LY 487379 hydrochloride
Positive allosteric modulator selective for mGlu2 receptors. Potentiates glutamate-stimulated [35S]GTPγS binding (EC50 values are 1.7 and > 10 μM for mGlu2 and mGlu3 receptors respectively). Devoid of any activity at mGlu5 and mGlu7 receptors. Promotes cognitive flexibility in a rat model.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 488.91. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.05 mL||10.23 mL||20.45 mL|
|5 mM||0.41 mL||2.05 mL||4.09 mL|
|10 mM||0.2 mL||1.02 mL||2.05 mL|
|50 mM||0.04 mL||0.2 mL||0.41 mL|
References are publications that support the products' biological activity.
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 PMID: 12852748
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 PMID: 14500736
Poisik et al (2005) Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus. Neuropharmacology 49 57 PMID: 15993439
Nikiforuk et al (2010) Effects of a positive allosteric modulator of group II metabotropic glutamate receptors, LY487379, on cognitive flexibility and impulsive-like responding in rats. J.Pharmacol.Exp.Ther. 335 665 PMID: 20739457
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Keywords: LY 487379 hydrochloride, supplier, Positive, allosteric, modulators, pam, selective, mGlu2, mGluR2, mGlur, Group, II, Receptors, Glutamate, Metabotropic, LY487379, hydrochloride, Glutamate, (Metabotropic), Group, II, Receptors, Glutamate, (Metabotropic), Group, II, Receptors, Tocris Bioscience
4 Citations for LY 487379 hydrochloride
Citations are publications that use Tocris products. Selected citations for LY 487379 hydrochloride include:
Scholler (2017) Allosteric nanobodies uncover a role of hippocampal mGlu2 receptor homodimers in contextual fear consolidation. Nat Commun 8 1967 PMID: 29213077
Motolese et al (2015) Targeting type-2 metabotropic glutamate receptors to protect vulnerable hippocampal neurons against ischemic damage. Neuropharmacology 8 66 PMID: 26496940
Copeland et al (2015) Neuronal activity patterns in the mediodorsal thalamus and related cognitive circuits are modulated by metabotropic glutamate receptors. Nat Commun 92 16 PMID: 25576798
Yin et al (2014) Selective actions of novel allosteric modulators reveal functional heteromers of metabotropic glutamate receptors in the CNS. J Neurosci 34 79 PMID: 24381270
Do you know of a great paper that uses LY 487379 hydrochloride from Tocris? If so please let us know.
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