GBR-13098
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GBR-13098
GBR-13098 is a psychostimulant and selective dopamine uptake inhibitor. Blocking the endogenous striatal dopamine (DA) transporter with GBR-13098 in mice has been shown to prevent damage to the DA nerve terminals caused by malonate. It was suggested that DA transporter inhibitors like GBR-13098 could be used to prevent or treat neurodegenerative disorders caused by the effect of mitochondrial dysfunction Mitochondrial disease is a group of disorders caused by mitochondrial dysfunction. Mitochondria are the organelles that generate energy for the cell and are found in every cell of the human body except red blood cells. They convert the energy of ... on DA homeostasis. See also * Vanoxerine * GBR-12783 * GBR-12935 * GBR-13069 * DBL-583 References Stimulants Dopamine reuptake inhibitors 1-(2-(Bis(4-fluorophenyl)methoxy)ethyl)piperazines {{nervous-system-drug-stub ...
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Dopamine Uptake 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 ha ...
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GBR-12783
GBR-12783 is a psychostimulant which acts as a selective 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 dopa .... See also * Vanoxerine * GBR-12935 * GBR-13069 * GBR-13098 * DBL-583 References Stimulants Dopamine reuptake inhibitors 1-(2-(Diphenylmethoxy)ethyl)piperazines {{nervous-system-drug-stub ...
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GBR-12935
GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor. It was originally developed in its 3H radiolabelled form for the purpose of mapping the distribution of dopaminergic neurons in the brain by selective labelling of dopamine transporter proteins. This has led to potential clinical uses in the diagnosis of Parkinson's disease, although selective radioligands such as Ioflupane (¹²³I) Ioflupane (123I) is the international nonproprietary name (INN) of a cocaine analogue which is a neuro-imaging radiopharmaceutical drug, used in nuclear medicine for the diagnosis of Parkinson's disease and the differential diagnosis of Parkin ... are now available for this application. GBR-12935 is now widely used in animal research into Parkinson's disease and the dopamine pathways in the brain. See also * Vanoxerine * GBR-12783 * GBR-13069 * GBR-13098 * DBL-583 References Dopamine reuptake inhibitors 1-(2-(Diphenylmethoxy)eth ...
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GBR-13069
GBR-13069 is a psychostimulant and selective dopamine reuptake inhibitor. See also * Vanoxerine * GBR-12783 * GBR-12935 * GBR-13098 * DBL-583 DBL-583 is a selective dopamine reuptake inhibitor of the piperazine chemical class. It is the decanoate ester In chemistry, an ester is a compound derived from an oxoacid (organic or inorganic) in which at least one hydroxyl group () is re ... References Dopamine reuptake inhibitors 1-(2-(Bis(4-fluorophenyl)methoxy)ethyl)piperazines Stimulants {{nervous-system-drug-stub ...
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DBL-583
DBL-583 is a selective dopamine reuptake inhibitor of the piperazine chemical class. It is the decanoate ester of a hydroxy vanoxerine. DBL-583 breaks down very slowly in the body, lasting for up to a month after a single injection. See also * GBR-12783 * GBR-12935 * GBR-13069 * GBR-13098 GBR-13098 is a psychostimulant and selective dopamine uptake inhibitor. Blocking the endogenous striatal dopamine (DA) transporter with GBR-13098 in mice has been shown to prevent damage to the DA nerve terminals caused by malonate The conjugat ... References Decanoate esters Dopamine_reuptake_inhibitors 1-(2-(Bis(4-fluorophenyl)methoxy)ethyl)piperazines {{nervous-system-drug-stub ...
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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 linked ...
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Mitochondrial Disease
Mitochondrial disease is a group of disorders caused by mitochondrial dysfunction. Mitochondria are the organelles that generate energy for the cell and are found in every cell of the human body except red blood cells. They convert the energy of food molecules into the ATP that powers most cell functions. Mitochondrial diseases take on unique characteristics both because of the way the diseases are often inherited and because mitochondria are so critical to cell function. A subclass of these diseases that have neuromuscular symptoms are known as mitochondrial myopathies. Types Examples of mitochondrial diseases include: * Mitochondrial myopathy * Diabetes mellitus and deafness (DAD) ** this combination at an early age can be due to mitochondrial disease ** Diabetes mellitus and deafness can be found together for other reasons * Leber's hereditary optic neuropathy (LHON) ** visual loss beginning in young adulthood ** eye disorder characterized by progressive loss of central v ...
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Vanoxerine
Vanoxerine is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor (DRI). Vanoxerine binds to the target site on the dopamine transporter (DAT) ~ 50 times more strongly than cocaine, but simultaneously inhibits the release of dopamine. This combined effect only slightly elevates dopamine levels, giving vanoxerine only mild stimulant effects. Vanoxerine has also been observed to be a potent blocker of the IKr (hERG) channel. Vanoxerine also binds with nanomolar affinity to the serotonin transporter. Vanoxerine as a treatment for cocaine dependence Vanoxerine has been researched for use in treating cocaine dependence both as a substitute for cocaine and to block the rewarding effects. This strategy of using a competing agonist with a longer half-life has been successfully used to treat addiction to opiates such as heroin by substituting with methadone. It was hoped that vanoxerine would be of similar use in treating cocaine addiction. Research als ...
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Stimulants
Stimulants (also often referred to as psychostimulants or colloquially as uppers) is an overarching term that covers many drugs including those that increase activity of the central nervous system and the body, drugs that are pleasurable and invigorating, or drugs that have Sympathomimetic drug, sympathomimetic effects. Stimulants are widely used throughout the world as prescription medicines as well as without a prescription (either legally or Prohibition (drugs), illicitly) as performance-enhancing substance, performance-enhancing or recreational drug use, recreational drugs. Among narcotics, stimulants produce a noticeable crash or ''Comedown (drugs), comedown'' at the end of their effects. The most frequently prescribed stimulants as of 2013 were lisdexamfetamine (Vyvanse), methylphenidate (Ritalin), and amphetamine (Adderall). It was estimated in 2015 that the percentage of the world population that had used cocaine during a year was 0.4%. For the category "amphetamines and p ...
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