154130-99-1
中文名称
化合物 T16445
英文名称
1,2,3,6-TETRAHYDRO-5-[3-(4-METHYLPHENYL)-5-ISOXAZOLYL]-1-PROPYLPYRIDINE OXALATE
CAS
154130-99-1
分子式
C18H22N2O
分子量
282.38
MOL 文件
154130-99-1.mol
154130-99-1 结构式
基本信息
中文别名
化合物 T16445 英文别名
PD 144418PD 144418 OXALATE
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
物理化学性质
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 in DMSO
酸度系数(pKa)8.10±0.40(Predicted)
形态固体
颜色米白色
应用领域
用途1
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.化合物 T16445价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/02/08 | HY-108512A | 化合物 T16445 PD 144418 oxalate | 154130-99-1 | 2mg | 950元 |
| 2025/02/08 | HY-108512A | 化合物 T16445 PD 144418 oxalate | 154130-99-1 | 5 mg | 1650元 |
| 2025/02/08 | HY-108512 | 化合物 T16445 PD 144418 | 154130-99-1 | 2mg | 1800元 |
常见问题列表
生物活性
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。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 |
| Result: | Antagonized mescaline-induced scratching at doses that did not alter spontaneous motor activity. |