Dopamine reuptake inhibitor
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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.
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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
- ↑ 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
Receptor agonists, antagonists, and reuptake inhibitors | |
|---|---|
| BA/M: 5-HT (serotonin) receptor | Serotonin receptor agonist • Serotonin antagonist (5-HT3) • Serotonin uptake inhibitor (SSRI) |
| BA/M: Dopamine receptor | Dopamine agonist • Dopamine antagonist • Dopamine reuptake inhibitor |
| BA/M: Adrenergic receptor | Adrenergic agonist (Alpha, Beta2) • Adrenergic antagonist (Alpha, Beta) • Adrenergic uptake inhibitor |
| BA/M: Histamine receptor | Histamine agonist • Histamine antagonist (H1, H2) |
| Acetylcholine receptor | Cholinergic (Muscarinic, Nicotinic) • Anticholinergic (Muscarinic, Nicotinic) • Acetylcholinesterase inhibitor |
| AA: GABA receptor | GABA agonist • GABA antagonist |
| AA: Glutamate receptor | NMDA receptor (NMDA receptor antagonist) |
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Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
