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Gabapentin

CAS No. : 60142-96-3

MCE 国际站：Gabapentin

产品活性：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。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：Calcium Channel

In Vitro: Gabapentin (0-300 μM) produces a concentration-dependent inhibition of the K⁺-induced [Ca²⁺]_i increase in synaptosomes (IC₅₀=14 μM; maximal inhibition by 36%).
Gabapentin (100  μM) decreases the K⁺-evoked release of endogenous aspartate and glutamate in neocortical slices by 16 and 18%, respectively.
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.

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.
Gabapentin (1-100 mg/kg; i.p.; once; male mice) has analgesic effect and reduces writhing in a dose-dependent manner.

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