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Gamma-secretase activating protein, a therapeutic target for Alzheimer's disease
Accumulation of neurotoxic amyloid-β is a major hallmark of Alzheimer’s disease. Formation of amyloid-β is catalysed by γ-secretase, a protease with numerous substrates. Little is known about theExpand
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Structural definition of the C5a C terminus by two‐dimensional nuclear magnetic resonance spectroscopy
The serum glycoprotein C5a, which is derived from the proteolytic cleavage of complement protein C5, has been implicated in the pathogenesis of a number of inflammatory and allergic conditions.Expand
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Preclinical profile of ITI-214, an inhibitor of phosphodiesterase 1, for enhancement of memory performance in rats
RationaleTherapeutic agents for memory enhancement in psychiatric disorders, such as schizophrenia, are urgently needed.ObjectiveThe aim of this study is to characterize the preclinical profile ofExpand
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Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases.
A diverse set of 3-aminopyrazolo[3,4-d]pyrimidinones was designed and synthesized. The structure-activity relationships of these polycyclic compounds as phosphodiesterase 1 (PDE1) inhibitors wereExpand
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CGS 9343B, a novel, potent, and selective inhibitor of calmodulin activity.
1,3-Dihydro-1-[1-[(4-methyl-4H,6H-pyrrolo[1,2-a][4,1]- benzoxazepin-4-yl)methyl]-4-piperidinyl]-2H-benzimidazol-2-o ne (1:1) maleate was synthesized in six steps from methyl anthranilate andExpand
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Serotonin modulates the dissociation of [3H]imipramine from human platelet recognition sites.
The dissociation of [3H]imipramine from human platelet membrane recognition sites was studied. Simple exponential dissociation kinetics were observed indicating an apparent homogeneous class of sitesExpand
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Isoform-Specific Localization of A-RAF in Mitochondria
ABSTRACT RAF kinase is a family of isoforms including A-RAF, B-RAF, and C-RAF. Despite the important role of RAF in cell growth and proliferation, little evidence exists for isoform-specific functionExpand
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Functional profile of a novel modulator of serotonin, dopamine, and glutamate neurotransmission
RationaleSchizophrenia remains among the most prevalent neuropsychiatric disorders, and current treatment options are accompanied by unwanted side effects. New treatments that better address coreExpand
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Human brain receptor alterations in suicide victims
A comparison was made of human postmortem muscarinic-cholinergic, beta-adrenergic and serotonergic (presynaptic) recognition sites in cortical tissues derived from suicide and homicide (control)Expand
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A fluorometric assay for peptidyl alpha-amidation activity using high-performance liquid chromatography.
A rapid and sensitive method for the determination of peptidyl alpha-amidation activity has been developed and is based on reverse-phase high-performance liquid chromatographic separation andExpand
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