| 货号 | 4256/50 |
| 别名 | (3R)-1-[4,4-Bis(3-methyl-2-thienyl) |
| 供应商 | Tocris |
| 生物活性 | GABA uptake inhibitor (IC50 = 67 nM in vivo). Exhibits high affinity and selectivity for the GAT-1 GABA transporter. Anticonvulsant; also attenuates established dynorphin-induced allodynia in a mouse model after systemic administration. |
| 运输条件 | Blue Ice |
| 存放说明 | Ambient |
| 纯度 | >99 % |
| 计算分子量 | 412.01 |
| 分子式 | C20H25NO2S2< |
| 可溶性/溶解性 | Soluble to 50 mM in water and to 100 mM in DMSO |
| 参考文献 | Laughlinet al (2002) Comparison of antiepileptic drugs tiagabine, lamotrigine, and gabapentin in mouse models of acute, prolonged, and chronic nociception. J.Pharmacol.Exp.Ther. 302 1168. PMID: 12183677. Dharet al (1994) Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA updake inhibitors: identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. J.Med.Chem. 37 2334. PMID: 8057281. Andersenet al (1993) The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate. J.Med.Chem. 36 1716. PMID: 8510100. |