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Re: Cariprazine » SLS

Posted by ed_uk2010 on February 12, 2012, at 13:27:26

In reply to Re: Cariprazine » ed_uk2010, posted by SLS on February 12, 2012, at 6:31:11

>I think the most important feature of cariprazine is that it is much more potent as a partial agonist at dopamine D3 receptors than at D2 receptors (higher D3/D2 ratio). D3 is the receptor of pleasure and reward, and is found in the following regions of the brain:
>
> - thalamic paraventricular nucleus
> - nucleus accumbans
> - ventral tegmental area
>
> Without D3 receptors, cocaine would have no pleasurable effect. As a matter of fact, D3 partial agonists can act as a sort of muffler, thereby reducing cocaine's effect. It occurs to me that cariprazine might help with cocaine addiction in much the same way as buprenorphine, a mu opioid receptor partial agonist, does with opioid addiction. Just a thought...
>
> Thanks for making me learn stuff.
>
> :-)
>
>
> - Scott

Very interesting, thanks. I wonder when it will be available. The positive Phase III trial in bipolar mania is encouraging. Perhaps they will apply for approval in this indication and look to add other indications later.

 

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poster:ed_uk2010 thread:1009756
URL: http://www.dr-bob.org/babble/20120212/msgs/1010071.html