Tiagabine hydrochloride 是一种有效的选择性 GABA 再摄取抑制剂，用作抗惊厥药，在突触体、神经元和神经胶质细胞中摄取 [3H]GABA 的 IC50 分别为 67、446 和 182 nM。
| Cas No. | 145821-59-6 |
| 别名 | 盐酸噻加宾; NO050328 hydrochloride; NO328 hydrochloride; TGB hydrochloride |
| 化学名 | (R)-1-(4,4-bis(3-methylthiophen-2-yl)but-3-en-1-yl)piperidine-3-carboxylic acid hydrochloride |
| Canonical SMILES | CC(C=CS1)=C1/C(C2=C(C=CS2)C)=C/CCN3CCC[C@](C(O)=O)([H])C3.Cl |
| 分子式 | C20H26ClNO2S2 |
| 分子量 | 412.01 |
| 溶解度 | ≥ 16.6mg/mL in DMSO |
| 储存条件 | Store at 2-8°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively[1]. References:
[1]. Braestrup C, et al. (R)-N-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl]nipecotic acid binds with high affinity to the brain gamma-aminobutyric acid uptake carrier. J Neurochem. 1990 Feb;54(2):639-47.
[2]. Sheehan, D.V., et al., An open-label study of tiagabine in panic disorder. Psychopharmacol Bull, 2007. 40(3): p. 32-40.
[3]. Henjum, S. and B. Hassel, High-affinity GABA uptake and GABA-metabolizing enzymes in pig forebrain white matter: a quantitative study. Neurochem Int, 2007. 50(2): p. 365-70. |
