Dopamine D3 antagonism combined with serotonin 5-HT1A and 5-HT2A receptor occupancy may represent a novel paradigm for developing innovative antipsychotics. The unique pharmacological features of 5i are a high affinity for dopamine D3, serotonin 5-HT1A and 5-HT2A receptors, together with a low affinity for dopamine D 2 receptors (to minimize extrapyramidal side effects), serotonin 5-HT2C receptors (to reduce the risk of obesity under chronic treatment), and for hERG channels (to reduce incidence of torsade des pointes). Pharmacological and biochemical data, including specific c-fos expression in mesocorticolimbic areas, confirmed an atypical antipsychotic profile of 5i in vivo, characterized by the absence of catalepsy at antipsychotic dose.copy; 2009 American Chemical Society.
Butini, S., Gemma, S., Campiani, G., Franceschini, S., Trotta, F., Borriello, M., et al. (2009). Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine d3 and serotonin 5-HT 1A and 5-HT2A receptors: Design, synthesis, and effects on behavior. JOURNAL OF MEDICINAL CHEMISTRY, 52(1), 151-169 [10.1021/jm800689g].
Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine d3 and serotonin 5-HT 1A and 5-HT2A receptors: Design, synthesis, and effects on behavior
Butini, Stefania;Gemma, Sandra;Campiani, Giuseppe;Trotta, Francesco;Ros, Sindu;Coccone, Salvatore Sanna;Bernetti, Matteo;De Angelis, Meri;Nacci, Vito;Fiorini, Isabella;
2009-01-01
Abstract
Dopamine D3 antagonism combined with serotonin 5-HT1A and 5-HT2A receptor occupancy may represent a novel paradigm for developing innovative antipsychotics. The unique pharmacological features of 5i are a high affinity for dopamine D3, serotonin 5-HT1A and 5-HT2A receptors, together with a low affinity for dopamine D 2 receptors (to minimize extrapyramidal side effects), serotonin 5-HT2C receptors (to reduce the risk of obesity under chronic treatment), and for hERG channels (to reduce incidence of torsade des pointes). Pharmacological and biochemical data, including specific c-fos expression in mesocorticolimbic areas, confirmed an atypical antipsychotic profile of 5i in vivo, characterized by the absence of catalepsy at antipsychotic dose.copy; 2009 American Chemical Society.File | Dimensione | Formato | |
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https://hdl.handle.net/11365/3132
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