메뉴 건너뛰기




Volumn 11, Issue 5, 2014, Pages 413-421

A multicenter, double-blind, placebo-controlled trial of the PDE9A inhibitor, PF-04447943, in Alzheimer's disease

Author keywords

Alzheimer's disease; PF 04447943; Phosphodiesterase 9 inhibitor

Indexed keywords

PF 04447943; PHOSPHODIESTERASE; PHOSPHODIESTERASE 9A; PHOSPHODIESTERASE 9A INHIBITOR; PHOSPHODIESTERASE INHIBITOR; PLACEBO; UNCLASSIFIED DRUG; 6-(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; PYRAZOLE DERIVATIVE; PYRIMIDINONE DERIVATIVE;

EID: 84904041713     PISSN: 15672050     EISSN: 18755828     Source Type: Journal    
DOI: 10.2174/1567205011666140505100858     Document Type: Article
Times cited : (69)

References (24)
  • 1
    • 0032546779 scopus 로고    scopus 로고
    • Isolation and characterization of PDE9A, a novel human cGMP-specific phosphodiesterase
    • Fisher DA, Smith JF, Pillar JS, St Denis SH, Cheng JB. Isolation and characterization of PDE9A, a novel human cGMP-specific phosphodiesterase. J Biol Chem 273: 15559-155564 (1998).
    • (1998) J Biol Chem , vol.273 , pp. 15559-155564
    • Fisher, D.A.1    Smith, J.F.2    Pillar, J.S.3    St Denis, S.H.4    Cheng, J.B.5
  • 2
    • 77956925425 scopus 로고    scopus 로고
    • Quantitative comparison of phosphodiesterase mRNA distribution in human brain and peripheral tissues
    • Lakics V, Karran EH, Boess FG. Quantitative comparison of phosphodiesterase mRNA distribution in human brain and peripheral tissues. Neuropharm 59(6): 367-374 (2010).
    • (2010) Neuropharm , vol.59 , Issue.6 , pp. 367-374
    • Lakics, V.1    Karran, E.H.2    Boess, F.G.3
  • 3
    • 84859991527 scopus 로고    scopus 로고
    • Phosphodiesterase9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo
    • Kleiman RJ, Chapin DS, Christoffersen C, Freeman J, Fonseca KR, Geoghegan KF, et al. Phosphodiesterase9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo. J Pharm Exp Ther 341: 396-409 (2012).
    • (2012) J Pharm Exp Ther , vol.341 , pp. 396-409
    • Kleiman, R.J.1    Chapin, D.S.2    Christoffersen, C.3    Freeman, J.4    Fonseca, K.R.5    Geoghegan, K.F.6
  • 4
    • 73249130591 scopus 로고    scopus 로고
    • Identification of a brain penetrant PDE9Ainhibitor utilizing prospective design and chemical enablement as a rapid leadoptimization strategy
    • Verhoest PR, Proulx-Lafrance C, Corman M, Chenard L, Helal CJ, Hou X, et al. Identification of a brain penetrant PDE9Ainhibitor utilizing prospective design and chemical enablement as a rapid leadoptimization strategy. J Med Chem 52: 7946-7949 (2009).
    • (2009) J Med Chem , vol.52 , pp. 7946-7949
    • Verhoest, P.R.1    Proulx-Lafrance, C.2    Corman, M.3    Chenard, L.4    Helal, C.J.5    Hou, X.6
  • 5
    • 77949362910 scopus 로고    scopus 로고
    • Phosphodiesterase inhibitors as potential cognition enhancing agents
    • Schmidt CJ. Phosphodiesterase inhibitors as potential cognition enhancing agents. Curr Topics Med Chem 10: 222-230 (2010).
    • (2010) Curr Topics Med Chem , vol.10 , pp. 222-230
    • Schmidt, C.J.1
  • 6
    • 77953530237 scopus 로고    scopus 로고
    • PF-04447943, a novel PDE9A inhibitor, increases cGMP levels in cerebrospinalfluid: Translation from non-clinical species to healthy human volunteers
    • Nicholas T, Evans R, Styren S, Qui R, Wang EQ, Nelson F, et al. PF-04447943, a novel PDE9A inhibitor, increases cGMP levels in cerebrospinalfluid: Translation from non-clinical species to healthy human volunteers. Alzheimers Dementia 5(4): P330 (2009).
    • (2009) Alzheimers Dementia , vol.5 , Issue.4
    • Nicholas, T.1    Evans, R.2    Styren, S.3    Qui, R.4    Wang, E.Q.5    Nelson, F.6
  • 7
    • 79959999316 scopus 로고    scopus 로고
    • 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
