Gabapentin hydrochloride

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CAS NO:

60142-95-2

加巴喷丁盐酸盐

Gabapentin hydrochloride 是一种口服有效的 P/Q 型 Ca²⁺通道阻滞剂。Gabapentin hydrochloride 抑制神经元 Ca²⁺内流和减少神经递质释放。Gabapentin hydrochloride 是 GABA 类似物，可用于缓解神经性疼痛。

生物活性

Gabapentin hydrochloride is a potent, orally activeP/Q type Ca²⁺channelblocker. Gabapentin hydrochloride inhibits neuronal Ca²⁺influx and reduction of neurotransmitter release. Gabapentin hydrochloride 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) hydrochloride produces a concentration-dependent inhibition of the K⁺-induced [Ca²⁺]_iincrease in synaptosomes (IC₅₀=14 μM; maximal inhibition by 36%)^[1]. Gabapentin (100 μM) hydrochloride decreases the K⁺-evoked release of endogenous aspartate and glutamate in neocortical slices by 16 and 18%, respectively^[1]. Gabapentin (0-1000 μM) hydrochloride reduces the K⁺-evoked [³H]-noradrenaline release in neocortical slices (IC₅₀=48 μM; maximal inhibition of 46%) but not from synaptosomes^[1].

体内研究
(In Vivo)

Gabapentin (5 and 10 mg/kg; i.p.; once; male BALB/c mice) hydrochloride 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) hydrochloride 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 . Decreased the transfer latency on second day in mEPM test . Prolonged retention latency in PA test .

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.

Clinical Trial

分子量

207.70

性状

Solid

Formula

C₉H₁₈ClNO₂

CAS 号

60142-95-2

中文名称

加巴喷丁盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : 50 mg/mL(240.73 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	4.8146 mL	24.0732 mL	48.1464 mL
5 mM	0.9629 mL	4.8146 mL	9.6293 mL
10 mM	0.4815 mL	2.4073 mL	4.8146 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-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: 10 mg/mL (48.15 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。