NS-11394
| CAS号 | 951650-22-9 | 货号 | BCP23679 |
| 中文名 | NS-11394 | ||
| 英文名 | NS-11394 | ||
| 中文别名 | |||
| 英文别名 | NS 11394; NS11394; | ||
| 分子式 | C23H19N3O | 分子量 | 353.42 |
| 生物活性 | NS-11394 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. | ||
| 信号通路 | Ion Channel/Membrane Transporter Neuro Signaling Pathway | ||
| 靶 点 | GABA Receptor | ||
结构式
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