P. Lestage

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Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system

Antoine Taly, Pierre Lestage, Pierre-Jean Corringer, 2009, Nature Reviews Drug Discovery.

Working memory deficits and related disinhibition of the cAMP/PKA/CREB are alleviated by prefrontal α4β2*-nAChRs stimulation in aged mice

D. Béracochéa, C. Louis, P. Lestage, 2013, Neurobiology of Aging.

Rapid and precise method to locate microdialysis probe implantation in the rodent brain

P. Lestage, M. Suaud-Chagny, B. Guiard, 2004, Journal of Neuroscience Methods.

New quinolinic derivatives as centrally active antioxidants.

P. Lestage, P. Casara, B. Lockhart, 2000, Bioorganic & medicinal chemistry letters.

Synthesis of a cytisine/epibatidine hybrid: a radical approach

P. Lestage, R. Bureau, J. Rouden, 2010 .

Structure-activity relationships in a series of 2(1H)-quinolones bearing different acidic function in the 3-position: 6,7-dichloro-2(1H)-oxoquinoline-3-phosphonic acid, a new potent and selective AMPA/kainate antagonist with neuroprotective properties.

P. Lestage, A. Cordi, P. Morain, 1996, Journal of medicinal chemistry.

Localization of cerebral protein synthesis alterations in response to water deprivation in rats.

M. Jouvet, P. Lestage, P. Bobillier, 1988, Neuroendocrinology.

Novel 2-alkylamino-1,4-benzoxazine derivatives as potent neuroprotective agents: structure-activity relationship studies.

P. Gressens, P. Lestage, L. Schwendimann, 2005, Journal of medicinal chemistry.

In vivo neuroprotective effects of the novel imidazolyl nitrone free-radical scavenger (Z)-alpha-[2-thiazol-2-yl)imidazol-4-yl]-N-tert-butylnitrone (S34176).

P. Lestage, S. Goldstein, B. Lockhart, 2005, European journal of pharmacology.

Protective effect of the antioxidant 6-ethoxy-2,2-pentamethylen-1,2-dihydroquinoline (S 33113) in models of cerebral neurodegeneration.

P. Lestage, P. Casara, B. Lockhart, 2001, European journal of pharmacology.

Molecular characterization of the AMPA-receptor potentiator S70340 in rat primary cortical culture: Whole-genome expression profiling

L. Danober, D. Caignard, P. Lestage, 2011, Neuroscience Research.

Plasma, Cerebrospinal Fluid, and Brain Distribution of 14C‐Melatonin in Rat: A Biochemical and Autoradiographic Study

P. Lestage, B. Claustrat, P. Vitte, 1988, Journal of pineal research.

Involvement of nicotinergic mechanisms in thyrotropin-releasing hormone-induced neurologic recovery after concussive head injury in the mouse.

P. Lestage, J. Lepagnol, A. Iris-Hugot, 1998, European journal of pharmacology.

Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors

O. Nosjean, P. Lestage, J. Arrang, 2017, European journal of pharmacology.

In vivo pharmacological profile of S 38093, a novel histamine H3 receptor inverse agonist

L. Danober, B. Martin, P. Lestage, 2017, European journal of pharmacology.

Synthesis and pharmacological evaluation of new 1,2-dithiolane based antioxidants.

P. Lestage, Y. Ginot, S. Goldstein, 2003, European journal of medicinal chemistry.

Synthesis and pharmacological evaluation of a second generation of pyridothiadiazine 1,1-dioxides acting as AMPA potentiators.

L. Danober, O. Diouf, P. Lestage, 2008, Bioorganic & medicinal chemistry.

Identification of 9-fluoro substituted (-)-cytisine derivatives as ligands with high affinity for nicotinic receptors.

P. Lestage, J. Rouden, M. Lasne, 2010, Bioorganic & medicinal chemistry letters.

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.

L. Danober, C. Louis, L. Olsen, 2014, Journal of medicinal chemistry.

Synthesis, pharmacological and structural characterization, and thermodynamic aspects of GluA2-positive allosteric modulators with a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide scaffold.

L. Danober, L. Olsen, P. Lestage, 2013, Journal of medicinal chemistry.

Development of thiophenic analogues of benzothiadiazine dioxides as new powerful potentiators of 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) receptors.

