For research use only. Not for therapeutic Use.
A 438079 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[1].
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].
| Catalog Number | I005382 |
| CAS Number | 899507-36-9 |
| Synonyms | 3-[[5-(2,3-dichlorophenyl)tetrazol-1-yl]methyl]pyridine |
| Molecular Formula | C13H9Cl2N5 |
| Purity | ≥95% |
| InChI | InChI=1S/C13H9Cl2N5/c14-11-5-1-4-10(12(11)15)13-17-18-19-20(13)8-9-3-2-6-16-7-9/h1-7H,8H2 |
| InChIKey | MMPAULQSJLVKHP-UHFFFAOYSA-N |
| SMILES | C1=CC(=C(C(=C1)Cl)Cl)C2=NN=NN2CC3=CN=CC=C3 |
| Reference | [1]. McGaraughty S, et al. P2X7-related modulation of pathological nociception in rats. Neuroscience. 2007 Jun 8;146(4):1817-28. [2]. Mesuret G, et al. CNS Neurosci Ther. 2014 Jun;20(6):556-64. [3]. Marcellino D, et al. On the role of P2X(7) receptors in dopamine nerve cell degeneration in a rat model of Parkinson’s disease: studies with the P2X(7) receptor antagonist A-438079. J Neural Transm (Vienna). 2010 Jun;117(6):681-7. [4]. Martins JP, et al. The role of P2X7 purinergic receptors in inflammatory and nociceptive changes accompanying cyclophosphamide-induced haemorrhagic cystitis in mice. Br J Pharmacol. 2012 Jan;165(1):183-96. |
