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A 438079 hydrochloride

CAS No. : 899431-18-6

MCE 站：A 438079 hydrochloride

产品活性：A 438079 hydrochloride 是一种有效的，选择性的 P2X₇ 受体拮抗剂，pIC₅₀ 值为 6.9。

研究领域：Membrane Transporter/Ion Channel

作用靶点：P2X 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.

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.) signi?cantly 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 signi?cantly prevents the 6-OHDA-induced depletion of striatal DA stores. Pretreatment with A 438079 reduces nociceptive behaviour scores in the HC model.

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