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。
| 生物活性 | A-887826 is a potent, selective, oral bioavailable and voltage-dependentNa(v)1.8sodium channelblocker with anIC50of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo[1]. |
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体外研究
(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[1].
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[1].
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[1].
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[1].
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体内研究
(In Vivo) | A-887826 (3-30 mg/kg; p.o.; 1 hour pre-treatment) significantly attenuates tactile allodynia in a rat neuropathic pain model[1].
| Animal Model: | Male Spraguee Dawley rats (200-300 g)[1] | | Dosage: | 3 mg/kg, 10 mg/kg, 30 mg/kg | | Administration: | Oral administration; 1 hour before testing; fourteen days after L5-L6 spinal nerve ligation | | Result: | Produced a dose-dependent attenuation of tactile allodynia in this experimental pain model. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(519.76 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.0790 mL | 10.3952 mL | 20.7905 mL | | 5 mM | 0.4158 mL | 2.0790 mL | 4.1581 mL | | 10 mM | 0.2079 mL | 1.0395 mL | 2.0790 mL |
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