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CAS No.: 899507-36-9

A 438079 Catalog No. CSN18547

A 438079 is a competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述ATP is a key neurotransmitter in this process of inducing and maintaining chronic pain. P2X₇ is the glial ATP receptor modulating the pathological pain. A 438079 can inhibits P2X₇ with an IC50 of 321nM in 1321N1 cells. In pharmacokinetic rats, treatment of 10 μM/kg showed low mean plasma and brain levels of the drug, suggesting 84% binding rate to plasma protein. In SNL and CCI rats, treatment of 100 and 300 μM/kg significantly improved withdrawal thresholds with the ED50 of 76 and 100 μM/kg respectively without affecting rat rotarod performance. Treatment of 80 μM/kg this drug in SNL rats didn't affect the von Frey-related discharges of hmWDR and mWDR but was effective against high intensity stimulation. Such an treatment also attenuated the evoked responses of neurons to thermal stimulation and decreased the level of spontaneous firing. Besides, A 438079 with concentration of 1 μM reduced the P2X₇ receptor agonist in non-neuronal DRG cells. IL-1β release was also inhibited by 75.6% at concentration of 3 μM in a dose- dependent manner^[1]. The drug also showed effect on seizure in P10 rat model with the dose range from 0.5 to 50 mg/kg in a dose-dependent manner. And seizure damage was also reduced at either 5 or 15 mg/kg as well as reduced TUNEL staining and decreasing score for neuronal damage. The plasma levels declined rapidly to 2.3 μg/mL within 10 min with the initial concentration of 5 mg/kg of A 438079 in the model, which did not affect cell apoptosis at either 5 or 50 mg/kg^[2].
动物研究
剂量
Mice: 80 mg/kg^[3], 50-200 μmol/kg^[4]
Rats: min = 5 mg/kg^[2], max = 30 mg/kg^[5]

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 80 mg/kg^[3], 50-200 μmol/kg^[4] Rats: min = 5 mg/kg^[2], max = 30 mg/kg^[5]
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2664 mL
- 16.3319 mL
- 32.6637 mL
- 5 mM
- 0.6533 mL
- 3.2664 mL
- 6.5327 mL
- 10 mM
- 0.3266 mL
- 1.6332 mL
- 3.2664 mL

技术信息

CAS号	899507-36-9	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C13H9Cl2N5	运输	蓝冰
分子量	306.15	别名

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