| 货号 | 1454/10 |
| 别名 | 4-(8-Methyl-9H-1,3-dioxolo[4,5-h][2 |
| 供应商 | Tocris |
| 生物活性 | Selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA- , kainate- and NMDA-induced responses respectively). Skeletal muscle relaxant and orally-active anticonvulsant. Has anti-proliferative effects in transformed cells. Also available as part of the AMPA Receptor Tocriset™. Also available as part of the Kainate Receptor Tocriset™. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >98 % |
| 计算分子量 | 366.24 |
| 分子式 | C17H15N3O2.2HCl |
| 可溶性/溶解性 | Soluble to 50 mM in DMSO and to 10 mM in water |
| CAS号 | 102771-26-6 |
| 参考文献 | Rzeskiet al (2001) Glutamate antagonists limit tumor growth. Proc.Natl.Acad.Sci.USA 98 6372. PMID: 11331750. Szabadoset al (2001) Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655. Brain Res.Bull. 55 387. PMID: 11489346. Paternainet al (1995) Selective antagonism of AMPA receptors unmasks kainate receptor-mediated responses in hippocampal neurons. Neuron 14 185. PMID: 7826635. Donevan and Rogawsk (1993) GYKI 52466, a 2,3-benzodiazepine, is a highly selective, non-competitive antagonist of AMPA/kainate receptor responses. Neuron 10 51. PMID: 7678966. Tarnawaet al (1989) Electrophysiological studies with a 2,3-benzodiazepine muscle relaxant: GYKI 52466. Eur.J.Pharmacol. 167 193. PMID: 2574112. |