Discovery of cariprazine (RGH-188): A novel antipsychotic acting on dopamine D3/D2 receptors
| Autor: | Mária Zájer-Balázs, Károly Tihanyi, Katalin Saghy, Mónika Vastag, Katalin Nogradi, Istvan Vago, Bela Kiss, Margit Kapás, István Greiner, Larisza Gémesi, Zsolt Szombathelyi, György M. Keserű, Éva Ágai-Csongor, Janos Galambos, Eva Schmidt, Istvan Gyertyan, György Domány, Judit Laszy, Aniko Gere, István Laszlovszky |
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| Rok vydání: | 2012 |
| Předmět: |
medicine.medical_treatment
Clinical Biochemistry Pharmaceutical Science Cariprazine Pharmacology Biochemistry Piperazines chemistry.chemical_compound Dopamine receptor D3 Dopamine receptor D2 Drug Discovery Area under curve medicine Animals Humans Receptor Antipsychotic Molecular Biology Receptors Dopamine D2 Chemistry Receptors Dopamine D4 Organic Chemistry Rats Safety profile Area Under Curve Molecular Medicine Antipsychotic Agents |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 22:3437-3440 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2012.03.104 |
| Popis: | Medicinal chemistry optimization of an impurity isolated during the scale-up synthesis of a pyridylsulfonamide type dopamine D3/D2 compound (1) led to a series of new piperazine derivatives having affinity to both dopamine D3 and D2 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. |
| Databáze: | OpenAIRE |
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