A-438079 hydrochloride 是一种选择性的P2X7受体拮抗剂，pIC50值为 6.9。

A-438079 hydrochloride is a potent and selective P2X7 receptor antagonist with pIC50 of 6.9.

A-438079可部分明显抑制6-OHDA诱导的纹状体DA存量的消耗.用A-438079预处理降低HC模型中疼痛行为指数.触发癫痫发作60分钟后腹腔注射A-438079（5和15 mg/kg）可减少海马内癫痫发作的严重程度和神经元死亡.神经病大鼠模型静脉注射80 μMol/kg A-438079,可减少不同类别脊髓神经元有害和无害的诱发活性.

A-438079在浓度达100 μM时对P2X7受体也有选择性。A-438079在稳定表达大鼠P2X7受体的1321N1细胞中,可阻断10 μM BzATP-引起的细胞内钙离子浓度变化,IC50为321 nM。

Human astrocytoma cells, 1321N1, are grown to stably express rat P2X7, human P2X4, P2X2a, P2X2/3, P2X1, P2Y1?and P2Y2 recombinant receptors. Agonist, BzATP, 2,3-O-(4-ben-zoylbenzoyl)-ATP or ATP-induced changes in intracellular Ca2+?concentrations are assessed in all of the cell lines using the Ca2+?chelating dye, Fluo-4, in conjunction with a Fluorometric Imaging Plate Reader. The cells are plated out the day before the experiment onto poly-D-lysine-coated black 96 well plates. After the agonist addition, changes in intracellular Ca2+ concentrations are recorded, per second, for 3 min. Ligands are tested at 11 half-log concentrations from 10-10 to 10-4 M. BzATP or ATP concentrations corresponds to the EC70?values for each receptor to enable comparison of antagonist potencies across the multiple P2 receptor subtypes. A 438079 is added to the cell plate and ?uorescence data are collected for 3 min before the addition of agonist, subsequently, data are then collected for another 2 min. The pEC50 or pIC50 values are derived from a single curve ?t.

899431-18-6

C13H10Cl3N5

342.61

A 438079 (hydrochloride);A-438079 hydrochloride;A-438079 HCl

DMSO:34.3 mg/mL (100 mM)
H2O:1.7 mg/mL (5 mM)),with gentle warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years