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/ GABA受体 / Tiagabine HCl/盐酸噻加宾

Tiagabine HCl/盐酸噻加宾 {[allProObj[0].p_purity_real_show]}

货号：A214929 同义名： 噻加宾盐酸盐 / TGB hydrochloride; NO328 hydrochloride

Tiagabine HCl is an inhibitor of gamma-aminobutyric acid (GABA) reuptake (IC50 = 67 nM in vivo) with anticonvulsant effect.

Tiagabine HCl/盐酸噻加宾 化学结构 CAS号：145821-59-6
Tiagabine HCl/盐酸噻加宾 化学结构
CAS号：145821-59-6
Tiagabine HCl/盐酸噻加宾 3D分子结构
CAS号：145821-59-6
Tiagabine HCl/盐酸噻加宾 化学结构 CAS号：145821-59-6
Tiagabine HCl/盐酸噻加宾 3D分子结构 CAS号：145821-59-6
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Tiagabine HCl/盐酸噻加宾 纯度/质量文件 产品仅供科研

货号：A214929 标准纯度： {[allProObj[0].p_purity_real_show]}
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Tiagabine HCl/盐酸噻加宾 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].

Tiagabine HCl/盐酸噻加宾 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 <<

Tiagabine HCl/盐酸噻加宾 参考文献

[1]Angehagen M, Ben-Menachem E, et al. Novel mechanisms of action of three antiepileptic drugs, vigabatrin, tiagabine, and topiramate. Neurochem Res. 2003 Feb;28(2):333-40.

[2]Hu RQ, Davies JA. Tigabine hydrochloride, an inhibitor of gamma-aminobutyric acid (GABA) uptake, induces cortical depolarizations in vitro. Brain Res. 1997 Apr 11;753(2):260-8.

[3]Hu RQ, Davies JA. Tigabine hydrochloride, an inhibitor of gamma-aminobutyric acid (GABA) uptake, induces cortical depolarizations in vitro. Brain Res. 1997 Apr 11;753(2):260-8.

[4]Chen L, Yung WH. Effects of the GABA-uptake inhibitor tiagabine in rat globus pallidus. Exp Brain Res. 2003 Sep;152(2):263-9.

[5]Iqbal S, Baziany A, Gordon S, Wright S, Hussain M, Miyashita H, Shuaib A, Hasan Rajput A. Neuroprotective effect of tiagabine in transient forebrain global ischemia: an in vivo microdialysis, behavioral, and histological study. Brain Res. 2002 Aug 16;946(2):162-70.

Tiagabine HCl/盐酸噻加宾 实验方案

计算器
存储液制备 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

Tiagabine HCl/盐酸噻加宾 技术信息

CAS号145821-59-6
分子式C20H26ClNO2S2
分子量 412.01
SMILES Code O=C([C@H]1CN(CC/C=C(C2=C(C)C=CS2)/C3=C(C)C=CS3)CCC1)O.[H]Cl
MDL No. MFCD07369025
别名 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
运输蓝冰
InChI Key YUKARLAABCGMCN-PKLMIRHRSA-N
Pubchem ID 91274
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

Tags: Tiagabine | 145821-59-6 | NO050328 | NO328 | TGB | NO 050328 | NO-050328 | NO 328 | NO-328 | GABA Receptor Inhibitor | Membrane Transporter/Ion Channel | Neuronal Signaling | GABA Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Tiagabine HCl/盐酸噻加宾 纯度/质量文件 | Tiagabine HCl/盐酸噻加宾 亚型比较 | Tiagabine HCl/盐酸噻加宾 生物活性 | Tiagabine HCl/盐酸噻加宾 临床数据 | Tiagabine HCl/盐酸噻加宾 参考文献 | Tiagabine HCl/盐酸噻加宾 实验方案 | Tiagabine HCl/盐酸噻加宾 技术信息

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