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Dopamine

Dopamine Reuptake Inhibitors (DARI), Dopamine Uptake Inhibitors, Dopamine Transporter Inhibitors are compounds that inhibit the reuptake of extracellular dopamine back into the presynaptic cell by blocking the cell membrane-spanning dopamine transporter. Dopamine is a powerful neurotransmitter that is responsible for reward and drive. It is involved in various feelings such as euphoria, orgasm, anger, addiction, love, pleasure. Dopamine reuptake inhibitors allow dopamine to remain in the synaptic cleft and activate the receptors for a longer period of time, and some drugs can create a drug induced euphoria. Cocaine, a DARI, is notorious for this effect. A few prescription drugs such as methylphenidate and to a lesser extent bupropion (Wellbutrin) have this mechanism of action as well. Side effects from these drugs can be mixed. In some they induce euphoria, and in others they may induce restlessness and irritability. Image File history File links Question_book-3. ... Dopamine structural diagram Created by Maxim Iorsh with xymtex documentclass{letter} usepackage{epic,carom,hetarom} pagestyle{empty} begin{document} begin{picture}(1200,1500) put(0,0){bzdrv{5==HO;6==HO}} put(340,0){sixunitv{}{2==NH$_2$}{bcde}} end{picture} end{document} File history Legend: (cur) = this is the... Dopamine structural diagram Created by Maxim Iorsh with xymtex documentclass{letter} usepackage{epic,carom,hetarom} pagestyle{empty} begin{document} begin{picture}(1200,1500) put(0,0){bzdrv{5==HO;6==HO}} put(340,0){sixunitv{}{2==NH$_2$}{bcde}} end{picture} end{document} File history Legend: (cur) = this is the... For other uses, see Dopamine (disambiguation). ... Reuptake, or re-uptake, is the reabsorption of a neurotransmitter by the neurotransmitter transporter of a pre-synaptic neuron after it has performed its function of transmitting a neural impulse. ... For other uses, see Dopamine (disambiguation). ... Illustration of the major elements in a prototypical synapse. ... The dopamine transporter or DAT is a monoamine transporter that is specific for clearing the neurotransmitter dopamine out of the synaptic cleft and into a glial cell or the presynaptic neuron. ... Chemical structure of D-aspartic acid, a common amino acid neurotransmitter. ... Look up euphoria, euphoric in Wiktionary, the free dictionary. ... An orgasm (sexual climax) is the conclusion of the plateau phase of the sexual response cycle, and may be experienced by both males and females. ... This article is about the emotion. ... This article is about the concept of addiction. ... For other uses, see Love (disambiguation). ... Look up Pleasure in Wiktionary, the free dictionary. ... For other uses, see Cocaine (disambiguation). ... Vitamin R redirects here. ... Bupropion (INN; also amfebutamone,[1] brand names Wellbutrin, Zyban, Budeprion and Buproban) is an atypical antidepressant, which acts as a norepinephrine reuptake inhibitor and dopamine reuptake inhibitor,[2] and a nicotinic antagonist. ... Look up euphoria, euphoric in Wiktionary, the free dictionary. ... Look up agitation in Wiktionary, the free dictionary. ... Irritability is an excessive response to stimuli. ...

Mechanism

DARIs bind at the transporter molecule and form a non-covalent complex with it.^{[citation needed]} When the DARI-molecule is large enough, which is normally the case, it suppresses the binding of other substances that are transporter substrates, such as endogenous compounds (like dopamine) and drugs (e.g. amphetamine).^{[citation needed]} Amphetamine or Amfetamine(Alpha-Methyl-PHenEThylAMINE), also known as beta-phenyl-isopropylamine and benzedrine, is a prescription stimulant commonly used to treat Attention-deficit hyperactivity disorder (ADHD) in adults and children. ...

Abuse

In general, the abuse potential of DAR inhibitors depends on how they affect the pattern of dopamine release and reuptake.

Compounds that inhibit reuptake and also induce release of dopamine, such as methamphetamine or phenmetrazine, or compounds that inhibit reuptake but have no effect on release, such as cocaine or methylphenidate, tend to be addictive drugs with potential for abuse in humans.^[1] This article is about the psychostimulant, d-methamphetamine. ... Phenmetrazine is an amphetamine-like drug. ... For other uses, see Cocaine (disambiguation). ... Vitamin R redirects here. ... Addiction is an uncontrollable compulsion to repeat a behavior regardless of its negative consequences. ...

