Gabapentin is a pharmaceutical drug. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.
Gabapentin, baclofen and CGP 44532 all reduced the electrically stimulated release of [3H]glutamic acid (IC50=20 microM, 0.8 microM and 2 microM, respectively). Gabapentin was without effect on the release of [3H]GABA, whilst baclofen (IC50=8 microM) and CGP 44532 (IC50=1 microM) inhibited [3H]GABA release. A large inhibition of calcium currents by gabapentin was observed in pyramidal neocortical cells (up to 34%).
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Stefani A, et al. Gabapentin inhibits calcium currents in isolated rat brain neurons. Neuropharmacology. 1998;37(1):83-91.
[2] Parker DA, et al. Gabapentin activates presynaptic GABAB heteroreceptors in rat cortical slices. Eur J Pharmacol. 2004 Jul 14;495(2-3):137-43.
分子式 C9H18ClNO2 |
分子量 207.7 |
CAS号 60142-95-2 |
储存方式 -20 ℃长期冷藏储存。冰袋运输 |
溶剂(常温) |
DMSO Soluble |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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