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Scientific Publications

NUPLAZID™ (also known as pimavanserin or ACP-103)

  • Cummings J, et al.: "Pimavanserin for patients with Parkinson's disease psychosis: a randomized, placebo-controlled phase 3 trial." The Lancet, 383, 533-540 (2014).
  • Hacksell U, et al.: "On the Discovery and Development of Pimavanserin: A Novel Drug Candidate for Parkinson's Psychosis." Neurochemistry Research, 39, 2008-2017 (2014).
  • Meltzer HY, et al.: "Pimavanserin, a serotonin 2A receptor inverse agonist for the treatment of Parkinson's disease psychosis." Neuropsychopharmacology, 35, 881-892 (2010).
  • Meltzer HY, et al.: "Pimavanserin, a selective serotonin (5-HT)2A-inverse agonist, enhances the efficacy and safety of risperidone, 2 mg/day, but does not enhance efficacy of haloperidol, 2 mg/day: Comparison with reference dose risperidone, 6 mg/day." Schizophrenia Research, 141, 144-152 (2012).
  • Ancoli-Israel S., et al.: "Pimavanserin tartrate, a 5-HT2A receptor inverse agonist, increases slow wave sleep as measured by polysomnography in healthy adult volunteers." Sleep Medicine, 12, 134-141 (2011).
  • Nordstrom AL, et al: "PET analysis of the 5-HT2A receptor inverse agonist ACP-103 in human brain." The International Journal of Neuropsychopharmacology, 11, 163-171 (2007).
  • Vanover KE, et al.: "Pharmacokinetics, Tolerability, and Safety of ACP-103 Following Single or Multiple Oral Dose Administration in Healthy Volunteers." The Journal of Clinical Pharmacology, 47, 704-714 (2007).
  • Vanover KE, et al.: "A 5-HT2A receptor inverse agonist, ACP-103, reduces tremor in a rat model and levodopa-induced dyskinesias in a monkey model." Pharmacology Biochemistry and Behavior, 90, 540-544 (2008).
  • McFarland, et al.: “Pimavanserin, a 5-HT2A inverse agonist, reverses psychosis-like behaviors in a rodent model of Parkinson’s disease.” Behavioural Pharmacology, 22, 681-692 (2011).
  • Hubbard D, et al.: "Behavioral effects of clozapine, pimavanserin, and quetiapine in rodent models of Parkinson's disease and Parkinson's disease psychosis: evaluation of therapeutic ratios." Behavioural Pharmacology, e-pub (2013).
  • Price DL, et al.: "Pimavanserin, a 5-HT2A receptor inverse agonist, reverses psychosis-like behaviors in a rodent model of Alzheimer’s disease." Behavioural Pharmacology, 23, 426-433 (2012).
  • Gardell LR, et al.: "ACP-103, A 5-Hydroxytryptamine 2A Receptor Inverse Agonist, Improves the Antipsychotic Efficacy and Side-Effect Profile of Haloperidol and Risperidone in Experimental Models." The Journal of Pharmacology and Experimental Therapeutics, 322, 862-870 (2007).
  • Vanover KE, et al.: "Pharmacological and Behavioral Profile of N-(4-Fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) Carbamide (2R, 3R)-Dihydroxybutanedioate (2:1) (ACP-103), a Novel 5-Hydroxytryptamine2A Receptor Inverse Agonist." The Journal of Pharmacology and Experimental Therapeutics, 317, 910-918 (2006).

Other relevant scientific publications:

  • McFarland K, et al.: "Low Dose Bexarotene Treatment Rescues Dopamine Neurons and Restores Behavioral Function in Models of Parkinson's Disease." ACS Chemical Neuroscience, e-pub (2013).
  • Ma JN, et al.: "The Protease Activated Receptor 2 (PAR2) Polymorphic Variant F240S Constitutively Activates PAR2 Receptors and Potentiates Responses to Small-Molecule PAR2 Agonists." The Journal of Pharmacology and Experimental Therapeutics, 347, 697-704 (2013).
  • George S, et al.: "Nonsteroidal Selective Androgen Receptor Modulators and Selective Estrogen Receptor Beta Agonists Moderate Cognitive Deficits and Amyloid-Beta Levels in a Mouse Model of Alzheimer's Disease." ACS Chemical Neuroscience, e-pub (2013).
  • Ma JN, et al.: "Characterization of highly efficacious allosteric agonists of the human calcium receptor." Journal of Pharmacology and Experimental Therapeutics, 337, 275-284 (2011).
  • Gaubert G., et al.: "Discovery of Selective Nonpeptidergic Neuropeptide FF2 Receptor Agonists." Journal of Medicinal Chemistry, 52, 6511-6514 (2009).
  • Del Tredici AL, et al.: "Identification of novel selective V2 receptor non-peptide agonists." Biochemical Pharmacology, 76, 1134-1141 (2008).
  • Piu F, et al.: "Broad modulation of neuropathic pain states by a selective estrogen receptor beta agonist." European Journal of Pharmacology, 590, 423-429 (2008).
  • Piu F, et al.: "Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator." The Journal of Steroid Biochemistry and Molecular Biology, 109, 129-137 (2008).
  • Burstein ES, et al.: "Integrative Functional Assays, Chemical Genomics and High Throughput Screening: Harnessing Signal Transduction Pathways to a Common HTS Readout." Current Pharmaceutical Design, 12, 1717-1729 (2006).
  • Weiner DM, et al.: "Psychosis of Parkinson's disease: Serotonin 2A receptor inverse agonists as potential therapeutics." Current Opinion in Investigational Drugs, 4, 815-819 (2003).
  • Weiner DM, et al.: "5-Hydroxytryptamine2A Receptor Inverse Agonists as Antipsychotics." The Journal of Pharmacology and Experimental Therapeutics, 299, 268-276 (2001).
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