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VU 0364770

Name: VU 0364770
Brand: Selleck Chemicals
SKU: S2862
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Catalog No.S2862

For research use only.

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.

CAS No. 61350-00-3

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GluR Signaling Pathway Map

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

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

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]

Protocol (from reference)

Animal Research:^[1]	Animal Models: Haloperidol-Induced Catalepsy Dosages: 1–56.6 mg/kg Administration: s.c.

References

[1] Jones CK, et al. J Pharmacol Exp Ther, 2012, 340(2), 404-421.

Solubility (25°C)

In vitro	DMSO	47 mg/mL (202.0 mM)
	Ethanol	47 mg/mL (202.0 mM)
	Water	Insoluble

Chemical Information

Molecular Weight	232.67
Formula	C₁₂H₉ClN₂O
CAS No.	61350-00-3
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1=CC=NC(=C1)C(=O)NC2=CC(=CC=C2)Cl

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