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A 839977

CAS No. : 870061-27-1

MCE 站：A 839977

产品活性：A 839977是一种选择性 P2X7 受体拮抗剂, 可阻断人和大小鼠 P2X7 受体的 BzATP 诱发的钙内流 (IC₅₀s=20 nM, 42 nM / 150 nM); 在体实验中, 通过阻断 IL-1β 释放产生抗痛觉过敏反应, 减弱模型动物的炎症反应与神经性疼痛.

研究领域：Membrane Transporter/Ion Channel

作用靶点：P2X Receptor

In Vitro: A 839977 selectively blocks BzATP-evoked calcium influx at mammalian P2X7 receptors, (IC₅₀=20-150 nM), which blocks agonist-evoked YO-PRO uptake and IL-1beta release from differentiated human THP-1 cells, it has been shown to reduce inflammatory and neuropathic pain in animal models.
A 839977 (50 nM, pre-treatment 1 hour) significantly prevents pressure-induced rise of IL-1β priming in optic nerve astrocytes.

In Vivo: A 839977 (30 μmol/kg, 100 μmol/kg, 300 μmol/kg; pre-injected 30mins) dose-dependently reduces thermal hyperalgesia produced by intraplantar administration of complete Freund's adjuvant (CFA) in rats.
A 839977 (10 μmol/kg, 30 μmol/kg, 100 μmol/kg; pre-injected 30mins) produces robust antihyperalgesia in the CFA model of inflammatory pain in wild-type mice, but it has no effect on IL-1alphabeta knockout mice.
A 839977 attenuates dorsal horn neuronal responses in cancer bearing animals.

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