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CRL-40,940
CRL-40,940 (also known as flmodafinil, bisfluoromodafinil and lauflumide) is the bisfluoro analog of modafinil. It is a eugeroic as well as a weak dopamine reuptake inhibitor. Its inventors claim that it is more effective than modafinil and adrafinil, with fewer side effects. It was patented in 2013, and pre-clinical trials have been underway since December 2015. See also * Adrafinil * Armodafinil * CE-123 * CRL-40,941 * Fluorenol Fluorenol, also known as hydrafinil, is an alcohol derivative of fluorene. In the most significant isomer, fluoren-9-ol or 9-hydroxyfluorene, the hydroxy group is located on the bridging carbon between the two benzene rings. Hydroxyfluorene can be ... References Acetamides Designer drugs Dopamine reuptake inhibitors Drugs with unknown mechanisms of action Fluoroarenes Nootropics Stimulants Sulfoxides {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Structural Analog
A structural analog (analogue in modern traditional English; Commonwealth English), also known as a chemical analog or simply an analog, is a compound having a structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is screened for structural analogs of a lead compound. Chemical analogues of i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Modafinil
Modafinil, sold under the brand name Provigil among others, is a central nervous system (CNS) stimulant medication used to treat sleepiness due to narcolepsy, shift work sleep disorder, and obstructive sleep apnea. While it has seen off-label use as a purported cognitive enhancer to improve wakefulness in animal and human studies, the research on its effectiveness for this use is not conclusive. Modafinil is taken by mouth. Modafinil’s side effects include headaches, anxiety, excessive adrenal gland overproduction, and nausea. Serious side effects in high doses include delusions, unfounded beliefs, paranoia, irrational thought, and transient depression, possibly due to its effects on dopamine receptors in the brain, as well as allergic reactions. The amount of medication used should be adjusted in those with kidney problems, as this medication has markedly increased side effects during renal insufficiency. It is not recommended in those with an arrhythmia, significan ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eugeroic
Eugeroics (originally "eugrégorique" or "eugregoric"), also known as wakefulness-promoting agents and wakefulness-promoting drugs, are a class of drugs that promote wakefulness and alertness. They are medically indicated for the treatment of certain sleep disorders including excessive daytime sleepiness (EDS) in narcolepsy or obstructive sleep apnea (OSA). Eugeroics are also often prescribed off-label for the treatment of EDS in idiopathic hypersomnia, a rare and often debilitating sleep disorder which currently has no official treatments approved by the Food and Drug Administration (FDA). In contrast to classical psychostimulants, such as methylphenidate and amphetamine, which are also used in the treatment of these disorders, eugeroics typically do not produce euphoria, and, consequently, have a lower addictive potential. Modafinil and armodafinil are each thought to act as selective, weak, atypical dopamine reuptake inhibitors (DRI), whereas adrafinil acts as a prod ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Reuptake Inhibitor
A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the postsynaptic neuron is blocked from re-entering the presynaptic neuron. This results in increased extracellular concentrations of dopamine and increase in dopaminergic neurotransmission. DRIs are used in the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy for their psychostimulant effects, and in the treatment of obesity and binge eating disorder for their appetite suppressant effects. They are sometimes used as antidepressants in the treatment of mood disorders, but their use as antidepressants is limited given that strong DRIs have a high abuse potential and legal restrictions on their use. Lack of dopamine reuptake and the increase in extracellular levels of dopamine have been l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adrafinil
Adrafinil, sold under the brand name Olmifon, is a wakefulness-promoting medication that was formerly used in France to improve alertness, attention, wakefulness, and mood, particularly in the elderly. It was also used off-label by individuals who wished to avoid fatigue, such as night workers or others who needed to stay awake and alert for long periods of time. Additionally, the medication has been used non-medically as a nootropic. Adrafinil is a prodrug; it is primarily metabolized ''in vivo'' to modafinil, resulting in very similar pharmacological effects. Unlike modafinil, however, it takes time for the metabolite to accumulate to active levels in the bloodstream. Effects usually are apparent within 45–60 minutes when taken orally on an empty stomach. Adrafinil was marketed in France until September 2011 when it was voluntarily discontinued due to an unfavorable risk–benefit ratio. Medical uses Adrafinil is a wakefulness-promoting agent and was used to promote al ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Armodafinil
