154130-99-1
中文名稱
化合物 T16445
英文名稱
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 結構式
基本信息
中文別名
化合物 T16445 英文別名
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
物理化學性質
沸點453.2±45.0 °C(Predicted)
密度1.067±0.06 g/cm3(Predicted)
儲存條件Desiccate at RT
溶解度<18.62mg/ml in DMSO
酸度系數(shù)(pKa)8.10±0.40(Predicted)
形態(tài)固體
顏色米白色
應用領域
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價格(試劑級)
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2025/05/22 | HY-108512A | 化合物 T16445 PD 144418 oxalate | 154130-99-1 | 2mg | 950元 |
| 2025/05/22 | HY-108512A | 化合物 T16445 PD 144418 oxalate | 154130-99-1 | 5 mg | 1650元 |
| 2025/05/22 | HY-108512 | 化合物 T16445 PD 144418 | 154130-99-1 | 2mg | 1800元 |
常見問題列表
生物活性
PD 144418 是一種高親和力，強效和選擇性的 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 具有潛在的抗精神病活性。靶點
Ki: 0.08 nM (σ1 receptor) and 1377 nM (σ2 receptor)
體外研究
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.
體內(nèi)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. |