On the other hand, compounds that inhibit reuptake but also inhibit release of dopamine, such as bupropion and vanoxerine, have mild stimulant effects and little abuse potential, and can be used to treat stimulant addiction. ^[2] Bupropion (INN; also amfebutamone,[1] brand names Wellbutrin, Zyban, Budeprion and Buproban) is an atypical antidepressant, which acts as a norepinephrine reuptake inhibitor and dopamine reuptake inhibitor,[2] and a nicotinic antagonist. ... Vanoxerine, also known as GBR-12909, is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor. ...

Some dopamine reuptake inhibitors

• Amineptine (Maneon, Survector)
• Bupropion (Wellbutrin, Zyban)
• Cocaine (an alkaloid)
• CFT (WIN-35428)
• Dextromethorphan (DXM)^{[citation needed]}
• Methylenedioxypyrovalerone (MDPV)
• Methamphetamine (Desoxyn) ^[3]
• Methylphenidate (Ritalin, Rubifen, Concerta)
• Phenmetrazine (Preludin)
• Troparil (CPT)
• Vanoxerine (GBR-12909)
• Venlafaxine (Effexor) (weakly)

Amineptine is an atypical tricyclic antidepressant that selectively inhibits the reuptake of dopamine and to a lesser extent norepinephrine, thus exerting a powerful and fast-acting antidepressant effect. ... Bupropion (INN; also amfebutamone,[1] brand names Wellbutrin, Zyban, Budeprion and Buproban) is an atypical antidepressant, which acts as a norepinephrine reuptake inhibitor and dopamine reuptake inhibitor,[2] and a nicotinic antagonist. ... For other uses, see Cocaine (disambiguation). ... (-)-2-β-Carbomethoxy-3-β-(4-fluorophenyl)tropane naphthalenedisulfonate (CFT) is a dopamine reuptake inhibitor structurally similar to cocaine. ... Dextromethorphan (DXM or DM) is an antitussive (cough suppressant) drug found in many over-the-counter cold and cough medicines. ... This page may meet Wikipedia’s criteria for speedy deletion. ... This article is about the psychostimulant, d-methamphetamine. ... Vitamin R redirects here. ... Phenmetrazine is an amphetamine-like drug. ... (-)-2β-Carbomethoxy-3β-phenyltropane (Troparil, β-CPT, WIN-35065-2) is a stimulant drug used in scientific research. ... Vanoxerine, also known as GBR-12909, is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor. ... Venlafaxine (Effexor) is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class first introduced by Wyeth in 1993. ...

See also

• Stimulant
• NERI
• SSRI
• NDRI
• SNRI
• SNDRI

Sustained-Release 15mg Dexedrine Spansules. ... Norepinephrine reuptake inhibitors (NRIs) are compounds that increase amounts of the neurotransmitter norepinephrine in the brain by inhibiting its reuptake at synapses. ... SSRI redirects here; for other uses, see SSRI (disambiguation). ... A Norepinephrine-dopamine reuptake inhibitor is a class of drugs that is both: Dopamine reuptake inhibitor Norepinephrine reuptake inhibitor An example is Bupropion. ... Serotonin Norepinephrine Serotonin-norepinephrine reuptake inhibitors (SNRIs) are a class of antidepressant used in the treatment of clinical depression and other affective disorders. ... Serotonin-norepinephrine-dopamine-reuptake-inhibitors (SNDRI) are a class of psychoactive antidepressants. ...

Further reading

• Runyon SP, Carroll FI (2006). "Dopamine transporter ligands: recent developments and therapeutic potential". Current topics in medicinal chemistry 6 (17): 1825-43. doi:10.2174/156802606778249775. PMID 17017960. 

A digital object identifier (or DOI) is a standard for persistently identifying a piece of intellectual property on a digital network and associating it with related data, the metadata, in a structured extensible way. ...

References

1. ^ Wise, R. A. 1981. Brain dopamine and reward. Pages 103-122,in Cooper, S. J., (ed.), Theory in psychopharmacology, Academic Press, London, NY.
2. ^ Elkashef, A.M. 2005. Bupropion for the Treatment of Methamphetamine Dependence. Pages 1162–1170, in Neuropsychopharmacology (2008) 33
3. ^ Heal DJ, Frankland AT, Gosden J, et al (1992). "A comparison of the effects of sibutramine hydrochloride, bupropion and methamphetamine on dopaminergic function: evidence that dopamine is not a pharmacological target for sibutramine". Psychopharmacology (Berl.) 107 (2-3): 303-9. PMID 1615130. 

External links

• MeSH Dopamine+uptake+inhibitors
• MeSH list of agents 82018765