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899431-18-6

中文名稱 A 438079 (hydrochloride)
英文名稱 A 438079 (hydrochloride)
CAS 899431-18-6
分子式 C13H10Cl3N5
分子量 342.611
MOL 文件 899431-18-6.mol
899431-18-6 結(jié)構(gòu)式 899431-18-6 結(jié)構(gòu)式

基本信息

中文別名
3-[[5-(2,3-二氯苯基)-1H-四唑-1-基]甲基]吡啶單鹽酸鹽
英文別名
A-438079 HCl
A-438079
A438079
A 438079
3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine monohydrochloride
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

儲存條件-20°C
溶解度溶于DMSO(>25mg/ml)
形態(tài)固體
顏色白色至灰白色
穩(wěn)定性可在-20°C下的DMSO溶液保存長達(dá)1個月。

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301

常見問題列表

生物活性
A 438079 hydrochloride 是一種有效的,選擇性的 P2X7 受體拮抗劑,pIC50 值為 6.9。
靶點

pIC50: 6.9

體外研究

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.

體內(nèi)研究

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.) signi?cantly 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 signi?cantly prevents the 6-OHDA-induced depletion of striatal DA stores. Pretreatment with A 438079 reduces nociceptive behaviour scores in the HC model.

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