Dopamine reuptake inhibitor

From Wikipedia, the free encyclopedia

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.

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]

A special kind of pseudo-DARI has been developed by scientists. It is a smaller compound, (metabolised/cracked into a small compound after DAT-binding), that binds covalently at the transporter, permanently blocking the binding of larger drugs like cocaine, but allowing small molecules like dopamine to pass through.[citation needed]

Amineptine is a potent dopamine reuptake inhibitor, and is now banned 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).

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]

  • Runyon SP, Carroll FI (2006): "Dopamine transporter ligands: recent developments and therapeutic potential", Curr.Top.Med.Chem. 6(17):1825-43. Abstract (Review)


Advanced Search
Included Web Search Engines


Safe Search

close

Top Matching Results

Occasionally Search.com will highlight specialized results that are based on the context of your query. Examples of specialized results include specific links to news, images, or video.

Top Matching Results may highlight information from other Search.com pages, content from the CNET Network of sites, or third party content. The listings are based purely on relevance. Search.com does not receive payment for listings in this section but our partners that provide this data may get paid for listing these products.

Sponsored Links

This section contains paid listings which have been purchased by companies that want to have their sites appear for specific search terms and related content. These listings are administered, sorted and maintained by a third party and are not endorsed by Search.com.

Search Results

Search.com sends your search query to several search engines at one time and integrates the results into one list which has been sorted by relevance using Search.com's proprietary algorithm. You can customize the list of search engines included in your metasearch from the preferences.

The search engines that are used in your metasearch may allow companies to pay to have their Web sites included within the results. To view the Paid Inclusion policy for a specific search engine, please visit their Web site. Search.com does not accept payment or share revenue with any search engine partner for listings in this section.