A selective group II mGlu2/3 receptor agonist
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LY379268

Item No. 15351

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1R,4R,5S,6R)-4-amino-2-oxabicyclo[3.1.0]hexane-4,6-dicarboxylic acid
CAS Number
191471-52-0
Molecular Formula
C7H9NO5
Formula Weight
187.2
Purity
≥99%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Water: 25 mM
SMILES
[H][C@]1([C@@H]2C(O)=O)[C@]2([H])[C@@](C(O)=O)(N)CO1
InChi Code
InChI=1S/C7H9NO5/c8-7(6(11)12)1-13-4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+/m1/s1
InChi Key
YASVRZWVUGJELU-MDASVERJSA-N
Shipping & Storage Information
Storage
4°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $55

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    5 mg

    $220

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    10 mg

    $359

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    Product Description

    LY379268 is a potent, brain-permeable, and selective agonist of group II metabotropic glutamate receptors (mGluRs), subtypes mGluR2 and mGluR3.1 In an assay of second messenger response, LY379268 exhibits EC50 values of 2.69 and 4.48 nM for human mGluR2 and mGluR3, respectively, with at least 80-fold selectivity over group I and III mGluRs.1 In a displacement assay, LY379268 displays no agonist or antagonist activity against NMDA, AMPA, or kainate receptors up to a concentration of 100 µM.1 However, it may influence the level of AMPA receptor trafficking in rat prefrontal cortical neurons.2 LY379268 confers a neuroprotective effect to the CA1 of the hippocampus in a gerbil model of induced ischemia at a dose of 10 mg/kg.3 In rats, LY379268 (3 mg/kg) raises the extracellular dopamine level to 168% of the basal level in the prefrontal cortex.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Monn, J.A., Valli, M.J., Massey, S.M., et al. Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): Identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptors. J. Med. Chem. 42(6), 1027-1040 (1999).

    2. Wang, M.-J., Li, Y.-C., Snyder, M.A., et al. Group II metabotropic glutamate receptor agonist LY379268 regulates AMPA receptor trafficking in prefrontal cortical neurons. PLoS One 8(4), e61787 (2013).

    3. Bond, A.D., Jones, N.M., Hicks, C.A., et al. Neuroprotective effects of LY379268, a selective mGlu2/3 receptor agonist: investigations into possible mechanism of action in vivo. J. Pharmacol. Exp. Ther. 294(3), 800-809 (2000).

    4. Cartmell, J., Perry, K.W., Salhoff, C.R., et al. The potent, selective mGlu2/3 receptor agonist LY379268 increases extracellular levels of dopamine, 3,4-dihydroxyphenylacetic acid, homovanillic acid, and 5-hydroxyindole-3-acetic acid in the medial prefrontal cortex of the freely moving rat. J. Neurochem. 75(3), 1147-1154 (2000).

    Product Citations

    Arias, H.R., Micheli, L., Jensen, A.A., et al. Ibogalogs decrease neuropathic pain in mice through a mechanism involving crosstalk between 5-HT2A and mGlu2 receptors. Biomed. Pharmacother. 184, 117887 (2025).