Tiagabine hydrochloride是GABA uptake inhibitor(摄取抑制剂), 抗惊厥剂。
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] Andersen et al (1993) The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate. J.Med.Chem. 36 1716. PMID: 8510100.
[2] Dhar et al (1994) Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA updake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. J.Med.Chem. 37 2334. PMID: 8057281.
[3] Laughlin et al (2002) Comparison of antiepileptic drugs tiagabine, lamotrigine, and gabapentin in mouse models of acute, prolonged, and chronic nociception. J.Pharmacol.Exp.Ther. 302 1168. PMID: 12183677.
分子式 C20H25NO2S2.HCl |
分子量 412.01 |
CAS号 145821-59-6 |
储存方式 ﹣20 ℃长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mM |
Water 50 mM |
Ethanol |
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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