tcsc1293 A 438079

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

IC50 & Target: pIC50: 6.9 (P2X₇ receptor)

In Vitro: 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^[1].

In Vivo: 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^[1]. 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)^[2]. A 438079 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores^[3]. Pretreatment with A 438079 reduces nociceptive behaviour scores in the HC model^[4].