomotor stimulation and brain monoamine levels in rodents, ENAP has been found to show attenuated monoamine elevations and a "flat" dose–response curve. Relatedly, it may have less misuse liability than other drugs like amphetamine, although more research is necessar ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
