生物活性

• 描述PF-04447943 is a potent, selective brain penetrant PDE9 inhibitor (Ki of 2.8, 4.5 and 18 nM) for human, rhesus and rat recombinant PDE9 respectively and high selectivity for PDE9 versus PDEs1-8 and 10-11.
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00832052	Healthy Elder... more >>ly Collapse <<	Phase 1	Completed	-	United States, Florida ... more >> Pfizer Investigational Site Gainesville, Florida, United States, 32608 Collapse <<
  NCT02114203	Phase 1 Sickle Cell	Phase 1	Completed	-	United States, Illinois ... more >> University of Illinois Hospital and Health Sciences System Chicago, Illinois, United States, 60612-5836 University of Illinois at Chicago Clinical Research Center Chicago, Illinois, United States, 60612 University of Illinois Hospital and Health Sciences System Chicago, Illinois, United States, 60612 United States, Massachusetts Boston Medical Center E7E Boston, Massachusetts, United States, 02118 Boston Medical Center Boston, Massachusetts, United States, 02118 Boston University Medical Center Boston, Massachusetts, United States, 02118 United States, New York Interfaith Medical Center Brooklyn, New York, United States, 11213 Interfaith Medical Center Brooklyn, New York, United States, 11238 United States, North Carolina UNC Hospitals' Investigational Drug Service Pharmacy Chapel Hill, North Carolina, United States, 27514 UNC School of Medicine Clinical and Translational Research Center Chapel Hill, North Carolina, United States, 27599 United States, Virginia Investigational Drug Services Richmond, Virginia, United States, 23298 Virginia Commonwealth University Richmond, Virginia, United States, 23298 Belgium Pfizer Clinical Research Unit Brussels, Belgium, B-1070 Italy Fondazione IRCCS Ca'Granda Ospedale Maggiore Policlinico Milano, Italy, 20122 A.O.O.R Villa Sofia - V. Cervello Palermo, Italy, 90146 Netherlands Centre for Human Drug Research Leiden, Netherlands, 2333 CL United Kingdom Royal Liverpool and Broadgreen University Hospital Trust Liverpool, Merseyside, United Kingdom, L7 8XP Guy's and St Thomas' NHS Foundation Trust London, United Kingdom, SE1 9RT King's College Hospital NHS Foundation Trust London, United Kingdom, SE5 9RS Imperial College Healthcare NHS Trust London, United Kingdom, W12 0HS Central Manchester University Hospitals NHS Foundation Trust Manchester, United Kingdom, M13 9WL Manchester Royal Infirmary Manchester, United Kingdom, M13 9WL Oxford University Hospitals NHS Trust Oxford, United Kingdom, OX3 7LE Collapse <<
  NCT02114203	-	-	Completed	-	-

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• 参考文献

• [1] Hutson PH, Finger EN, et al. The selective phosphodiesterase 9 (PDE9) inhibitor PF-04447943(6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl] -1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d] pyrimidin-4-one) enhances synaptic plasticity and cognitive function in rodents. Neuropharmacology. 2011 Sep;61(4):665-76.

  [2] Kleiman RJ, Chapin DS, et al. Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo. J Pharmacol Exp Ther. 2012 May;341(2):396-409.