Armodafinil (trade name Nuvigil) is the enantiopure compound of the eugeroic modafinil (Provigil). It consists of only the (''R'')-(−)-enantiomer of the racemic modafinil. Armodafinil is produced by the pharmaceutical company Cephalon Inc. and was approved by the U.S. Food and Drug Administration (FDA) in June 2007. In 2016, the FDA granted Mylan rights for the first generic version of Cephalon's Nuvigil to be marketed in the U.S. Because armodafinil has a longer half-life than modafinil does, it may be more effective at improving wakefulness in patients with excessive daytime sleepiness. Medical uses Armodafinil is currently FDA-approved to treat excessive daytime sleepiness associated with obstructive sleep apnea, narcolepsy, and shift work disorder. It is commonly used off-label to treat attention deficit hyperactivity disorder, chronic fatigue syndrome, and major depressive disorder, and has been repurposed as an adjunctive treatment for bipolar disorder. It has ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CE-123
CE-123 is an analog of modafinil, the most researched of a series of structurally related heterocyclic derivatives. In animal studies, CE-123 was found to improve performance on tests of learning and memory in a manner consistent with a nootropic effect profile. See also * Adrafinil * CRL-40,940 * JZ-IV-10 JZ-IV-10 is a piperidine derivative related to cocaine which acts as a highly potent serotonin–norepinephrine–dopamine reuptake inhibitor A serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI), also known as a triple reuptak ... References Acetamides Designer drugs Dopamine reuptake inhibitors Nootropics Stimulants Sulfoxides Thiazoles {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CRL-40,941
CRL-40,941 (also known as fladrafinil and fluorafinil) is a eugeroic closely related to adrafinil and modafinil Modafinil, sold under the brand name Provigil among others, is a central nervous system (CNS) stimulant medication used to treat sleepiness due to narcolepsy, shift work sleep disorder, and obstructive sleep apnea. While it has seen off-la .... It is the bis(''p''-fluoro) ring-substituted derivative of adrafinil. CRL-40,941 was found to produce antiaggressive effects in animals, which adrafinil does not produce, and is purportedly 3 - 4 times stronger than adrafinil. See also * Adrafinil * Armodafinil * CRL-40,940 * Fluorenol * CE-123 References Abandoned drugs Benzene derivatives Designer drugs Drugs with unknown mechanisms of action Fluoroarenes Hydroxamic acids Prodrugs Stimulants Sulfoxides {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fluorenol
Fluorenol, also known as hydrafinil, is an alcohol derivative of fluorene. In the most significant isomer, fluoren-9-ol or 9-hydroxyfluorene, the hydroxy group is located on the bridging carbon between the two benzene rings. Hydroxyfluorene can be converted to fluorenone by oxidation. It is a white-cream colored solid at room temperature. Toxicity Fluorenol is toxic to aquatic organisms including algae, bacteria, and crustaceans. Fluorenol was patented as an insecticide in 1939, and is an algaecide against the green algae ''Dunaliella bioculata''.MSDS Its toxicity and icity in humans are unknown. Mechanism of action The exact mechanism of actio ...[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acetamides
Acetamide (systematic name: ethanamide) is an organic compound with the formula CH3CONH2. It is the simplest amide derived from acetic acid. It finds some use as a plasticizer and as an industrial solvent. The related compound ''N'',''N''-dimethylacetamide (DMA) is more widely used, but it is not prepared from acetamide. Acetamide can be considered an intermediate between acetone, which has two methyl (CH3) groups either side of the carbonyl (CO), and urea which has two amide (NH2) groups in those locations. Acetamide is also a naturally occurring mineral with the IMA symbol: Ace. Production Laboratory scale Acetamide can be produced in the laboratory from ammonium acetate by dehydration: : H4CH3CO2] → CH3C(O)NH2 + H2O Alternatively acetamide can be obtained in excellent yield via ammonolysis of acetylacetone under conditions commonly used in reductive amination. It can also be made from anhydrous acetic acid, acetonitrile and very well dried hydrogen chloride gas, usin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Designer Drugs
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 as new psychoactive substances (NPS) as well as analogs of performance-enhancing drugs such as designer steroids. Some of these 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 trials, the use of some of these drugs may result ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Reuptake Inhibitors
A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the postsynaptic neuron is blocked from re-entering the presynaptic neuron. This results in increased extracellular concentrations of dopamine and increase in dopaminergic neurotransmission. DRIs are used in the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy for their psychostimulant effects, and in the treatment of obesity and binge eating disorder for their appetite suppressant effects. They are sometimes used as antidepressants in the treatment of mood disorders, but their use as antidepressants is limited given that strong DRIs have a high abuse potential and legal restrictions on their use. Lack of dopamine reuptake and the increase in extracellular levels of dopamine have been l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
