Tiagabine hydrochloride 是具有抗惊厥特性的选择性GABA 再摄取抑制剂,在突触体、神经元和神经胶质中,能够抑制 [3H]GABA 的重摄取,IC50值分别为 67、446 和 182 nM。
产品描述
Tiagabine Hydrochloride is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
体外活性
Tiagabine is a potent inhibitor of GABA uptake into neurons and glial cells. It is involved in modulating GABA levels, especially in areas such as the hippocampus and thalamus[2]. Tiagabine not only affected the decay kinetics of the IPSCs, it also reduced the frequency of occurrence of both spontaneous and miniature IPSCs[4].
体内活性
Tiagabine offers a significant neuroprotection in global ischemia in gerbils when given 30 min before ischemia but not when given 3 h after ischemia[3].
Cas No.
145821-59-6
分子式
C20H26ClNO2S2
分子量
412.0
别名
NO328 hydrochloride;Gabitril hydrochloride;Gabitril;盐酸噻加宾;NO050328 hydrochloride;TGB hydrochloride
储存和溶解度
DMSO:41.2 mg/mL (100 mM)
H2O:20.6 mg/mL (50 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years