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List Of Modafinil Analogues And Derivatives
This page lists chemical compounds similar to modafinil, known as modafinil analogues and derivatives. These are structural analogues and derivatives of modafinil, a drug that affects dopamine levels in the brain in an unusual way (atypical dopamine reuptake inhibitor or DRI). Modafinil is a drug that helps keep people awake and alert (wakefulness-promoting agent or "eugeroic"). Most of the listed modafinil analogues are drugs that specifically target dopamine reuptake (reabsorption of a neurotransmitter by a neurotransmitter transporter) with stronger effects ( selective DRIs with improved potency) compared to modafinil. The modafinil analogues are of interest in the potential treatment of a condition involving the misuse of stimulant drugs ( psychostimulant use disorder or PSUD), as drugs that help increase motivation ( pro-motivational agents) to treat motivational disorders, and for treatment of neurodegenerative diseases such as Alzheimer's disease. Modafinil analogues ... [...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, significant hyp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Motivational Disorders
Disorders of diminished motivation (DDM) are a group of disorders involving diminished motivation and associated emotions. Many different terms have been used to refer to diminished motivation. Often however, a spectrum is defined encompassing apathy, abulia, and akinetic mutism, with apathy the least severe and akinetic mutism the most extreme. DDM can be caused by psychiatric disorders like depression and schizophrenia, brain injuries, strokes, and neurodegenerative diseases. Damage to the anterior cingulate cortex and to the striatum, which includes the nucleus accumbens and caudate nucleus and is part of the mesolimbic dopamine reward pathway, have been especially associated with DDM. Diminished motivation can also be induced by certain drugs, including antidopaminergic agents like antipsychotics, selective serotonin reuptake inhibitors (SSRIs), and cannabis, among others. DDM can be treated with dopaminergic and other activating medications, such as dopamine reuptake ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Heart Condition
Cardiovascular disease (CVD) is a class of diseases that involve the heart or blood vessels. CVD includes coronary artery diseases (CAD) such as angina and myocardial infarction (commonly known as a heart attack). Other CVDs include stroke, heart failure, hypertensive heart disease, rheumatic heart disease, cardiomyopathy, abnormal heart rhythms, congenital heart disease, valvular heart disease, carditis, aortic aneurysms, peripheral artery disease, thromboembolic disease, and venous thrombosis. The underlying mechanisms vary depending on the disease. It is estimated that dietary risk factors are associated with 53% of CVD deaths. Coronary artery disease, stroke, and peripheral artery disease involve atherosclerosis. This may be caused by high blood pressure, smoking, diabetes mellitus, lack of exercise, obesity, high blood cholesterol, poor diet, excessive alcohol consumption, and poor sleep, among other things. High blood pressure is estimated to account for approximate ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
HERG
hERG (the human '' Ether-à-go-go''-Related Gene) is a gene () that codes for a protein known as Kv11.1, the alpha subunit of a potassium ion channel. This ion channel (sometimes simply denoted as 'hERG') is best known for its contribution to the electrical activity of the heart: the hERG channel mediates the repolarizing ''I''Kr current in the cardiac action potential, which helps coordinate the heart's beating. When this channel's ability to conduct electrical current across the cell membrane is inhibited or compromised, either by application of drugs or by rare mutations in some families, it can result in a potentially fatal disorder called long QT syndrome. Conversely, genetic mutations that increase the current through these channels can lead to the related inherited heart rhythm disorder Short QT syndrome. A number of clinically successful drugs in the market have had the tendency to inhibit hERG, lengthening the QT and potentially leading to a fatal irregularity of th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cognitive Enhancer
Nootropics ( , or ) (colloquial: smart drugs and cognitive enhancers, similar to adaptogens) are a wide range of natural or synthetic supplements or drugs and other substances that are claimed to improve cognitive function or to promote relaxation, particularly boosting mood, executive functions, attention, memory, creativity, or motivation in healthy individuals. The use of cognition-enhancing supplements by healthy individuals in the absence of a medical indication spans numerous controversial issues, including the ethics and fairness of their use, concerns over adverse effects, and the diversion of prescription drugs for non-medical uses. Nonetheless, the international sales of cognitive- or mood-enhancing supplements have continued to grow over time and in 2012 reached 0.69 billion. With sales supported by global health trends, the market is expected to reach US$33.85 billion by the year 2030, at a CAGR of 14.8%. While most nootropics are not regulated, there are othe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nootropic
