Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Philippe Pichat"'
Autor:
Guy Griebel, Jeanne Stemmelin, Mati Lopez-Grancha, Valérie Fauchey, Franck Slowinski, Philippe Pichat, Gihad Dargazanli, Ahmed Abouabdellah, Caroline Cohen, Olivier E. Bergis
Publikováno v:
Scientific Reports, Vol 8, Iss 1, Pp 1-25 (2018)
Abstract Enhancing endogenous cannabinoid (eCB) signaling has been considered as a potential strategy for the treatment of stress-related conditions. Fatty acid amide hydrolase (FAAH) represents the primary degradation enzyme of the eCB anandamide (A
Externí odkaz:
https://doaj.org/article/080f7bdc1656430e82c1cafc30cdcfa0
Autor:
Philippe Pichat, Franck Slowinski, Olivier Bergis, Jeanne Stemmelin, Guy Griebel, Ahmed Abouabdellah, Gihad Dargazanli, Valérie Fauchey, Mati Lopez-Grancha, Caroline Cohen
Publikováno v:
Scientific Reports, Vol 8, Iss 1, Pp 1-25 (2018)
Scientific Reports
Scientific Reports
Enhancing endogenous cannabinoid (eCB) signaling has been considered as a potential strategy for the treatment of stress-related conditions. Fatty acid amide hydrolase (FAAH) represents the primary degradation enzyme of the eCB anandamide (AEA), oleo
Autor:
David Stefany, Pascal George, Philippe Pichat, Hall Daniel A, Raisa Nagorny, James A. Hendrix, Nicolas Moindrot, Hurst William J, Czechtizky Werngard, Zhongli Gao
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6269-6273
Lead optimization guided by histamine H3 receptor (H3R) affinity and calculated physico-chemical properties enabled simultaneous improvement in potency and PK properties leading to the identification of a potent, selective, devoid of hERG issues, ora
Autor:
Raisa Nagorny, Pascal George, Zhongli Gao, Philippe Pichat, Hendrix James A, Siegfried Stengelin, Czechtizky Werngard, Lothar Schwink, Dominique Françon, Guy Griebel, Hurst William J
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6141-6145
Previous studies have shown that compound 1 displayed high affinity towards histamine H3 receptor (H3R), (human (h-H3R), K(i)=8.6 nM, rhesus monkey (rh-H3R), K(i)=1.2 nM, and rat (r-H3R), K(i)=16.5 nM), but exhibited high affinity for hERG channel. H
Autor:
Mark D. Black, Denis Boulay, Rosy Sher, Guy Griebel, Sukhveen Sahni, Robert E. Featherstone, Franck Slowinski, Sathapana Kongsamut, Vanessa Naimoli, C. Desvignes, Kosley Raymond W, Geoffrey B. Varty, Xavier Vigé, Olivier Bergis, Lisa Potestio, Philippe Pichat, Henry Defex
Publikováno v:
Scientific Reports
Normalization of altered glutamate neurotransmission through activation of the mGluR2 has emerged as a new approach to treat schizophrenia. These studies describe a potent brain penetrant mGluR2 positive allosteric modulator (PAM), SAR218645. The com
Publikováno v:
Pharmacology Biochemistry and Behavior. 102:415-422
The selective antagonist at the CRF₁ receptor, SSR125543, has been shown to produce anxiolytic-like effects in a number of animal models. The aim of the present study was to verify whether these effects are mediated by an action on the hypothalamic
Autor:
Sandra Beeské, Ina Weiner, Mark D. Black, Michal Arad, Geoffrey B. Varty, Antonio Castro, Marie-Pierre Pruniaux, Elisabeth Genet, Etienne Guillot, Guy Griebel, Philippe Pichat, Segev Barak, Mati Lopez-Grancha, Terranova Jean-Paul, Amaya De Levie, Juan Antonio Sánchez
Publikováno v:
Pharmacology Biochemistry and Behavior. 102:203-214
SAR110894 is a novel histamine H₃-R ligand, displaying high and selective affinity for human, rat or mouse H₃-Rs. SAR110894 is a potent H₃-R antagonist at native receptors, reversing R-α-methylhistamine-induced inhibition of electrical field s
Publikováno v:
European Journal of Medicinal Chemistry. 46:4035-4041
Synthesis and biological evaluation of new derivatives of Morphine-6-Glucuronide (M6G) are described. M6G is an active metabolite of morphine which displays more analgesia than morphine with a superior side effect profile but with a less efficiently
Publikováno v:
Behavioural Brain Research. 221:149-154
The experience of traumatic stress often leads to long-lasting alteration in sleep quality and behavior. The objective of the present experiment was to investigate the short- and long-term effects of acute inescapable stress (i.e. two electric foot-s
Autor:
Bruno Biton, Guy Griebel, Caroline Cohen, Pascal George, Philippe Pichat, Mireille Sevrin, Genevieve Estenne-Bouhtou, Nancy Rogacki, C. Desvignes, Bernard Scatton, Patrick Avenet, Xavier Vigé, Jeanne Stemmelin, Olivier Bergis, Annick Coste, Denis Boulay, Christophe Lanneau, Jean Paul Terranova, Régis Steinberg, R. Alonso, Gihad Dargazanli, F. Oury-Donat
Publikováno v:
Pharmacology Biochemistry and Behavior. 91:47-58
On native human, rat and mouse glycine transporter-1(GlyT1), SSR130800 behaves as a selective inhibitor with IC50 values of 1.9, 5.3 and 6.8 nM, respectively. It reversibly blocked glycine uptake in mouse brain cortical homogenates, increased extrace