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Re: GBR 12909 causes sedation » linkadge

Posted by Astounder on November 2, 2007, at 17:31:56

In reply to GBR 12909 causes sedation, posted by linkadge on November 2, 2007, at 15:11:23

> http://www.biopsychiatry.com/gbr12909.htm
>
> The selective dopamine reuptake inhibitor causes dose dependant *sedation* in human volunteers.
>
> I still argue that it is norepinephrine which is mainly responsible for the "stimulating" aspects of stimulants. Yet dopamine is more involved in reward.
>
> Linkadge

That selective DRIs are not psychostimulants can be explained in that NET blockade is necessary to increase DA levels in the frontal cortex, as NET plays a greater role in clearing away extracellular DA in this area than does DAT. Furthermore, cortical glial uptake of DA depends more on NET than DAT.

http://www.ncbi.nlm.nih.gov/sites/entrez?Db=pubmed&Cmd=ShowDetailView&TermToSearch=11784783&ordinalpos=15&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum
http://www.ncbi.nlm.nih.gov/sites/entrez?Db=pubmed&Cmd=ShowDetailView&TermToSearch=12444505&ordinalpos=1&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum

I believe dopamine is essential to the alertfulness-promoting effects of psychostimulants. Solely noradrenergic drugs do not reduce daytime sleepiness in narcolepsy, though they can be used to treat other symptoms, like cataplexy. Selective D2 antagonists like Haldol reverse the arousal from psychostimulants without affecting NE.


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poster:Astounder thread:791344
URL: http://www.dr-bob.org/babble/20071027/msgs/793014.html