Dopamine reuptake inhibitor
This article needs additional citations for verification. (June 2006) (Learn how and when to remove this template message) |
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.[citation needed] This usually results in an elevated extracellular dopamine level.
Contents
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]
Types
Amineptine is a potent dopamine reuptake inhibitor, and is now scheduled in most countries, including the USA. Other drugs which impact the level of dopamine in the brain include bupropion (Wellbutrin, Zyban), venlafaxine (Effexor), duloxetine (Cymbalta), sertraline (Zoloft) (at high doses), MAOIs, cocaine, Benztropine, Nomifensine, Mazindol, amphetamines and a new class of reuptake inhibitors, the GBR series, such as GBR12909 (vanoxerine).
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.[citation needed]
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.[citation needed]
Dopamine reuptake inhibitors
- Amineptine (Maneon, Survector)
- Bupropion (Wellbutrin, Zyban)
- Cocaine
- CFT (WIN-35428)
- Dextromethorphan (DXM)
- Methylenedioxypyrovalerone (MDPV)
- Methamphetamine (Desoxyn) [1]
- Methylphenidate (Ritalin, Rubifen, Concerta)
- Phenmetrazine (Preludin)
- Troparil (CPT)
- Vanoxerine (GBR-12909)
See also
Further reading
- Runyon SP, Carroll FI (2006). "Dopamine transporter ligands: recent developments and therapeutic potential". Current topics in medicinal chemistry. 6 (17): 1825–43. PMID 17017960.
References
External links
- Dopamine+uptake+inhibitors at the US National Library of Medicine Medical Subject Headings (MeSH)
- MeSH list of agents 82018765
- CS1 maint: Explicit use of et al.
- CS1 maint: Multiple names: authors list
- Articles needing additional references from June 2006
- Articles with invalid date parameter in template
- All articles needing additional references
- All articles with unsourced statements
- Articles with unsourced statements from February 2007
- Dopamine reuptake inhibitors