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Scientific Publications

Pimavanserin (also known as ACP-103)

  • 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, e-pub (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).
  • 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:

  • 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).
  • Seitzberg JG, et al.: "Discovery of Potent and Selective Small-Molecule PAR-2 Agonists." Journal of Medicinal Chemistry, 51, 5490-5493 (2008).
  • Vanover KE, et al.: "Antipsychotic-Like Behavioral Effects and Cognitive Enhancement by a Potent and Selective Muscarinic M1 Receptor Agonist, AC-260584." Behavioral Neuroscience, 122, 570-575 (2008).
  • Schiffer HH, et al.: "Pharmacology and Signaling Properties of Epidermal Growth Factor Receptor Isoforms Studied by Bioluminescence Resonance Energy Transfer." Molecular Pharmacology, 71, 508-518 (2007).
  • 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).
  • Ottesen LK, et al.: "Iron-Catalyzed Cross-Coupling of Imidoyl Chlorides with Grignard Reagents." Organic Letters, 8, 1771-1773 (2006).
  • Spalding TA, et al.: "Structural Requirements of Transmembrane Domain 3 for Activation by the M1 Muscarinic Receptor Agonists AC-42, AC-260584, Clozapine, and N-Desmethylclozapine: Evidence for Three Distinct Modes of Receptor Activation." Molecular Pharmacology, 70, 1974-1983 (2006).
  • Lund BW, et al.: "Discovery of a Potent, Orally Available, and Isoform-Selective Retinoic Acid ß2 Receptor Agonist." Journal of Medicinal Chemistry, 48, 7517-7519 (2005).
  • Bertozzi F, et al.: "A Combinatorial Scaffold Approach Based upon a Multicomponent Reaction." Organic Letters, 5, 1551-1554 (2003).
  • 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).
  • Croston GE, et al.: "Discovery of the First Nonpeptide Agonist of the GPR14/Urotensin-II Receptor: 3-(4-Chlorophenyl)-3-(2-(dimethylamino)ethyl)isochroman-1-one (AC-7954)." Journal of Medicinal Chemistry, 45, 4950-4953 (2002).
  • 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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