2015年10月26日星期一

A-438079 HCl|cas 899431-18-6|DC Chemicals

A-438079 HCl|cas 899431-18-6|DC Chemicals

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

Product Name: A-438079 HCl |Catalog Number:  DC8406 | cas: 899431-18-6 | Other names: A-438079,A438079,A 438079 | Chemical name:3-((5-(2,3-dichlorophenyl)-1H-tetrazol-1-yl)methyl)pyridine hydrochloride | Molecule Formula: C13H10Cl3N5 | MW: 342.61

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]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] 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.

For research and scientific purpose only, not for human use.

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