作者
Brice Campo, Mikhail Kalinichev, Nathalie Lambeng, M El Yacoubi, Isabelle Royer-Urios, Manfred Schneider, Coline Legrand, Delphine Parron, Francoise Girard, Abdelhak Bessif, Sonia Poli, Jean-Marie Vaugeois, Emmanuel Le Poul, Sylvain Celanire
发表日期
2011/12/1
期刊
Journal of neurogenetics
卷号
25
期号
4
页码范围
152-166
出版商
Taylor & Francis
简介
There is growing evidence suggesting that antagonists of group II metabotropic glutamate receptors (mGluR2/3) exhibit antidepressant-like properties in several preclinical models of depression. However, all those studies have been performed using competitive group II non-selective orthosteric antagonists. In this study we extensively characterized a group II selective negative allosteric modulator (4-[3-(2,6-Dimethylpyridin-4-yl)phenyl]-7-methyl-8-trifluoromethyl-1,3-dihydrobenzo[b][1,4]diazepin-2-one, namely RO4491533, Woltering et al., 2010) in several in vitro biochemical assays and in vivo models of depression. In vitro, RO4491533 completely blocked the glutamate-induced Ca2 + mobilization and the glutamate-induced accumulation in [35S]GTPγS binding in cells expressing recombinant human or rat mGluR2 and in native tissues. Results from Schild plot experiments and reversibility test at the target on …
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B Campo, M Kalinichev, N Lambeng, ME Yacoubi… - Journal of neurogenetics, 2011