132449-89-9
| 中文名称 | 132449-89-9 |
|---|---|
| 中文同义词 | 来索吡琼二盐酸盐;化合物 T11839 |
| 英文名称 | lesopitron |
| 英文同义词 | Lesopitron (dihydrochloride);E4424;Lesopitron (dihydrochloride) (E4424) |
| CAS号 | 132449-89-9 |
| 分子式 | C15H22Cl2N6 |
| 分子量 | 357.28 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 132449-89-9.mol |
| 结构式 |  |
132449-89-9 性质
| 熔点 | 194-197.5° |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
|
5-HT 1A Receptor 125 nM (IC 50 , in rat hippocampal membranes) |
In vitro binding and autoradiographic studies with [ 3 H]8-OH-DPAT and [ 3 H]Lesopitron as radioligands confirm that Lesopitron binds to 5-HT 1A receptors in the rat brain with a relatively high affinity (pK i =7.35). As expected of a full agonist at postsynaptic 5-HT 1A receptors, Lesopitron (IC 50 =125 nM) inhibits forskolin-stimulated adenylate cyclase activity in rat hippocampal membranes to the same extent as 5-HT. Lesopitron inhibits the firing of serotoninergic neurons both in vitro (in brainstem slices, IC 50 =120 nM).
Lesopitron inhibits the firing of serotoninergic neurons both in vivo (in chloral hydrate-anaesthetized rats, ID 50 =35 μg/kg i.v.). Lesopitron administered at a dose which induces anxiolytic behaviour in rats (30 μg/kg, i.p.) markedly reduces 5-HT levels (to 45% of the basal value) in cortical perfusates.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-101609 | Lesopitron dihydrochloride | 1 mg | 8500元 | |
| 2023/03/20 | HY-101609 | 132449-89-9 Lesopitron dihydrochloride | 132449-89-9 | 5mg | 29000元 |