    • Hutson PH, Finger EN, Magliaro BC, Smith SM, Converso A, Sanderson PE, 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 61: 665-676 (2011).
    • (2011) Neuropharmacology , vol.61 , pp. 665-676
    • Hutson, P.H.1    Finger, E.N.2    Magliaro, B.C.3    Smith, S.M.4    Converso, A.5    Sanderson, P.E.6
  • 8
    • 81555212312 scopus 로고    scopus 로고
    • The selective phosphodiesterase 9 inhibitor PF-04447943 attenuates a scopolamine-induced deficit in a novel rodent attention task
    • Vardigan JD, Converso A, Hutson PH, Uslaner JM. The selective phosphodiesterase 9 inhibitor PF-04447943 attenuates a scopolamine-induced deficit in a novel rodent attention task. J Neurogenetics 25(4): 120-126 (2011).
    • (2011) J Neurogenetics , vol.25 , Issue.4 , pp. 120-126
    • Vardigan, J.D.1    Converso, A.2    Hutson, P.H.3    Uslaner, J.M.4
  • 9
    • 84868551510 scopus 로고    scopus 로고
    • Dendritic spine density deficits in the hippocampal CA1 region of young Tg2576 mice are ameliorated with the PDE9A inhibitor PF-04447943
    • Kleiman RJ, Lanz TA, Finley, JE, Bove SE, Majchrzak MJ, Becker SL, et al. Dendritic spine density deficits in the hippocampal CA1 region of young Tg2576 mice are ameliorated with the PDE9A inhibitor PF-04447943. Alzheimers Dementia 6(4): S563 (2010).
    • (2010) Alzheimers Dementia , vol.6 , Issue.4
    • Kleiman, R.J.1    Lanz, T.A.2    Finley, J.E.3    Bove, S.E.4    Majchrzak, M.J.5    Becker, S.L.6
  • 10
    • 0028883271 scopus 로고
    • Reduced nitric oxide responsive soluble guanylyl cyclase activity in the superior temporal cortex of patients with Alzheimer's disease
    • Bonkdale WL, Winblad B, Ravid R, Cowburn RF. Reduced nitric oxide responsive soluble guanylyl cyclase activity in the superior temporal cortex of patients with Alzheimer's disease. Neurosci Letters 187: 5-8 (1995).
    • (1995) Neurosci Letters , vol.187 , pp. 5-8
    • Bonkdale, W.L.1    Winblad, B.2    Ravid, R.3    Cowburn, R.F.4
  • 11
    • 9744227184 scopus 로고    scopus 로고
    • Reduced expression of NO-sensitive guanylyl cyclase in reactive astrocytes of Alzheimer disease, Crutzfeldt-Jakob disease, and multiple sclerosis brains
    • Baltrons MA, Pifarre P, Ferrer, Carot JM, Garcia A. Reduced expression of NO-sensitive guanylyl cyclase in reactive astrocytes of Alzheimer disease, Crutzfeldt-Jakob disease, and multiple sclerosis brains. Neurobiol Dis 17: 462-472 (2004).
    • (2004) Neurobiol Dis , vol.17 , pp. 462-472
    • Baltrons, M.A.1    Pifarre, P.2    Ferrer, C.J.M.3    Garcia, A.4
  • 12
    • 34249871389 scopus 로고    scopus 로고
    • Expression of the cGMP-specific phosphodiesterases 2 and 9 in normal and Alzheimer's disease human brains
    • Reyes-Irisarri E, Markerick-Van Ittersum M, Mengod G, de Vente J. Expression of the cGMP-specific phosphodiesterases 2 and 9 in normal and Alzheimer's disease human brains. Eur J Neurosci 25: 3332-3338 (2007).
    • (2007) Eur J Neurosci , vol.25 , pp. 3332-3338
    • Reyes-Irisarri, E.1    Markerick-Van Ittersum, M.2    Mengod, G.3    de Vente, J.4
  • 13
    • 84870465485 scopus 로고
    • American Psychiatric Association, Fourth Edition (DSM-IV); Washington DC
    • American Psychiatric Association. Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition (DSM-IV); Washington DC (1994).
    • (1994) Diagnostic and Statistical Manual of Mental Disorders
  • 14
    • 0021271971 scopus 로고
    • Clinical diagnosis of Alzheimer's disease: Report of the NINCDS-ADRDA Work Group under the auspices of Department of Health and Human Services Task Force on Alzheimer's Disease
    • McKhann G, Drachman D, Folstein M, Katzman R, Price D, Stadlan EM. Clinical diagnosis of Alzheimer's disease: report of the NINCDS-ADRDA Work Group under the auspices of Department of Health and Human Services Task Force on Alzheimer's Disease. Neurology 34(7): 939-944 (1984).
