Selective Serotonin 2a/2c Receptor Inverse Agonists As Therapeutics For Neurodegenerative Diseases


Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.

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  • Publication: Dec 31, 2013
  • Application: Jan 25, 2013
    US US 201313750778 A
  • Priority: Jan 25, 2013
    US US 201313750778 A
  • Priority: Jun 29, 2012
    US US 201213539011 A
  • Priority: Jun 27, 2011
    US US 201113169893 A
  • Priority: Apr 13, 2010
    US US 75966210 A
  • Priority: May 3, 2006
    US US 41652706 A
  • Priority: Jan 15, 2004
    US US 75956104 A
  • Priority: Jun 17, 2003
    US US 47934603 P
  • Priority: Jan 16, 2003
    US US 44140603 P

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