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1391054-02-6

中文名称 4-氨基-5-己烯酸盐酸盐
英文名称 Vigabatrin (Hydrochloride)
CAS 1391054-02-6
分子式 C6H12ClNO2
分子量 165.618
MOL 文件 1391054-02-6.mol
更新日期 2023/03/20 15:41:21
1391054-02-6 结构式 1391054-02-6 结构式

基本信息

中文别名
盐酸氨己烯酸
4-氨基-5-己烯酸盐酸盐
VIGABATRIN(中间体)
英文别名
Vigabatrin HCL
Vigabatrin (Hydrochloride)
4-aminohex-5-enoic acid hydrochloride
4-Amino-5-hexenoic acid hydrochloride (1:1)
Γ-VINYL-GABA HYDROCHLORIDE
SABRIL HYDROCHLORIDE

物理化学性质

储存条件-20°C储存
溶解度少许溶于甲醇和水
形态固体
颜色灰白色至浅棕色
稳定性吸湿性

常见问题列表

生物活性
Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride),一种抑制性神经递质 GABA 乙烯基衍生物,是一种具有口服活性且不可逆的 GABA 转氨酶 (GABA transaminase) 抑制剂。 Vigabatrin hydrochloride 是一种抗癫痫剂,通过抑制 GABA transaminase 对 GABA 的分解代谢来增加脑中 GABA 的水平。
体外研究

A significant increase in seizure threshold is observed following systemic (i.p.) administration of high (600 or 1200 mg/kg) doses of Vigabatrin. Bilateral microinjection of Vigabatrin (10 μg) into either the anterior or posterior substantia nigra pars reticulata (SNr) also increased seizure threshold, but less markedly than systemic treatment. Focal delivery into the subthalamic nucleus (STN) increased seizure threshold more markedly than either intranigral or systemic administration of Vigabatrin.

体内研究

Vigabatrin inhibits the uptake of taurine in Caco-2 and MDCK cells to 34% and 53%, respectively, at a concentration of 30 mM. In Caco-2 cells the uptake of Vigabatrin under neutral pH conditions is concentration-dependent and saturable with a Km-value of 27 mM. Vigabatrin is able to inhibit the uptake of taurine in intestinal and renal cell culture models.

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