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Your search keyword '"E. Boucherat"' showing total 3 results
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3 results on '"E. Boucherat"'

1. Evaluation of the Reproducibility of Nasal Allergen Challenge in Mild Allergic Asthmatics to Support Drug Development

Author

J. Smith, Imran Satia, Suzanne Beaudin, E. Boucherat, Paul M. O'Byrne, M. Hokom, Prajna Banerjee, Paul K. Keith, Gizette Sperinde, John-Paul Oliveria, Y. Xie, Tracy Staton, N. Alsaji, Jennifer Wattie, Gail M. Gauvreau, Xiaotian Ju, Roma Sehmi, Jonathan MacLean, Rebecca N. Bauer, Olga Li, Lesley Wiltshire, Caroline Munoz, Doron D. Sommer, and Ruth P. Cusack

Subjects
Allergen challenge, Reproducibility, Drug development, business.industry, Immunology, Medicine, business
Published
2020
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2. Identification of a series of 1,3,4-oxadiazol-2-amines as potent alpha-7 agonists with efficacy in the novel object recognition model of cognition.

Author

Skidmore J, Atcha Z, Boucherat E, Castelletti L, Chen DW, Coppo FT, Cutler L, Dunsdon RM, Heath BM, Hutchings R, Hurst DN, Javed S, Martin S, Maskell ES, Norton D, Pemberton DJ, Redshaw S, Rutter R, Sehmi SS, Scoccitti T, Temple HE, Theobald P, Ward RW, and Wilson DM

Subjects
Animals, Dogs, Nicotinic Agonists chemistry, alpha7 Nicotinic Acetylcholine Receptor, Cognition drug effects, Nicotinic Agonists pharmacology, Receptors, Nicotinic drug effects
Abstract

A series of α7 nicotinic acetylcholine receptor full-agonists with a 1,3,4-oxadiazol-2-amine core has been discovered. Systematic exploration of the structure-activity relationships for both α7 potency and selectivity with respect to interaction with the hERG channel are described. Further profiling led to the identification of compound 22, a potent full agonist showing efficacy in the novel object recognition model of cognition enhancement., (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Published
2012
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3. The discovery of 2-fluoro-N-(3-fluoro-4-(5-((4-morpholinobutyl)amino)-1,3,4-oxadiazol-2-yl)phenyl)benzamide, a full agonist of the alpha-7 nicotinic acetylcholine receptor showing efficacy in the novel object recognition model of cognition enhancement.

Author

Skidmore J, Atcha Z, Boucherat E, Castelletti L, Chen DW, Coppo FT, Cutler L, Dunsdon RM, Heath BM, Hutchings R, Hurst DN, Javed S, Martin S, Maskell ES, Norton D, Pemberton DJ, Redshaw S, Rutter R, Sehmi SS, Scoccitti T, Temple HE, Theobald P, Ward RW, and Wilson DM

Subjects
Animals, Dose-Response Relationship, Drug, Rabbits, Receptors, Nicotinic chemistry, alpha7 Nicotinic Acetylcholine Receptor, Cognition drug effects, Nicotinic Agonists pharmacology, Receptors, Nicotinic drug effects
Abstract

A series of α7 nicotinic acetylcholine receptor full agonists with a 1,3,4-oxadiazol-2-amine core has been discovered. Early lead 1 was found to have a limited therapeutic index with respect to its potential for cardiovascular side effects. Further optimisation of this series led to the identification of 22 a potent full agonist showing efficacy at a dose of 0.1mg/kg in the novel object recognition model of cognition enhancement. Comparison of 1 with 22 demonstrated the latter to have an improved oral pharmacokinetic profile and cardiovascular therapeutic index., (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Published
2012
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