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Re: Cariprazine, potential new AAP

Posted by psychobot5000 on May 29, 2012, at 1:07:05

In reply to Cariprazine, potential new AAP, posted by b2chica on May 24, 2012, at 13:19:34

> http://www.medscape.com/viewarticle/764391?sssdmh=dm1.787602&src=nldne
>
>
> Oral cariprazine, which is also known as RGH-188, is a "D3-preferring dopamine D3/D2 receptor partial agonist,"
> "Higher affinity for and greater receptor antagonism at D3 versus D2 receptors may be associated with antipsychotic efficacy...and beneficial effects on mood," they add.
>


High affinity is okay, but high -antagonism- of D3 receptors would appear to be a BAD thing, not a good one, for depression and bipolar (especially depression).


> The experimental drug also has a "low potency at other receptor sites such as 5-HT2c, histamine H1, muscarinic, and adrenergic receptor sites, which have been associated with adverse events."
>

Still, perhaps if one took it at the right (tiny?) dosage, one could benefit from a medication which hits D3 receptors with partial agonism while not otherwise messing with you much? ...The increased antagonism still seems bad.

It's a thought, at any rate.

May those more educated than me feel free to correct any mistaken presumptions,
PB5000


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