1794760-28-3
中文名称
PD 144418草酸盐
英文名称
IWSFHSVGBKPYFN-UHFFFAOYSA-N
CAS
1794760-28-3
分子式
C20H24N2O5
分子量
372.42
MOL 文件
1794760-28-3.mol
1794760-28-3 结构式
常见问题列表
生物活性
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。靶点
Ki: 0.08 nM (σ1 receptor) and 1377 nM (σ2 receptor)
体外研究
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.
体内研究
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. |