A 438079 (hydrochloride)
| 中文名称 | A 438079 (hydrochloride) |
|---|---|
| 中文同义词 | 3-[[5-(2,3-二氯苯基)-1H-四唑-1-基]甲基]吡啶单盐酸盐;化合物A-438079 HYDROCHLORIDE;A-438079盐酸盐;3-((5-(2,3-二氯苯基)-1H-四唑-1-基)甲基)吡啶 盐酸盐;A 438079,COMPETITIVE P2X7 RECEPTOR拮抗剂;化合物A-438079 HYDROCHLORIDE,10 MM DMSO 溶液 |
| 英文名称 | A 438079 (hydrochloride) |
| 英文同义词 | 3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine monohydrochloride;A-438079 HCl;A-438079;A438079;A 438079;P2X Receptor,A-438079,P2XRs,A 438079 hydrochloride,A438079,Inhibitor,inhibit,A 438079;A 438079, competitive P2X7 receptor antagonist;A 438079 hydrochloride, 10 mM in DMSO |
| CAS号 | 899431-18-6 |
| 分子式 | C13H10Cl3N5 |
| 分子量 | 342.611 |
| EINECS号 | 604-604-1 |
| 相关类别 | 小分子抑制剂;小分子抑制剂，天然产物;Inhibitors |
| Mol文件 | 899431-18-6.mol |
| 结构式 |  |
A 438079 (hydrochloride) 性质
| 储存条件 | -20°C |
|---|---|
| 溶解度 | 溶于DMSO(>25mg/ml) |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
| 稳定性 | 可在-20°C下的DMSO溶液保存长达1个月。 |
pIC50: 6.9
In 1321N1 cells stably expressing rat P2X 7 receptors, A 438079 blocks BzATP-(10 μM) evoked changes in intracellular calcium concentrations with an IC 50 of 321 nM. A 438079 is also selective for the P2X 7 receptor, at concentrations up to 100 μM.
A 438079 (80 μmol/kg, i.v.) reduces noxious and innocuous evoked activity of different classes of spinal neurons in neuropathic rats. A 438079 (100 and 300 μmol/kg, i.p.) significantly raises withdrawal thresh-olds in both the SNL and CCI models. Intraperitoneal injection of A 438079 (5 and 15 mg/kg) 60 min after triggering seizures reduces seizure severity and neuronal death within the hippocampus. A 438079 has superior neuroprotective effects compared with an equally dose of phenobarbital (25 mg/kg). A 438079 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores. Pretreatment with A 438079 reduces nociceptive behaviour scores in the HC model.