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

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

  • Bioorg Med Chem Lett. 2012 May 15;22(10):3437-40. doi: 10.1016/j.bmcl.2012.03.104.
Eva Agai-Csongor 1,  György Domány,  Katalin Nógrádi,  János Galambos,  István Vágó,  György Miklós Keserű,  István Greiner,  István Laszlovszky,  Anikó Gere,  Eva Schmidt,  Béla Kiss,  Mónika Vastag,  Károly Tihanyi,  Katalin Sághy,  Judit Laszy,  István Gyertyán,  Mária Zájer-Balázs,  Larisza Gémesi,  Margit Kapás,  Zsolt Szombathelyi
Affiliations

Affiliation

PMID: 22537450 DOI: 10.1016/j.bmcl.2012.03.104
Abstract

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, excellent brain penetration and advantageous safety profile. Based on its successful clinical development we are looking forward to the NDA filing of cariprazine in 2012.

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