1. Preparation of aryl piperazine derivatives useful for the treatment of neuropsychiatric disorders
- Author
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Campiani, Giuseppe, Butini, Stefania, Franceschini, Silvia, Thale, Zia Irene, Nielsen, Karin Sandager, Scheel Krueger, Joergen, Madsen, Lars S.i.i.m., FATTORUSSO, CATERINA, Campiani, Giuseppe, Butini, Stefania, Fattorusso, Caterina, Franceschini, Silvia, Thale, Zia Irene, Nielsen, Karin Sandager, Scheel Krueger, Joergen, and Madsen, Lars S. i. i. m.
- Subjects
modulators of dopamine and serotonin receptors schizophrenia - Abstract
The title compds. I [R1-R3 = H, Me, OH, OMe, halo, CF3, CN or CO2H] having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, 5HT1A and 5-HT2A receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders, including schizophrenia, were prepd. E.g., a multi-step synthesis of I [R1-R3 = H], starting from 6-methylquinoline, was given. The affinity of compds. I for the dopamine and serotonin receptor subtypes was detd. using std. receptor binding assays. Thus, compds. I were found to be selective for dopamine D3 and having a Ki in the subnanomolar range (no specific data given). Pharmaceutical compn. comprising the compd. I is claimed.
- Published
- 2008