Gabapentin 是一种口服有效的 P/Q 型 Ca2+通道阻滞剂。Gabapentin 抑制神经元 Ca2+内流和减少神经递质释放。Gabapentin 是 GABA 类似物，可用于缓解神经性疼痛。
| 生物活性 | Gabapentin is a potent, orally activeP/Q type Ca2+channelblocker. Gabapentin inhibits neuronal Ca2+influx and reduction of neurotransmitter release. Gabapentin is a GABA analog that can be used to relieve neuropathic pain[1][2][3]. |
体外研究
(In Vitro) | Gabapentin (0-300 μM) produces a concentration-dependent inhibition of the K+-induced [Ca2+]iincrease in synaptosomes (IC50=14 μM; maximal inhibition by 36%)[1].
Gabapentin (100 μM) decreases the K+-evoked release of endogenous aspartate and glutamate in neocortical slices by 16 and 18%, respectively[1].
Gabapentin (0-1000 μM) reduces the K+-evoked [3H]-noradrenaline release in neocortical slices (IC50=48 μM; maximal inhibition of 46%) but not from synaptosomes[1].
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体内研究
(In Vivo) | Gabapentin (5 and 10 mg/kg; i.p.; once; male BALB/c mice) has improving effects on spatial and emotional cognitive performance of naive mice in Morris water maze (MWM), passive avoidance (PA) and modified elevated plus maze (mEPM) tasks[2].
Gabapentin (1-100 mg/kg; i.p.; once; male mice) has analgesic effect and reduces writhing in a dose-dependent manner[3].
| Animal Model: | Male BALB/c mice (35-45 g)[2] | | Dosage: | 5 and 10 mg/kg | | Administration: | Intraperitoneal injection; once | | Result: | Increased the time spent in target quadrant and decreased the distance to platform in MWM test
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Decreased the transfer latency on second day in mEPM test
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Prolonged retention latency in PA test
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| Animal Model: | Male mice (26-30 g)[3] | | Dosage: | 1, 5, 10, 50 and 100 mg/kg | | Administration: | Intraperitoneal injection; once | | Result: | Produced 45-70% inhibition of writhing. |
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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: H2O : 50 mg/mL(291.99 mM;Need ultrasonic) DMSO : 1 mg/mL(5.84 mM;Need ultrasonic) 配制储备液 | 1 mM | 5.8398 mL | 29.1988 mL | 58.3976 mL | | 5 mM | 1.1680 mL | 5.8398 mL | 11.6795 mL | | 10 mM | 0.5840 mL | 2.9199 mL | 5.8398 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 25 mg/mL (145.99 mM); Clear solution; Need ultrasonic and warming and heat to 60℃
*以上所有助溶剂都可在本网站选购。 |
