Cariprazine, a new, orally active dopamine D2/3 receptor partial agonist for the treatment of schizophrenia, bipolar mania and depression

@article{Veselinovi2013CariprazineAN,
  title={Cariprazine, a new, orally active dopamine D2/3 receptor partial agonist for the treatment of schizophrenia, bipolar mania and depression},
  author={Tanja Veselinovi{\'c} and Michael Paulzen and Gerhard Gr{\"u}nder},
  journal={Expert Review of Neurotherapeutics},
  year={2013},
  volume={13},
  pages={1141 - 1159}
}
Cariprazine is a novel drug with partial agonist activity at dopamine D2/3 receptors and six- to eightfold higher affinity for human dopamine D3 over D2 receptors. Results from several placebo-controlled Phase II/III trials in patients with a The Diagnostic and Statistical Manual of Mental Disorders IV diagnosis of schizophrenia or bipolar I disorder suggest that cariprazine is superior to placebo with respect to antipsychotic and antimanic activity. Reports concerning safety and tolerability… 
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[Psychopharmacology of anxiety and depression: Historical aspects, current treatments and perspectives].
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TLDR
The antipsychotic activity of cariprazine was demonstrated in animal models, and data also suggest that the propensity for extrapyramidal side effects is low and that the drug may have procognitive properties.
Cariprazine (RGH-188), a D3-preferring dopamine D3/D2 receptor partial agonist antipsychotic candidate demonstrates anti-abuse potential in rats
TLDR
Results in rats with a history of cocaine self-administration after a period of complete abstinence in a relapse to cocaine-seeking paradigm may predict a relapse-preventing action for cariprazine in humans in addition to its existing antipsychotic and antimanic efficacy.
Cariprazine, a dopamine D3-receptor-preferring partial agonist, blocks phencyclidine-induced impairments of working memory, attention set-shifting, and recognition memory in the mouse
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In an animal model of PCP-induced cognitive impairment, cariprazine pretreatment significantly diminishedPCP-triggered cognitive deficits, and studies on knockout mice show that dopamine D3 receptors contribute to this effect.
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This Phase II trial evaluated the efficacy, safety, and tolerability of cariprazine versus placebo in the treatment of acute manic or mixed episodes associated with bipolar I disorder.
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