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.
Weiner; David M. (San Diego, CA), Davis; Robert E. (San Diego, CA), Brann; Mark R. (Rye, NH), Andersson; Carl-Magnus A. (Hjarup, SE), Uldam; Allan K. (Vaerloese, DK)
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