An mGluR4 and mGluR6 positive allosteric modulator and mGluR5 antagonist
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VU0364770

Item No. 22927

Technical Information
Formal Name
N-(3-chlorophenyl)-2-pyridinecarboxamide
CAS Number
61350-00-3
Molecular Formula
C12H9ClN2O
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 25 mg/mlEthanol: 5 mg/ml
λmax
219, 277 nm
SMILES
ClC1=CC(NC(C2=NC=CC=C2)=O)=CC=C1
InChi Code
InChI=1S/C12H9ClN2O/c13-9-4-3-5-10(8-9)15-12(16)11-6-1-2-7-14-11/h1-8H,(H,15,16)
InChi Key
SUYUTNCKIOLMAJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    VU0364770 is a positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4; EC50 = 1.1 µM in a calcium mobilization assay).1 It is also a positive allosteric modulator of mGluR6 (EC50 = 6.8 µM) and an antagonist of mGluR5 (IC50 = 17.9 µM). VU0364770 binds to monoamine oxidase A (MAO-A) and MAO-B (Kis = 8.5 and 7.2 µM, respectively), as well as the human norepinephrine transporter in a panel of 68 receptors, ion channels, and transporters at 10 µM. It decreases haloperidol-induced catalepsy and reduces increases in the number of premature reactions in response to a light cue, indicating improved attentional control, in a 6-hydroxydopamine (6-OHDA; Item No. 25330) rat model of Parkinson’s disease when administered at a dose of 56.6 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jones, C.K., Bubser, M., Thompson, A.D., et alThe metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with ʟ-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson’s disease. J. Pharmacol. Exp. Ther. 340(2), 404-421 (2012).