| 货号 | 1081/50 |
| 别名 | 1-(4,4-Diphenyl-3-butenyl)-3-piperi |
| 供应商 | Tocris |
| 生物活性 | A potent GABA uptake inhibitor, selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). Inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). Able to pass the blood-brain barrier after systemic administration and is active in vivo. |
| 运输条件 | Blue Ice |
| 存放说明 | 4℃ |
| 纯度 | >99 % |
| 计算分子量 | 371.91 |
| 分子式 | C22H25NO2.HCl |
| 可溶性/溶解性 | Soluble to 100 mM in water with gentle warming and to 100 mM in DMSO |
| CAS号 | 85375-15-1 |
| 参考文献 | Krause and Schwarz (2005) Identification and selective inhibition of the channel mode of the neuronal GABA transporter 1. Mol.Pharmacol. 68 1728. PMID: 16150932. Murali Dha (1996) On the bioactive conformation of the GABA uptake inhibitor SK&F 89976-A. Bioorg.Med.Chem.Lett. 61535. Aliet al (1985) Orally active and potent inhibitors of γ-aminobutyric acid. J.Med.Chem. 28 653. PMID: 2985785. |