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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. 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.
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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
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]
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]
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)
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. doi:. PMID 17017960.
References
- ^ Wise, R. A. 1981. Brain dopamine and reward. Pages 103-122,in Cooper, S. J., (ed.), Theory in psychopharmacology, Academic Press, London, NY.
- ^ Elkashef, A.M. 2005. Bupropion for the Treatment of Methamphetamine Dependence. Pages 1162–1170, in Neuropsychopharmacology (2008) 33
- ^ 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.
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Wikipedia content modification information:
- This page was last modified on 21 June 2008, at 16:47.
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