Catalog Number: 3283
Chemical Name: 2,2,2-Trifluoro-N-[4-(2-methoxyphenoxy)phenyl]-N-(3-pyridinylmethyl)ethanesulfonamide hydrochloride
Biological Activity
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.
Technical Data
  • M.Wt:
    488.91
  • Formula:
    C21H19F3N2O4S.HCl
  • Solubility:
    Soluble to 100 mM in DMSO and to 50 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    353229-59-1
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.
Background References
  1. 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.
    Johnson et al.
    J.Med.Chem., 2003;46:3189
  2. Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2.
    Schaffhauser et al.
    Mol.Pharmacol., 2003;64:798
  3. Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus.
    Poisik et al.
    Neuropharmacology, 2005;49:57
  4. Effects of a positive allosteric modulator of group II metabotropic glutamate receptors, LY487379, on cognitive flexibility and impulsive-like responding in rats.
    Nikiforuk et al.
    J.Pharmacol.Exp.Ther., 2010;335:665
Citations:

The citations listed below are publications that use Tocris products. Selected citations for LY 487379 hydrochloride include:

3 Citations: Showing 1 - 3
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  1. Neuronal activity patterns in the mediodorsal thalamus and related cognitive circuits are modulated by metabotropic glutamate receptors.
    Authors: Copeland Et al.
    Nat Commun 2015;92:16
  2. Targeting type-2 metabotropic glutamate receptors to protect vulnerable hippocampal neurons against ischemic damage.
    Authors: Motolese Et al.
    Neuropharmacology 2015;8:66
  3. Selective actions of novel allosteric modulators reveal functional heteromers of metabotropic glutamate receptors in the CNS.
    Authors: Yin Et al.
    J Neurosci 2014;34:79

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