A positive allosteric modulator of mGluR2
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LY487379

Item No. 45330

Technical Information
Formal Name
2,2,2-trifluoro-N-[4-(2-methoxyphenoxy)phenyl]-N-(3-pyridinylmethyl)-ethanesulfonamide
CAS Number
353231-17-1
Molecular Formula
C21H19F3N2O4S
Formula Weight
Purity
≥98%
A crystalline solid
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=S(N(CC1=CC=CN=C1)C2=CC=C(C=C2)OC3=C(OC)C=CC=C3)(CC(F)(F)F)=O
InChi Code
InChI=1S/C21H19F3N2O4S/c1-29-19-6-2-3-7-20(19)30-18-10-8-17(9-11-18)26(14-16-5-4-12-25-13-16)31(27,28)15-21(22,23)24/h2-13H,14-15H2,1H3
InChi Key
ALMACYDZFBMGOR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LY487379 is a positive allosteric modulator of metabotropic glutamate receptor 2 (mGluR2).1 It is selective for mGluR2 over mGluR3 in cells expressing recombinant mGluR2 or mGluR3 (IC50s = 1.7 and >10 µM, respectively). LY487379 reduces MK-801-induced superoxide dismutase (SOD) activity in mouse frontal cortex and hippocampal homogenates.2 In vivo, LY487379 (30 mg/kg) increases cognitive flexibility in the attentional set-shifting task and decreases impulsive behavior in the differential reinforcement of low rate 72s (DRL72) schedule of food reinforcement in rats.3 It also decreases the severity of dyskinesia and psychotic-like behaviors induced by L-DOPA (Item No. 13248) in a 6-MPTP-lesioned marmoset model of Parkinson's disease when administered at a dose of 1 or 10 mg/kg.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schaffhauser, H., Rowe, B.A., Morales, S., et al. Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2. Mol. Pharmacol. 64(4), 798-810 (2003).

    2. Burnat, G., Santocki, M., Kalinowski, L., et al. The impact of muscarinic and mGlu receptors modulators on MK-801-induced impairments in NO-dependent processes both in vitro and in vivo. Pharmacol. Rep. 77(5), 1309-1322 (2025).

    3. Nikiforuk, A., Popik, P., Drescher, K.U., et al. 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(3), 665-673 (2010).

    4. Sid-Otmane, L., Hamadjida, A., Nuara, S.G., et al. Selective metabotropic glutamate receptor 2 positive allosteric modulation alleviates L-DOPA-induced psychosis-like behaviours and dyskinesia in the MPTP-lesioned marmoset. Eur. J. Pharmacol. 873, 172957 (2020).