Nootropics ( , or ) ( colloquial: smart drugs and cognitive enhancers, similar to adaptogens) are a wide range of natural or synthetic supplements or drugs and other substances that are claimed to improve cognitive function or to promote relaxation, particularly boosting mood, executive functions, attention, memory, creativity, or motivation in healthy individuals. The use of cognition-enhancing supplements by healthy individuals in the absence of a medical indication spans numerous controversial issues, including the ethics and fairness of their use, concerns over adverse effects, and the diversion of prescription drugs for non-medical uses. Nonetheless, the international sales of cognitive- or mood-enhancing supplements have continued to grow over time and in 2012 reached 0.69 billion. With sales supported by global health trends, the market is expected to reach US$33.85 billion by the year 2030, at a CAGR of 14.8%. While most nootropics are not regulated, there a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Modafiendz
Modafiendz, also known as ''N''-methyl-4,4-difluoromodafinil or as ''N''-methylbisfluoromodafinil, is a wakefulness-promoting agent related to modafinil that was never marketed. It is sold online and used non-medically as a nootropic (cognitive enhancer). Modafiendz is the ''bis''-fluoro and ''N''- methylated derivative of modafinil as well as the ''N''-methyl analogue of flmodafinil (CRL-40,940; bisfluoromodafinil) and fladrafinil (CRL-40,941; bisfluoroadrafinil). Modafinil and its analogues have been found to act as selective dopamine reuptake inhibitors and this is thought to be involved in their wakefulness-promoting effects. See also * List of modafinil analogues and derivatives This page lists chemical compounds similar to modafinil, known as modafinil analogues and derivatives. These are structural analogues and derivatives of modafinil, a drug that affects dopamine levels in the brain in an unusual way (atypical do ... References 4-Fluorophenyl compou ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fladrafinil
CRL-40,941 (also known as fladrafinil and fluorafinil) is a eugeroic closely related to adrafinil and modafinil. 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 CE-123 is an Structural analog, 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 consiste ... 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] |
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 a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JJC8-088
JJC8-088 is a dopamine reuptake inhibitor (DRI) that was derived from the wakefulness-promoting agent modafinil. It has substantially higher affinity for the dopamine transporter (DAT) than modafinil (Ki = 6.72nM vs. 2,600nM; 387-fold). In contrast to modafinil and other analogues, which are atypical DRIs, JJC8-088 is a typical cocaine-like DRI. It has potent cocaine-like psychostimulant effects, produces robust and dose-dependent increases in dopamine levels in the nucleus accumbens, and is readily self-administered by and substitutes for cocaine in animals. Similarly to cocaine, but unlike modafinil and other analogues, JJC8-088 stabilizes the DAT in an outward-facing open conformation. It has been theorized that cocaine-like DRIs may actually act as dopamine releasing agent-like DAT "inverse agonists" rather than as simple transporter blockers. In addition to its affinity for the DAT, JJC8-088 has low affinity for the serotonin transporter (SERT) (Ki = 213nM; 32-fold less ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cocaine
Cocaine (from , from , ultimately from Quechua: ''kúka'') is a central nervous system (CNS) stimulant mainly used recreationally for its euphoric effects. It is primarily obtained from the leaves of two Coca species native to South America, '' Erythroxylum coca'' and '' Erythroxylum novogranatense''. After extraction from coca leaves and further processing into cocaine hydrochloride (powdered cocaine), the drug is often snorted, applied topically to the mouth, or dissolved and injected into a vein. It can also then be turned into free base form (crack cocaine), in which it can be heated until sublimated and then the vapours can be inhaled. Cocaine stimulates the reward pathway in the brain. Mental effects may include an intense feeling of happiness, sexual arousal, loss of contact with reality, or agitation. Physical effects may include a fast heart rate, sweating, and dilated pupils. High doses can result in high blood pressure or high body temperature. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
JJC8-016
JJC8-016 is an atypical dopamine reuptake inhibitor (DRI) chemical derivative, derived from modafinil. It was an early lead in the development of novel modafinil structural analog, analogues with improved properties for potential use in the treatment of psychostimulant use disorder (PSUD). Pharmacology The affinity (pharmacology), affinities of JJC8-016 for the monoamine transporters are 114nM for the dopamine transporter (DAT), 3850nM for the norepinephrine transporter (NET) (34-fold lower than for the DAT), and 354nM for the serotonin transporter (SERT) (3.1-fold lower than for the DAT). JJC8-016 also has high affinity for the dopamine D2 receptor, D2 receptor (Ki = 228nM), the dopamine D3 receptor, D3 receptor (Ki = 65.9nM), the dopamine D4 receptor, D4 receptor (Ki = 28.1nM), and the sigma receptor, sigma sigma-1 receptor, σ1 receptor (Ki = 159nM). It has much higher affinity for the DAT than modafinil (Ki = 2600nM; 23-fold difference), but is also much less binding selec ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
