化合物 T16445
| 中文名称 | 化合物 T16445 |
|---|---|
| 中文同义词 | 化合物 T16445;化合物 PD 144418 |
| 英文名称 | 1,2,3,6-Tetrahydro-5-[3-(4-methylphenyl)-5-isoxazolyl]-1-propylpyridine oxalate |
| 英文同义词 | PD 144418 OXALATE;PD 144418;Pyridine,1,2,3,6-tetrahydro-5-[3-(4-methylphenyl)-5-isoxazolyl]-1-propyl-;1,2,3,6-Tetrahydro-5-[3-(4-methylphenyl)-5-isoxazolyl]-1-propylpyridine oxalate |
| CAS号 | 154130-99-1 |
| 分子式 | C18H22N2O |
| 分子量 | 282.38 |
| EINECS号 | |
| 相关类别 | Amines;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pfizer Compounds;Pharmaceuticals |
| Mol文件 | 154130-99-1.mol |
| 结构式 |  |
化合物 T16445 性质
| 沸点 | 453.2±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.067±0.06 g/cm3(Predicted) |
| 储存条件 | Desiccate at RT |
| 溶解度 | <18.62mg/ml，溶于 DMSO |
| 形态 | 固体 |
| 酸度系数(pKa) | 8.10±0.40(Predicted) |
| 颜色 | 米白色 |
PD 144418 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 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 |
| Result: | Antagonized mescaline-induced scratching at doses that did not alter spontaneous motor activity. |
用途
PD 144418 is high affinity, selective 蟽1 ligand (Ki values are 0.08 and 1377 nM for 蟽1 and 蟽2 respectively). PD 144418 displays no significant activity at a wide range of other receptors, ion channels
and enzymes. PD 144418 antagonizes mescaline-induced scratching in mice following i.p. administration.安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/09/15 | HY-108512 | 化合物 T16445 PD 144418 | 154130-99-1 | 2mg | 1800元 |
| 2026/09/15 | HY-108512 | 化合物 T16445 PD 144418 | 154130-99-1 | 5 mg | 3200元 |