3,3'-Difluorobenzaldazine

3,3'-Difluorobenzaldazine用途

3,3'-Difluorobenzaldazine (DFB) 是一种选择性 mGluR5 正变构调节剂。3,3'-Difluorobenzaldazine 可增强 mGlu5 激动剂 (Glutamate, Quisqualate, 3,5-Dihydroxyphenylglycine) 的 3-6 倍作用,EC50 在 2 到 5 μM 范围内。

3,3'-Difluorobenzaldazine名称

[ CAS 号 ]:
15332-10-2

[ 中文名 ]:
DFB,mGlu5受体的正变构调节剂

[ 英文名 ]:
DFB

[英文别名 ]:

m-Fluor-benzaldazin
3,3'-Difluorobenzaldazine
3,3'-DIFLUOROBENZALDAZINE
DFB

3,3'-Difluorobenzaldazine生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 谷氨酸受体

研究领域 >> 神经疾病

[体外研究]

在本实验中,3,3'-二氟苯扎嗪(DFB)引起人mGluR5 CHO细胞对300 nM谷氨酸的反应的浓度依赖性增强。在该浓度的谷氨酸盐下,最大增强约为3.1倍,增强的EC50为2.6μM。3,3'-二氟苯扎嗪可使人mGluR5和大鼠mGluR5 CHO细胞对谷氨酸、奎斯奎酸盐和DHPG的反应具有相似的增强作用[1]。

[体内研究]

3,3'-二氟苯扎嗪(40-100 nmol；icv)可减轻氯胺酮引起的运动过度活跃、运动不协调和认知障碍[2]。动物模型：雄性NMRI和ICR小鼠(8～9周,33～40g)[2]剂量：40～100nmol(~9.7～24.4μg)给药：ICV结果：减轻氯胺酮所致的运动过度活跃、运动不协调和认知障碍。

[参考文献]

[1]. O'Brien JA, et al, Chen TB, et al. A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol Pharmacol. 2003;64(3):731-740.

[2]. O'Brien JA, et al. A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5. Mol Pharmacol. 2003;64(3):731-740.

3,3'-Difluorobenzaldazine物理化学性质

[ 密度 ]:
1.12g/cm3

[ 沸点 ]:
326.6ºC at 760mmHg

[ 分子式 ]:
C₁₄H₁₀F₂N₂

[ 分子量 ]:
244.23900

[ 闪点 ]:
151.3ºC

[ 精确质量 ]:
244.08100

[ PSA ]:
24.72000

[ LogP ]:
3.41780

[ 蒸汽压 ]:
0.000406mmHg at 25°C

[ 折射率 ]:
1.539

[ 储存条件 ]:
2-8°C，避光

3,3'-DifluorobenzaldazineMSDS

3,3'-Difluorobenzaldazine安全信息

[ 符号 ]:

GHS07, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H400

[ 警示性声明 ]:
P273

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;N: Dangerous for the environment;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S60

[ 危险品运输编码 ]:
UN 3077 9/PG 3

[ 海关编码 ]:
2928000090

3,3'-Difluorobenzaldazine合成路线

3,3'-Difluorobenzaldazine上下游产品

3,3'-Difluorobenzaldazine上游产品

3,3'-Difluorobenzaldazine下游产品

3,3'-Difluorobenzaldazine海关

[ 海关编码 ]: 2928000090

[ 中文概述 ]:
2928000090 其他肼（联氨）及胲（羟胺）的有机衍生物。监管条件:无。增值税率:17.0%。退税率:9.0%。最惠国关税:6.5%。普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2928000090 other organic derivatives of hydrazine or of hydroxylamine VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%

3,3'-Difluorobenzaldazine文献

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A main challenge in food safety research is to demonstrate that processing of foodstuffs does not lead to the formation of substances for which the safety upon consumption might be questioned. This is...

Metabotropic glutamate receptor 5 positive allosteric modulators are neuroprotective in a mouse model of Huntington's disease.

Br. J. Pharmacol. 169 , 909-21, (2013)

Huntington's disease (HD) is an autosomal dominant neurodegenerative disorder caused by a polyglutamine expansion in the huntingtin protein. We have previously demonstrated that the cell signalling of...

A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.

Mol. Pharmacol. 64 , 731-740, (2003)

We have identified a family of highly selective allosteric modulators of the group I metabotropic glutamate receptor subtype 5 (mGluR5). This family of closely related analogs exerts a spectrum of eff...

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