Zobrazeno 1 - 10
of 112
pro vyhledávání: '"Jean-François Liégeois"'
Autor:
Stephan A. Pless, Marie Vitello, Dominique Engel, Vincent Seutin, Sofian Ringlet, Laurent Massotte, Jean-François Liégeois, Jochen Roeper, Kevin Jehasse, Bernard Lakaye, Sebastian Hartmann, Han Chow Chua, Romain Vitello
Publikováno v:
Neuropharmacology. 197
Although several ionic mechanisms are known to control rate and regularity of the slow pacemaker in dopamine (DA) neurons, the core mechanism of pacing is controversial. Here we tested the hypothesis that pacemaking of SNc DA neurons is enabled by an
Autor:
Jivago Ropke, Fabrício A. Moreira, Lívia Carla de Melo Rodrigues, Yane C P Andrade, Elaine Aparecida Del Bel, A.C. Issy, Chiara Fanelli, Thércia G. Viana, Jean-François Liégeois, Luara A. Batista, Elisa Minaldi
Publikováno v:
Behavioural pharmacology. 32(1)
The pyridobenzoxazepine compound, 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13), has been developed as a potential antipsychotic drug. We tested the hypothesis that JL13 is efficacious in both dopaminergic and glutamaterg
Autor:
Jean-François Liégeois, Sylvia Hartmann, Dominique Engel, Sofian Ringlet, Laurent Massotte, Jochen Roeper, Kevin Jehasse, Seutin, Romain Vitello, Stephan A. Pless, Bernard Lakaye, Vitello M, Han Chow Chua
Although several ionic mechanisms are known to control rate and regularity of the pacemaker in dopamine (DA) neurons from the substantia nigra pars compacta (SNc), a conductance essential for pacing has yet to be defined. Here we provide pharmacologi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::34d78b10051e6961e16bb31d08c1d6e1
https://doi.org/10.1101/2020.12.16.423073
https://doi.org/10.1101/2020.12.16.423073
Publikováno v:
Acta Physiol (Oxf)
AIM: Small-conductance Ca(2+)-activated potassium (SK) channels are activated exclusively by increases in intracellular Ca(2+), that binds to calmodulin constitutively associated with the channel. Wild-type SK2 channels are activated by Ca(2+) with a
Publikováno v:
Journal of Chemical Information and Modeling. 56:1324-1331
The resurgence of interest in 5-HT1A receptors as a therapeutic target requires the existence of highly selective 5-HT1A ligands. To date, WAY-100635 has been the prototypical antagonist of these receptors. However, this compound also has significant
Autor:
Jean-François Liégeois, Fabien Dufour, Vincent Seutin, Sébastien Dilly, Johan Wouters, Iolanda Nistor, Philippe Hubert, Eduard Badarau
Publikováno v:
Journal of Molecular Structure. 1074:435-440
Reduction of symmetrical bis-isoquinolinium derivatives with sodium borohydride generates normally a mixture of three 1,2,3,4-tetrahydroisoquinoline stereoisomers. In a series of 8-isopropyl analogues, chiral resolution failed for the analogues with
Autor:
Eduard Badarau, Attilio Ceccato, Pierre Lebrun, Radu Oprean, Fabien Dufour, Frédéric Lecomte, Ines Slama, Iolanda Nistor, Philippe Hubert, Eric Rozet, Katina Sourou Sylvestre Dossou, Jean-François Liégeois, Marianne Fillet
Publikováno v:
Journal of Pharmaceutical and Biomedical Analysis. 74:273-283
This paper focuses on implementing a design space approach and on the critical process parameters (CPPs) to consider when applying the Quality by Design (QbD) concepts outlined in ICH Q8(R2), Q9 and Q10 to analytical method development and optimizati
Moderate chemical modifications of WAY-100635 improve the selectivity for 5-HT1A versus D4 receptors
Autor:
Jon Evans, Sébastien Dilly, Floriane Mangin, Benoît Joly, Vincent Setola, Bryan L. Roth, Jacqueline Scuvée-Moreau, Jean-François Liégeois
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4550-4554
The selectivity for 5-HT1A versus D4 receptors is significantly increased when the basic side chain of WAY-100635 is replaced by a 4-phenylpiperazine (3e) or a 4-phenyl-1,2,3,6-tetrahydropyridine moiety (3i). The 4-phenyl-1,2,3,6-tetrahydropyridine c
Autor:
Frank I. Tarazi, Mélissa Résimont, Cédric Lamy, Floriane Mangin, Sébastien Dilly, Marine Deville, Jean-François Liégeois
Publikováno v:
Journal of Medicinal Chemistry. 55:1572-1582
A series of new pyridobenzoxazepine derivatives with various heterocyclic amine side chains were synthesized to explore two main parameters related to the distal basic nitrogen. These compounds were tested for their affinity for dopamine D(2L) and D(
Autor:
Sylvie Poncin, Fabien Dufour, Jean-François Liégeois, Sébastien Dilly, Eduard Badarau, Vincent Seutin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6756-6759
A structure–activity relationship study of N-methyl-laudanosine, a SK channel blocker, has indicated that the 6,7-dimethoxy group could be successfully replaced by a hydrophobic moiety such as an isopropyl substituent in position 8 of the isoquinol