O. Nosjean, L. Danober, P. Lestage, 2013, Journal of medicinal chemistry.

New substituted aryl esters and aryl amides of 3,4-dihydro-2H-1,2,4- benzothiadiazine 1,1-dioxides as positive allosteric modulators of AMPA receptors

L. Danober, P. Tullio, P. Lestage, 2011 .

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.

L. Danober, P. Tullio, P. Lestage, 2007, Journal of medicinal chemistry.

4H-1,2,4-Pyridothiadiazine 1,1-dioxides and 2,3-dihydro-4H-1,2, 4-pyridothiadiazine 1,1-dioxides chemically related to diazoxide and cyclothiazide as powerful positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid receptors: design, synthesis, pharmacology,

J Delarge, P Lebrun, M. Spedding, 1998, Journal of medicinal chemistry.

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.

L. Danober, T. Colson, P. Lestage, 2021, ACS chemical neuroscience.

Synthesis, structure, and neuroprotective properties of novel imidazolyl nitrones.

P. Lestage, B. Lockhart, E. Raimbaud, 2000, Journal of medicinal chemistry.

Thermodynamic Characterization of New Positive Allosteric Modulators Binding to the Glutamate Receptor A2 Ligand-Binding Domain: Combining Experimental and Computational Methods Unravels Differences in Driving Forces

Chris Oostenbrink, Lars Olsen, Ann-Beth Nørholm, 2014, J. Chem. Inf. Model..

Chemical and pharmacological aspects of heteroaryl-nitrones.

P. Lestage, S. Goldstein, 2000, Current medicinal chemistry.

Synthesis, structure, and neuroprotective properties of novel imidazolyl nitrones.

P. Lestage, B. Lockhart, E. Raimbaud, 2000, Journal of Medicinal Chemistry.

An In Vivo Kinetic Model with L‐[35S]Methionine for the Determination of Local Cerebral Rates for Methionine Incorporation into Protein in the Rat

G. Debilly, P. Lestage, P. Vitte, 1987, Journal of neurochemistry.

Apomorphine-induced inhibition of substantia nigra dopamine neurons: Effects of unilateral injection through the internal carotid artery

G. Chouvet, P. Lestage, P. Vitte, 1989, Neuroscience Letters.

Novel quinolinone-phosphonic acid AMPA antagonists devoid of nephrotoxicity.

B. Meldrum, P. Lestage, A. Cordi, 2002, Farmaco.

S 17092: a prolyl endopeptidase inhibitor as a potential therapeutic drug for memory impairment. Preclinical and clinical studies.

P. Lestage, R. Jochemsen, G. de Nanteuil, 2006, CNS drug reviews.

Differential effects of chronic dehydration on protein synthesis in neurons of the rat hypothalamus

M. Jouvet, G. Debilly, P. Lestage, 1985, Neuroscience Letters.

Partial agonist and neuromodulatory activity of S 24795 for alpha7 nAChR responses of hippocampal interneurons

R. Papke, P. Lestage, A. Placzek, 2007, Neuropharmacology.

A chronic arterial and venous cannulation method for freely moving rats

R. Minot, E. Broussolle, P. Lestage, 1985, Journal of Neuroscience Methods.

Effects of positive modulators of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type glutamate receptors in a benzodiazepine-induced deficit of spatial discrimination in mice

D. Béracochéa, C. Louis, P. Lestage, 2012, Journal of psychopharmacology.

Inhibition of l-homocysteic acid and buthionine sulphoximine-mediated neurotoxicity in rat embryonic neuronal cultures with α-lipoic acid enantiomers

P. Lestage, B. Lockhart, D. Peyroulan, 2000, Brain Research.

The effects of melatonin and pinealectomy upon local cerebral glucose utilization in awake unrestrained rats are restricted to a few specific regions

P. Lestage, B. Claustrat, P. Vitte, 1989, Brain Research.

Ring-fused thiadiazines as core structures for the development of potent AMPA receptor potentiators.

L. Danober, P. Lestage, B. Pirotte, 2010, Current medicinal chemistry.

New procognitive enhancers acting at the histamine H3 and AMPA receptors reverse natural forgetting in mice: comparisons with donepezil and memantine in the object recognition task

D. Béracochéa, L. Danober, C. Louis, 2019, Behavioural pharmacology.

Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors

D. Bertrand, L. Danober, C. Louis, 2017, PloS one.

Synthesis and Pharmacology of Mono-, Di-, and Trialkyl-Substituted 7-Chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-Dioxides Combined with X-ray Structure Analysis to Understand the Unexpected Structure-Activity Relationship at AMPA Receptors.

