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68506-86-5

中文名稱 4-氨基己-5-烯酸
英文名稱 (±)-4-aminohex-5-enoic acid
CAS 68506-86-5
分子式 C6H11NO2
分子量 129.16
MOL 文件 68506-86-5.mol
68506-86-5 結(jié)構(gòu)式 68506-86-5 結(jié)構(gòu)式

基本信息

中文別名
氨己烯酸雜質(zhì)
4-氨基己-5-烯酸
英文別名
CPP 109
(+/-)-Vigabatrin
SABRIL
Γ-VINYL-GABA
5-Hexenoic acid, 4-amino-
(±)-4-aminohex-5-enoic acid
Vigabatrin, racemic mixture
rac-VigabatrinDiscontinued See V253010
Vigabatrin hydrochloride salt, racemic mixture

物理化學(xué)性質(zhì)

熔點(diǎn)209℃
沸點(diǎn)277.7±28.0 °C(Predicted)
密度1.064±0.06 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度少許溶于甲醇和水
酸度系數(shù)(pKa)4.36±0.10(Predicted)
形態(tài)neat
顏色米白色
水溶解性溶于水至100mM

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS08
警示詞危險(xiǎn)
危險(xiǎn)性描述H372
危險(xiǎn)品標(biāo)志Xi
危險(xiǎn)類別碼36/37/38
安全說明26-36
WGK Germany3
RTECS號(hào)MP7745000
海關(guān)編碼2922498050
毒害物質(zhì)數(shù)據(jù)68506-86-5(Hazardous Substances Data)
毒性LD50 oral in rat: 3gm/kg

常見問題列表

生物活性
Vigabatrin (γ-Vinyl-GABA),一種抑制性神經(jīng)遞質(zhì) GABA 乙烯基衍生物,是一種具有口服活性且不可逆的 GABA 轉(zhuǎn)氨酶 (GABA transaminase) 抑制劑。 Vigabatrin 是一種抗癲癇劑,通過抑制 GABA transaminase 對(duì) GABA 的分解代謝來增加腦中 GABA 的水平。
體外研究

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.

體內(nèi)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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