Search Results - "Chapin, Douglas"
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Reduction of brain kynurenic acid improves cognitive function
Published in The Journal of neuroscience (06-08-2014)“…The elevation of kynurenic acid (KYNA) observed in schizophrenic patients may contribute to core symptoms arising from glutamate hypofunction, including…”
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Discovery 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 Schizophrenia
Published in Journal of medicinal chemistry (27-08-2009)“…By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase (PDE) 10A inhibitors was identified. The structure-based drug…”
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3
Inhibition of the striatum-enriched phosphodiesterase PDE10A: A novel approach to the treatment of psychosis
Published in Neuropharmacology (01-08-2006)“…Phosphodiesterase 10A (PDE10A) is a recently identified cyclic nucleotide phosphodiesterase expressed primarily in dopaminoreceptive medium spiny neurons of…”
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4
Genetic deletion of the striatum-enriched phosphodiesterase PDE10A: Evidence for altered striatal function
Published in Neuropharmacology (01-08-2006)“…PDE10A is a newly identified phosphodiesterase that is highly expressed by the medium spiny projection neurons of the striatum. In order to investigate the…”
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5
Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo
Published in The Journal of pharmacology and experimental therapeutics (01-05-2012)“…Cyclic nucleotides are critical regulators of synaptic plasticity and participate in requisite signaling cascades implicated across multiple neurotransmitter…”
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6
Behavioral and neurochemical characterization of mice deficient in the phosphodiesterase-4B (PDE4B) enzyme
Published in Psychopharmacologia (01-03-2008)“…Rationale Phosphodiesterases (PDEs) belonging to the PDE4 family control intracellular concentrations of cyclic adenosine monophosphate (cAMP) by catalyzing…”
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CP-809,101, a selective 5-HT2C agonist, shows activity in animal models of antipsychotic activity
Published in Neuropharmacology (01-02-2007)“…CP-809,101 is a potent, functionally selective 5-HT(2C) agonist that displays approximately 100% efficacy in vitro. The aim of the present studies was to…”
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Antipsychotic profile of rolipram : efficacy in rats and reduced sensitivity in mice deficient in the phosphodiesterase-4b (PDE4B) enzyme
Published in Psychopharmacologia (01-06-2007)“…Recent studies provide evidence for reduced phosphodiesterase-4B (PDE4B) as a genetic susceptibility factor as well as suggesting an association of several…”
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Use of Structure-Based Design to Discover a Potent, Selective, In Vivo Active Phosphodiesterase 10A Inhibitor Lead Series for the Treatment of Schizophrenia
Published in Journal of medicinal chemistry (14-07-2011)“…Utilizing structure-based virtual library design and scoring, a novel chimeric series of phosphodiesterase 10A (PDE10A) inhibitors was discovered by…”
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Pharmacology of selective acetylcholinesterase inhibitors: implications for use in Alzheimer's disease
Published in European journal of pharmacology (13-02-2004)“…Cholinesterase inhibitors vary in their selectivity for acetylcholinesterase versus butyrylcholinesterase. We examined several cholinesterase inhibitors and…”
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Behavioral characterization of mice deficient in the phosphodiesterase-10A (PDE10A) enzyme on a C57/Bl6N congenic background
Published in Neuropharmacology (01-02-2008)“…The phenotype of genetically modified animals is strongly influenced by both the genetic background of the animal as well as environmental factors. We have…”
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Discovery 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 Schizophrenia † Coordinates of the PDE10A crystal structures have been deposited in the Protein Data Bank for compound 1 (3HQW), 2 (3HQY), 3 (3HQW) and 9 (3HR1)
Published in Journal of medicinal chemistry (27-08-2009)“…By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase (PDE) 10A inhibitors was identified. The structure-based drug…”
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13
Nuclear safety. Nuclear power plants and their fuel as terrorist targets
Published in Science (American Association for the Advancement of Science) (20-09-2002)Get full text
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14
The U.S. Election Assistance Commission: What Role in the Administration of Elections?
Published in Publius (01-10-2005)“…What role in the administration of elections will the new U.S. Election Assistance Commission (EAC) play, and how does that role differ from past federal…”
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15
Novel Benzisoxazole Derivatives as Potent and Selective Inhibitors of Acetylcholinesterase
Published in Journal of medicinal chemistry (01-08-1994)“…A series of N-benzylpiperidine benzisoxazoles has been developed as potent and selective inhibitors of the enzyme acetylcholinesterase (AChE). The…”
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16
Cross-site strain comparison of pharmacological deficits in the touchscreen visual discrimination test
Published in Psychopharmacology (01-11-2015)“…The low rate of success for identifying effective treatments for cognitive dysfunction has prompted recent efforts to improve pharmaceutical discovery and…”
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17
Non-Precinct Place Voting and Election Administration
Published in Election law journal (22-06-2011)Get full text
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18
Nuclear Power Plants and Their Fuel as Terrorist Targets
Published in Science (American Association for the Advancement of Science) (20-09-2002)“…In the wake of the 11 September attack on the World Trade Center, a large number of outrageous public statements appeared, claiming that any attack on a…”
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Design and Synthesis of 1-Heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one Derivatives as Potent, Selective Acetylcholinesterase Inhibitors
Published in Journal of medicinal chemistry (01-03-1995)“…Herein is described the synthesis and structure--activity relationship of a novel series of aromatic and heteroaromatic 3-(1-benzyl-4-piperidinyl)propan-1-one…”
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Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase
Published in Journal of medicinal chemistry (01-02-1991)“…A series of quinazolinediones and azaquinazolinediones is described which possess potent inhibitory activity toward the calcium-independent phosphodiesterase…”
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