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VU0364770

VU0364770 (VU 0364770) 是一种选择性mGlu4正变构调节剂，对 mGlu5 具有拮抗活性，对 mGlu6 具有正变构调节活性。它还对 MAO 具有活性，对人 MAO-A 和 MAO-B 的 Ki 值分别为8.5 和 0.72 μM。

CAS号

61350-00-3

分子式

C12H9ClN2O

主要靶点

GluR

仅限科研使用

Cat No : CM05103

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Synonyms

VU 0364770

验证数据展示

  • CAS No.: 61350-00-3

    VU0364770
    CAS#: 61350-00-3

产品信息

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

CAS号 61350-00-3
分子式 C12H9ClN2O
主要靶点 GluR
主要通路 神经科学
分子量 232.67
纯度 99.92%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 VU 0364770

靶点活性

mGlu4:1.1 μM(EC50)

体内活性

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]

体外活性

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]

溶解度

DMSO:23.3 mg/mL (100 mM)

参考文献

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

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