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 D2 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.

Discovery of a New Class of Potential Multifunctional Atypical Antipsychotic Agents Targeting Dopamine D3 and Serotonin 5-HT1A and 5-HT2A Receptors: Design, Synthesis, and Effects on Behavior

Brindisi M.;NOVELLINO, ETTORE;FATTORUSSO, CATERINA
2009

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 D2 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.
File in questo prodotto:
File Dimensione Formato  
JMC09_antipsicotici.pdf

non disponibili

Tipologia: Documento in Post-print
Licenza: Accesso privato/ristretto
Dimensione 1.03 MB
Formato Adobe PDF
1.03 MB Adobe PDF   Visualizza/Apri   Richiedi una copia
JMC09_antipsicotici_SI.pdf

non disponibili

Tipologia: Altro materiale allegato
Licenza: Accesso privato/ristretto
Dimensione 78.21 kB
Formato Adobe PDF
78.21 kB Adobe PDF   Visualizza/Apri   Richiedi una copia

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/364478
Citazioni
  • ???jsp.display-item.citation.pmc??? 17
  • Scopus 76
  • ???jsp.display-item.citation.isi??? 69
social impact