Zobrazeno 1 - 10 of 13 pro vyhledávání: '"Jean-Michel Linget"'
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Akademický článek
Expression of drug transporters in the human skin: comparison in different species and models and its implication for drug development
Autor: Hanan Osman-Ponchet, Alexandre Gaborit, Jean-Michel Linget, Claire E. Wilson
Publikováno v: ADMET and DMPK, Vol 5, Iss 2, Pp 75-84 (2017)
It is clear that many drug transporters (both ABCs and SLCs) are present in the human skin. Different in vitro skin models can be used to investigate the role of drug transporters in the skin despite quantitative differences in expression profile acr
Externí odkaz: https://doaj.org/article/579dd159d3b445a3bdf71668f41747aa
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2
Application of the Tissue Composition–Based Model to Minipig for Predicting the Volume of Distribution at Steady State and Dermis-to-Plasma Partition Coefficients of Drugs Used in the Physiologically Based Pharmacokinetics Model in Dermatology
Autor: Severine H. Collet, Patrick Poulin, Claire E. Wilson, Nicolas Atrux-Tallau, Laurent F. Hennequin, Jean-Michel Linget
Publikováno v: Journal of Pharmaceutical Sciences. 108:603-619
The minipig continues to build a reputation as a viable alternative large animal model to predict humans in dermatology and toxicology studies. Therefore, it is essential to describe and predict the pharmacokinetics in that species to speed up the cl
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::994838e6c747b92246b183caf1ccbfd4
https://doi.org/10.1016/j.xphs.2018.09.001
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3
Comparison of the Effect of Skin Preparation Pads on Transepidermal Water Loss in Ex Vivo Human Skin
Autor: Jean-Michel Linget, Orla Duffy-Roger, Magali Kouidhi, Claire E. Wilson, Hanan Osman-Ponchet, Jeanne Marceau-Suissa, Alexandre Gaborit, Sandrine Anglars
Publikováno v: Dermatology and Therapy
Introduction Pre-treatment of the skin to remove scales and crusts prior to photodynamic therapy (PDT) is essential to enhance the uptake of topically applied methyl aminolevulinate (MAL) and to improve treatment efficacy. This study compared the eff
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d422384d7fde45bb874ee530872db9b
https://pubmed.ncbi.nlm.nih.gov/28710659
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4
Expression of drug transporters in the human skin: comparison in different species and models and its implication for drug development
Autor: Jean-Michel Linget, Hanan Osman-Ponchet, Claire E. Wilson, Alexandre Gaborit
Publikováno v: ADMET and DMPK
Volume 5
Issue 2
ADMET and DMPK, Vol 5, Iss 2, Pp 75-84 (2017)
It is clear that many drug transporters (both ABCs and SLCs) are present in the human skin. Different in vitro skin models can be used to investigate the role of drug transporters in the skin despite quantitative differences in expression profile acr
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b92a1af4fc8f349e7d3c971caae51bfd
https://hrcak.srce.hr/183283
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5
Conversion of 4-cyanomethyl-pyrazole-3-carboxamides into CB1 antagonists with lowered propensity to pass the blood–brain-barrier
Autor: Cooper Martin, Pia Karina Nørregaard, Jean-Michel Linget, Emelie Bjurling, Jean-Marie Receveur, Peter Aadal Nielsen, Anthony Murray, Thomas Högberg
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:453-457
A series of amides, amidines and amidoximes have been made from the corresponding nitrile compounds, to provide potent antagonists and inverse agonists for the CB1 receptor with considerably lower lipophiliciy, higher polar surface area and improved
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa1d4234d82a51c4fa6c2b46aad74f0e
https://doi.org/10.1016/j.bmcl.2009.12.003
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6
Evaluation of the GADD45α-GFP GreenScreen HC assay for rapid and reliable in vitro early genotoxicity screening
Autor: Jean-Michel Linget, Guy Bouvier, Nicolas Orsini, Anne-Pascale Luzy
Publikováno v: Journal of Applied Toxicology.
Twenty-two of Galderma's proprietary compounds were tested in the GADD45α-GFP ‘GreenScreen HC’ assay (GS), the SOS-ChromoTest and the Mini-Ames to evaluate GSs performance for early genotoxicity screening purposes. Forty more characterized compo
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::476e56a663c5b00d92d0654842346d09
https://doi.org/10.1002/jat.2793
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9
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues
Autor: Anne-Charlotte de Gouville, Pascal Grondin, Cécile Ruault, Jean Michel Linget, Francois Hyafil, Richard Frederic Labaudiniere, Alain Claude-Marie Daugan, Jorge Kirilovsky, Hervé Coste
Publikováno v: Journal of medicinal chemistry. 46(21)
Modification of the hydantoin ring in the previously described lead compound 2a has led to the discovery of compound 12a, tadalafil, a highly potent and highly selective PDE5 inhibitor. The replacement of the hydantoin in compound 2a by a piperazined
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa7f3a8a7236df75151a560bbf5d9d73
https://pubmed.ncbi.nlm.nih.gov/14521415
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10
Automation of metabolic stability studies in microsomes, cytosol and plasma using a 215 Gilson liquid handler
Autor: Jean-Michel Linget, Pierre du Vignaud
Publikováno v: Journal of pharmaceutical and biomedical analysis. 19(6)
A 215 Gilson liquid handler was used to automate enzymatic incubations using microsomes, cytosol and plasma. The design of automated protocols are described. They were based on the use of 96 deep well plates and on HPLC-based methods for assaying the
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ef7ec0eb6308ddd8697a72d7c2bc801
https://pubmed.ncbi.nlm.nih.gov/10698555
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