L. Danober, P. Lestage, J. Kastrup, 2016, ACS Chemical Neuroscience.

DRUG FOCUS: S 18986: A Positive Allosteric Modulator of AMPA‐Type Glutamate Receptors Pharmacological Profile of a Novel Cognitive Enhancer

L. Danober, P. Lestage, K. Bernard, 2010, CNS neuroscience & therapeutics.

S 18986 reverses spatial working memory impairments in aged mice: comparison with memantine

D. Béracochéa, C. Louis, P. Lestage, 2011, Psychopharmacology.

The Serotonin1A Receptor Partial Agonist S15535 [4-(Benzodioxan-5-yl)1-(indan-2-yl)piperazine] Enhances Cholinergic Transmission and Cognitive Function in Rodents: A Combined Neurochemical and Behavioral Analysis

R. Jaffard, M. Millan, A. Gobert, 2004, Journal of Pharmacology and Experimental Therapeutics.

Cognition enhancing or neuroprotective compounds for the treatment of cognitive disorders: why? when? which?

P. Lestage, B. Lockhart, 2003, Experimental Gerontology.

Pharmacological modulation of contextual “episodic-like” memory in aged mice

D. Béracochéa, C. Louis, P. Lestage, 2010, Behavioural Brain Research.

Effects of S 18986-1, a novel cognitive enhancer, on memory performances in an object recognition task in rats.

P. Lestage, C. Lebrun, E. Pillière, 2000, European journal of pharmacology.

Neuroprotection: Present and future.

R. Bordet, P. Lestage, B. Onténiente, 2007, Therapie.

Differential inhibition of [3H]-oxotremorine-M and [3H]-quinuclinidyl benzilate binding to muscarinic receptors in rat brain membranes with acetylcholinesterase inhibitors

P. Lestage, C. Steward, M. Closier, 2001, Naunyn-Schmiedeberg's Archives of Pharmacology.

[In vivo exploration of cerebral ischemia: use of neuroprotective agents in animal studies].

P. Lestage, B. Lockhart, A. Roger, 2002, Therapie.

S18986: a positive modulator of AMPA-receptors enhances (S)-AMPA-mediated BDNF mRNA and protein expression in rat primary cortical neuronal cultures.

J. Boutin, P. Lestage, J. Galizzi, 2007, European journal of pharmacology.

S 18986, a positive modulator of AMPA receptors with cognition-enhancing properties, increases ACh release in the hippocampus of young and aged rat

M. Giovannini, P. Lestage, S. Rosi, 2004, Neuroscience Letters.

(S)-2,3-dihydro-[3,4]cyclopentano-1,2,4-benzothiadiazine-1,1-dioxide: (S18986-1) a positive modulator of AMPA receptors enhances (S)-AMPA-mediated [3H]noradrenaline release from rat hippocampal and frontal cortex slices.

P. Lestage, M. Closier, B. Lockhart, 2000, European journal of pharmacology.

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.

L. Danober, P. Chiap, P. Lestage, 2010, Journal of Medicinal Chemistry.

In Vivo Cross-sectional Characterization of Cerebral Alterations Induced by Intracerebroventricular Administration of Streptozotocin

F. Petit, M. Dhenain, C. Jan, 2012, PloS one.

Modulatory effects of S 38232, a non α-7 containing nicotine acetylcholine receptor agonist on network activity in the mouse hippocampus

E. Cherubini, L. Danober, P. Lestage, 2010, Neuropharmacology.

S 17092-1, A New Post-Proline Cleaving Enzyme Inhibitor: Memory Enhancing Effects and Substance P Neuromodulatory Activity

P. Lestage, D. Favale, P. Grève, 1998 .

Pharmacological profile of S 76892, a new ligand at nicotinic α7-subtype receptors

D. Béracochéa, L. Danober, C. Louis, 2015 .

Stress and local cerebral blood flow: studies on restrained and unrestrained rats

P. Lestage, J. Seylaz, F. Lasbennes, 2004, Experimental Brain Research.

S 12024-2, A Cognitive Enhancer, Interacts with Nicotinic Neurotransmission

P. Lestage, M. Méen, P. Morain, 1998 .