Zobrazeno 1 - 10
of 63
pro vyhledávání: '"Pari, Malherbe"'
Autor:
Stephen R Morairty, Florent G Revel, Pari Malherbe, Jean-Luc Moreau, Daniel Valladao, Joseph G Wettstein, Thomas S Kilduff, Edilio Borroni
Publikováno v:
PLoS ONE, Vol 7, Iss 7, p e39131 (2012)
The hypocretin (orexin) system is involved in sleep/wake regulation, and antagonists of both hypocretin receptor type 1 (HCRTR1) and/or HCRTR2 are considered to be potential hypnotic medications. It is currently unclear whether blockade of either or
Externí odkaz:
https://doaj.org/article/869b204300724eeea846840bc51ce84a
Publikováno v:
Neuropharmacology
Neuropathic pain is associated with impaired inhibitory control of spinal dorsal horn neurons, which are involved in processing pain signals. The metabotropic GABAB receptor is an important component of the inhibitory system and is highly expressed i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d98dd6b41580995e9352fe64e459d3a9
Autor:
Valentina Bini, Alessandra Pardu, Andrew Thomas, Giuliano Pillolla, Marco Bortolato, Paola Devoto, Pari Malherbe, Roberto Frau
Publikováno v:
CNS Neuroscience & Therapeutics. 20:679-684
Converging evidence points to the involvement of γ-amino-butyric acid B receptors (GABABRs) in the regulation of information processing. We previously showed that GABABR agonists exhibit antipsychotic-like properties in rodent models of sensorimotor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::965bd4b618585576b0029ec5365b4179
https://doi.org/10.1111/cns.12261
https://doi.org/10.1111/cns.12261
Autor:
Anne Marcuz, Schnider Patrick, Pari Malherbe, Caterina Bissantz, Claudia Bohnert, Torsten Hoffmann
Publikováno v:
Journal of Medicinal Chemistry. 55:5061-5076
The neurokinins are neuropeptides that elicit their effect through three GPCRs called NK1, NK2, and NK3. Compounds 5 and 6 are dual hNK1 (Ki of 0.7 and 0.3 nM) and hNK3 (Ki of 2.9 and 1.7 nM) antagonists. Both compounds exhibit an insurmountable mode
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5d25c3fc51057387f65affac4c1b0b20
https://doi.org/10.1021/jm2017072
https://doi.org/10.1021/jm2017072
Publikováno v:
Expert Opinion on Therapeutic Patents. 21:637-655
The neurokinin 3 (NK(3)) receptor is a GPCR that has been shown to modulate monoaminergic systems within regions of the brain implicated in schizophrenia. Preclinical and Phase II clinical results of osanetant and talnetant in schizophrenic patients
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b965ebe5dae8cb14283e2b7ed5c56814
https://doi.org/10.1517/13543776.2011.568482
https://doi.org/10.1517/13543776.2011.568482
Autor:
Anne Marcuz, Pari Malherbe, Olivier Roche, Claudia Kratzeisen, Joseph G. Wettstein, Caterina Bissantz
Publikováno v:
Molecular Pharmacology. 78:81-93
The orexins and their receptors are involved in the regulation of arousal and sleep–wake cycle. Clinical investigation with almorexant has indicated that this dual OX antagonist is efficacious in inducing and maintaining sleep. Using site-directed
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::195e5c9b026ae9d3fbafdc0bc260a541
https://doi.org/10.1124/mol.110.064584
https://doi.org/10.1124/mol.110.064584
Publikováno v:
Molecular Pharmacology. 76:618-631
Recent preclinical and clinical research has shown that almorexant promotes sleep in animals and humans without disrupting the sleep architecture. Here, the pharmacology and kinetics of [(3)H]almorexant binding to human orexin 1 receptor (OX(1))- and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afe058889cf26991657995fd0d4c9584
https://doi.org/10.1124/mol.109.055152
https://doi.org/10.1124/mol.109.055152
Autor:
Andrew Thomas, André Alker, Pari Malherbe, Roger David Norcross, Francois Grillet, Raffaello Masciadri
Publikováno v:
Synthetic Communications. 38:3398-3405
The GABAB positive allosteric modulator (R,S)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one (1) was synthesized in one pot from the anhydrous lithium salt of 2,4-di-tert-butylphenol and methyl trifluoropyruvate mediated by a stoic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::04836b19aae1bd2cca0659dc68d7d835
https://doi.org/10.1080/00397910801979403
https://doi.org/10.1080/00397910801979403
Autor:
Pari Malherbe, Richard L.M. Faull, Gareth J. Ellis, Ernst‐Jürgen Schlaeger, Agnes Nilly, Brian S. Roughley, Jürg Messer, Zaiga Bleuel, Veit Metzler, J. Grayson Richards, Sylvie Chaboz, Geo Adam, Vincent Mutel
Publikováno v:
Journal of Neurochemistry. 75:2590-2601
We have investigated the binding properties of [(3)H]quisqualate to rat metabotropic glutamate (mGlu) 1a and 5a receptors and to rat and human brain sections. Saturation isotherms gave K:(D) values of 27 +/- 4 and 81 +/- 22 nM: for mGlu1a and mGlu5a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b75dd818765e3e2b63027f7955554246
https://doi.org/10.1046/j.1471-4159.2000.0752590.x
https://doi.org/10.1046/j.1471-4159.2000.0752590.x
Autor:
Martin Stahl, Pari Malherbe, Georg Jaeschke, Marie-Thérèse Zenner, Andreas Mühlemann, Paul R. Gerber, Richard H.P. Porter, Christophe Fischer, Nicole A. Kratochwil
Publikováno v:
Journal of Neurochemistry. 98:601-615
Fenobam [N-(3-chlorophenyl)-N'-(4,5-dihydro-1-methyl-4-oxo-1H-imidazole-2-yl)urea], a clinically validated non-benzodiazepine anxiolytic, has been shown to be a potent and non-competitive metabotropic glutamate (mGlu)-5 receptor antagonist. In the pr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d16f252bdc7348f66a5ccf23df67f50
https://doi.org/10.1111/j.1471-4159.2006.03886.x
https://doi.org/10.1111/j.1471-4159.2006.03886.x