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Your search keyword '"Boléa, Christelle"' showing total 12 results
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12 results on '"Boléa, Christelle"'

1. Effect of the Metabotropic Glutamate Receptor Type 5 Negative Allosteric Modulator Dipraglurant on Motor and Non-Motor Symptoms of Parkinson’s Disease

Author

Epping-Jordan, Mark P., primary, Girard, Françoise, additional, Bessis, Anne-Sophie, additional, Mutel, Vincent, additional, Boléa, Christelle, additional, Derouet, Francis, additional, Bessif, Abdelhak, additional, Mingard, Brice, additional, Barbier, Stéphanie, additional, Paradis, Justine S., additional, Rocher, Jean-Philippe, additional, Lütjens, Robert, additional, Kalinichev, Mikhail, additional, and Poli, Sonia, additional

Published
2023
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4. Characterization of the Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 ADX88178 in Rodent Models of Neuropsychiatric Disorders

Author

Kalinichev, Mikhail, primary, Le Poul, Emmanuel, additional, Boléa, Christelle, additional, Girard, Françoise, additional, Campo, Brice, additional, Fonsi, Massimiliano, additional, Royer-Urios, Isabelle, additional, Browne, Susan E., additional, Uslaner, Jason M., additional, Davis, Matthew J., additional, Raber, Jacob, additional, Duvoisin, Robert, additional, Bate, Simon T., additional, Reynolds, Ian J., additional, Poli, Sonia, additional, and Celanire, Sylvain, additional

Published
2014
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5. A Potent and Selective Metabotropic Glutamate Receptor 4 Positive Allosteric Modulator Improves Movement in Rodent Models of Parkinson's Disease

Author

Le Poul, Emmanuel, primary, Boléa, Christelle, additional, Girard, Francoise, additional, Poli, Sonia, additional, Charvin, Delphine, additional, Campo, Brice, additional, Bortoli, Julien, additional, Bessif, Abdhelak, additional, Luo, Bin, additional, Koser, Amy Jo, additional, Hodge, Lisa M., additional, Smith, Karen M., additional, DiLella, Anthony G., additional, Liverton, Nigel, additional, Hess, Fred, additional, Browne, Susan E., additional, and Reynolds, Ian J., additional

Published
2012
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6. Discovery of 1,5-Disubstituted Pyridones: A New Class of Positive Allosteric Modulators of the Metabotropic Glutamate 2 Receptor

Author

Cid, Jose María, primary, Duvey, Guillaume, additional, Cluzeau, Philippe, additional, Nhem, Vanthea, additional, Macary, Karim, additional, Raux, Alexandre, additional, Poirier, Nicolas, additional, Muller, Jessica, additional, Boléa, Christelle, additional, Finn, Terry, additional, Poli, Sonia, additional, Epping-Jordan, Mark, additional, Chamelot, Emilie, additional, Derouet, Francis, additional, Girard, Francoise, additional, Macdonald, Gregor J., additional, Vega, Juan Antonio, additional, de Lucas, Ana Isabel, additional, Matesanz, Encarnación, additional, Lavreysen, Hilde, additional, Linares, María Lourdes, additional, Oehlrich, Daniel, additional, Oyarzábal, Julen, additional, Tresadern, Gary, additional, Trabanco, Andrés A., additional, Andrés, Jose Ignacio, additional, Le Poul, Emmanuel, additional, Imogai, Hassan, additional, Lutjens, Robert, additional, and Rocher, Jean-Philippe, additional

Published
2010
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12. mGluR5 negative allosteric modulators overview: a medicinal chemistry approach towards a series of novel therapeutic agents.

Author

Rocher JP, Bonnet B, Boléa C, Lütjens R, Le Poul E, Poli S, Epping-Jordan M, Bessis AS, Ludwig B, and Mutel V

Subjects
Allosteric Regulation drug effects, Chemistry, Pharmaceutical, Drug Design, Heterocyclic Compounds chemical synthesis, Heterocyclic Compounds chemistry, Positron-Emission Tomography, Pyridines chemical synthesis, Pyridines chemistry, Receptor, Metabotropic Glutamate 5, Receptors, Metabotropic Glutamate chemistry, Receptors, Metabotropic Glutamate metabolism, Structure-Activity Relationship, Heterocyclic Compounds pharmacology, Pyridines pharmacology, Receptors, Metabotropic Glutamate antagonists & inhibitors
Abstract

Allosteric modulators of metabotropic glutamate receptors (mGluR) subtypes 1-8 have been shown to offer a valid way to develop small molecule non aminoacid-like therapeutics that can be administered orally and that readily cross the blood-brain barrier. Allosteric modulators of glutamatergic receptors and in particular mGluR5 have emerged as a novel and highly desirable class of compounds for the treatment of central nervous system (CNS) disorders and peripheral disorders. This article provides medicinal chemistry highlights around the chemical classes of potent and highly selective mGluR5 negative allosteric modulators (NAMs) and their therapeutic potential. In addition, it describes the medicinal chemistry approach from the discovery to the clinical candidate selection of a new series of heteroaryl-butynylpyridines targeting mGluR5. The multiparametric optimization of the initial starting point which ended in the selection of potential clinical candidates combining the best pharmacophoric features is presented. The pharmacological properties are reported and support the interest of these agents for new therapeutic approaches. Furthermore, a summary of the diverse mGluR5 Positron Emission Tomography (PET) radioligands is reported.

Published
2011
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