JZ-IV-10
JZ-IV-10 is a piperidine derivative related to cocaine which acts as a highly potent serotonin–norepinephrine–dopamine reuptake inhibitor (also called SNDRI, or triple reuptake inhibitor). The eugeroic modafinil was used as a lead to fuel this compound's discovery. See also * 1-Methyl-3-propyl-4-(p-chlorophenyl)piperidine * JJC8-088 * N,O-Dimethyl-4-(2-naphthyl)piperidine-3-carboxylate * Nocaine (+)-CPCA (nocaine, 3α-carbomethoxy-4β-(4-chlorophenyl)-''N''-methylpiperidine aka CTDP 31,446) is a stimulant drug similar in structure to pethidine (an opioid that possesses NDRI actions) and to RTI-31, but nocaine lacks the two-carbon brid ... References Stimulants Carboxamides 4-Phenylpiperidines 4-Chlorophenyl compounds Serotonin–norepinephrine–dopamine reuptake inhibitors {{nervous-system-drug-stub ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Nocaine
(+)-CPCA (nocaine, 3α-carbomethoxy-4β-(4-chlorophenyl)-''N''-methylpiperidine aka CTDP 31,446) is a stimulant drug similar in structure to pethidine (an opioid that possesses NDRI actions) and to RTI-31, but nocaine lacks the two-carbon bridge of RTI-31's tropane skeleton. This compound was first developed as a substitute agent for cocaine. Since then, many substituted phenylpiperidine derivatives have been discovered, hybridizing the basic nocaine structure with that of other similar molecules such as methylphenidate, meperidine and modafinil to create a large family of derivatives with a range of activity profiles and potential applications. This is a significant field of research with much ongoing work, with dozens of novel compounds having been developed although none have yet come to market. The nocaine family includes a diverse assortment of piperidine based cocaine mimetics. The parent compound nocaine was developed in an attempt to create a substitute drug for cocai ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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1-Methyl-3-propyl-4-(p-chlorophenyl)piperidine
1-Methyl-3-propyl-4-(''p''-chlorophenyl)piperidine is a drug developed by a team led by Alan Kozikowski, which acts as a potent dopamine reuptake inhibitor, and was developed as a potential therapeutic agent for the treatment of cocaine addiction. As with related compounds such as nocaine, it is a structurally simplified derivative of related phenyltropane compounds. Its activity at the serotonin and noradrenaline transporters has not been published, though most related 4-phenylpiperidine derivatives are relatively selective for inhibiting dopamine reuptake over the other monoamine neurotransmitters. While several of its isomers are active, the (3''S'',4''S'')-enantiomer is by far the most potent. The rearranged structural isomer 2- -(4-chlorophenyl)butyliperidine is also a potent inhibitor of dopamine reuptake. : See also * 4-Fluoropethidine 4-Fluoropethidine is a drug that is a derivative of pethidine (meperidine), which combines pethidine's opioid analgesic effects with i ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Serotonin–norepinephrine–dopamine Reuptake Inhibitor
A serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI), also known as a triple reuptake inhibitor (TRI), is a type of drug that acts as a combined reuptake inhibitor of the monoamine neurotransmitters serotonin, norepinephrine, and dopamine. Monoamine structures (including neurotransmitters) contain a singular amino group (mono) linked to an aromatic ring by a chain of two carbons. SNDRIs prevent reuptake of these monoamine neurotransmitters through the simultaneous inhibition of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT), respectively, increasing their extracellular concentrations and, therefore, resulting in an increase in Serotonin, serotonergic, adrenergic, and dopaminergic neurotransmission. SNDRIs were developed as potential antidepressants and treatments for other disorders, such as obesity, cocaine addiction, attention-deficit hyperactivity disorder (ADHD), and chronic pain. The increase in neurotransmitter ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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JJC8-088
JJC8-088 is a dopamine reuptake inhibitor (DRI) that was chemical derivative, derived from the wakefulness-promoting agent modafinil. It has substantially higher affinity (pharmacology), affinity for the dopamine transporter (DAT) than modafinil (Ki = 6.72nM vs. 2,600nM; 387-fold). In contrast to modafinil and other structural analog, analogues, which are atypical DRIs, JJC8-088 is a typical cocaine-like DRI. It has potency (pharmacology), potent cocaine-like psychostimulant effects, produces robust and dose dependence, dose-dependent increases in dopamine levels in the nucleus accumbens, and is readily self-administration, 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 reuptake inhibitor, transport ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Piperidine
