Search Results - "Thomas, Jean‐Yves"
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Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors
Published in PloS one (08-09-2017)“…S 47445 is a novel positive allosteric modulator of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors (AMPA-PAM). S 47445 enhanced…”
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In vivo pharmacological profile of S 38093, a novel histamine H3 receptor inverse agonist
Published in European journal of pharmacology (15-05-2017)“…S 38093, a novel histamine H3 receptor inverse agonist, was tested in a series of neurochemical and behavioral paradigms designed to evaluate its procognitive…”
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Development of Thiochroman Dioxide Analogues of Benzothiadiazine Dioxides as New Positive Allosteric Modulators of α‑Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors
Published in ACS chemical neuroscience (21-07-2021)“…On the basis of the activity of 1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of AMPA receptors, thiochroman 1,1-dioxides were designed…”
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New Fluorinated 1,2,4-Benzothiadiazine 1,1-Dioxides: Discovery of an Orally Active Cognitive Enhancer Acting through Potentiation of the 2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic Acid Receptors
Published in Journal of medicinal chemistry (25-02-2010)“…In the search of a potent cognitive enhancer, a series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as positive…”
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Positive Allosteric Modulators of 2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic Acid Receptors Belonging to 4-Cyclopropyl-3,4-dihydro-2 H -1,2,4-pyridothiadiazine Dioxides and Diversely Chloro-Substituted 4-Cyclopropyl-3,4-dihydro-2 H -1,2,4-benzothiadiazine 1,1-Dioxides
Published in Journal of medicinal chemistry (26-11-2014)Get full text
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Design, Synthesis, and Pharmacology of Novel 7-Substituted 3,4-Dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of AMPA Receptors
Published in Journal of medicinal chemistry (28-06-2007)“…A series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as potentiators of AMPA receptors. Attention was paid to the…”
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Synthesis and pharmacological evaluation of a second generation of pyridothiadiazine 1,1-dioxides acting as AMPA potentiators
Published in Bioorganic & medicinal chemistry (01-12-2008)“…Taking into account structure-activity relationships obtained with our previous series, new diversely substituted 1,2,4-pyridothiadiazine 1,1-dioxides were…”
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DRUG FOCUS: S 18986: A Positive Allosteric Modulator of AMPA‐Type Glutamate Receptors Pharmacological Profile of a Novel Cognitive Enhancer
Published in CNS neuroscience & therapeutics (01-10-2010)“…Alpha‐amino‐3‐hydroxy‐5‐methyl‐4‐isoxazole‐propionic acid (AMPA) type glutamate receptors are critical for synaptic plasticity and induction of long‐term…”
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Positive Allosteric Modulators of 2‑Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic Acid Receptors Belonging to 4‑Cyclopropyl-3,4-dihydro‑2H‑1,2,4-pyridothiadiazine Dioxides and Diversely Chloro-Substituted 4‑Cyclopropyl-3,4-dihydro‑2H‑1,2,4-benzothiadiazine 1,1-Dioxides
Published in Journal of medicinal chemistry (26-11-2014)“…Two 4-ethyl-substituted pyridothiadiazine dioxides belonging to α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor positive allosteric…”
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Novel quinolinone-phosphonic acid AMPA antagonists devoid of nephrotoxicity
Published in Farmaco (Società chimica italiana : 1989) (01-10-2002)“…We reported previously the synthesis and structure–activity relationships (SAR) in a series of 2-(1 H)-oxoquinolines bearing different acidic functions in the…”
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In vivo characterization of s44858, a positive allosteric modulator of ampa receptors and GluN2B selective non-competitive nmda antagonist
Published in Alzheimer's & dementia (01-07-2015)Get full text
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