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899507-36-9

中文名称 3-[[5-(2,3-二氯苯基)-1H-四唑-1-基]甲基]吡啶
英文名称 3-[[5-(2,3-DICHLOROPHENYL)-1H-TETRAZOL-1-YL]METHYL]PYRIDINE HYDROCHLORIDE
CAS 899507-36-9
分子式 C13H9Cl2N5
分子量 306.15
MOL 文件 899507-36-9.mol
更新日期 2024/12/03 15:40:32
899507-36-9 结构式 899507-36-9 结构式

基本信息

中文别名
3-[[5-(2,3-二氯苯基)-1H-四唑-1-基]甲基]吡啶
英文别名
A 438079
A 438079 HCI
A 438079 HYDROCHLORIDE
3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine
Pyridine, 3-[[5-(2,3-dichlorophenyl)-1H-tetrazol-1-yl]methyl]-
3-{[5-(2,3-DICHLOROPHENYL)-1H-1,2,3,4-TETRAZOL-1-YL]METHYL}PYRIDINE
3-[[5-(2,3-DICHLOROPHENYL)-1H-TETRAZOL-1-YL]METHYL]PYRIDINE HYDROCHLORIDE

物理化学性质

储存条件Desiccate at RT
溶解度Soluble in DMSO
形态Powder
颜色White to off-white

安全数据

危险性符号(GHS)GHS hazard pictograms
GHS06
警示词危险
危险性描述H301

常见问题列表

生物活性
A 438079 是一种有效的,选择性的 P2X7 受体拮抗剂,pIC50 值为 6.9。
靶点

pIC50: 6.9 (P2X 7 receptor)

体外研究

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.

体内研究

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.) 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.

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