Piperidine is an organic compound with the molecular formula (CH2)5NH. This heterocyclic amine consists of a six-membered ring containing five methylene bridges (–CH2–) and one amine bridge (–NH–). It is a colorless liquid with an odor described as objectionable, typical of amines. The name comes from the genus name '' Piper'', which is the Latin word for pepper. Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids, such as natural-occurring solenopsins. Production Piperidine was first reported in 1850 by the Scottish chemist Thomas Anderson and again, independently, in 1852 by the French chemist Auguste Cahours, who named it. Both of them obtained piperidine by reacting piperine with nitric acid. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst: : C5H5N + 3 H2 → C5H10NH Pyridine can also be reduce ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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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 ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Georgetown University
Georgetown University is a private university, private Jesuit research university in Washington, D.C., United States. Founded by Bishop John Carroll (archbishop of Baltimore), John Carroll in 1789, it is the oldest Catholic higher education, Catholic institution of higher education in the United States, the oldest university in Washington, D.C., and the nation's first University charter#Federal, federally chartered university. The university has eleven Undergraduate education, undergraduate and Postgraduate education, graduate schools. Its main campus, located in the Georgetown (Washington, D.C.), Georgetown historic neighborhood, is on a hill above the Potomac River and identifiable by Healy Hall, a National Historic Landmark. It is Carnegie Classification of Institutions of Higher Education, classified among List_of_research_universities_in_the_United_States#Universities_classified_as_"R1:_Doctoral_Universities_–_Very_high_research_activity", "R1: Doctoral Universities – V ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Eugeroic
A eugeroic, or eugregoric, is a type of drug that increases wakefulness. The term has been used inconsistently and in multiple ways in the scientific literature, either to refer specifically to modafinil-type wakefulness-promoting agents or to refer to wakefulness-promoting agents generally. It was first introduced in the French literature in 1987 as a descriptor for modafinil-like wakefulness-promoting drugs and for purposes of distinguishing such drugs from psychostimulants. However, the term "eugeroic" has not been widely adopted in the literature, and instead the term "wakefulness-promoting agent" (and variations thereof) has been more widely used, both for modafinil-type drugs and other agents. Eugeroics, in the sense of modafinil-type wakefulness promoting agents, include modafinil itself, armodafinil, and adrafinil, among others. They are medically indicated for the treatment of certain sleep disorders, including excessive daytime sleepiness (EDS) in narcolepsy or ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Modafinil
Modafinil, sold under the brand name Provigil among others, is a central nervous system (CNS) stimulant and wakefulness-promoting agent, eugeroic (wakefulness promoter) medication used primarily to treat narcolepsy, a sleep disorder characterized by excessive daytime sleepiness and sudden Microsleep, sleep attacks. Modafinil is also approved for stimulating wakefulness in people with sleep apnea and shift work sleep disorder. It is taken by mouth. Modafinil is not approved by the US Food and Drug Administration (FDA) for use in people under 17 years old. Common side effects of Modafinil include anxiety, insomnia, dizziness, and headache. Modafinil has potential for causing severe allergic reactions, Psychiatry, psychiatric effects, hypersensitivity, adverse effect, adverse drug interaction, interactions with prescription drugs, and misuse or drug abuse, abuse. Modafinil may harm the fetus if taken during or two months prior to pregnancy. While modafinil is used as a Nootropi ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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N,O-Dimethyl-4-(2-naphthyl)piperidine-3-carboxylate
''N'',''O''-Dimethyl-4β-(2-naphthyl)piperidine-3β-carboxylate (DMNPC) is a piperidine based stimulant drug which is synthesised from arecoline. It is similar to nocaine in chemical structure, and has two and a half times more activity than cocaine as a dopamine reuptake inhibitor. However it is also a potent serotonin reuptake inhibitor, with similar affinity to fluoxetine. DMNPC has four stereoisomers, each of which has different binding affinities, with the 3S,4S enantiomer having the highest overall activity. The 3R,4S enantiomer demonstrates the highest selectivity for 5-HTT. In animal studies, DMNPC exhibits similar potency as fluoxetine, but with greater activity for DAT and NET. ''N''-Demethylation of DMNPC has shown to produce a 3-fold increase in potency for 5-HTT. Synthesis A racemic mixture of DMNPC can be synthesized from freebase arecoline in a grignard reaction with 2-naphthylmagnesium bromide. Further reactions and separation methods can be used to produce en ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |
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Stimulants
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 ... [...More Info...]       [...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]   |