Home Neuronal Signaling GluR agonist VU 0364770 For research use only.

VU 0364770

VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.

VU 0364770 Chemical Structure

VU 0364770 Chemical Structure

CAS No. 61350-00-3

Purity & Quality Control

Batch: S286201 DMSO]47 mg/mL]false]Ethanol]47 mg/mL]false]Water]Insoluble]false Purity: 99.98%
99.98

VU 0364770 Related Products

Signaling Pathway

GluR Signaling Pathways

GluR Signaling Pathway

Biological Activity

Description VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.
Targets
mGlu4 [1]
1.1 μM(EC50)
In vitro
In vitro VU0364770 is a potent and effective positive allosteric modulator of mGlu4. VU0346770 exhibits a potency of 1.1 ± 0.2 μM at human mGlu4 in the presence of an EC20 concentration of glutamate and shifts the glutamate concentration-response curve 31.4 ± 4.0-fold to the left. VU0364770 exhibits a potency of 290 ± 80 nM at rat mGlu4 and induces an 18.1 ± 1.7-fold left shift of the glutamate concentration-response curve. [1]
In Vivo
In vivo VU0364770 shows efficacy alone or when administered in combination with l-DOPA or an adenosine 2A (A2A) receptor antagonist preladenant currently in clinical development. When administered alone, VU0364770 exhibits efficacy in reversing haloperidol-induced catalepsy, forelimb asymmetry-induced by unilateral 6-hydroxydopamine (6-OHDA) lesions of the median forebrain bundle, and attentional deficits induced by bilateral 6-OHDA nigrostriatal lesions in rats. In addition, VU0364770 enhances the efficacy of preladenant to reverse haloperidol-induced catalepsy when given in combination. The effects of VU0364770 to reverse forelimb asymmetry are also potentiated when the compound is coadministered with an inactive dose of l-DOPA, suggesting that mGlu4 positive allosteric modulator may provide l-DOPA-sparing activity. [1]
Animal Research Animal Models Haloperidol-Induced Catalepsy
Dosages 1–56.6 mg/kg
Administration s.c.

Chemical Information & Solubility

Molecular Weight 232.67 Formula

C12H9ClN2O
CAS No. 61350-00-3 SDF Download VU 0364770 SDF
Smiles C1=CC=NC(=C1)C(=O)NC2=CC(=CC=C2)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 47 mg/mL ( (202.0 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 47 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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