LY 487379 hydrochloride is a positive allosteric modulator selective for mGluR-2. LY 487379 hydrochloride potentiates glutamate-stimulated [35S]GTPγS binding (EC50 values are 1.7 and > 10 µM for mGluR-2 and mGluR-3 receptors respectively). LY 487379 hydrochloride is devoid of any activity at mGluR-5 and mGluR-7.
Johnson et al (2003) Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor: synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,-trifluoroethylsulfonyl)pyrid-3-ylmethyl-amine. J.Med.Chem. 46 3189. Schaffhauser et al (2003) Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2. Mol.Pharmacol. 64 798. Poisik et al (2005) Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus. Neuropharmacology 49 57.
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