Search

Background and purpose:Specific and selective inhibitors for mGlu1 receptors are presently inadequate. A new generation of non-competitive mGlu1 antagonists with low nanomolar potencies is emerging. We evaluated two new compounds, YM-298198 and JNJ16259685, for effectiveness, potency and specificity for the first time in a brain slice preparation.Experimental approach:Patch-clamp recording of Purkinje neurones in cerebellar slices were obtained. The slow mGlu1-mediated EPSP was used to establish a concentration-response curve. Fast excitatory synaptic inputs were tested for non-specific effects.Key results:YM-298198 and JNJ16259685 inhibited the synaptic activation of mGlu1 in a concentration-dependent manner (IC50 values of 24 nM and 19 nM, respectively). The antagonists were slow to inhibit and to reverse on washout, probably due to their lipophilic nature. There were no non-specific effects on fast AMPA receptor-mediated synaptic transmission in the cerebellum.Conclusions and implications:These compounds are more than a thousand-fold more potent than previously available compounds. Their selectivity and specificity will be very useful for studying the role of mGlu1 receptors both in vitro and in vivo.British Journal of Pharmacology (2007) 151, 870–876; doi:10.1038/sj.bjp.0707286; published online 14 May 2007 [ABSTRACT FROM AUTHOR]

The article presents a study which evaluates the induction of cytochrome P450 in Hep G2 cells and mutagenicity of extract of sediments in a waste disposal site in Osaka, Japan. HepG2 is a highly differentiated human hepatoma cell line, which retains many of the cellular functions often lost by cells in culture. In this research, researchers assumed that the cell viability has decreased due to the toxicity of chemicals contained in the extract. A comparison between the mutagenicity in the Ames assay and the ECOD-inducing activity in Hep G2 cells showed that sensitivity of ECOD-inducing activity on the sediment extracts was far superior to that of the Ames assay.

The article presents a study that analyzes the indoor air chlordane concentration and its seasonal variation among the residential houses in Japan. The study is undertaken by analyzing chlordane through the use of activated charcoal and gas chromatography to calculate the repair air concentrations. The results of the study show that indoor chlordane originates from indoor chlordane residue through the volatilization process.