Tiagabine HCl
产品说明书
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同义名 : | 噻加宾盐酸盐 ;TGB hydrochloride; NO328 hydrochloride; Tiagabine; NO 328; NO 050328; HSDB 7527; Gabatril; (R)-Tiagabine; ABT-569; Tiagabine (hydrochloride); Gabitril hydrochloride; NO050328 hydrochloride; Tiagabine hydrochloride |
| CAS号 : | 145821-59-6 | |
| 货号 : | A214929 | |
| 分子式 : | C20H26ClNO2S2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 412.01 | |
| MDL号 : | MFCD07369025 | |
| 存储条件： |
Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Tiagabine Hydrochloride is the hydrochloride form of tiagabine. It is a derivative of piperidine carboxylic acid and has anticonvulsant effect. It is a selective inhibitor of GABA reabsorption. Perfusion of tiagabine (50 microM) for 15 min, evoked large, slow depolarizations with a frequency of 6-8/h which persisted for 4-5 h[3]. Superfusion of tiagabine significantly prolonged the decay kinetics of both action potential-dependent and -independent (tetrodotoxin-resistant) inhibitory postsynaptic currents (IPSCs) that were mediated by GABA(A) receptors. Furthermore, it decreased the frequency of these IPSCs. In the behaving animal, tiagabine when injected unilaterally into the globus pallidus caused consistent ipsilateral rotation of the rats indicative of increased inhibition of globus pallidus activity[4]. Moreover, tiagabine offers a significant neuroprotection in global ischemia in gerbils when given 30 min before ischemia but not when given 3 h after ischemia[5]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01381523 | - | Completed | - | - | |
| NCT02727101 | Epilepsy | Phase 4 | Terminated(slow enrollment) | - | United States, Maryland ... 展开 >> MidAtlantic Epilepsy and Sleep Center Bethesda, Maryland, United States, 20817 收起 << |
| NCT00404248 | Brain and Central Nervous Syst... 展开 >>em Tumors 收起 << | Phase 1 Phase 2 | Completed | - | United States, Alabama ... 展开 >> UAB Comprehensive Cancer Center Birmingham, Alabama, United States, 35294-3410 United States, Florida H. Lee Moffitt Cancer Center and Research Institute at University of South Florida Tampa, Florida, United States, 33612-9497 United States, Georgia Winship Cancer Institute of Emory University Atlanta, Georgia, United States, 30322 United States, Maryland Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Baltimore, Maryland, United States, 21231 United States, Massachusetts Massachusetts General Hospital Boston, Massachusetts, United States, 02114 United States, Michigan Josephine Ford Cancer Center at Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, North Carolina Wake Forest University Comprehensive Cancer Center Winston-Salem, North Carolina, United States, 27157-1096 United States, Ohio Cleveland Clinic Taussig Cancer Center Cleveland, Ohio, United States, 44195 United States, Pennsylvania Abramson Cancer Center of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104-4283 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.43mL 0.49mL 0.24mL |
12.14mL 2.43mL 1.21mL |
24.27mL 4.85mL 2.43mL |
| 参考文献 |
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