Philippe Pichat
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Explore the profile of Philippe Pichat including associated specialties, affiliations and a list of published articles.
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Articles
15
Citations
414
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Recent Articles
1.
Griebel G, Stemmelin J, Lopez-Grancha M, Boulay D, Boquet G, Slowinski F, et al.
Sci Rep
. 2019 Dec;
9(1):18045.
PMID: 31792284
Glycogen synthase kinase 3 (GSK3) has been identified as a promising target for the treatment of Alzheimer's disease (AD), where abnormal activation of this enzyme has been associated with hyperphosphorylation...
2.
Griebel G, Stemmelin J, Lopez-Grancha M, Fauchey V, Slowinski F, Pichat P, et al.
Sci Rep
. 2018 Feb;
8(1):2416.
PMID: 29403000
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...
3.
Griebel G, Pichat P, Boulay D, Naimoli V, Potestio L, Featherstone R, et al.
Sci Rep
. 2016 Oct;
6:35320.
PMID: 27734956
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...
4.
Griebel G, Pichat P, Beeske S, Leroy T, Redon N, Jacquet A, et al.
Sci Rep
. 2015 Jan;
5:7642.
PMID: 25560837
Monoacylglycerol lipase (MAGL) represents a primary degradation enzyme of the endogenous cannabinoid (eCB), 2-arachidonoyglycerol (2-AG). This study reports a potent covalent MAGL inhibitor, SAR127303. The compound behaves as a selective...
5.
Griebel G, Ravinet-Trillou C, Beeske S, Avenet P, Pichat P
Front Endocrinol (Lausanne)
. 2014 May;
5:49.
PMID: 24782829
Disruption of circadian clock enhances the risk of metabolic syndrome, obesity, and type 2 diabetes. Circadian clocks rely on a highly regulated network of transcriptional and translational loops that drive...
6.
Gao Z, Hurst W, Czechtizky W, Hall D, Moindrot N, Nagorny R, et al.
Bioorg Med Chem Lett
. 2013 Oct;
23(23):6269-73.
PMID: 24139584
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...
7.
Gao Z, Hurst W, Czechtizky W, Francon D, Griebel G, Nagorny R, et al.
Bioorg Med Chem Lett
. 2013 Oct;
23(22):6141-5.
PMID: 24076172
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...
8.
Griebel G, Pichat P, Pruniaux M, Beeske S, Lopez-Grancha M, Genet E, et al.
Pharmacol Biochem Behav
. 2012 May;
102(2):203-14.
PMID: 22542742
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...
9.
Trecant C, Dlubala A, George P, Pichat P, Ripoche I, Troin Y
Eur J Med Chem
. 2011 Jun;
46(9):4035-41.
PMID: 21689868
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...
10.
Black M, Stevens R, Rogacki N, Featherstone R, Senyah Y, Giardino O, et al.
Psychopharmacology (Berl)
. 2010 Dec;
215(1):149-63.
PMID: 21181124
Rationale: The psychotomimetic effects of cannabis are believed to be mediated via cannabinoid CB1 receptors. Furthermore, studies have implicated CB1 receptors in the pathophysiology of schizophrenia. Objective: These studies investigated...