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A-887826

CAS No. : 1266212-81-0

MCE 站：A-887826

产品活性：A-887826 是一种高效、选择性的，口服有效的，电压依赖性的 Na(v)1.8 钠通道阻滞剂，其 IC₅₀ 值为 11 nM。在体内，A-88782 6可减轻神经性触觉痛。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Sodium Channel

In Vitro: A-887826 is approximately 3 fold less potent to block Na(v)1.2, approximately 10 fold less potent to block tetrodotoxin-sensitive sodium (TTX-S Na(+)) currents and is >30 fold less potent to block Na(v)1.5 channels.
A-887826 potently blocks tetrodotoxin-resistant sodium (TTX-R Na(+)) currents (IC₅₀=8 nM) from small diameter rat dorsal root ganglion (DRG) neurons in a voltage-dependent fashion.
A-887826 effectively suppresses evoked action potential firing when DRG neurons are held at depolarized potentials and reversibly suppresses spontaneous firing in small diameter DRG neurons from complete Freund´s adjuvant inflamed rats.
A-887826 (100 nM) shifts the mid-point of voltage-dependent inactivation of TTX-R currents by approximately 4mV without affecting voltage-dependent activation and do not exhibit frequency-dependent inhibition.

In Vivo: A-887826 (3-30 mg/kg; p.o.; 1 hour pre-treatment) significantly attenuates tactile allodynia in a rat neuropathic pain model.

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