PD 144418草酸盐
| 中文名称 | PD 144418草酸盐 |
|---|---|
| 中文同义词 | PD 144418草酸盐 |
| 英文名称 | IWSFHSVGBKPYFN-UHFFFAOYSA-N |
| 英文同义词 | IWSFHSVGBKPYFN-UHFFFAOYSA-N |
| CAS号 | 1794760-28-3 |
| 分子式 | C20H24N2O5 |
| 分子量 | 372.42 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1794760-28-3.mol |
| 结构式 |  |
PD 144418草酸盐 性质
| 溶解度 | 在DMSO中溶解至50mM |
|---|---|
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
PD 144418 oxalate 是一种高亲和力，强效和选择性的 sigma 1 受体 (σ1 receptor) 配体 (对 σ1 和 σ2 的 Ki 值分别为 0.08 nM 和 1377 nM)，对其他受体，离子通道和酶没有任何显着的亲和力。PD 144418 oxalate 具有潜在的抗精神病活性。
Ki: 0.08 nM (σ1 receptor) and 1377 nM (σ2 receptor)
In vitro, PD 144418 reverses the N-methyl-D-aspartate (NMDA)-induced increase in cyclic GMP (cGMP) in rat cerebellar slices without affecting the basal levels, suggesting that σ1 sites may be important in the regulation of glutamine-induced actions. PD 144418 potentiates the decrease in 5-hydroxytryptophan caused by Haloperidol in the mesolimbic region, but by itself has no effect in 5-HT and dopamine (DA) synthesis.
PD 144418 (10 mg/kg; intraperitoneal injection; male CD-1 mice) treatment antagonizes Mescaline-induced scratching at doses that did not alter spontaneous motor activity, with PD 144418 showing ED 50 values of 7.0 mg/kg i.p..
| Animal Model: | Male CD-1 mice induced with Mescaline |
| Dosage: | 10 mg/kg |
| Administration: | Intraperitoneal injection; once |
| Result: | Antagonized mescaline-induced scratching at doses that did not alter spontaneous motor activity. |