PD 144418草酸鹽
| 中文名稱 | PD 144418草酸鹽 |
|---|---|
| 中文同義詞 | PD 144418草酸鹽 |
| 英文名稱 | IWSFHSVGBKPYFN-UHFFFAOYSA-N |
| 英文同義詞 | IWSFHSVGBKPYFN-UHFFFAOYSA-N |
| CAS號(hào) | 1794760-28-3 |
| 分子式 | C20H24N2O5 |
| 分子量 | 372.42 |
| EINECS號(hào) | |
| 相關(guān)類別 | |
| Mol文件 | 1794760-28-3.mol |
| 結(jié)構(gòu)式 |  |
PD 144418草酸鹽 性質(zhì)
| 溶解度 | 在DMSO中溶解至50mM |
|---|---|
| 形態(tài) | 固體 |
| 顏色 | 白色至米白色 |
PD 144418 oxalate 是一種高親和力，強(qiáng)效和選擇性的 sigma 1 受體 (σ1 receptor) 配體 (對 σ1 和 σ2 的 Ki 值分別為 0.08 nM 和 1377 nM)，對其他受體，離子通道和酶沒有任何顯著的親和力。PD 144418 oxalate 具有潛在的抗精神病活性。
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. |