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Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length constructDiscovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitorsStructural basis for the catalytic mechanism of human phosphodiesterase 9Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophreniaPotent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's diseaseUse of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophreniaPhosphodiesterases in the CNS: targets for drug developmentGlutamate receptor ion channels: structure, regulation, and functionInhibition of Phosphodiesterase 10A Increases the Responsiveness of Striatal Projection Neurons to Cortical StimulationPhosphodiesterase 10A inhibitor MP-10 effects in primates: comparison with risperidone and mechanistic implicationsImmunohistochemical localization of PDE10A in the rat brainInhibition of the striatal specific phosphodiesterase PDE10A ameliorates striatal and cortical pathology in R6/2 mouse model of Huntington's diseaseQuantification of MPTP-induced dopaminergic neurodegeneration in the mouse substantia nigra by laser capture microdissection.Antiparkinsonian actions of CP-101,606, an antagonist of NR2B subunit-containing N-methyl-d-aspartate receptors.The NR2B-selective NMDA receptor antagonist CP-101,606 exacerbates L-DOPA-induced dyskinesia and provides mild potentiation of anti-parkinsonian effects of L-DOPA in the MPTP-lesioned marmoset model of Parkinson's disease.Inhibition of the striatum-enriched phosphodiesterase PDE10A: a novel approach to the treatment of psychosis.The phencyclidine-like discriminative stimulus effects and reinforcing properties of the NR2B-selective N-methyl-D-aspartate antagonist CP-101 606 in rats and rhesus monkeys.An innovative design to establish proof of concept of the antidepressant effects of the NR2B subunit selective N-methyl-D-aspartate antagonist, CP-101,606, in patients with treatment-refractory major depressive disorder.The distribution of phosphodiesterase 2A in the rat brain.MPX-004 and MPX-007: New Pharmacological Tools to Study the Physiology of NMDA Receptors Containing the GluN2A Subunit.Differential Effects of an NR2B NAM and Ketamine on Synaptic Potentiation and Gamma Synchrony: Relevance to Rapid-Onset Antidepressant Efficacy.Translational psychiatry--light at the end of the tunnel.Effects of a NR2B selective NMDA glutamate antagonist, CP-101,606, on dyskinesia and Parkinsonism.Molecular mechanism of AMPA receptor noncompetitive antagonism.Prevention of ketamine-induced working memory impairments by AMPA potentiators in a nonhuman primate model of cognitive dysfunction.Phosphodiesterase 5A inhibitors improve functional recovery after stroke in rats: optimized dosing regimen with implications for mechanism.Quinazolin-4-one alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists: structure-activity relationship of the C-2 side chain tether.Functional characterization of CP-465,022, a selective, noncompetitive AMPA receptor antagonist.Positive allosteric modulation of AMPA receptors from efficacy to toxicity: the interspecies exposure-response continuum of the novel potentiator PF-4778574.CP-465,022, a selective noncompetitive AMPA receptor antagonist, blocks AMPA receptors but is not neuroprotective in vivo.Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists.Repeated estradiol treatment prevents MPTP-induced dopamine depletion in male mice.Pramipexole inhibits MPTP toxicity in mice by dopamine D3 receptor dependent and independent mechanisms.NR2B selective NMDA receptor antagonist CP-101,606 prevents levodopa-induced motor response alterations in hemi-parkinsonian rats.Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.Phosphodiesterase 10 inhibition reduces striatal excitotoxicity in the quinolinic acid model of Huntington's disease.Synthesis of novel pyrrolo[3,4-d]pyrazole-dicarboxylic acids and evaluation of their interaction with glutamate receptors.New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists.Synthesis, chiral resolution, and enantiopharmacology of a potent 2,3-benzodiazepine derivative as noncompetitive AMPA receptor antagonist.Role of estrogen receptors in neuroprotection by estradiol against MPTP toxicity.
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hulumtues
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հետազոտող
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Frank S. Menniti
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Frank S. Menniti
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Frank S. Menniti
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Frank S. Menniti
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Frank S. Menniti
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Frank S. Menniti
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Frank S. Menniti
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Frank S. Menniti
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Frank S. Menniti
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Frank S. Menniti
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Frank Menniti
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Frank S. Menniti
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Frank S. Menniti
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Frank S. Menniti
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Frank S. Menniti
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Frank S. Menniti
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P106
P1153
7003918109
P21
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0000-0003-2612-9534