| 產(chǎn)品編號(hào) | D51255 |
| 英文名稱 | NS11394 |
| 中文名稱 | |
| 別 名 | GABAA受體正變構(gòu)調(diào)節(jié)劑 |
| 克 隆 號(hào) | |
| CAS | 951650-22-9 |
| 理論分子量 | 353.42 kDa |
| 檢測(cè)分子量 | |
| 性 狀 | Lyophilized |
| 保存條件 | Store in dry, dark place for one year. |
| 注意事項(xiàng) | This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications. |
| 產(chǎn)品介紹 |
NS11394 is a drug which acts as a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes. NS-11394 has been researched as an analgesic for use in chronic or neuropathic pain. NS-11394 possesses a functional selectivity profile at GABA(A) receptors of alpha(5) > alpha(3) > alpha(2) > alpha(1) based on oocyte electrophysiology with human GABA(A) receptors. Compared with other subtype-selective ligands, NS11394 is unique in having superior efficacy at GABA(A)-alpha(3) receptors while maintaining low efficacy at GABA(A)-alpha(1) receptors. NS11394 has an excellent pharmacokinetic profile, which correlates with pharmacodynamic endpoints (CNS receptor occupancy). NS11394 is potent and highly effective in rodent anxiety models. NS11394 has a significantly reduced side effect profile in rat (sedation, ataxia, and ethanol interaction) and mouse (sedation), even at full CNS receptor occupancy. NS11394 has a unique subtype-selective GABA(A) receptor profile and represents an excellent pharmacological tool to further understanding on the relative contributions of GABA(A) receptor subtypes in various therapeutic areas. |
