A-438079 HCl

Cas No.:	899431-18-6
Chemical Name:	3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine Hydrochloride
Synonyms:	3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine Hydrochloride;A 438079 hydrochloride;A-438079 (hydrochloride);A-438079 Hydrochloride
SMILES:	ClC1=C(Cl)C(C2=NN=NN2CC3=CC=CN=C3)=CC=C1.[H]Cl
Formula:	C13H9N5Cl2.HCl
M.Wt:	342.611
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	A 438079 (hydrochloride) is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.
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].
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].