A selective positive allosteric modulator of mGluR4
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VU0155041 (sodium salt)

Item No. 21775

Technical Information
Formal Name
(1R,2S)-rel-2-[[(3,5-dichlorophenyl)amino]carbonyl]-cyclohexanecarboxylic acid, monosodium salt
CAS Number
1259372-69-4
Molecular Formula
C14H14Cl2NO3 • Na
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMSO: 1 mg/mlPBS (pH 7.2): 2 mg/ml
λmax
217, 252 nm
SMILES
ClC1=CC(NC([C@H]2[C@@H](C([O-])=O)CCCC2)=O)=CC(Cl)=C1.[Na+]
InChi Code
InChI=1S/C14H15Cl2NO3.Na/c15-8-5-9(16)7-10(6-8)17-13(18)11-3-1-2-4-12(11)14(19)20;/h5-7,11-12H,1-4H2,(H,17,18)(H,19,20);/q;+1/p-1/t11-,12+;/m1./s1
InChi Key
ZFDOLOCYGVTGDQ-LYCTWNKOSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    VU0155041 is a positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4) with an EC50 value of 2.5 μM for glutamate response in a thallium flux assay.1 It is selective for mGluR4, exhibiting no effect on radioligand binding at 67 G protein-coupled receptors, ion channels, and transporters, and lacking antagonist activity at NMDA receptors in striatal medium spiny neurons at a concentration of 10 μM. In vivo, VU0155041 decreases catalepsy induced by haloperidol (Item No. 12014) and reverses askinesias induced by reserpine (Item No. 16474) in rat models of Parkinson’s disease. Chronic treatment with VU0155041 restores social behavior in the Oprm-/- mouse model of autism.2 It also increases the percentage of time spent in the open arms of the elevated plus maze, a measure of decreased anxiety, in mice.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Niswender, C.M., Johnson, K.A., Weaver, C.D., et alDiscovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol. Pharmacol. 74(5), 1345-1358 (2008).

    2. Becker, J.A., Clesse, D., Spiegelhalter, C., et alAutistic-like syndrome in mu opioid receptor null mice is relieved by facilitated mGluR4 activity. Neuropsychopharmacology 39(9), 2049-2060 (2014).

    3. Duvoisin, R.M., Villasana, L., Davis, M.J., et alOpposing roles of mGluR8 in measures of anxiety involving non-social and social challenges. Behav. Brain Res. 221(1), 50-54 (2011).