Search Results - "Bryce, Dianne K."
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Negative allosteric modulation of the mGluR5 receptor reduces repetitive behaviors and rescues social deficits in mouse models of autism
Published in Science translational medicine (25-04-2012)“…Neurodevelopmental disorders such as autism and fragile X syndrome were long thought to be medically untreatable, on the assumption that brain dysfunctions…”
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Positive allosteric modulation of AMPA receptors from efficacy to toxicity: the interspecies exposure-response continuum of the novel potentiator PF-4778574
Published in The Journal of pharmacology and experimental therapeutics (01-10-2013)“…α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) positive allosteric modulation (i.e., "potentiation") has been proposed to overcome…”
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Characterization of the Onset, Progression, and Reversibility of Morphological Changes in Mouse Lung after Pharmacological Inhibition of Leucine-Rich Kinase 2 Kinase Activity
Published in The Journal of pharmacology and experimental therapeutics (01-04-2021)“…Gain-of-function mutations in leucine-rich kinase 2 (LRRK2) are associated with increased incidence of Parkinson disease (PD); thus, pharmacological inhibition…”
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The Discovery and Characterization of the α‑Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Potentiator N‑{(3S,4S)‑4-[4-(5-Cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242)
Published in Journal of medicinal chemistry (28-05-2015)“…A unique tetrahydrofuran ether class of highly potent α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor potentiators has been identified using…”
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Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models
Published in Journal of medicinal chemistry (11-02-2010)“…A novel alpha 7 nAChR agonist, 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (24, CP-810,123), has been identified as a potential…”
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Discovery and Characterization of a Novel Dihydroisoxazole Class of α‑Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) Receptor Potentiators
Published in Journal of medicinal chemistry (27-11-2013)“…Positive allosteric modulators (“potentiators”) of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors (AMPAR) enhance excitatory…”
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Discovery of 4-(5-Methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a Novel α7 Nicotinic Acetylcholine Receptor Agonist for the Treatment of Cognitive Disorders in Schizophrenia: Synthesis, SAR Development, and in Vivo Efficacy in Cognition Models
Published in Journal of medicinal chemistry (11-02-2010)“…A novel α7 nAChR agonist, 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (24, CP-810,123), has been identified as a potential treatment…”
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Activity and Distribution of Binding Sites in Brain of a Nonpeptide Substance P (NK$_1$) Receptor Antagonist
Published in Science (American Association for the Advancement of Science) (25-01-1991)“…CP-96,345, a nonpeptide substance P antagonist, is selective for the tachykinin NK$_1$ receptor. The compound binds to a single population of sites in guinea…”
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Biaryl piperidines as potent and selective delta opioid receptor ligands
Published in Bioorganic & medicinal chemistry letters (15-01-2010)“…The design and synthesis of novel opiates are reported. Based on the message-address principle a novel class of 4,4- and 3,3-biaryl piperidines was designed…”
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5-Phenyl-3-ureidobenzazepin-2-ones as Cholecystokinin-B Receptor Antagonists
Published in Journal of medicinal chemistry (01-10-1994)Get full text
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Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist
Published in Bioorganic & medicinal chemistry letters (03-02-1998)“…The synthesis and SAR of benzylamine side chain analogs of the NK-1 receptor antagonist CP-99,994 are described. The 5-trifluoromethoxy analog, CP-122,721,…”
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Synthesis of conformationally restricted substance P antagonists
Published in Bioorganic & medicinal chemistry letters (01-01-1995)“…Reaction of CP-99,994 ( 1) with benzyl chloromethyl ether under basic conditions produced the novel 1,6-diazabicyclo[3.2.1]octane system in good yield; analogs…”
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Discovery of CP-96,345 and its characterization in disease models involving substance P
Published in Regulatory peptides (02-07-1993)“…Studies with CP-96,345, a potent, selective, orally active, nonpeptide NK1 receptor antagonist, have provided considerable insight into SP pharmacology. Rather…”
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Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel μ opioid receptor ligands
Published in Bioorganic & medicinal chemistry letters (20-03-2000)“…3-Amino-3-phenylpropionamide derivatives were produced as small molecule mimics of the cyclic octapeptide octreotide from readily available imine 1. The…”
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Aza-Tricyclic Substance P Antagonists
Published in Journal of medicinal chemistry (01-09-1994)“…The synthesis and structure-activity relationships of a series of aza-tricyclic analogs of the quinuclidine substance P (SP) antagonist 1 are described. The SP…”
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A water soluble benzazepine cholecystokinin-B receptor antagonist
Published in Bioorganic & medicinal chemistry letters (07-09-1995)“…A series of 5-substituted-3-ureidobenzazepin-2-ones bearing ioizable functionality was synthesized as potential cholecystokinin-B (CCK-B) receptor antagonists…”
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Design of novel cholecystokinin-B receptor ligands based on the ‘double-ring system’ approach
Published in Regulatory peptides (27-08-1996)“…A structurally novel series of cholecystokinin-B (CCK-B) receptor ligands has been designed and synthesized based on the ‘double-ring system’ theory of…”
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