Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.

@article{gaiCsongor2012DiscoveryOC,
  title={Discovery of cariprazine (RGH-188): a novel antipsychotic acting on dopamine D3/D2 receptors.},
  author={{\'E}va {\'A}gai-Csongor and G. Domány and K. N{\'o}gr{\'a}di and J. Galambos and I. V{\'a}g{\'o} and G. Keserű and I. Greiner and I. Laszlovszky and A. Gere and {\'E}. Schmidt and B. Kiss and M. Vastag and K. Tihanyi and K. Sághy and J. Laszy and I. Gyertyán and M{\'a}ria Z{\'a}jer-Bal{\'a}zs and L. Gémesi and M. Kapás and Z. Szombathelyi},
  journal={Bioorganic \& medicinal chemistry letters},
  year={2012},
  volume={22 10},
  pages={
          3437-40
        }
}
Medicinal chemistry optimization of an impurity isolated during the scale-up synthesis of a pyridylsulfonamide type dopamine D(3)/D(2) compound (1) led to a series of new piperazine derivatives having affinity to both dopamine D(3) and D(2) receptors. Several members of this group showed excellent pharmacokinetic and pharmacodynamic properties as demonstrated by outstanding activities in different antipsychotic tests. The most promising representative, 2m (cariprazine) had good absorption… Expand
Discovery of Cariprazine (RGH‐188): A Novel Antipsychotic Acting on Dopamine D3/D2 Receptors.
Medicinal chemistry optimization of an impurity isolated during the scale-up synthesis of a pyridylsulfonamide-type compound as a high-affinity dopamine D3/D2 receptor ligand leads to a series of newExpand
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Cariprazine: chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability
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  • Medicine
  • Expert opinion on drug metabolism & toxicology
  • 2013
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The chemistry, pharmacodynamic profile, pharmacokinetics, and clinical profile of cariprazine, an atypical antipsychotic in clinical development for the treatment of schizophrenia and bipolar mania/mixed episodes, are described. Expand
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