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Description: Pimavanserin (also known as ACP-103) is a novel, potent, efficacious, orally active and selective inverse agonist of the 5-HT2A (serotonin receptor subtype 2A) receptor with pIC50 and pKd of 8.73 and 9.3, respectively. ACP-103 reduced tacrine-induced tremulous jaw movements in rats. In addition, ACP-103 administered in combination with levodopa caused a dose-related reduction in dyskinesias in monkeys. These data suggest that ACP-103 may have the potential to reduce tremor and levodopa-induced dyskinesias in Parkinson's disease.
References: Pharmacol Biochem Behav. 2008 Oct; 90(4):540-4; J Pharmacol Exp Ther. 2006 May; 317(2):910-8.
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