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(R,S)-CHPG

(R,S)-CHPG用途

CHPG 是一个选择性的 mGluR5 激动剂,并且通过 TSG-6/NF-κB 途径减弱 BV2 小神经胶质细胞 SO2 诱导的氧化应激和炎症。 CHPG 通过 ERK 和 Akt 途径在体外和体内预防创伤性脑损伤 (TBI)。

(R,S)-CHPG名称

[ CAS 号 ]:
170846-74-9

[ 英文名 ]:
(R,S)-CHPG

[英文别名 ]:

Pregnanolone
CHPG
2-chloro-5-hydroxyphenylglycine

(R,S)-CHPG生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> PI3K/Akt/mTOR 信号通路 >> AKT

研究领域 >> 炎症/免疫

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 谷氨酸受体

信号通路 >> MAPK/ERK信号通路 >> ERK

信号通路 >> 干细胞及 Wnt 通路 >> ERK

[ 靶点 ]

mGluR5

NF-κB

ERK

Akt

[体外研究]

CHPG(10-500_μM; 24_小时)显着增加细胞活力并降低SO2衍生物处理后的LDH释放[1]。CHPG(0.5mM; 30分钟)保护BV2细胞免受SO2诱导的细胞凋亡[1]。CHPG(0.5 mM; 30 min)单独治疗可增加TSG-6在mRNA和蛋白质水平的表达[1]。细胞活力测定[1]细胞系：BV2小胶质细胞浓度：10,50,100和500μM培养时间：24小时结果：提高细胞活力。细胞凋亡分析[1]细胞系：BV2小胶质细胞浓度：0.5mM培养时间：30分钟结果：保护BV2细胞免受SO2诱导的细胞凋亡。Western Blot分析[1]细胞系：BV2小胶质细胞浓度：0.5mM培养时间：30分钟结果：增加TSG-6在mRNA和蛋白质水平的表达。

[体内研究]

CHPG(注射；250 nM；持续7天)可显著减少脑损伤体积[2]。动物模型：成年Sprague-Dawley雄性大鼠,体重280-320g[2]剂量：250nM给药：注射；7天结果：脑损伤体积明显减少。

[参考文献]

[1]. Qiu JL, et al. The selective mGluR5 agonist CHPG attenuates SO₂-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. Neurochem Int. 2015 Jun-Jul;85-86:46-52.

[2]. Chen T, et al. The selective mGluR5 agonist CHPG protects against traumatic brain injury in vitro and in vivo via ERK and Akt pathway. Int J Mol Med. 2012 Apr;29(4):630-6.

(R,S)-CHPG物理化学性质

[ 分子式 ]:
C₈H₈ClNO₃

[ 分子量 ]:
201.60700

[ 精确质量 ]:
201.01900

[ PSA ]:
83.55000

[ LogP ]:
1.83030

[ 储存条件 ]:
2-8°C，密封，干燥

(R,S)-CHPGMSDS

详细MSDS(安全技术说明书)

(R,S)-CHPG安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

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

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26

[ 危险品运输编码 ]:
NONH for all modes of transport

(R,S)-CHPG文献

mGluR5 in the nucleus accumbens shell regulates morphine-associated contextual memory through reactive oxygen species signaling.

Addict. Biol. 20 , 927-40, (2015)

Emerging evidence indicates that metabotropic glutamate receptor 5 (mGluR5) critically modulates drug and drug-related behaviors. However, the role of mGluR5 in the opiate-induced contextual memory re...

Modulatory effects of activation of metabotropic glutamate receptors on GABAergic circuits in the mouse thalamus.

J. Neurophysiol. 113 , 2646-52, (2015)

Metabotropic glutamate receptors (mGluRs) are widely distributed in the central nervous system and modulate the release of neurotransmitters in different ways. We have previously shown that activation...

Stimulation-evoked Ca2+ signals in astrocytic processes at hippocampal CA3-CA1 synapses of adult mice are modulated by glutamate and ATP.

J. Neurosci. 35(7) , 3016-21, (2015)

To date, it has been difficult to reveal physiological Ca(2+) events occurring within the fine astrocytic processes of mature animals. The objective of the study was to explore whether neuronal activi...

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