Name | 3-{[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl}pyridine hydrochloride (1:1) |
Synonyms | A 438079 A 438079 HCI A 438079 hydrochlori A 438079 HYDROCHLORIDE 3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine Pyridine, 3-[[5-(2,3-dichlorophenyl)-1H-tetrazol-1-yl]methyl]- 3-{[5-(2,3-DICHLOROPHENYL)-1H-1,2,3,4-TETRAZOL-1-YL]METHYL}PYRIDINE 3-[[5-(2,3-DICHLOROPHENYL)-1H-TETRAZOL-1-YL]METHYL]PYRIDINE HYDROCHLORIDE 3-[[5-(2,3-Dichlorophenyl)-1H-tetra-zol-1-yl]methyl]pyridine hydrochloride |
CAS | 899507-36-9 |
InChI | InChI=1S/C13H9Cl2N5.ClH/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;1H |
Molecular Formula | C13H9Cl2N5 |
Molar Mass | 306.15 |
Storage Condition | Desiccate at RT |
In vitro study | In 1321N1 cells stably expressing rat P2X 7 receptors, A 438079 blocks BzATP-(10 μM) evoked changes in intracellular calcium concentrations with an IC 50 of 321 nM. A 438079 is also selective for the P2X 7 receptor, at concentrations up to 100 μM. |
In vivo study | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.266 ml | 16.332 ml | 32.664 ml |
5 mM | 0.653 ml | 3.266 ml | 6.533 ml |
10 mM | 0.327 ml | 1.633 ml | 3.266 ml |
5 mM | 0.065 ml | 0.327 ml | 0.653 ml |
biological activity | A 438079 is A potent, selective P2X7 receptor antagonist with A pIC50 value of 6.9. |
Target | pIC50: 6.9 (P2X 7 receptor) |