A-438079 hydrochloride

Research use only, not for human use.

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

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

In 1321N1 cells stably expressing rat P2X7 receptors, A 438079 blocks BzATP-(10 μM) evoked changes in intracellular calcium concentrations with an IC50 of 321 nM. A 438079 is also selective for the P2X7 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.

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Neuroscience

P2 Receptor

P2X7

Neurological Disease

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899431-18-6

342.61

C13H10Cl3N5

>98% (HPLC)

Ethanol: 20 mg/mL warmed (58.37 mM); Water: 61 mg/mL (178.04 mM); DMSO: 61 mg/mL (178.04 mM)

Cl.ClC1=CC=CC(C2=NN=NN2CC2=CN=CC=C2)=C1Cl

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(-20℃)

With Ice Pack

≥ 2 years