    • (1984) Neurology , vol.34 , Issue.7 , pp. 939-944
    • McKhann, G.1    Drachman, D.2    Folstein, M.3    Katzman, R.4    Price, D.5    Stadlan, E.M.6
  • 15
    • 0016823810 scopus 로고
    • "Mini-mental state". A practical method for grading the cognitive state of patients for the clinician
    • Folstein MF, Folstein SE, McHugh PR. "Mini-mental state". A practical method for grading the cognitive state of patients for the clinician. J Psychiatr Res 12(3): 189-198 (1975).
    • (1975) J Psychiatr Res , vol.12 , Issue.3 , pp. 189-198
    • Folstein, M.F.1    Folstein, S.E.2    McHugh, P.R.3
  • 16
    • 0018887732 scopus 로고
    • Pathological verification of ischemic score in differentiation of dementias
    • Rosen WG, Terry RD, Fuld PA, Katzman R, Peck A. Pathological verification of ischemic score in differentiation of dementias. Ann Neurol 7: 486-488 (1980).
    • (1980) Ann Neurol , vol.7 , pp. 486-488
    • Rosen, W.G.1    Terry, R.D.2    Fuld, P.A.3    Katzman, R.4    Peck, A.5
  • 17
    • 84868597007 scopus 로고    scopus 로고
    • Safety and pharmacokinetics of PF-04447943, a PDE9A inhibitor, in single and multiple dose Phase 1 studies in healthy volunteers
    • Evans R, Nicholas T, Le V, Qiu R, Martin W, Martin D, et al. Safety and pharmacokinetics of PF-04447943, a PDE9A inhibitor, in single and multiple dose Phase 1 studies in healthy volunteers. Alzheimers Dementia 6(4): S135 (2010).
    • (2010) Alzheimers Dementia , vol.6 , Issue.4
    • Evans, R.1    Nicholas, T.2    Le, V.3    Qiu, R.4    Martin, W.5    Martin, D.6
  • 18
    • 0021520020 scopus 로고
    • A new rating scale for Alzheimer's disease
    • Rosen WG, Mohs RC, Davis KL. A new rating scale for Alzheimer's disease. Am J Psychiatry 14(11): 1356-1364 (1984).
    • (1984) Am J Psychiatry , vol.14 , Issue.11 , pp. 1356-1364
    • Rosen, W.G.1    Mohs, R.C.2    Davis, K.L.3
  • 19
    • 0027985334 scopus 로고
    • The Neuropsychiatric Inventory: Comprehensive assessment of psychopathology in dementia
    • Cummings JL, Mega M, Grya K. Rosenberg-Thompson S, CarusiDA, Gornbein J. The Neuropsychiatric Inventory: comprehensive assessment of psychopathology in dementia. Neurology 44(12): 2308-2314 (1994).
    • (1994) Neurology , vol.44 , Issue.12 , pp. 2308-2314
    • Cummings, J.L.1    Mega, M.2    Grya, K.3    Rosenberg-Thompson, S.4    Carusi, D.A.5    Gornbein, J.6
  • 20
    • 0003412410 scopus 로고
    • Rockville, MD, U. S. Department of Health, Education, and Welfare, Public Health Service, Alcohol, Drug Abuse, and Mental Health Administration, NIMH
    • Guy W. ECDEU Assessment Manual for Psychopharmacology. Rockville, MD, U. S. Department of Health, Education, and Welfare, Public Health Service, Alcohol, Drug Abuse, and Mental Health Administration, NIMH (1976).
    • (1976) ECDEU Assessment Manual for Psychopharmacology
    • Guy, W.1
  • 22
    • 0032507788 scopus 로고    scopus 로고
    • Donepezil improves cognition and global function in Alzhiemer disease
    • Rogers SL, Doody RS, Mohs RC, Friedhoff LT. Donepezil improves cognition and global function in Alzhiemer disease. Arch Intern Med 158: 1021-1031 (1998).
    • (1998) Arch Intern Med , vol.158 , pp. 1021-1031
    • Rogers, S.L.1    Doody, R.S.2    Mohs, R.C.3    Friedhoff, L.T.4
  • 24
    • 10744228025 scopus 로고    scopus 로고
    • Decreased cerebrospinal fluid cGMP levels in patients with amyotrophic lateral sclerosis
    • Itzecka J. Decreased cerebrospinal fluid cGMP levels in patients with amyotrophic lateral sclerosis. J Neural Transm 111: 167-172 (2004).
    • (2004) J Neural Transm , vol.111 , pp. 167-172
    • Itzecka, J.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.